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    Icaritin inhibits survival and migration of basal cell carcinoma cells through Hedgehog signaling pathway
    HU Wen-long, WU Ping-ping, LIU Ling-hua, LIU You-rao
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1091-1097.   DOI: 10.16333/j.1001-6880.2022.7.001
    Abstract799)      PDF(pc) (1692KB)(6)       Save
    The purpose of the present study was to investigate the effect and its mechanism of icaritin on basal cell carcinoma cell line A431. A431 cells were treated with icaritin at different concentrations and/or GANT 61. The viability and migration of A431 cells were assayed by CCK-8 method and Transwell assay. The expression of Hedgehog,Smo,Gli1,Bcl-2,Bax and MMP-9 was detected by qPCR and Western blot. Flow cytometry and Caspase-3 activity assay were used to investigate the effects of icaritin and/or GANT 61 on apoptosis of cells. The results showed that,both icaritin and GANT 61 could significantly inhibit the viability of A431 cells,down-regulate the expression of Hedgehog,Smo,Gli1,Bcl-2,MMP-9 and up-regulate the expression of Bax,enhance the activity of Caspase-3 and mediated the apoptosis,inhibited the migration of A431 cells. However,icaritin could not enhance these effects on the basis of Gant 61. Icaritin could promote apoptosis and inhibit migration by Hedgehog signaling pathway in basal cell carcinoma cells. These results suggest that icaritin may promote the expression of apoptotic-related factors,and mediate the apoptosis,down-regulate the expression of MMP-9,and inhibit the migration of basal cell carcinoma cells mainly by inhibiting Hedgehog signaling pathway.
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    Extraction technology optimization of dietary fiber from Hippophae rhamnoides
    GUO Jing-jing, LI Ya-xuan, FAN Zi-yi, CHEN Xuan-tong, WANG Qi, FU Qun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1181-1188.   DOI: 10.16333/j.1001-6880.2022.7.011
    Abstract762)      PDF(pc) (1138KB)(13)       Save
    In order to reuse the processing waste of forest resources,this experiment used Hippophae rhamnoides pomace as raw material,using ultrasonic-assisted enzyme method,and analyzed the effects of four factors,namely cellulase addition,ultrasonic temperature,ultrasonic time and material liquid ratio,on the extraction effect of dietary fiber.With the yield ratio of soluble dietary fiber (SDF) and insoluble dietary fiber (IDF) as the index,response surface methodology was used to analyze the extraction effect of dietary fiber.The results showed that the SDF/IDF was 0.21±0.01,and the swelling capacity and oil holding capacity of total dietary fiber (TDF) were 3.12±0.13 mL/g,(4.47±0.41)% respectively under the optimum conditions of 5% cellulase and ultrasonic treatment at 60℃ for 50 min.Therefore,ultrasonic-assisted enzyme method can effectively improve the extraction efficiency of products,and has certain significance for promoting the development and utilization of Hippophae rhamnoide by-product resources.
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    Biological characteristics of Pythium ultimum causing damping-off disease of Dendrobium officinale and the screening of antifungal plants against it
    TAN Zhi-yong, ZHOU Zhen-yu, YANG Wen-ming, LI Ya-juan, LU Zhi-hong
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1189-1195.   DOI: 10.16333/j.1001-6880.2022.7.012
    Abstract687)      PDF(pc) (1567KB)(3)       Save
    The biological characteristics of Pythium ultimum causing damping-off disease of Dendrobium officinale and the screening of antifungal plants against P. ultimum were studied to lay a theoretical foundation for the prevention and control of damping-off disease of D. officinale. The inhibitory effect and biological characteristics of aqueous extracts of different Chinese herbal medicines on the  P. ultimum were determined by mycelium growth rate method.The average mycelial growth rate of the  P. ultimum on the PDA medium was 0.22 cm/h.The optimum temperature was 30 °C,the optimum pH was 6-7,the optimum carbon source were glucose and soluble starch,and the optimum nitrogen source was yeast extract. The light has no significant impact on the growth of mycelium. When the concentration of aqueous extract was 40 mg DW/mL,the inhibition rates of aqueous extract of Eugenia caryophyllata Thunb. and Mentha haplocalyx Briq. were 100% and 96.48%,respectively. The water extracts of E. caryophyllata and M. haplocalyx have good application potential in the control of Dendrobium officinale damping-off disease.
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    Screening of anti-allergic components from Corni Fructus and their effects on RBL-2H3 cells degranulation
    ZHANG Ge-ke, LIU Xue, YANG Cheng, SUN Ya-juan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1196-1203.   DOI: 10.16333/j.1001-6880.2022.7.013
    Abstract679)      PDF(pc) (1361KB)(8)       Save
    In the present study,the potential anti-allergic constituents in Corni Fructus were investigated. The anti-allergic components of Corni Fructus were preliminarily screened by hyaluronidase inhibition assay. The fractions with high hyaluronidase inhibition activity were further evaluated by the degranulation inhibition test of RBL-2H3 cells in vitro. The anti-allergic components were analyzed by gas chromatography-mass spectrometry (GC-MS). The results showed that the petroleum ether extract of Corni Fructus (COPE) had a significantly anti-hyaluronidase activity with an IC50 value of 3.11 mg/mL. Four fractions with higher anti-hyaluronidase activity were separated by silica gel column chromatography,among which COPE-8 had a more significant inhibitory effect on RBL-2H3 cell degranulation in a dose-dependent manner and showed low cytotoxicity. After treatment with 20 μg/mL COPE-8,the histamine and β-hexosaminidase released from RBL-2H3 cells were reduced by 46% and 39%,respectively. The main active components in COPE-8 were α-amyrin,β-amyrin,and sclareol,by GC-MS analysis. These findings signpost that COPE-8 has remarkable anti-allergic activity and has potential application in the development of anti-allergic active substances.
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    Study on the metabolites and pharmacokinetics of a chalcone extract from Millettia velutina Dunn
    NI Heng-fan, LIU Ling, WAN Li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1213-1222.   DOI: 10.16333/j.1001-6880.2022.7.015
    Abstract657)      PDF(pc) (1719KB)(7)       Save
    The UPLC-QE-Orbitrap-MS assay was used to compare the 2,5-dimethoxyfurano[4″,5″:3,4]chalcone (1) samples cultured in rat,mouse,rhesus monkey,Beagle dog and human liver microsomes for 0 min and 60 min in vitro,and compare the plasma,feces,and urine samples of intravenous injection of the compound and blank C57 mice to study its metabolites in vitro and in vivo.It was preliminarily concluded that there were two kinds of metabolites M1 and M2 in vitro after incubation,and five kinds of metabolites M1,M2,M3,M4 and M5 in vivo.M5 was further metabolized from M1,and the metabolite M1 was obtained by organic synthesis. Ultrafast liquid chromatography-mass spectrometry (UFLC-MS/MS) detection method was used to determine the plasma concentrations of 1 and M1.The change trend of the compound and M1 in rats was quantitatively studied and the pharmacokinetic parameters were calculated.Rats were randomly divided into groups and given drugs,and blood was collected at a set series of time points.The plasma concentrations of 1 and M1 were determined.The pharmacokinetic parameters were calculated by DAS2.0 software.The Cmax of 1 was 405.96 μg/L,Tmax=0.083 h,AUC0-t=190.64 μg/(L·h),T1/2=3.74 h.The Cmax of M1 was 281.291 μg/L,Tmax=0.083 h,AUC0-t=561.30 μg/(L·h),T1/2 =3.01 h.These results showed that 2,5-dimethoxyfuran[4″,5″:3,4]chalcone undergoes reduction,demethylation,ring opening,and hydroxylation reactions during the metabolism of the body.The main metabolite is M1,and M1 is further metabolized to M5.This study laid a material foundation for revealing its pharmacological effects.
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    Analysis on the difference of chemical constituents in Taxilli Herba from different host plants
    YUAN Jia-huan, WU Nan, WANG Wen-xin, CAI Zhi-chen, YIN Sheng-xin, CHEN Hai-jie, LIU Xun-hong, LI Li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1119-1128.   DOI: 10.16333/j.1001-6880.2022.7.004
    Abstract641)      PDF(pc) (2804KB)(4)       Save
    In order to study the influence of host plants regarding the synthesis and accumulation of metabolites in Taxilli Herba,Ultra-fast liquid chromatography coupled with triple quadrupole-time of flight tandem mass spectrometry (UFLC-Triple TOF-MS/MS) combined with multivariate statistical analysis was used to analyze the differences of chemical constituents in Taxilli Herba from different host plants.Through the analysis of the multistage tandem mass spectrometry,the characteristic peaks were extracted with mass spectrometry data peak matching,peak alignment,and noise filtering.Principal component analysis (PCA) and partial least-squares discriminant analysis (PLS-DA) were used to analyze the data.The constituents were identified according to MS accurate mass and MS/MS spectrometry fragmentation information,combined with the software of database search,comparison with reference standards and literature.The results showed that the chemicals constituents in Taxilli Herba from 10 host plants were clearly distinguished.A total of 19 chemical constituents were screened and identified.Among them,4 common differential chemical constituents ((+)-Catechin,quercetin 3-O-D-glucuronide,hyperoside,quercitrin) presented different changing laws.Our research may provide basic data for revealing the effect of host plants on the synthesis and accumulation of metabolites of Taxilli Herba and evaluating the quality of Taxilli Herba from different host plants.
