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    Secondary metabolites of endophytic fungus Letendraea helminthicola derived from Amomum villosum
    ZHANG Jie, LIU Hong-xin, LIU Zhao-ming, LI Sai-ni, CHEN Yu-chan, ZHANG Wei-min , GUO Bo-hong
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 773-778.   DOI: 10.16333/j.1001-6880.2021.5.008
    Abstract372)      PDF(pc) (593KB)(264)       Save
    To study the secondary metabolites of endophytic fungus Letendraea helminthicola derived from Amomum villosum,eight compounds were isolated and purified from the culture of the fermentation by the silica gel,reverse phase gel silica,Sephadex LH-20 and high performance liquid chromatograohy (HPLC),their structures were identified by physical and chemical properties and spectroscopic data.Eight compounds including one new sesquiterpene 11-hydroxyl tricinonoic acid (1) and seven known compounds were isolated and identified as methyl 3-(3,5-di-ter-butyl-4-hydroxyphenyl) propionate (2),gibepyrone F (3),gibepyrone D (4),p-hydroxybenzaldehyde (5),p-methoxyphenylacetic acid (6),m-hydroxyphenylacetic acid (7),ergosterol (8).Compounds 2-8 were first isolated from the genus Letendraea.Compounds 1-5 were evaluated for their cytotoxic activities against human tumor cell lines by the SRB assay and their antibacterial activities against bacteria were evaluated by microdilution method.However,all the measurement compounds showed no antimicrobial and anticancer activities even at the concentration at 100 μg/mL.

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    The quality evaluation of Psidii Guajavae Folium from different areas based on fingerprints and hemometrics
    LI Dan, FENG Jing-wen, CHEN Hong-ping, LIU You-ping, HU Yuan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 899-912.   DOI: 10.16333/j.1001-6880.2021.6.001
    Abstract374)      PDF(pc) (1969KB)(227)       Save
    Psidii Guajavae Folium(PGF) are dry leaves of Psidium guajava Linn.A plant of Myrtle family,mainly distributed in Guangdong,Guangxi,Fujian,Hainan,Sichuan and Yunnan.In this study,the high performance liquid chromatography (HPLC) fingerprint was used to evaluate the quality of guava leaves from different habitats.Similarity evaluation,cluster analysis,principal component analysis and orthogonal partial least squares-discriminant analysis were adopted to analyze fingerprint data.The results showed that 31 batches of PGF have 14 common peaks with similarity ranged from 0.720 to 0.928,among which PGF with a similarity less than 0.8 were mainly produced in Guangxi and Guangdong,while those with a similarity more than 0.9 were mainly produced in Sichuan and Yunnan.According to the cluster analysis and principal component analysis,the samples of PGF could be roughly divided into two types in terms of the origin,namely coastal areas (Guangxi,Guangdong,Fujian,Hainan) and southwest areas (Sichuan,Yunnan),with differences in the quality of PGF from different origins.Orthogonal partial least squares method was used to screen out 7 components with quality differences,including ellagic acid,isoquercetin,guaijaverin,reynoutrin and hyperoside.According to the quantitative analysis of ellagic acid,isoquercetin,guaijaverin,reynoutrin and hyperoside,the total amount of the five components in southwest China outweighed that in coastal areas,which demonstrates a significant difference.In this study,the method combining the HPLC fingerprint of PGF with chemical measurement was simple and accurate,which could provide references for the quality control and evaluation of PGF.

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    Mechanism of safflower on ischemic stroke based on network pharmacology and molecular docking
    LIANG Rui-min, WANG Kai, CHEN Yue, CAO Jin-yi, QIAO Yi, FENG Zhi-jun, YANG Zhi-fu
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1214-1222.   DOI: 10.16333/j.1001-6880.2021.7.017
    Abstract284)      PDF(pc) (2229KB)(210)       Save
    In this study,network pharmacology and molecular docking were used to explore the main active components and targets of safflower in the treatment of ischemic stroke.The common targets of safflower and ischemic stroke disease were searched by TCMSP,Genecards,Venny and DAVID databases,and the interaction network diagram was drawn.GO and KEGG enrichment analysis were performed.AutoDock Tools was used to verify the molecular docking between the main active components of safflower and key targets.Twenty-two safflower active ingredients and 459 related targets were collected from TCMSP database,and the target gene names were converted by Uniprot.Then 73 common targets of safflower active ingredients and ischemic stroke disease were obtained in Venny 2.1.0,and the network diagram of “safflower-active ingredients-cerebral ischemia common target” was constructed.Molecular docking results showed that the main active components showed good affinity to key targets,respectively.Therefore,the combination of the main active components of safflower with key targets to regulate AGE-RAGE,TNF and IL-17 signaling pathways may be an important mechanism of safflower in the treatment of ischemic stroke.

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    Study on the mechanism of Astragalus Radix against liver cancer based on network pharmacology and molecular docking
    YAO Hong, REN Jin-hong, HOU Yu-xin, WANG Yu-xuan, XUE Hui-qing, LI Qing-shan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 1020-1031.   DOI: 10.16333/j.1001-6880.2021.6.017
    Abstract624)      PDF(pc) (3298KB)(181)       Save
    Based on network pharmacology and molecular docking to explore the active ingredients and molecular mechanism of Astragalus Radix anti-liver cancer.Acquire the active components of Astragalus Radix from TCMSP database,predict component targets by Swiss Target Prediction,use Genecards database and OMIM database to collect liver cancer targets,Venny phase maps Astragalus Radix anti-liver cancer targets,String database combined with Cytoscape 3.7.2 software to draw liver cancer targets the protein interaction network (PPI) and the "Astragalus Radix-component-pathway-liver cancer " interaction network,the DAVID database analyzes the function enrichment and pathway enrichment of core target genes.Surflex-Dock software verifies the molecular docking between key components of Astragalus Radix and core targets.MTT method was used to detect the effects of quercetin,calycosin,kaempferol, formononetin,isorhamnetin and jaranol on liver cancer cells (HepG2).The RT-qPCR method verified the relative levels of Jaranol on the expression of TP53,MAPK1,AKT1,IL6,MAPK8 and VEGFA genes.In this study,20 active components of Astragalus Radix were screened,involving 202 targets and 100 KEGG signal pathways,and GO analysis showed 487 biological functions.Network pharmacology analysis Astragalus Radix may play an anti-liver cancer effect through key targets such as TP53,MAPK1,AKT1, IL6,MAPK8 and VEGFA.Molecular docking shows that the target and the component have a certain degree of binding.MTT showed that Jaranol has a stronger inhibitory effect on liver cancer cells (HepG2) than the other five components.RT-qPCR verified that the expression levels of the six genes of Jaranol at different concentrations were all up-regulated,which was consistent with the genes involved in the KEGG pathway analysis.This study preliminarily explored the potential mechanism of Astragalus Radix with multiple targets and multiple pathways in the treatment of liver cancer,and provided a basis for subsequent verification of the molecular mechanism of Astragalus Radix against liver cancer.

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    Ameliorating effect of Mume Fructus on dysbiosis of murine gut microbiota induced by antibiotics
    LI Yi-fei, MA Wan-ting, CAO Yuan, CHEN Yu-gen, WU Xin-hua
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 717-726.   DOI: 10.16333/j.1001-6880.2021.5.001
    Abstract630)      PDF(pc) (2922KB)(178)       Save
    This study aimed to investigate the ameliorating effects of Mume Fructus (MF) on dysbiosis of murine gut microbiota induced by antibiotics, and to supply scientific basis for further development and utilization of Mume Fructus. Forty ICR mice were randomly divided into a blank group of 8 and an intestinal dysbiosis group of 32, which were randomly divided into model, high-dose MF (H), medium-dose MF (Me) and low-dose MF (L) groups. Thirty-two mice with intestinal dysbiosis received respectively treatment for 15 days, and simultaneously antibiotics (ig) from the tenth day. The murine weight was monitored, the pathological changes of tissues were observed by hematoxylin and eosin (HE) staining, and the murine gut miocrobiota determined by high-throughput sequencing and inflammatory factors detected by enzyme-linked immunosorbent assay (ELISA). Compared with normal group, H and Me groups reduced the average body weight and reversed the weight gain induced by antibiotics. The Me group restored the inflammatory markers, TNF-α,IL-1β and IL-6 to normal. Observations from a HE staining experiment demonstrated that H group had gastric irritation. At the phylum level, compared with the model group, the relative abundance of Proteobacteria had decreased in the L and Me groups. Meanwhile, at the genus level, the relative abundance of Lactobacillus and Faecalibaculum had increased in the L and Me groups, and those of Bifidobacterium and Blautia had increased in the L and H groups. This study provided a scientific basis for clinical medication of MF from the perspective of microecology, and revealed its potential as intestinal microecological modulator. 
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    The antioxidant activity in vitro of sulfated polysaccharides from marine sources
    YANG Wen-sheng, YUAN Chun-hong, HAN Hua
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1081-1085.   DOI: 10.16333/j.1001-6880.2021.7.001
    Abstract433)      PDF(pc) (843KB)(170)       Save
    To screen out the marine antioxidants with activity,we extracted and isolated four polysaccharides from Undaria pinnatifida,Porphyra,Sargassum fusiforme and Holothuria scabra through different polar solvents.The antioxidant activities of sulfated polysaccharide were determined via peroxide value (POV),polyphenol oxidase (PPO),and two free radical tests(DPPH·and O2).The results showed that four kinds of sulfated polysaccharides significantly inhibited the peroxidation of lard,scavenged free radicals in DPPH and superoxide anion system,and exhibited considerable antioxidant activities against PPO,with a certain concentration dependence.In conclusion,these four sulfated polysaccharides have the potential to develop into natural antioxidants.
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    Research progress on diterpenes from endophytic fungi
    QUAN Chen-xi, DING Jian-hai
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 878-891.   DOI: 10.16333/j.1001-6880.2021.5.020
    Abstract363)      PDF(pc) (1810KB)(168)       Save
    The diterpenes in plant endophytic fungi have novel structure and remarkable biological activity.Among them,12 kinds of skeleton type compounds,such as taxane type,labdane type,harzianone type,isopimarane type,guanacastane type,fusoporin type,indole diterpene type,ginkgolide type,phomactin type,cyclopiane type,norcyclostane type,abietane type,have various biological activities such as anti-tumor,anti-virus,anti-inflammatory,antibacterial and insecticidal.Through sorting out and analyzing relevant literature,a comprehensive review of 137 diterpenoids and their biological activities produced from plant endophytic fungi,and an introduction to some of the biological activity mechanisms and structure-activity relationships,in order to provide a reference for the better development and utilization of plant endophytic fungi diterpenoids.

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    Research advance on structural modification and structure-activity relationship of iridoids
    KONG Yuan-fang, YANG Bin, HU Yu-long, DONG Chun-hong
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1236-1250.   DOI: 10.16333/j.1001-6880.2021.7.019
    Abstract724)      PDF(pc) (2318KB)(160)       Save
    Iridoids,important active ingredient,are widely distributed in varieties of Chinese herbal medicines and have varieties of pharmacological activities,such as antitumor,anti-inflammatory,hypoglycemic and so on.It is generally recognized that the biological activity and mechanism of iridoids depended on their structures.At present,there is no reports on the summary of the structure modification and structure-activity relationship of iridoids,so it is very important and significant to summarize in details the structure and structure-activity relationship of iridoids for providing new ideas on the study of the structural activities of iridoids.In this review,the relationship between the chemical structure,biological activity,and the mechanism of iridoids by investigating literature research are analyzed and summarized in the world.It will be beneficial to the activity prediction and structure optimization of iridoids,and will provide a research basis for the new iridoid drugs with higher activity in the future.