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    Analysis of chemical components in alcohol extract of Rosa sertata×Rosa rugosa based on UPLC-Q-TOF-MS
    DU Shao-bo, CHEN Xiao-wen, DONG Zhi-qiang, XIE Hui-chun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1129-1142.   DOI: 10.16333/j.1001-6880.2022.7.005
    Abstract550)      PDF(pc) (1604KB)(8)       Save
    In order to quickly analyze and identify the chemical components of the alcohol extract of Rosa sertata×Rosa rugosa,ultra performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) was used in this study,Waters ACQUITY UPLC HSS T3 column (100 mm×2.1 mm,1.8 μm) was used with The mobile phase is 0.1% formic acid aqueous solution (A) and 0.01% formic acid acetonitrile solution (B) and gradient elution.The MSE data were collected under the negative ion condition of electrospray ion source (ESI).Sixty-three main components were detected according to the exact relative molecular mass,mass spectrometry fragmentation information,and related literature and reference materials,including 26 flavonoids,11 polyphenols(4 phenolic acids and 7 tannins),7 triterpenoids,4 phenylpropanoids,8 organic acids,1 iridoid terpene,1 volatile oil and 5 unidentified components.Twenty-eight compounds such as pectolinarin,melilotoside and asiatic acid were identified in this genus for the first time.UPLC-Q-TOF-MS method was used to further improve the chemical constituents of Rosa sertata×Rosa rugosa,which provided a reference basis for the basic study of pharmacodynamic substances.
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    Mechanism of apoptosis induced by exopolysaccharides from Fusarium graminearum on SGC-7901 cells#br#
    WANG Jiao-jiao, YUAN Ping-chuan, XU Han-chi, CHEN Ying, ZHANG Si-jia, TIAN Meng-yun, YU Zi-qi, LIU Chun-yan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1204-1212.   DOI: 10.16333/j.1001-6880.2022.7.014
    Abstract539)      PDF(pc) (1886KB)(0)       Save
    To investigate the effect and mechanism of exopolysaccharides from Fusarium graminearum (FGEPS) on human gastric cancer SGC-7901 cells.Fusarium graminearum was fermented in liquid medium.The exopolysaccharides were separated by alcohol precipitation,decolorization,deproteinization and dialysis,and analyzed by high performance gel permeation chromatography (HPGPC),infrared (IR) and ultraviolet (UV) spectroscopy.CCK-8 method was used to detect the proliferation inhibition activity of SGC-7901,BGC-823,and MGC-803 cells.Effects of FGEPS on apoptosis of SGC-7901 cells were analyzed by Annexin V-FITC/PI,JC-1 and Hoechst 33258 staining.The expressions of pro-apoptotic proteins Bax,Cleaved Caspase-3,Cleaved Caspase-9 and anti-apoptotic protein Bcl-2 were detected by Western blot.FGEPS was isolated from the fermentation broth of Fusarium graminearum,which had the characteristic absorption of polysaccharides and contained four components. In vitro anti-tumor activity assay showed that FGEPS inhibited SGC-7901 cells more significantly than BGC-823 and MGC-803 cells.FGEPS could significantly reduce the mitochondrial membrane potential of SGC-7901 cells,induce the concentration of nuclear chromatin,and produce apoptotic bodies (P<0.05 or P<0.01).FGEPS could raise the expression of pro-apoptotic proteins Bax,Cleaved Caspase-3 and Cleaved Caspase-9 in SGC-7901 cells (P<0.01 or P<0.001),and reduce the expression of anti-apoptotic protein Bcl-2 (P<0.001).In summary,FGEPS isolated from the fermentation broth of Fusarium graminearum could induce apoptosis of SGC-7901 cells through mitochondrial pathway.
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    Extraction optimization,structure characterization and anti-inflammatory activity of polysaccharides from Sparassis subalpina
    LUO Dian-hui, ZHANG Ze-tong
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1110-1118.   DOI: 10.16333/j.1001-6880.2022.7.003
    Abstract456)      PDF(pc) (2260KB)(4)       Save
    To study the isolation,purification,structure properties and anti-inflammatory activities of polysaccharides from Sparassis subalpina.Response surface methodology was used to obtain the optimal processing conditions of total sugar from S. subalpina and the method of column chromatography was used for the purification of a S. subalpina polysaccharide (SSP).Using gas chromatography,NMR spectroscopy and electron microscopies,the structure was studied.Anti-inflammatory activity was determined using RT-qPCR,et al.The results showed that the experimental yield was (18.21 ± 0.68)% under the optimal processing conditions (liquid to solid ratio 80 mL/g,extraction time 60 min,extraction temperature 70 ℃).The average molecular weight of SSP was calculated to be 50 kDa and SSP consisted of glucose,mannose,galactose and arabinose with a molar ratio of 6.5∶1.3∶1∶1.The repeated unit in SSP was determined as →3)-α-D-Galp-(1→2)-β-D-Glup-(1→3)-β-L-Araf-(1→3)-α-D-Manp-(1→,and SSP showed a non-branched and netted state.SSP demonstrated significant inhibitory effects on the gene expressions of TNF-α,COX-2 and iNOS in LPS-stimulated RAW 264.7 cells (P<0.05).The results evidenced the potential effects of SSP with the non-branched and netted state on anti-inflammatory activities.
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    Comparative study of chemical components in different organs of Macleaya cordata by HPLC fingerprint and chemometrics
    YANG Min, LIU Xiao-rong, ZENG Mei, ZHOU Xin-ru, WANG Zhi-hui, TONG Qiao-zhen, ZHOU Ri-bao, LIU Xiang-dan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1098-1109.   DOI: 10.16333/j.1001-6880.2022.7.002
    Abstract403)      PDF(pc) (2919KB)(7)       Save
    In this study,the chemical fingerprints of roots,leaves,fruits and stems of Macleaya cordata were established by HPLC,and the contents of protopine,allocryptine,sanguinarine and chelerythrine were determined;orthogonal partial least squares discriminant analysis (OPLS-DA) was used to evaluate the quality of roots,leaves and fruits of M. cordata.The fingerprint results showed that 17 batches of root samples were calibrated with 10 common peaks,14 batches of leaf samples were calibrated with 9 common peaks,14 batches of fruit samples were calibrated with 9 common peaks,and 10 batches of stem samples were calibrated with 6 common peaks.The order of the total contents of four alkaloids in different organs of M. cordata is:fruit > root > leaf > stem;the contents of the above four alkaloids were higher in the fruit and were lower in the stem;the contents of protopine and allocryptine higher in the root and leaf.The resources of M. cordata roots are large,and the contents of protopine and allocryptopine are higher than those of fruits and leaves,it can be developed and utilized with M. cordata fruits and leaves as the above alkaloid extraction raw materials.The results of OPLS-DA showed that if VIP > 1,allocriptine and chelerythrine could be used as potential quality markers of M. cordata roots;sanguinarine and chelerythrine can be used as potential quality markers of M. cordata leaves;protopine,allocryptine and sanguinarine can be used as potential quality markers of M. cordata fruits.The results of this study provide a research basis for the identification and evaluation of the roots,leaves,fruits and stems of  M. cordata and the development and utilization of M. cordata roots.
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    Study on the mechanism of Gastrodiae Rhizoma-Chuanxiong Rhizoma herb pair in the treatment of hypertension based on network pharmacology and molecular docking technology
    WANG Mei, QIAO An-ping, JIA Xiao-gang, LIU Lin, LI Jia, ZHANG Xiao-fei, SHI Ya-jun, DUAN Lin-yu
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 473-483.   DOI: 10.16333/j.1001-6880.2022.3.015
    Abstract343)      PDF(pc) (2980KB)(12)       Save
    This study aims to explore the active components and pharmacological mechanisms of Gastrodiae Rhizoma-Chuanxiong Rhizoma in promoting blood circulation and removing blood stasis by the network pharmacology and molecular docking.The chemical constituents and target genes of Gastrodiae Rhizoma-Chuanxiong Rhizoma herb pairs were screened by the systematic pharmacological analysis platform (TCMSP).The potential active components of Gastrodiae Rhizoma-Chuanxiong Rhizoma herb pairs were screened under the conditions of bioavailability (OB) ≥ 30% and drug-like (DL) ≥ 0.18.The disease target of hypertension was searched through Drugbank and CTD,which was mapped with the potential target of herb pair,and the Wayne diagram was drawn.The target gene of the mapped active component was introduced into Cytoscape 3.2.1 to construct the drug pair-disease-component-target network map.The protein interaction map was constructed with string database,and go function analysis and KEGG pathway enrichment analysis were performed;the results of active components and key targets were verified the molecular docking by Discovery Studio 4.5 software.A total of 107 active ingredients and 1 010 targets were screened for the Gastrodiae Rhizoma-Chuanxiong Rhizoma herb pair.Hypertension corresponds to 2 268 targets.Through mapping,70 active ingredients and 83 intersection targets were selected.The traditional Chinese medicine-active components-target regulation network contains 155 nodes and 1 217 edges.GO function enrichment results mainly involve the blood circulation,circulatory system process,nuclear receptor activity,transcription factor activity,and so on;KEGG enrichment results mainly involve the neuroactive ligand-receptor interaction,pathways in cancer,cAMP signaling pathway,calcium signaling pathway,and so on.The results of molecular docking showed that the core targets had strong affinity with m-hydroxybenzoic acid,oleic acid,mandenol,trans-β-farnesene and tetradecane.Gastrodiae Rhizoma-Chuanxiong Rhizoma herb pair may play a role in the treatment of hypertension through TNF,PTGS2,EDN1 and other key targets,and through the regulation of neuroactive ligand-receptor interaction,Ca2+ signaling pathway,in cancer pathways and other signal pathways.This study reveals the pharmacological mechanisms of Gastrodiae Rhizoma-Chuanxiong Rhizoma on multi-component,multi-channel and multi-target synergistic in the treatment of hypertension from the perspective of network pharmacology.
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    Chemical composition,antioxidant and anti-inflammatory activities of volatile oil from Turpiniae Folium
    LIU Zhao, LI Li, TANG Yang-qiannan, LIN Li-mei, XIA Bo-hou
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (5): 723-738.   DOI: 10.16333/j.1001-6880.2022.5.001
    Abstract335)      PDF(pc) (1410KB)(8)       Save
    Turpiniae Folium is widely used as a functional food or medicine in China.However,little investigations are performed on the chemical composition and biological activity of its volatile oil.In this work,Turpiniae Folium oil extracts (Supercritical extraction) were systematically characterized for the first time.The low polar substances were identified by GC-MS (methyl esterification and non-methylesterification),and LC-MS method was applied to conduct analysis of the intermediate polar substances.Also,the anti-oxidant (DPPH and ABTS method) and anti-inflammatory (LPS-induced RAW 264.7 cell model) activity of the oil from Turpiniae Folium were performed.80 chemical components were identified by GC-MS (38 for non-methyl esterification and 42 for methyl esterification,respectively),most of which were linoleic acid,γ-sitosterol,squalene,2,2′-methylenebis-(4-methyl -6-tert-butylphenol),trans-9-octadecenoic acid,palmitic acid and other substances.In the positive and negative ion mode of LC-MS,a total of 256 compounds were identified,most of which were terpenes,phenylpropanoids,phenols,flavonoids,alkaloids,coumarins and their derivatives,fatty acyls,semi-terpenoids,fatty acids and other compounds.Moreover,the volatile oil from Turpiniae Folium had good ability to resist DPPH and ABTS free radicals,and could significantly inhibit the release of NO and IL-6 in RAW 264.7 cells induced by LPS in a dose-dependent manner.Generally,these results proved the anti-bacterial,anti-inflammatory,and immunoregulatory effects of the volatile oil from Turpiniae Folium,thus providing a reference for the application of PVO as a food or drug.
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    Chemical constituents from Acanthus leucostachyus and their anti-inflammatory and antioxidant activities
    JIA Hui-zhen, SUN Peng, LU Jian-mei, WU Min, XU You-kai
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 407-412.   DOI: 10.16333/j.1001-6880.2022.3.007
    Abstract327)      PDF(pc) (579KB)(14)       Save
    To study the chemical constituents from the whole herb of Acanthus lecucostachyus.Thirteen compounds (1-13) were isolated and purified by column chromatography on microporous resin,silica gel and SephadexLH-20.The structure of the compounds was identified by comparing their NMR,MS spectroscopic data with those in the literatures.These compounds were identified as 2-benzoxazolinone(1), 3-hydroxylacetyl-indole(2),catechol(3),vanillic acid(4),methyl 3,4-dihydroxy-benzoate(5),N-(2-hydroxyphenyl) formamide(6), carbazole(7),dibutyl phthalate(8),ethyl p-methoxy-trans-cinnamate(9),ethyl cinnamate(10),stigmasterol(11),3-hydroxy-4-methoxypyridine(12),stigmasterol-3-O-β-D-glucopyranoside(13).All compounds were isolated from this plant for the first time,in addition,compound 7 was found in the genus Acanthus for the first time.All isolates were evaluated for antioxidant activity by DPPH free radical scavenging method and anti-inflammatory activities by lipopolysaccharide (LPS) induced mouse monocyte macrophage RAW 264.7 to generate NO inflammatory model.Among those compounds,compound 3 showed moderate antioxidant activity with IC50 value of 105.18 μM;Compounds 3,6 and 9 showed significant anti-inflammatory activity with IC50 values of 18.49,22.84 and 41.22 μM,respectively.
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    Chemical constituents in Carpesium cernuum and their cytotoxic activity
    FENG Shu-hui, ZHANG Wei-qing, SUN Mao, GUO Hong-wei, SUN Gui-ping, ZHU Cheng-guang, WANG Tian-yuan, YAN Chen
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 383-389.   DOI: 10.16333/j.1001-6880.2022.3.004
    Abstract323)      PDF(pc) (699KB)(10)       Save
    To study the chemical constituents of the medicinal plant Carpesium cernuum and their cytotoxic activity,ten compounds were obtained from the ethyl acetate fraction of 95% ethanol extract of C. cernuum by ap-plying various chromatographic techniques.Their structures were elucidated and identified as(5Z)-6-[(acetyloxy)methyl]-2-oxo-2,10,14-trimethylhexadeca-5,13-diene-11α-ol(1),(2E,10E)-1,12-dihydroxy-18-acetoxy-3,7,15-trimethylhexadeca-2,10,14-triene(2),(2E,6Z,10E,12R)-7-[(acetyloxy)methyl]-3,11,15-trimethylhexadeca-2,6,10,14-tetraene-1,12-diol(3),(2E,6Z,11S,12R)-3,7,11,15-tetramethylhexadeca-2,6,14-triene-7-[(acetyloxy)methyl]-1,12,19-triol(4),plaunotol(5),S-(+)-dehydrovomifoliol(6),pubinernoid A(7),stigmasterol (8),aurantiamide acetate (9),E-p-hydroxycinnamic acid (10) respectively,based on the spectral data.Compound 1 is a new compound.The cytotoxic effect of compounds 1-4 on Human breast cancer MDA-MB-231 cell were investigated by MTT.Compound 2 exhibited strong cytotoxic activity with IC50 values of 6.80 μmol/L,and compounds 1,3 and 4 had moderate cytotoxic activity.
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    Chemical constituents from the aerial parts of Ficus tikoua Bur. and their antioxidant activity
    HE Zhi-yun, SHI Song-yun, WEI Xue-jiao, LIU Cheng-xiong, CHEN Jian-feng, ZOU Kun, CHENG Fan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (5): 810-817.   DOI: 10.16333/j.1001-6880.2022.5.009
    Abstract300)      PDF(pc) (755KB)(14)       Save
    To study the chemical constituents and antioxidant activity of the aerial parts of Ficus tikoua,a folk medicine of Tujia nationality.Its ethanol extract was separated and purified using silica gel column chromatography,gel column chromatography,macroporous resin column chromatography combined with semi-preparative high performance liquid chromatography and other methods.The structure of the compounds was identified by nuclear magnetic resonance spectroscopy,mass spectrometry and other methods,and seventeen compounds were separated.These compounds were identified as alpinumisoflavone (1),(+)-catechin (2),nodakenin (3),psoralen (4),bergapten (5),(+)-lyoniresinol-3α-O-β-D-glucopyranoside (6),(+)-lyoniresinol-3α-O-β-D-xylopyranoside (7),(-)-isolariciresinol-9-O-β-D-glucopyranoside (8),ssioriside (9),huazhongilexin (10),(+)-isolariciresinol (11),(7R,8S)-3,5′-dimethoxy-4′,7-epoxy-8,3′-neolignane-5,9,9′-triol (12),6,7-dimethoxy-4-hydroxy-1-naphthoic acid (13),ethy-3,4-dihydroxybenzoate (14),bluemenol A (15),3,3′,4,4′-tetrahydroxy diphenyl (16),ethyl chlorogenate (17).Compounds 1-4,6-17 were isolated from this plant for the first time.Three indicators of DPPH radical scavenging rate,total antioxidant capacity,and superoxide anion scavenging capacity were used to determine the antioxidant activity of 17 compounds.The results show that lignans 9,10,and polyphenols 13,14,16 have significant DPPH free radical scavenging ability and total antioxidant ability,and their antioxidant activity is equivalent to that of ascorbic acid at the same concentration.