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    Analysis of polyphenols from Mesona chinensis by UPLC-Q-TOF-MS/MS
    HUANG Jia-jin, HUANG Zhi-lin, CHEN Hong-geng, LIU Kun, WANG Li-kang, ZHI Hui, DING Li-jun, ZHENG Jun-xia
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 758-766.   DOI: 10.16333/j.1001-6880.2021.5.006
    Abstract540)      PDF(pc) (1339KB)(158)       Save
    Meisona chinensis Benth.,a characteristic herb of south of China,is known as “Immortal herb” because of its excellent functions of heat elimination,heat clearing,detoxification and so on.Ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass/mass spectrometry (UPLC-Q-TOF-MS) was selected for the study.A BEH C18 column (2.1 mm × 100 mm,1.7 μm) was used with the mobile phase of eluent (A) MeCN containing 0.1% formic acid and eluent B 0.1% formic acid in water.Q-TOF-MS and electrospray ion (ESI) source were applied for the analysis under the negative ions.Fifty-one compounds were identified including 40 polyphenols,3 terpenoids,and 8 other compounds,whereas 1 phenylpropionic acids,1 lignan dimers,2 lignan trimmers,3 flavonoids and 3 terpenoids were firstly identified in Meisona chinensis Benth.
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    Study on the protective effect of bergenin on acute liver injury in rats based on IL-6/JAK2/STAT3 signaling pathway
    LAN Ying, ZHANG Ke-feng, LIAN Yuan-yu, CHEN Jun-jie, YANG Chao-yue, WANG Yue-feng, GAO Ya
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (9): 1445-1451.   DOI: 10.16333/j.1001-6880.2021.9.001
    Abstract381)      PDF(pc) (832KB)(158)       Save
    To explore the hepatoprotective effect and mechanism of bergenin on acute liver injury induced by CCl4 in rats based on IL-6/JAK2/STAT3 signal pathway.A total of 60 SD rats were randomly divided into normal group,model group,silymarin group (120 mg/kg),and bergenin low,middle and high dose (20,40,80 mg/kg) groups with 10 rats in each group.Rats in silymarin group and bergenin groups were given intragastric administration according to 10 mL/kg,while normal group and model group were given corresponding volume of solvent once a day for a week.Two hours after the last administration,except the normal group,the other groups were intraperitoneally injected with 25% CCl4 olive oil solution 2 mL/kg,to establish the rat model of acute liver injury.After fasting,the blood was taken from the eyeball and the liver was collected after 16 hours of fasting.The levels or activities of alanine transaminase(ALT),aspartate transaminase(AST),albumin(ALB),malondialdehyde (MDA),glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) in serum were determined by biochemical method.The contents of interleukin-6 (IL-6),tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in liver tissue were measured by enzyme-linked immunosorbent assay (ELISA).The pathological changes of liver tissue were observed by HE staining,and the expression level of IL-6 in liver tissue was observed by immunohistochemical (IHC).The protein expression levels of JAK2,p-JAK2,STAT3,p-STAT3,NF-κB p65 and p-NF-κB p65 were detected by Western blot.The results showed that inflammation,necrosis and IL-6 expression of liver tissue were reduced in different doses of bergenin and silymarin groups compared with model group,bergenin significantly reduced the activities or levels of ALT,AST,MDA in serum,TNF-α,IL-6 and IL-1β in liver tissue,up-regulated the activities or levels of ALB,SOD and GSH-Px in serum,and inhibited the expression of proteins related to IL-6/JAK2/STAT3 pathway.In conclusion,bergenin has a protective effect on acute liver injury induced by CCl4 in rats,and the liver protection mechanism may be related to the inflammatory response and antioxidant mediated by IL-6/JAK2/STAT3 signaling pathway.

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    Study on the anti-inflammatory activity of iridoids from Valeriana jatamansi on macrophages
    JIANG Ming-yan, RAO Kai-rui, LIAO Cai-cen, LIU Huan, LI Hong-mei, LI Rong-tao, LIU Dan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 913-920.   DOI: 10.16333/j.1001-6880.2021.6.002
    Abstract326)      PDF(pc) (1262KB)(155)       Save
    Valeriana jatamansi Jones,a traditional herbal medicine used by many ethnic groups in China,has a wide range of medicinal value.Studying the active ingredients of V. jatamansi and its mechanism of action is of great significance to the comprehensive development and utilization of V. jatamansi.In this study,RAW264.7 cells treated with lipopolysaccharide (LPS) were used as an inflammatory cell model to investigate the anti-inflammatory activities of 14 iridoids isolated from the dried roots and rhizomes of V. jatamansi.The results showed that compounds 1,2,3,5,8 and 9 could significantly inhibit the production of NO,among which compounds 1 and 2 Chad the most significant inhibitory effect,with IC50 values of 0.88 and 0.62 μmol/L,respectively.Further experiments showed that compounds 1 and 2 could inhibit the secretion of TNF-α,IL-1β and IL-6,down-regulate the expression of iNOS,COX-2,NLRP3 and the phosphorylation levels of IκBα,STAT3 and mTOR in LPS-induced RAW264.7 cells,but had no significant effect on the MAPKs protein family.In summary,compounds 1 and 2 may reduce the expression of inflammation-related proteins and the secretion of inflammatory factors by down-regulating NF-κB and mTOR/STAT3 signaling pathways,thereby reducing the LPS-induced inflammatory response of macrophages.

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    Study on the chemical constituents of Penicillium crustosum,an endophytic fungus from Ophiocordyceps sinensis 
    JU Feng, LUO Fan, FENG Dan, GUO Da-le, REN Bo, DENG Yun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1147-1155.   DOI: 10.16333/j.1001-6880.2021.7.009
    Abstract414)      PDF(pc) (829KB)(153)       Save
    To investigate the compounds produced by the endophytic fungus Penicillium crustosum from Ophiocordyceps sinensis and their antibacterial activities,16 compounds were isolated and purified by reversed-phase silica gel column chromatography,MCI column chromatography,preparative HPLC,and other methods.Their structures were elucidated on the basis of NMR and MS spectroscopic evidences.The compounds were identified as Ac-L-Leu-L-Pro-OCH31),(E)-3-benzylidene-4-methyl-3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione(2),(Z)-3-benzylidene-4-methyl-3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione(3),cyclopenin(4),(3S)-1,4-benzodiazepine-2,5-diones(5),O-acetyl-β-paxitriol(6),roquefortine C(7),isoroquefortine C(8),aflaquinolone G(9),3-hydroxy-4-phenylquinolin-2(1H)-one(10),viridicatol(11),cyclo(Pro-Leu)(12),N-(phenylmethyl) carbamic acid (13),(5S,6R,7S,8R)-5-amino-(2Z,4Z)-1,2,3-trihydroxybuta-2,4-dienyloxy-pentane-6,7,8,9-tetraol (14),2′,4′-dihydroxy-3′,5′-dimethylacetophenone (15), and conidiogenone B (16).The compounds isolated are mainly benzodiazepines,indole diterpenes and quinolone alkaloids.Compounds 1 and 2 were isolated as new natural products,and compounds 1-4,6,9,12-14 and 16 were isolated from this strain for the first time.