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    Study on the treatment of benign prostatic hyperplasia with modified Guizhi Fuling Pill based on network pharmacology and experiment verification
    LIU Dan, CHEN Ya-fei, LIU Zhe-jun, TANG Tian, YU Shu-jun, LIU Gui-min, TANG Yi-bo, LIU Zhen-quan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1234-1249.   DOI: 10.16333/j.1001-6880.2022.7.017
    Abstract271)      PDF(pc) (5407KB)(15)       Save
    To explore the potential mechanism of modified Guizhi Fuling Pill (MGFP) in the treatment of benign prostatic hyperplasia (BPH) by network pharmacology and molecular docking.Then,the BPH model rats were established to verify the key targets from molecular docking.First,the candidate components and target information of plant herbs in MGFP were determined through TCMSP and TCMID databases,while the animal drug Hirudo was determined through relevant literature.Then,the drug-candidate component-target network diagram was constructed using Cytoscape 3.7.1.The potential targets of BPH were determined through GeneCards,OMIM,TTD,DisGeNET and DRUGBANK databases.The intersection targets of components and disease were selected and imported into STRING 11.0 platform,and PPI network diagram was constructed with Bisogenet 3.0.0 plug-in.Subsequently,Metascape platform and KOBAS 3.0 database were used to perform GO functional annotation,KEGG pathway enrichment analysis and network diagram drawing.Then,the core components and key targets with higher degree values in the network diagram were screened,which will be used for molecular docking in AutoDock 4.2.6 and PyMOL 2.2.0 software.Finally,BPH rat model was established by castration combined with subcutaneous injection of testosterone propionate and intragastrical treatment.Then,according to the immunohistochemical results,the expression of BAX in the prostate tissue of rats in each group was observed.The results of network pharmacology analysis showed that a total of 133 candidate components of MGFP were screened out,of which quercetin,β-sitosterol,kaempferol,baicalein,and ellagic acid could act on BPH.The main targets were AKT1,BAX,BCL2,JUN,TGFB1,TNF,IL6,VEGFA and EGFR,which are mainly concentrated in PI3K-AKT signaling pathway and VEGF signaling pathway to participate in the processes of apoptosis,angiogenesis,and inflammation.Molecular docking results showed that all core components and key targets could spontaneously bind,and BAX and β-sitosterol had the strongest binding capacity.Animal experiments showed that compared with the model group,the expression of BAX was significantly increased when the MGFP doses were 6.57,13.14 and 26.28 g/kg (P < 0.01).All these indicated that MGFP might mainly act on the target of BAX to treat BPH.
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    Rapid detection of authenticity and adulteration of bear bile powder by FTIR spectroscopy combined with chemometrics
    YUAN Ming-hao, ZHOU Tao, ZHONG Wen-xiao, ZHOU Qiang, LEI Ke-lu, ZENG Da-fu, LI Jian-gang, GUO Li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (5): 856-863.   DOI: 10.16333/j.1001-6880.2022.5.015
    Abstract260)      PDF(pc) (1379KB)(8)       Save
    To establish a rapid quality evaluation method of bear bile powder,infrared spectroscopy was introduced to distinguish bear bile powder from its counterfeits and adulterants.In addition,the adulterated proportion was predicted by infrared spectroscopy combined with chemometrics.Infrared spectra of 94 batches of bear bile powder,70 batches of its counterfeits (pig bile powder,cow bile powder,goat bile powder,rabbit bile powder,chicken bile powder,duck bile powder and goose bile powder) and 180 batches of its adulterants (bear bile powder adulterated with pig bile powder,bear bile powder adulterated with cow bile powder) were collected.Orthogonal partial least squares discriminant analysis (OPLS-DA) was used to establish the qualitative correction models of bear bile powder,its counterfeits and adulterants.Partial least squares regression (PLSR) was used to establish the quantitative correction models of adulterated proportions of different kinds of adulterants.The accuracy of the qualitative correction model for bear bile powder,its counterfeits and adulterants was 99.64% (calibration set) and 95.65% (verification set),respectively.According to further discriminant analysis,the category of the counterfeit and adulterated bear bile powder could be identified with an accuracy greater than 95%.In the two quantitative correction models,the correlation coefficients of the validation set (R2V) and the root mean square error of prediction (RMSEP) were 0.987 4,2.630 0% (bear bile powder adulterated with pig bile powder) and 0.982 6,3.188 7% (bear bile powder adulterated with cow bile powder),respectively.The three qualitative models and two quantitative models all showed excellent predictive ability.The method of infrared spectroscopy combined with chemometrics established in this study can realize the rapid identification of bear bile powder,its counterfeits and adulterants as well as the determination of adulterated proportion.It also provides a meaningful reference for quality control and evaluation of bear bile powder.
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    Study on chemical constituents and anti-inflammatory activity of Zingiber officinale Roscoe
    LIAO Huai-yu, HAN Jia-ying, HAN Hong-yuan, LIU Wen-bo, CHANG Xia, YANG Jing, ZHANG Hai-yan, ZHAO Tian-zeng
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (5): 818-823.   DOI: 10.16333/j.1001-6880.2022.5.010
    Abstract254)      PDF(pc) (566KB)(23)       Save
    For the first time,the chemical components of national geographical indication product Zingiber officinale Roscoe from Boai County,were systematically separated,so as to provide a basis for its material basis research,development and utilization.Its ethyl acetate fraction in 70% ethanol extract was repeatedly chromatographied on Silica gel column,ODS column and semi preparative HPLC to give compounds 1-12.By using of NMR analysis as well as the literatures,the 12 compounds were identified as (-)-muurola-4,11-diene (1),dibutyl phthalate (2),(2Z)-neral acetal-[6]-gingerdiol (3),6-gingerol (4),6-shogoal (5),8-shogoal (6),10-shogoal (7),10-gingerol (8),6-paradol (9),dihydroferulic acid ethyl ester (10),(3R,5S)-3,5-diacetoxy-1-(4-hydroxy-3-methoxy-phenyl)decane (11),p-hydroxybenzaldehyde (12).Among which,compounds 1,2,10 and 12 were firstly isolated from the plant of Zingiber genus,and compounds 1-4 and 6-12 were firstly isolated from Zingiber officinale Roscoe.The anti-inflammatory activities of compounds 1,3,6,7,9 and 11 were screened.The result showed that compounds 3,6,9 and 11 had obvious inhibitory effect on the NO production in LPS induced RAW 264.7 mouse monocyte macrophages.
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    Inhibitory effects of nisin combined with meropenem on methicillin resistant Staphylococcus aureus
    LI Jing, SHI Lu, LIU Jin, WANG Jun, DA Rong, HAN Bei
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 368-374.   DOI: 10.16333/j.1001-6880.2022.3.002
    Abstract250)      PDF(pc) (1363KB)(11)       Save
    This study explored the antibacterial effect of nisin (NIS) combined with meropenem (MEM) on methicillin resistant Staphylococcus aureus(MRSA).The minimum inhibitory concentration (MIC) was detected by micro broth dilution method,and the fractional inhibitory concentration index (FICI) was calculated by chessboard combined bacteriostasis test to evaluate the inhibitory effect.Crystal violet staining test was used to quantitatively detect the effect of drug combination on the biofilm formation of MRSA isdates.Galleria mellonella model infected by different treated MRSA was established to compare the survival rate.The results showed that the combination of MEM and NIS had synergistic inhibitory effects on the tested three MRSA strains,and the FICI values were 0.375,0.5 and 0.375 respectively.After 6 hours of treatment,both the combination group (MEM+NIS) and the NIS group could inhibit biofilm formation without statistical difference (P > 0.05).The survival rate of G. mellonella showed that after five days,the survival rates of larvae infected by three MRSA strains were 30%,80%,and 30% respectively.For strain Yn2020051 and Yn2020078,the MEM+NIS group had higher survival rate than that of NIS group,MEM group and positive control (PC) group (P<0.05).

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    Study on content of total polyphenols and total anthraquinones in rhubarb and its spectrum-effect relationship of anti-oxidation in vitro
    LI Dong-hui, WU Hong-wei, LI Guo-feng, YANG Xin-rong, LI Xian-wei, SONG Qin-jie, LI Yang, LI Yue-feng
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 541-552.   DOI: 10.16333/j.1001-6880.2022.4.001
    Abstract246)      PDF(pc) (1908KB)(16)       Save
    This research aims to study the total anthraquinone content and total polyphenol content of 20 batches of rhubarb palm decoction pieces,and to preliminarily analyze the spectrum-effect relationship of antioxidant activity in vitro.The total anthraquinone content of rhubarb was determined by HPLC,the total polyphenol content was determined by UV spectrophotometry,DPPH and ABTS methods were used to evaluate the antioxidant activity of rhubarb in vitro.HPLC fingerprint was used to take the common peak as the research object,and cluster analysis,principal component analysis,partial least square analysis,gray correlation analysis and Pearson correlation coefficient method were used to analyze the antioxidant activity.The change of chromatographic peak area before and after the reaction was used as the supplement of spectral analysis.The results showed that the total anthraquinone content was 1.06 ± 0.08 - 4.82 ± 0.12 mg/g,and the total polyphenol content was 4.921 ± 0.21 - 10.02 ± 0.11 mg/g.Cluster analysis and principal component analysis showed that 20 batches of rhubarb samples could be divided into 4 class,namely Longxi County and Lintao County are the first category,Dangchang County and Li County are the first category,Min County and Zhang County are the first category,and Weiyuan County is the first category.Common peaks 7 (aloe emodin-8-O-glucoside),1,10 (emodin),2,9 (aloe emodin) had scavenging effect on DPPH free radical activity,and common peaks 7,1,10,3,8,12(emodin) and 14 (emodin methyl ether) had scavenging effect on ABTS free radical activity.This is basically consistent with the change of common peak area before and after the reaction.Correlation analysis shows that the common peaks 10 and 7 are positively correlated with the activity of scavenging DPPH free radicals,and total anthraquinones are negatively correlated with the activity of scavenging DPPH free radicals.Common peaks 2 and 11 are negatively correlated with the activity of scavenging ABTS free radicals,and total polyphenols are significantly positively correlated with the activity of scavenging ABTS free radicals.This research provides a theoretical basis for the screening of antioxidative active ingredients of rhubarb and the differentiation of rhubarb from different origins.
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    Study on preparation and anti-allergy efficacy of Chinese herbal extracts
    WANG Ling, DONG Yin-mao, ZHANG Shou-wen
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 448-456.   DOI: 10.16333/j.1001-6880.2022.3.012
    Abstract242)      PDF(pc) (1386KB)(7)       Save
    In this paper,six kinds of traditional Chinese medicine:Herba Moslae,Pseudobulbus Cremastrae Seu Pleiones,Radix Angelicae Pubescentis,Rhizoma Sparganii,Catechu,Radix Polygalae were extracted,and the activity of the extract was verified by inhibiting hyaluronidase activity,scavenging free radicals,and inhibiting histamine release.And it was added to the emulsion formula to evaluate the efficacy of soothing.The results showed that the inhibition rate of 6% prescription extract on hyaluronidase was 80.06%,and the scavenging rates on Superoxide anion radical,Hydroxyl radical,and DPPH radical were more than 70%.The histamine release rate of 200 μg/mL group extract was 52%,which indicated that the group extract had certain inhibition or scavenging effect on hyaluronidase,histamine release and three kinds of free radicals.The results of human efficacy evaluation showed that the emulsion with compound extract could significantly reduce the skin heme (P<0.01),reduce the skin water loss (P<0.01),and increase the skin water content (P<0.01).This shows that the emulsion can effectively relieve skin allergic symptoms and enhance skin barrier function.
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    Analysis of medicinal components in the flower of Hibiseu manihot L.
    WANG Rui-jun, TIAN Yu, WU Jia-wen, WANG Yan-feng, JIA Ze-han, BAI Zhen-qing, ZHANG Xiu-juan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 588-597.   DOI: 10.16333/j.1001-6880.2022.4.006
    Abstract242)      PDF(pc) (2302KB)(6)       Save
    The flower of Hibiseu manihot L. has rich flavonoid compositions which have high utilization value in food,medicine and health care.To compare the chemical composition differences in the flowers of H. manihot with different medicinal methods and determine the best medicinal period of H. manihot This experiment uses ultra-high performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) analyzed the complete components of dried flowers,buds and fresh flowers of H. manihot.A total of 141 compounds were identified.Some of the flavonoids and organic acid compounds in the fresh flowers were higher than those in dried flowers and buds.In addition,fresh flowers and dried flowers have more medicinal ingredients and higher content than buds.The results showed that there are differences in the chemical composition of the flowers in different ways of medicine,and it should be picked and used according to the needs.All in all,this research provides a theoretical basis for the rational development and utilization of H. manihot.
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    Phytotoxic eremophilane sesquiterpenes isolated from Ligularia cymbulifera
    CHEN Jia, LI Ming-ming, XIN Hai-jing, ZHENG Guo-wei, PU Shi-biao
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 570-578.   DOI: 10.16333/j.1001-6880.2022.4.004
    Abstract230)      PDF(pc) (1040KB)(7)       Save
    Sesquiterpenes were the main allelopathic active ingredients in Ligularia plants and often exhibit phytotoxic activity.In order to find the major compounds from allelochemicals for developing the eco-friendly natural herbicides,the phytotoxic eremophilane sesquiterpenes in Ligularia cymbulifera were studied.Thirteen eremophilane sesquiterpenes were isolated and purified by several chromatographic techniques from the root of L. cymbulifera.Their structures were identified by physicochemical property and analysis of spectroscopic data,including a new eremophilane sesquiterpenes,ligulacymlactam A(1),3β-angeloyloxy-8β-hydroxyeremophil-7(11)-ene-12,8α(14β,6α)-diolide(2),8β-hydroxyeremophil-7(11)-en-12,8α-olide(3),10β-hydroxy-8β-methoxyeremophilenolide(4),6β,8β-dihydroxyeremophil-7(11)-en-12,8α-olide(5),8β-H-eremophil-3,7(11)-dien-12,8α;15,6α-diolide(6),8β-hydroxyeremophil-3,7(11)-diene-8α,12(6α,15)-diolide(7),8β-methoxyeremophil-3,7(11)-diene-8α,12(6α,15)-diolide(8),eremophil-7(11)-ene-12,8α,14β,6α-diolide(9),8β-hydroeremophil-7(11)-en-12β,8α(14β,6α)-diolide(10),3-(methacryloyloxy)furanoeremophilan-15,6α-olide(11),furanoeremophilan-14,6α-olide(12),10β-hydroxy-6β-isobutyrylfuranoeremophilane(13.The phytotoxic activities against A. thaliana of compounds 1-13 were measured by agar germination method.None of them showed inhibitory activities on seed germination,but some of them could promote the germinate time earlier than blank about 1-2 days.As well as,all compounds showed weak root growth inhibitory activity,and compound 13 was the most active compound (EC50 =44.15±5.21 μg/mL).Further structure-activity relationship analysis suggests that the furanermophilane sesquiterpenes which containing the 10-position hydroxyl group and the 6-position side chain substitution have potential to be the lead compound for eco-friendly natural herbicides.
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    Research progress on chemical constituents,pharmacological activities and clinical application of Euphorbia kansui
    MA Li, MENG Xian-hua, YANG Jun-li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 699-712.   DOI: 10.16333/j.1001-6880.2022.4.018
    Abstract220)      PDF(pc) (1899KB)(14)       Save
    The dry root tuber of Euphorbia kansui T.N.Liou ex T.P.Wang(Euphorbia genus in Euphorbiaceae) is a unique Chinese herbal medicine in China.The main chemical constituents and active components of E. kansui are jatrophane diterpenes,ingenane diterpenes,euphane triterpenes and tirucallane triterpenes,which have many pharmacological activities such as anti-tumor,anti-virus,anti-inflammatory,insecticidal,antioxidant and immune system inhibition.This review comprehensively summarized 102 terpenes and 14 steroids and their structural characteristics,and systematically summarized the pharmacological activity,processing and clinical application of  E. kansui,in order to provide reference for clinical rational drug use,quality control,resource comprehensive utilization and development of  E. kansui.