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    Chemical constituents of Dendrobium huoshanense C.Z.Tang et S.J.Cheng
    ZHAO Hong-su, XU Feng-qing, CHEN Xiao-xiao, HU Jiang-miao, ZENG Fan-jun, PENG Dai-yin, WU De-ling
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (9): 1491-1498.   DOI: 10.16333/j.1001-6880.2021.9.006
    Abstract554)      PDF(pc) (459KB)(146)       Save
    To investigate the chemical constituents of Dendrobium huoshanense Tang et Cheng.29 compounds were isolated from this plant by multiple column chromatography,such as silica gel,Sephadex LH-20,MCI gel,Rp-18 and semi-preparation HPLC,their structures were elucidated by means of extensive spectroscopic analysis and identified as follows:4,4′-dihydroxy-3,5-dimethoxybibenzyl (1),batatasin III (2),5,4′-dihydroxy-3-methoxybibenzyl (3),dihydroconiferyl dihydrop-hydroxycinnamate (4),methyl 3-propionate (5),dihydroconiferyl alcohol (6),dihydroferulic acid (7),4-O-β-D-glucopyranosyl coniferyl aldehyde (8),4-allyl-2,6-dimethoxyphenyl glucopyranoside (9),erythrosyringoylglycerol-4-O-β-D-glucopyranoside (10),3,4,5-trihydroxyallylbenzene-3-O-β-D-glucopyranosyl-4-O-β-D-glucopyranoside (11),(7S,8R)-syringylglycerol-8-O-4′-sinapyl ether 4-O-β-D-glucopyranoside (12),3,4-dihydroxy-5-methoxybenzaldehyde (13),p-hydroxybenzoic acid (14),5-hydroxylated isobenzofuran-1(3H)-one (15),3,5-dihydroxy-4-hydroxy benzaldehyde (16),4-hydroxy-3-methoxybenzaldehyde (17),3,4,5-trimethoxyphenol-1-O-β-D-glucopyranoside (18),gastrodin (19),(+)-syringaresinol (20),(+)-syringaresinol-4-O-β-D-glucopyranoside (21),liriodendrin (22),naringenin (23),2,6-dimethoxy-p-benzoquinone (24),5-hydroxymethyl furfural (25),tetrahydro-5-oxo-2-furancarboxylic acid methyl ester (26),methyl pyroglutamate (27),periloyrine (28) and uridine (29).Compounds 5-19,21-29 were isolated from this plant for the first time and 8,10,11,15,16,18,26,28 were isolated from this genus.
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    Terpenes from Carpesium abrotanoides L. and their anti-tumor activity
    YANG Bao-jia, ZENG Zheng-quan, SONG Yu, HAO Xiao-jiang, LI Shun-lin
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 951-955.   DOI: 10.16333/j.1001-6880.2021.6.007
    Abstract350)      PDF(pc) (451KB)(141)       Save
    Nine terpenoids were isolated from the petroleum ether extract of Carpesium abrotanoides L. by various column chromatography.Their structures were identified as 8-hydroxy-9,10-diisobutyryloxy-thymol (1),8,10-dihydroxy-9-isobutyryloxy-thymol (2),9-hydroxy-thymol (3),10-hydroxy-8,9-dioxy-isopropylidene-thymol (4),8-hydroxy-9,10-dioxy-isopropylidene-thymol (5),(3R,6R,7E)-3-hydroxy-4,7-megastigmadien-9-one (6),blumenol A (7),4-(3-oxobut-l-enylidene)-3,5,5-trimethylcyclohex-2-en-l-one (8),loliolide (9) by analysis of their NMR and MS data as well as by comparison with the literature.All the above compounds were isolated from C. abrotanoides for the first time,among which 3-8 were identified from this genus for the first time.All isolated compounds exhibited in vitro cytotoxicity against the HL60,A549,SMMC7721,MCF7 and SW480 cell line at the concertration of 40 μM.In addition,compound 2 displayed significant anti-tumor activity MCF-7,SW480,with the inhibitory rates are 72% and 81%,respectively.
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    Action mechanism of Lysimachiae Herba in the treatment of gout based on network pharmacology and molecular docking
    WANG Bai-ling , LUO Lun, GE Zhen-kai, QIU Jing-ran, WANG Yuan, HUANG Wan-jun, HAO Xin-cai, ZHAO Yong-heng,
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 859-867.   DOI: 10.16333/j.1001-6880.2021.5.018
    Abstract795)      PDF(pc) (2554KB)(139)       Save
    To explore the action mechanisms of Lysimachiae Herba for the treatment of gout disease,network pharmacology and molecular docking method were applied.Ingredients of Lysimachiae Herba and drug targets were detected and fished based on TCMSP,TCMID,ETCM,Sym-Map,BATMAN-TCM database,and the literature data from PubMed,CNKI,and WANFANGD database.The targets related to gout were searched based on GeneCards,TTD,OMIM,and DisGeNET database.The ingredients-gout-target targets were collected by matching ingredients -targets and disease-targets.The ingredients-targets network and protein interaction network (PPI) was drawn through the STRING database and Cytoscape software.The molecular docking was carried out to verify the results of network analysis.Gene ontology (GO) functional enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis were performed by utilizing the CludterProfiler Software package of RStudio software.15 active ingredients,including quercetin,kaempferol,isorhamnetin,etc.,and 99 important targets,including IL6,AKT1,MAPK8,IL1B,JUN,MAPK1, VEGFA,CXCL8,PTGS2,EGF,MMP9,RELA,CCL2,etc.were fished out.Docking results showed that the predicted active ingredients had a good binding activity with the key targets.GO enrichment items were obtained,including the 1 999 biological process,137 molecular functions,and 55 cellular components.And 133 KEGG pathways were obtained,including the TNF signaling pathway,IL-17 signaling pathway,etc.The study revealed that Lysimachiae Herba may play therapeutic effect of gout disease through regulating multiple ingredients,multiple pathways,and multiple targets,which provide a basis for the further study of Lysimachiae Herba.

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    Study on the chemical constituents of Cyperus papyrus
    DUAN Wen-lan, LOU Jia-hao, WANG Qiang, ZHAO Zi-yan, LAI Qi, PEI Shao-fei, ZENG Guang-zhi, YIN Jun-lin
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1129-1136.   DOI: 10.16333/j.1001-6880.2021.7.007
    Abstract816)      PDF(pc) (588KB)(139)       Save
    The aim of the research is to study the chemical components of Cyperus papyrus.Chromatographic techniques such as Sephadex LH-20,normal phase silica gel,MCI and high pressure liquid chromatography (HPLC) were adopted to isolate and purify the compounds,and the spectral methods were used to elucidate their structures.Nineteen compounds have been isolated from the petrol ether and ethyl acetate extraction sections of the methanol extract of C. papyrus including α-cyperone (1),cyperenoic acid (2),isopatchoulenol (3),3,4,8,8-tetramethyl-4,5,6,7,8,8a-hexahydro-1H-3a,7-methanoazulen-4-ol (4),(6S)-patchoulan-4-ene-6-ol (5),(+)-5βH-eudesma-3,11-diene (6),β-sitosterol (7),(24R)-24-ethylcholest-4-en-3,6-dione (8),stigmast-4,22-dien-3-one (9),(24R)-24-ethyl-5α-cholestan-3β,5-diol-6-one (10),stigmasterol (11),stigmast-4-en-6β-ol-3-one (12),stigmasta-3,6-dione (13),stigmast-4-en-3-one (14),cis,cis-9,12-octadecadienoic acid (15),methyl hexadecanoate (16),octacasanoic acid (17),3-nonyloxirane-2-carboxylic acid methyl ester (18) and methyl 9,10-dichlorostearate (19).All the compounds were isolated from C. papyrus for the first time.Compounds 1,2,3,5,6,10,12,13 and 16 could inhibit TNF-α-induced NF-κB activation in plasmid transfected HEK293T cells with the IC50 values between 34.96 and 98.23 μM.
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    Study on the mechanism of action of Folium Mori-Flos Chrysanthemi on hypertension based on network pharmacology and molecular docking
    GUO Jin-chen, WANG Jing, SUN Yu-jie, FENG Ye
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 847-858.   DOI: 10.16333/j.1001-6880.2021.5.017
    Abstract962)      PDF(pc) (2432KB)(138)       Save
    This study aims to explore the potential molecular mechanism of Folium Mori-Flos Chrysanthemi(FM-FC) on the treatment of hypertension by network pharmacology and molecular docking methods.Firstly,the gene chip data was downloaded from GEO database,differentially expressed genes were screened with R language limma package,the effective components and corresponding target proteins of FM-FC were screened from Traditional Chinese Medicine System Pharmacology Database(TCMSP),the intersection targets of drugs and diseases were extracted with Venn software,the construction of "compound-target" network and visual analysis were completed by Cytoscape3.7.2 software,the protein network interaction and topology analysis of key targets were performed by Bisogenet and CytoNCA plug-ins.Then,David database and R language clusterProfiler package were used for GO function enrichment and KEGG pathway analysis of key targets.Finally,the results of active components and key targets were verified by AutoDock Vina software.The results showed that FM-FC acted on 41 targets of hypertension,156 core target information was revealed by topological analysis.A total of 80 enrichment results including 52 biological processes,13 molecular functions and 15 cell composition were obtained through GO analysis.KEGG pathway analysis found 39 items,involving IL-17 signal pathway,fluid shear stress and atherosclerosis signal pathway,TNF signal pathway,etc.The molecular docking results showed that quercetin and luteolin were components that docked well with key targets.We have revealed preliminarily that FM-FC exerts a hypotensive effect through the synergistic effect of "multi-component-multi-target-multi-pathway" in this study,which will lay a foundation for further study of its material basis and mechanism of action.

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    A review of screening methods for acetylcholinesterase inhibitors from natural sources
    XUE Xin-yi, ZHANG Yi, LIU Ya-yue
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 892-897.   DOI: 10.16333/j.1001-6880.2021.5.021
    Abstract534)      PDF(pc) (633KB)(136)       Save
    Acetylcholinesterase inhibitors are currently the first choice for the clinical treatment of AD.With the improvement of science and technology,the screening methods are also in constant innovation.This article introduced the research progress of AD therapeutic targets and drug research based on the"cholinergic damage theory",and then emphatically expounded the current methods that could be used for acetylcholinesterase inhibitors’screening,which including Ellman's colorimetric method based on ultraviolet spectrophotometer,thin layer biological autoradiography method,fluorescence analysis method,and ultra-high performance liquid chromatography-mass spectrometry combined with their principles and advantages or disadvantages.We hoped that it would be more effectively and quickly to screen new acetylcholinesterase inhibitors from natural products by summarizing the experience and keeping innovating.

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    Study on the molecular mechanism of Astragali Radix in treating idiopathic pulmonary fibrosis based on network pharmacology and molecular docking
    ZHAO Meng-ya, JIANG Meng-bi, YANG Xin, ZHANG Hao-yu, LIU Yang, HUANG Gao, CHEN Lei-lei
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (9): 1582-1592.   DOI: 10.16333/j.1001-6880.2021.9.016
    Abstract1279)      PDF(pc) (2264KB)(133)       Save
    To study the molecular mechanism of Astragali Radix for idiopathic pulmonary fibrosis,we used the active ingredients of Astragali Radix as an entry point,based on network pharmacology and molecular docking.Firstly,the active ingredients of Astragali Radix were screened by TCMSP.The potential targets of Astragali Radix chemical components were predicted by Swiss Target Prediction.GeneCards and CTD were used to screen out the related genes of idiopathic pulmonary fibrosis,and obtain the potential targets of Astragali Radix for idiopathic pulmonary fibrosis.Bioinformatics analysis of the potential targets were conducted to clarify the key targets.Secondly,molecular docking (SYBYL 2.1.1) was used to verify the degree of binding between key targets and the chemical components of Astragali Radix.Then,HE staining,Masson staining and ELISA were used to verify the results of network pharmacological enrichment analysis.Finally,through network pharmacology preliminary screening,29 signal pathways and 25 targets of Astragali Radix were obtained for idiopathic pulmonary fibrosis,among which the IL-17 signal pathway,EGFR signal pathway and HIF-1 signal pathway were disease-related pathways.And PTGS2,VEGFA,MMP-9,STAT3 and EGFR were the key targets.Through molecular docking,we found that the six chemical components in Astragali Radix had good combination with the five key targets.Both HE staining and Masson staining suggested that Astragali Radix and its active ingredient folic acid had therapeutic effect on bleomycin-induced idiopathic pulmonary fibrosis in rats,and could reduce the degree of idiopathic pulmonary fibrosis in rats.ELISA showed that Astragali Radix and its active ingredient folic acid could reduce the expression of IL-17 and MMP-9 in serum of rats.This study clarified the key targets and main chemical components of Astragali Radix for idiopathic pulmonary fibrosis through network pharmacology,molecular docking and experimental verification,and provides new ideas and methods for the development of the effective components and mechanism of Astragali Radix for idiopathic pulmonary fibrosis and provides a theoretical basis for the clinical application of Astragali Radix for idiopathic pulmonary fibrosis.