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    Chemical constituents from Lycopodium fargesii and their anti-osteoporotic activity
    TENG Xi-feng, LIU Ya-lan, YANG Fei, WANG Hai-juan, HE Lin
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (2): 226-231.   DOI: 10.16333/j.1001-6880.2022.2.007
    Abstract220)      PDF(pc) (554KB)(15)       Save
    To investigate anti-osteoporosis active constituents of Lycopodium fargesii Hert.,the ethanol extracts of L. fargesii were isolated by silica gel,MCI,RP-18,Sephadex LH-20 column chromatography and semi-preparative HPLC methods.Eighteen compounds were obtained from the ethyl acetate fraction.Their structures were elucidated as α-onocerin(1),26-nor-8-oxo-α-onocerin(2),serrat-14-en-3β,21α,24-triol(3),serrat-14-en-3β,21β,24-triol(4),1,20-eicosanediol(5),tricosane(6),glycerolmonolinoleate(7),glyceryl linolentate(8),3-(4′-formylphenoxy)-4-methoxybenzaldehyde(9),apigenin(10),4-hydroxybenzaldehyde(11),vanillic acid(12),3-hydroxy-4-methoxybenzoic acid(13),2-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-propan-1-one(14),3-hydroxy-4-methoxyzimtaldehyde(15),8-acetoxy-5-hydroxyumbelliprenin(16),trans-4-hydroxy-2-nonenoic acid(17) and decane-1-thiol(18) by analysis of their NMR and HR-ESI-MS data as well as by comparison with the literature reported data.Compounds 1-18 were isolated from L. fargesii for the first time.Compound 16 displayed significant anti-osteoclasts activity with IC50 value of 1.98 μM.
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    Study on chemical constituents and antibacterial activity of Carpesium faberi
    CHEN Jie, WANG Dan, ZHANG Xiong, PENG Ming-you, XU Ran, YAN Ying, WANG Ying
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 598-605.   DOI: 10.16333/j.1001-6880.2022.4.007
    Abstract218)      PDF(pc) (687KB)(7)       Save
    In order to study the chemical composition and antibacterial activity of Carpesium faberi, 14 compounds were obtained from the ethanol extract of C. faberi by applying various chromatographic techniques.Their structures were elucidated and identified as granilin (1),4α,10α-dihydroxy-1βH,5βH-guai-11(13)-en-12,8α-olide (2),4β,10β-dihydroxy-5α(H)-1,11(13)-guaidien-8α,12-olide (3),4-epi-isoinuviscolide (4),11(13)-dehydroivaxillin (5),carabrone (6),vomifoliol (7),cassipourol (8),4′,5′-dehydrodiodictyonema A (9),(3R)-8-Hydroxylinalool (10),cholest-7-en-3β-ol (11),stigmasterol (12),5,8-epidioxy-5α,8α-ergosta-6,22E-dien-3β-ol (13),stigmasta-5,22-diene-3β,7α-diol (14).Among them,compounds 2 and 7-14 were obtained from this plant for the first time.The antibacterial activity of compounds 1-14 was preliminarily evaluated,and compound 1 showed weak activity against Bacillus subtilis;compounds 6 and 10 showed weak activity against Candida albicans.
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    Study on the chemical constituents and anti-tumor activity of Homalomena occulta
    YIN Wei, HU Qi, LI Xin-zhang, ZHOU Qing-hao, YU Yang, XU Zhen-guo, FAN Gao-fu, ZHANG Guo-sheng
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 563-569.   DOI: 10.16333/j.1001-6880.2022.4.003
    Abstract215)      PDF(pc) (1040KB)(11)       Save
    In order to explore the chemical composition and anti-tumor activity of Homalomena occulta,10 compounds were separated from the ethanol extract of Homalomena occulta by using normal phase silica gel,medium-pressure liquid chromatography,Sephadex LH-20 and other chromatographic separation methods.According to spectral analysis method,the obtained compounds include betulinic acid (1),3β-acetoxyolean-12-en-28-oic acid (2),ursolic acid (3),antriptolactone (4),cleo-lignan C (5),bullatantriol (6),pineapple coriander (7),mucrolidin (8),pinocembrin (9),and 3-(4-hydroxy-3-methoxyphenyl)-propenal (10).Except for compounds 7 and 8,the remaining compounds isolated in this experiment were isolated from Homalomena occulta for the first time.The in vitro cytotoxicity and single-cell gel electrophoresis comparison tests of compounds 2,4,and 9 with the anti-tumor drug methotrexate showed that the anti-tumor cell effects of compounds 2,4,and 9 were significant.The anti-tumor comparative test in mice also showed that it has a strong inhibitory effect on tumor tissue growth.The study of compounds 2,4,and 9 against 4 kinds of tumor cell lines including human lung cancer cells (A549) is reported for the first time.
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    Study on mechanism of Cistanches Herba in the treatment of liver fibrosis based on network pharmacology,molecular docking and experimental verification
    ZHANG Bo-rui, MA Qian-qian, WANG Wen-yi, ZHANG Shi-lei, LIU Tao, ZHAO Jun, MA Long
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 677-686.   DOI: 10.16333/j.1001-6880.2022.4.016
    Abstract210)      PDF(pc) (3306KB)(20)       Save
    To study the mechanism of active components of Cistanches Herba in the treatment of liver fibrosis from the point of view of drugs,diseases and targets.The effective components of Cistanches Herba were collected through traditional Chinese medicine system pharmacology database and analysis platform (TCMSP),traditional Chinese medicine encyclopedia database (ETCM),traditional Chinese medicine research comprehensive database (TCMID),CNKI database,PubMed and other databases.The target genes of active components of Cistanches Herba were obtained by Uniprot database,and the disease genes of liver fibrosis were collected by GeneCards database and OMIM database,the active component targets were intersected with liver fibrosis targets,and the traditional Chinese medicine-active components-disease network was drawn.Protein interaction network (PPI) was constructed by String database and Cytoscape 3.7.1 software.GO function and KEGG pathway were enriched by DAVID database.Animal model of liver fibrosis was established,the contents of LN,HA,PCIII and Col IV in mouse liver tissue were detected by ELISA kit,liver histopathological changes were observed by HE and Masson staining,and the transcription of PI3K and AKT mRNA was detected by real-time fluorescence quantitative PCR.Eight active components of Cistanches Herba,157 targets and 1 005 targets of liver fibrosis were collected and screened,and 92 targets intersected with each other,involving 5 main signal pathways,including cancer signal pathway,hepatitis B virus signal pathway,PI3K-AKT signal pathway,tumor necrosis factor signal pathway,proteoglycan and cancer.The animal experiment showed that compared with the model group,the high,middle and low dose groups of total phenylethanol glycosides of Cistanches Herba (700,350,175 mg/kg) could significantly reduce the contents of LN,HA,PCIII and Col IV in liver tissue of mice with liver fibrosis.The pathological observation of liver tissue showed that total phenylethanol glycosides of Cistanches Herba could reduce hepatocyte injury and collagen fiber deposition.The real-time fluorescence quantitative PCR detection showed that the mRNA expression of PI3K and AKT in the liver tissue of model group was significantly up-regulated compared with normal group.Compared with model group,the mRNA expression of PI3K and AKT in the high,middle and low dose groups of total phenylethanol glycosides of Cistanches Herba significantly decreased,and its mechanism may delay the progression of liver fibrosis by inhibiting the activation of PI3K-AKT pathway.The total phenylethanol glycosides of Cistanches Herba have the effect of anti-fibrosis,which lays a foundation for further study on the pharmacological effects of Cistanches Herba.
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    Study on the antioxidant activity of fermented and aqueous-extracted Pueraria lobata and their effect on delaying Caenorhabditis elegans aging
    ZHAO Dan, WU Di, LI Meng, WANG Chang-tao, ZHANG Jia-chan, WANG Dong-dong
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 639-646.   DOI: 10.16333/j.1001-6880.2022.4.012
    Abstract198)      PDF(pc) (1071KB)(16)       Save
    To explore the application of Pueraria lobata in antioxidant and anti-aging field,two methods of fermentation and aqueous extraction were used to extract the active substances of P.lobata.The biochemical experiments were detected to evaluate the antioxidant activity of the extracts and Caenorhabditis elegans were used as model animal to detect the anti-aging effect.Results showed that 6.8% fermented broth of P. lobata (FBP) had better antioxidant ability than aqueous extract of P. lobata (AEP).The antioxidant ability included the total antioxidant capacity,the scavenging capacity of hydroxyl free radicals and superoxide anions.Compared with control group,FBP could significantly prolong the lifespan of C .elegans (P<0.05),and promote the fecundity of C. elegans by 4.8%.At the same time,the heat-resistant time of C. elegans was increased to 111.6% of the control group.Real-time quantitative PCR results showed that FBP could inhibit the expression of the pro-aging gene daf-2 and up-regulate the expression of the anti-aging gene daf-16.In addition,the FBP promote the expression of the downstream heat-resistant genehsp-16.2 and the antioxidant gene of sod-3.In conclusion,the FBP could prolong the lifespan of C. elegans by improving the antioxidant activity and heat resistance of the C. elegans.The good antioxidant and anti-aging effect of FBP provide a reference for its application in the field of anti-aging related food and cosmetics.