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    Advances in phytochemical constituents and antibacterial and anti-inflammatory activity of Camellia oleifera Abel.
    DUAN Yan, ZHOU Yan-hui, LI Shun-xiang, LI Juan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (9): 1603-1615.   DOI: 10.16333/j.1001-6880.2021.9.018
    Abstract613)      PDF(pc) (867KB)(129)       Save
    Camellia oleifera Abel.,a unique woody oil crop in China,with high edible and medicinal value contained many of chemical compounds such as sterols,triterpenoids,and phenols.Among these constituents,triterpenoids and phenols are the most predominant chemical compounds in C. oleifera.According to pharmacological research,both seed extract of C. oleifera(Camellia oil) and some triterpenoids (tea saponin) and phenols all showed significant antibacterial and anti-inflammatory activities.This article systematically summarizes the chemical compounds and their anti-bacterial and anti-inflammatory activities of C. oleifera,in order to provide a certain theoretical basis for the rational development of C. oleifera resources.

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    Aronia melanocarpa anthocyanins protect SH-SY5Y cells against Aβ1-42 induced oxidative stress and apoptosis through a Nrf2 mechanism
    MENG Ling-shuai, CAO Sen, PENG Lin, MA Li-zhi, MENG Xian-jun, ZHOU Xiao-li
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1086-1095.   DOI: 10.16333/j.1001-6880.2021.7.002
    Abstract264)      PDF(pc) (2616KB)(129)       Save
    We investigated the cytoprotective effects of anthocyanins,including cyanidin-3-O-(galactoside,glucoside,arabinoside,xyloside),from Aronia melanocarpa against oxidative stress and apoptosis induced by Aβ1-42.The MTT assay was conducted by MTT colorimetric assay and cell group was done,oxidative stress related indicators,including reactive oxygen species (ROS),hydrogen peroxide (H2O2),superoxide dismutase (SOD),were measured using ROS,H2O22,SOD detection kit,respectively,apoptosis was detected by Annexin-V-PI/FITC apoptosis detection kit.Besides,the gene transcription and protein expression of antioxidase-related gene nuclear factor erythroid (Nrf2),heme oxygenase-1 (HO-1),quinone oxidoreductase (NQO1) and apoptosis-related genes (Bcl-2,Bax) were analyzed by RT-PCR and Western blot.These results showed that anthocyanins pretreatment significantly inhibited Aβ1-42-induced increase in intracellular ROS,H2O2,and increased the SOD expression through upregulating the Nrf2,HO-1,NQO-1 expression.Apoptosis was significantly inhibited by anthocyanins via down-regulation of Bax and up-regulation of Bcl-2.It can be concluded that high-purity Aronia melanocarpa anthocyanins could protect SH-SY5Y cell from Aβ1-42-induced oxidative stress and apoptosis through a Nrf2 mechanism.

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    Study on chemical constituents from the Chloranthus henryi
    BIAN Yu-ting, CHEN Fang-you, HUANG Wei-ming, ZHANG Rui-zeng, LIU Ding-ping, SHUANG Peng-cheng, LUO Yong-ming
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 956-963.   DOI: 10.16333/j.1001-6880.2021.6.008
    Abstract501)      PDF(pc) (635KB)(128)       Save
    To study the chemical constituents from the Chloranthus henryi and their anti-inflammatory activities in vitro,various column chromatography techniques such as column chromatography on silica gel,Sephadex LH-20 were used to isolate and purify compounds and their structures were identified by modern spectroscopy techniques including NMR and HR-MS spectroscopic data.Some compounds were evaluated for their inhibitory effects on lipopolysaccharide -induced nitric oxide production in RAW264.7 cells.Nineteen compounds were obtained from the dichloromethane extract from Chloranthus henryi and their chemical structures identified as atractylenolid III(1),(1E,4Z)-8-hydroxy-6-oxogermacra-1(10),4,7(11)-trieno-12,8-lactone(2),curcuzederone(3),curcolonol(4),(1R,3S,5S,8S,10R)-14-acetylshizukanolide(5),ent-8(9)-pimarene-20-hydroxy-16-nor-15-oic acid(6),labda-8(17),13-dien-15,12R-olid-19-oic acid(7),(11E)-(4S,5R,9S,10S)-15,16-bisnor-13-oxo-8(17),11-labdadien-19-ol(8),14(15)-bisnor-13-oxolabd-8(17),11(E)-dien-19-oic acid(9),guaianediol(10),N-trans-cinnamoyltyramine(11),N-benzoyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate(12),N(N′-benzoyl-S-phenylala ninyl)-S-phenylalaninol benzoate(13),N-2-phenylethylcinnamamide(14),N-trans-cumaroiltiramina(15),5,7,4′-trimethoxyflavanone(16),2-propenoic acid-3-phenyl-methyl ester(17),trans-cinnamic acid(18),trans-p-hydroxycinnamic acid ethyl ester(19.Compounds 5-19 were isolated form the species for the first time,among which compounds 7 -10,12 and 13 were obtained form genus Chloranthus Swartz for the first time.The in vitro nitric oxide (NO) production inhibitory tests of some compounds showed that compound 2 shows good anti-inflammatory activity with the NO inhibition rate of is 58.74%±8.17% at 10 μmol/L.

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    Study on the secondary metabolites from the deep-sea-derived fungus Neoroussoella sp.and their biological activities 
    ZHONG Jin-qian, CHEN Yu-chan, CHEN Shan-chong, LIU Zhao-ming, LIU Hong-xin, ZHANG Wei-min, YAN Han-jing
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1165-1171.   DOI: 10.16333/j.1001-6880.2021.7.011
    Abstract306)      PDF(pc) (726KB)(125)       Save
    The secondary metabolites of a deep-sea-derived fungus Neoroussoella sp. FS526 and their biological activities were investigated.The solid fermentation extraction of strain FS526 was isolated and purified by silica gel column,Sephadex LH-20 gel column,and high performance liquid chromatography,which led to the isolation of fifteen known compounds.The chemical structures of the isolates were identified by spectrum analysis as amestolkolide B (1),thailandolide B (2),aspergillumarins A-B (3 and 4),de-O-methyldiaporthin (5),4-(2-acetoxyethyl)phenol (6),5,6,8-trihydroxy-4-(1′-hydroxyethyl)isocoumarin (7),sescandelin (8),penicifuran A (9),7-hydroxy-5-methoxy-4,6-dimethylphthalidc (10),pestalotiolactone A (11),2′,4′-dihydroxy-6′-methoxy-3′-methylacetophenone (12),1-(2,4-dihydroxy-6-methoxy-3-methylphenyl)ethanone (13),2,5-dimethylresorcinol (14),and 3,5-dihydroxytoluene (15).All the isolated compounds were firstly reported from the genus Neoroussoella.Compound 1 showed weak cytotoxic activity with the IC50 values of 41.44-77.89 μM,and compound 7 showed strong antioxidant activity with the IC50 value of 13.93 μM.

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    Research progress in application and mechanism of Danshen in the prevention and treatment of liver disease
    YIN Ai-wu, GAO Peng-fei
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 1057-1062.   DOI: 10.16333/j.1001-6880.2021.6.020
    Abstract1235)      PDF(pc) (598KB)(124)       Save
    Danshen is the dry roots and rhizomes of perennial herbs of Labiatae plants of Salvia miltiorrhiza Beg. It had been found that Danshen had showed better effects for the prevention and treatment of cholestatic liver damage,immune liver damage,liver fibrosis,liver cancer and drug-induced liver injury in clinical and pharmacological studies.It was reviewed in this article that the applications and mechanism studies of Danshen for the prevention and treatment of liver disease, which will be helpful for the developing of liver-protecting drugs from Danshen and providing guidelines for clinical rational drug use.

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    Study on the identification,biocontrol and growth-promoting function of endophytic strain BN7 from Chrysanthemum morifolium Ramat ‘Boju’
    LU Juan#, TANG Juan#, WANG Gui-sheng, YU Mei-xia, TANG Jun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (8): 1301-1307.   DOI: 10.16333/j.1001-6880.2021.8.005
    Abstract550)      PDF(pc) (1241KB)(123)       Save
    Plant endophytic bacteria can enhance not only the ability of host plants to resist biological and abiotic stresses,but also the ability of decomposition and absorption of mineral elements such as phosphorus and potassium,thus it confers to promote plants growth.In this article the antagonistic effect of endophytic strain BN7 isolated from Chrysanthemum morifolium Ramat ‘Boju’ was tested on six plant pathogenic fungi,including Curvularia lunata,Fusarium oxysporum,F. graminearum,F. moniliforme,Colletotrichum lagenarium and Pestalotiopsis theae.And its ability of dissolving phosphorus and potassium,producing indoleacetic acid and scavenging DPPH was tested,too.Strain BN7 was identified based on the morphological characteristics,physiological and biochemical characteristics and 16S rDNA sequence analysis.Results showed that endophytic strain BN7 had the ability to inhibit the six plant pathogens mentioned above with varying degrees.The available phosphorus in organic phosphorus fermentation broth and inorganic phosphorus fermentation broth increased to 108.38 mg/L and 68.71 mg/L,respectively.And the available potassium increased to 32.03 mg/L,IAA reached to 164.39 mg/L.The strain had the highest cellulase activity after incubation for three days.The CMC enzyme activity and FPA activity reached 168.78 and 79.87 U/mL,respectively.The DPPH scaveging rate reached 82.13% by fermentation supernatant of BN7 incubated for seven days.According to the morphological characteristics,physiological and biochemical characteristics and 16S rDNA sequence analysis,strain BN7 was identified as Bacillus megaterium.Therefore,strain BN7 is identified as Bacillus megateriumwith the ability of antagonistic effect on plant pathogenic fungi,disolving phosphorus and potassium,producing IAA,and the ability of cellulose degradation.
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    Study on the optimization of the extraction technology by response surface methodology and inhibitory activity of α-glucoside of total saponins from the bran of Chenopodium quinoa Willd.
    DONG Qi , TAN Liang, HU Na, WANG Hong-lun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 935-942.   DOI: 10.16333/j.1001-6880.2021.6.005
    Abstract413)      PDF(pc) (1859KB)(123)       Save
    Response surface methodology was used to optimize the ultrasonic extraction process of saponins from the bran of Chenopodium quinoa Willd.and the inhibitory activity of the extract against α-glucosidase was investigated under the optimal extraction conditions.The enzyme reaction kinetics equation was established to analyze the inhibition kinetics and mechanism.The results showed that the optimal extraction conditions of saponins from quinoa bran were as follows:liquid-solid ratio of 15 mL/g,ultrasonic extraction with 75% ethanol,ultrasonic time of 1.5 h,ultrasonic temperature of 45 ℃.Under these conditions,the extraction yield of saponins from quinoa bran was 2.370% ± 0.022%.α-Glucosidase inhibitory activity of the extract was stronger than that of acarbose (P < 0.05),and the IC50 value was 0.620 ± 0.057 mg/mL.Enzyme kinetics study showed that total saponins extract of quinoa bran was a reversible mixed inhibition type.This study provides a reference for clarifying the mechanism of quinoa bran extract in reducing postprandial blood glucose and a basis for the development and utilization of quinoa bran.