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    Identification and antimicrobial activity of an antagonistic endophytic strain HJ-3 from Polygonatum cyrtonema 
    LYU Cai-yun, XIA Juan, LIN Yong-xiang, LIU Xiao-zhuang, XIANG Ai-biao, ZHENG Ya-wen, BAI Xiao-hui
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 399-406.   DOI: 10.16333/j.1001-6880.2022.3.006
    Abstract195)      PDF(pc) (1442KB)(20)       Save
    In this study,an endophytic strain HJ-3 was screened from Polygonatum cyrtonema,an original medicinal material from Anhui Province.The antagonistic effects of HJ-3 on eight plant pathogenic fungi were observed by five-point confrontation culture method.The activated HJ-3 strain was fermented into fermentation products with different concentrations,its antibacterial activities against four tested bacteria were detected by filter paper diffusion method,and the extracted fermentation products were detected by LC-MS.The results showed that the endophytic bacteria HJ-3 showed obvious antagonistic activities against eight common plant pathogenic fungi,among which the antagonistic activities against seven pathogenic fungi such as Rhizoctonia solani Kühn were obvious,and the antagonistic activities against Collettrichum gloeosporioides Penz was weak.In addition,it was found that the fermentation products of different concentrations had certain antibacterial effects on the four kinds of tested bacteria,among which the antibacterial effects on Staphylococcus aureus and Bacillus subtilis were better.The endophytic strain HJ-3 was identified and named as Bacillus velezensis by morphological analysis and 16S rRNA gene sequencing.A 5,5′-methylenebis(2-tert-butyl-4-methylphenol) phenolic substance and three similar compounds were obtained by LC-MS analysis.The results of this study laid a foundation for the development of endophytic bacteria from Polygonatum cyrtonema,it also provides the basis for the extensive application of endophytic drugs.
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    Progress in biosynthesis and application of L-ergothioneine
    MUKAIDAISI·Maihemuti, CHEN Jian, JIAO Chun-wei, XIE Yi-zhen
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (4): 713-721.   DOI: 10.16333/j.1001-6880.2022.4.019
    Abstract191)      PDF(pc) (865KB)(2)       Save
    L-Ergothioneine (L-EGT) is a sort of uncommon thimidazole amino acid with strong antioxidant activity,which cannot be degrated at high temperature and pH.L-EGT only can synthesized by some bacteria,cynobacteria and fungi,but plants,animal and human unable to synthesized.Mammals absorb L-EGT via transporter OCTN1 which distribution in different tissues,thus diverse tissues may influence concentration of L-EGT.With the unique physiological and pharmacological activities made it have extensive application prospect in the field of medicine,food,health care products and cosmetics.Here,we reviewed the recent advances in biosynthetic pathway of L-EGT,and in-depth exploration its roles in food,human health and diseases.
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    Analysis on chemical components of Thesium chinense Turcz. alcohol extract based on UPLC-Q-TOF-MS/MS 
    ZHOU Si-qian, FANG Yan, TAN Jin-tao, TIAN Jing, HE Miao, MA Dan-feng, LONG Hong-ping
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (10): 1633-1646.   DOI: 10.16333/j.1001-6880.2022.10.001
    Abstract191)      PDF(pc) (2932KB)(10)       Save
    To clarify the chemical constituents of alcohol extract from Thesium chinense Turcz.,ultra performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS/MS) was analyzed in this study.The molecular ion peak information was analyzed by Mass Hunter B.07.00 data processing software.The molecular formula with error within 5×10-6 was compared with the TCM database to identify the compounds,combined with reference the related literature and control comparison,combining the precise relative molecular mass and mass spectrometry fragment information.A total of Fifty four chemical compounds in T. chinense,The main chemical constituents included 16 flavonoids,10 alkaloids,5 diterpenes,5 organic acids and other compounds.Twenty-five compounds such as oxymatrine, 4-O-feruloylquinic acid,quercetin-7-O-glucopyranoside,and quercetin-3-O-neohesperidoside were identified in this genus for the first time.The mass fragmentation pattern of alkaloids,flavonoids and diterpenes was further explored.Using UPLC-Q-TOF-MS/MS technology can quickly and accurately identify the alcohol extract of chemical constituents from T. chinense,which will expand new ideas for further clinical application,and will provide the scientific theory basis for its clinical application and quality control.
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    Study on the chemical constituents from Achillea alpine
    ZHAO Chen-guang, XUE Jin-feng, MA Rui-xiao, LIANG Xu-bo, DU Kun, SI Ying-ying, FENG Wei-sheng, XUE Gui-min
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (2): 185-193.   DOI: 10.16333/j.1001-6880.2022.2.002
    Abstract188)      PDF(pc) (717KB)(13)       Save
    To study the chemical constituents from the whole plant of Achillea alpine L..Various column chromatography,such as macroporous resin,ODS,Sephadex LH-20 and preparative HPLC were adopted to isolate and purify the compounds,and the structures of compounds 1-16 were identified by NMR,MS and other spectroscopic techniques.Sixteen compounds have been isolated from the 95% ethanol extract of A. alpine,and they were identified as (2E,4E)-N-(2-methylbutyl) deca-2,4-dienamide (1),pellitorine (2),(E,E,Z)-2,4,8-decatrienoicacid isobutylamide-8,9-dehydropellitorine(3),N-2′-methylbutyl-(EE)-2,4-decadienam(4),methyl-(E,E)-2,4,9-oxooctadeca-10,12-dienoate(5),(S)-14-(E,E)-10,12-methyl 14-hydroxy-9-oxo-octadeca-10,12-dienoate(6),(EE)-2,4-undecadiene-8,10-diynamide-N-(2-methylpropyl)(7),(EE)-2,4-decadienoic acid p-hydroxyphenethylamide(8),sinapyl alcohol diisovalerate(9),(S)-13-hydroxyoctadeca-(Z,E)-9,11-dienoic acid(10),(EE)-2,4-decadienamide acid p-methoxyphenethylamide(11),erythro-N-isobutyl-4,5-dihydroxy-2- (E)-decenamide(12,3-O-feruloylquinic acid (13),cinnamic acid (14),chlorogenic acid (15),3-O-caffeoyl-5-O-feruloylquinic acid (16).Compound 1 was a new amide.Compounds 4-6,9,10,12,13,16 were isolated from the Achillea genus for the first time.Compounds 8 and 11 were isolated from this plant for the first time.Cytotoxic effects of compounds 1-11 were screened on four different gastric cancer cell lines,and the results showed that compounds 2,5 and 9 had weak activities on MGC-803 cell line at 50 μM with the inhibitory rates at 38.7%,34.7%,31.5%,respectively.
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    Two new lignans from the Rhododendron minutiflorum
    FAN Xian-zhe, ZHU Yang-li, YUAN Rong-wen, DENG Li, WU Nian-rong, ZHANG Li-jun, LIAO Hai-bing
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (2): 177-184.   DOI: 10.16333/j.1001-6880.2022.2.001
    Abstract184)      PDF(pc) (794KB)(17)       Save
    To study the chemical constituents and their α-glucosidase inhibitory activity of Rhododendron minutiflorum.Nine compounds were isolated and purified from the 95% ethanol extract of R. minutiflorum by repeated column chromatography such as silica gel,Sephadex LH-20,ODS and HPLC.These chemical structures were identified as rhodominutinan A (1),rhodominutinan B (2),3,4-di(4-hydroxy-3-methoxybenzyl) tetrahydrofuran (3),venkatasin (4),methyl orsellinate (5),ethyl orsellinate (6),methyl 2,4-dihydroxy-3,6-dimethylbenzoate (7),apigenin (8),kaempferol (9) by spectroscopic data analysis and comparison with literatures reported.In addition,compounds 1 and 2 are new lignans,and 3-9 are isolated from the R. minutiflorum for the first time.The in vitro hypoglycemic activity of the obtained compounds was evaluated by the α-glucosidase inhibitor screening method.The results showed that compounds 8 and 9 display moderate inhibitory activity against α-glucosidase with IC50 values of 57.51±6.35,54.70±3.67 μM,respectively.

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    Study on the differential changes of primary and secondary metabolites between green and ripe Zizyphus jujuba var. spinosa fruits based on principal component analysis
    YANG Xing-jing, LIU Yan-ru , TANG Zhi-shu , SONG Zhong-xing, CHANG Bai-jin, ZHAO Yan-ting, ZHAO Meng-li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (5): 824-835.   DOI: 10.16333/j.1001-6880.2022.5.011
    Abstract180)      PDF(pc) (3101KB)(6)       Save
    In order to characterize the component differentiation from unripe and ripe Zizyphus jujuba var. spinosa,the approach of mass spectrometric technology was adopted to make the coupled chemometric analysis in this experiment.Firstly,the ultra performance liquid chromatography tandem time-of-flight mass spectrometry (UPLC-Q-TOF-MS/MS) technology was utilized to identify the main components from the unripe and ripe fruits.In addition,32 of the primary and secondary metabolites from the two forms of fruits were characterized,and they were classified into 5 kinds of structures.Next,primary metabolites and secondary metabolites from these two forms of fruits were clustered and their varied components were derived via the principal component analysis (PCA).According to PCA analysis,the samples were divided into two categories and 10 of components were selected as the candidate variables to differentia those two forms of fruits.Then,the candidate components from the primary metabolites to secondary metabolites were enriched in their metabolite pathways and biosynthetic pathways via KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway enrichment analysis.At the same time,the candidate components were determined by a mass spectrometry multiple reaction detection (MRM) based methodology.With a good linear relationship from 0.002 3 to 800.00 μg/mL (r<0.99),the average recoveries were 96.38%-104.15% with the RSDs of 1.16%-2.46% (n=6).According to the established methodology,the effects related components from two growing periods of Zizyphus jujuba var. spinosa were oleanolic acid and jujuboside B,which involved in triterpenoids pathways;the flavor-related components were catechin and epicatechin,which involved in flavonoids pathways.
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    Recent progress of plant-derived anti-HIV natural compounds
    YANG Jin-xuan, FANG Hao, CHEN Huan, ZHENG Yong-tang
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (7): 1250-1260.   DOI: 10.16333/j.1001-6880.2022.7.018
    Abstract177)      PDF(pc) (863KB)(6)       Save
    AIDS,also known as acquired immunodeficiency syndrome,is an infectious disease caused by human immunodeficiency virus.At present,there is no drug that can completely eradicate HIV/AIDS,and no related vaccine has been successfully developed.Plant-derived natural products have become an indispensable part of the prevention and treatment of AIDS or lead compounds due to their rich variety,diverse structures,and lower side effects.This article briefly reviews some plant-derived natural products with anti-HIV activity in recent five years,hopes provides potential lead compounds for the development of anti-HIV drugs by summarizes related research progress.
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    An study on the anti-rheumatoid arthritis effects of Chimonanthus zhejiangensis essential oil based on human mast cells
    LI Shu-hang, WANG Wen-cui, YAO Lei
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (增刊1): 33-38.   DOI: 10.16333/j.1001-6880.2022.S.005
    Abstract172)      PDF(pc) (1159KB)(8)       Save
    This study is aimed to explore the inhibitory effect of essential oil from Chimonanthus zhejiangensis on mast cell activation in rheumatoid arthritis and the efficacy of its main monomer.The essential oil was extracted by hydrodistillation,and gas chromatography-mass spectrometry (GC-MS) was used to analyze the volatile chemical compositions and determine the content of the main component.The cell toxicity of essential oil and the main component was tested by cell counting kit 8 (CCK-8).LAD2 was stimulated by C48/80.The degranulation and release of cytokines from LAD2 at different concentrations of essential oil and its main component were detected by linked immunosorbent assay (ELISA).The positive drug methotrexate was selected as the control.The results showed that the main component of essential oil from C. zhejiangensis was eucalyptol,and its content was 0.805 g/mL;essential oil and eucalyptol could inhibit mast cell degranulation at low,medium and high concentrations,and significantly reduced the release of cytokines including IL-4,IL-8,TNF-α and VEGF;the inhibitory effect of essential oil was better than that of eucalyptol at the same concentration,which was close to the effect of the positive drug.In a conclusion,both the essential oil from C. zhejiangensis and eucalyptol can inhibit the degranulation and inflammatory reaction of mast cells.It can be inferred that the essential oil from C. zhejiangensis has the effect on relieving rheumatoid arthritis,in which eucalyptol plays an important role as the main component.
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    Advances in chemical constituents and pharmacological activities of lignans from Kadsura coccinea
    SUN Ya-hui, CAO Chun-ya , JIN An, WU Wei-hua
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 491-504.   DOI: 10.16333/j.1001-6880.2022.3.017
    Abstract167)      PDF(pc) (994KB)(9)       Save

    Kadsura coccinea is an economic plant with medicinal,edible,ornamental and other values.The research on chemical constituents and pharmacological effects of K. coccinea has achieved rapid progress.More than 200 compounds have been reported so far,including 121 lignans.These lignans have various pharmacological effects,such as anti-inflammatory,anti-tumor,anti-HIV,anti-coagulation,anti-oxidation,liver-protection,ect.The chemical constituents and pharmacological effects of lignans in K. coccinea are reviewed here to provide a reference for the further development and utilization.

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    The mechanism of Astragali Radix-Cordyceps on the treatment of IgA nephropathy based on network pharmacology, molecular docking and rat experiments 
    FU Yi, CHEN Bang-ming, LI Xin, FU Yi, WU Hong-ze, LIU Yong-fang
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (9): 1573-1581.   DOI: 10.16333/j.1001-6880.2022.9.015
    Abstract167)      PDF(pc) (1588KB)(21)       Save
    To screen the targets and related signaling pathways of Astragali Radix-Cordyceps in the treatment of IgA nephropathy (IgAN) by network pharmacology,to clarify its mechanism of action,and to verify it experimentally.TCMSP and BATMAN-TCM databases combined with literature mining were used to obtain the active components and targets of Astragali Radix-Cordyceps;the disease targets of chronic IgAN were obtained through GeneCards and OMIM databases;Venny 2.1 was used to draw a Venn diagram of common targets;STRING was used to build a common target interaction network (PPI);Cytoscape 3.7.1 software was used to build an interaction network of Astragali Radix-Cordyceps pills-target;through R language software GO analysis of common targets and KEGG analysis of chronic IgA nephropathy targets were performed to screen out potential pathways and their mechanisms of action were analyzed.Molecular docking technology was used to verify the binding efficacy of the active components of Astragali Radix-Cordyceps and key targets.IgA nephropathy model rats (model group and Astragali Radix-Cordyceps dose group with high,medium and low doses) were taken for 21 days,respectively,and the kidney tissue was collected to detect the expression of VEGFA protein in the kidney tissue of the rats in each group by Western blot.Five bioactive components were screened out from Astragali Radix-Cordyceps,which acted on 37 common targets of IgAN.The core targets were VEGFA,HIF1A,NOS3,and CASP3,which mainly involved cysteine-type steroid binding and apoptosis,endopeptidase activity,estrogen receptor binding,cholesterol binding and other biological processes are mainly enriched in lipid and atherosclerosis signaling pathway,AGE-RAGE signaling pathway,fluid shear stress and atherosclerosis pathway,PI3K-Akt signaling pathway and other signaling pathways.The molecules showed good binding potency between the main components and key targets.Compared with model group,the expression of VEGFA in the high and low dose groups of Astragali Radix-Cordyceps decreased (P<0.05),and there was no significant difference between the high-dose group and the middle-dose group (P> 0.05).Astragali Radix-Cordyceps may act on key targets such as VEGFA,HIF1A,NOS3,and CASP3,and achieve therapeutic effects on IgA nephropathy through fibrosis and other signaling pathways.
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    Research progress on volatile oil of Eucalyptus and its biological activities
    HUANG Li-ping, WU Ying-yao, LAI Jun-jie, ZHOU Zhong-liu
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2022, 34 (3): 505-539.   DOI: 10.16333/j.1001-6880.2022.3.018
    Abstract165)      PDF(pc) (1970KB)(14)       Save
    Eucalyptus is an evergreen tree belonging to the Eucalyptus L. Herit of Myrtaceae family.There are more than 600 types of Eucalyptus in the world,mainly planted in tropical and subtropical regions around the world.Nearly 80 species of Eucalyptus were introduced into China,which mainly cultivated in south China.Guangdong and Guangxi are important production base for Eucalyptus planting.According to pharmacological research,the volatile oil of Eucalyptus showed insecticidal and repellent,anti-bacterial,anti-inflammatory,analgesic,and anti-oxidant activities.Research progress on chemical constituents and biological activities of 948 volatile oils from 120 Eucalyptus species were reviewed in this paper,including 685 terpenoids,29 aliphatic compounds,39 aromatic compounds and 195 other compounds,and in order to make references for further research on the constituents and pharmacological activities of the volatile oil of Eucalyptus.
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