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    Preparation and property study of hydroxypropyl-β-cyclodextrin inclusion complex of Chuanxiong Rhizoma volatile oil
    YANG Yu-ting, LIU Yun-hua, LIU Yu-hong, HUANG Zhi-fang, CHEN Yan, YI Jin-hai
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 734-742.   DOI: 10.16333/j.1001-6880.2021.5.003
    Abstract375)      PDF(pc) (1302KB)(118)       Save
    To improve the poor solubility and stability,Chuanxiong Rhizoma volatile oil-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex was prepared.It was prepared by single-phase method,taking the inclusion rate as evaluation index,and the inclusion process conditions were optimized by orthogonal test.The inclusion complex was characterized by SEM and IR,as well as,the solubility and stability were evaluated.The optimal process conditions for single-phase method to prepare the inclusion complex were as follows: Ethanol concentration: 95%,volatile oil∶HP-β-CD(W/W)=1∶10,HP-β-CD∶ethanol(W/V)=1∶3,the inclusion rate reached 92.34%.The characterization results showed that the inclusion complex had been formed,HP-β-CD significantly improved the solubility of Chuanxiong Rhizoma volatile oil,in addition,the inclusion complex had good stability at 60 ℃ for 10 days.The optimized inclusion process of HP-β-CD inclusion complex of Chuanxiong Rhizoma volatile oil is simple and efficient with good reproducibility and high inclusion rate,which could significantly improve the solubility and stability of Chuanxiong Rhizoma volatile oil.

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    Study on aroma components and antioxidant activity of Dendrobium bensoniae Rchb.f.
    YANG Yu-han, XIE Wen-ting, ZHAO Jie, DU Zhi-zhi
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (8): 1292-1300.   DOI: 10.16333/j.1001-6880.2021.8.004
    Abstract722)      PDF(pc) (922KB)(118)       Save
    In order to explore the aroma composition and antioxidant activity of Dendrobium bensoniae Rchb.f.flower,the volatile extract of D. bensoniae was obtained by solvent-assisted flavor evaporation (SAFE) and the antioxidant activities of its extracts were evaluated by three kinds of free radical scavenging models in vitro combined with SOD activity repair model in human immortalized cortical cells.The chemical composition of the volatiles was analyzed by GC-MS and the relative percentage of each compound was determined by peak area normalization method.Odor active value of each compound was calculated based on its relative percentage and accordingly odor threshold,which indicated the key aroma compounds in D. bensoniae flower.The research results showed that a total of 51 compounds were identified from the flower volatiles,accounting for 90.0% of the total content.Among them,16 key aroma compounds,6 modified aroma compounds and 3 potential aroma compounds were identified,including benzyl alcohol (45.5%),vanillin (17.0%),hexanal (3.4%) and phenylethyl alcohol (2.7%),which responsible for the aroma characteristics of grass,sweet and floral notes of the flower.The material extracted by high concentration ethanol from D. bensoniae flower showed strong antioxidant activity in hydroxyl free radical scavenging,DPPH free radical scavenging,ABTS free radical scavenging bio-assays and SOD activity repair model in human immortalized cortical cells.The results of the present study provide a scientific basis for the research and development of D. bensoniae flower related products and antioxidant substances.

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    Quality evaluation of Yupingfeng Powder based on HPLC fingerprint,determination of multi-index components and chemometrics analysis
    SHEN Ya-jun, AN Qi, DING Xiao-ying, LI Heng-yang, GUO Long, ZHENG Yu-guang, ZHENG Qian, ZHANG Dan
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1121-1128.   DOI: 10.16333/j.1001-6880.2021.7.006
    Abstract276)      PDF(pc) (1072KB)(118)       Save
    To establish an analysis method of Yupingfeng Powder based on HPLC fingerprint combined with chemometrics analysis,and determined the contents of 11 components in it,which provides the scientific basis for quality control of Yupingfeng Powder.The chromatographic column was Shimadzu Inertsil ODS-2 C18 (250 mm× 4.6 mm,5 μm),the mobile phase was composed of the acetonitrile-water solution in gradient elution manner at a flow rate of 1.0 mL/min,the column temperature was set at 30 ℃,the detection wavelength was set at 230 nm.The HPLC fingerprint of 15 batches of Yupingfeng Powder was established,the similarity was more than 0.83,24 common peaks were calibrated and 11 chromatographic peaks were identified.They are prim-O-glucosylcimifugin,calycosin-7-O-β-D-glucoside,cimifugin,5-O-methylvisammioside,sec-O-glucosylhamaudol, calycosin, formononetin, ononin, astragaloside III,astragaloside I,astragaloside II,respectively.The results of content determination were 0.104-0.449,0.048-0.121,0.047-0.111,0.129-0.550,0.017-0.037,0.025-0.053,0.030-0.118,0.009-0.025,0.148-0.615,0.088-0.382,0.073-0.385.The results were analyzed by using SPSS 23.0,SIMCA-P 13.0,and other software to perform HCA,PCA,and OPLS-DA,and other chemometric analyses of 15 batches of Yupingfeng Powder,fifteen batches of samples were grouped into two groups.The established quality evaluation method of Yupingfeng Powder is stable and reproducible and can be used for the quality control and evaluation of Yupingfeng Powder.

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    Research progress of plant O-methoxide flavonoids and O-methyltransferases
    CHEN Jian-hua, LI Xiao-man, YANG Wen-yu, , LIU Jiang
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 1072-1079.   DOI: 10.16333/j.1001-6880.2021.6.022
    Abstract444)      PDF(pc) (756KB)(118)       Save
    Plant flavonoids are important medicinal ingredients,whose biological function is closely related to chemical structure,and its stability,protein affinity and bioavailability can be improved by O-methylation modification,thereby enhancing its medicinal activity.O-Methyltransferase(OMT)catalyzes the synthesis of O-methylated derivatives of flavonoids,which is a key modifying enzyme in the flavonoid metabolism.This article reviews the chemical structure,medicinal function,and mechanism of medicinal value enhancement of plant O-methylated flavonoids.It is summarized in this article the biological function,expression regulation,and potential of plant flavonoid O-methyltransferases,in order to provide new ideas and ways for the further research of plant methylated flavonoids.

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    Study on the mechanism of ginger volatile oil in treating head wind disease based on network pharmacology and molecular docking technology
    YAN Fei, GAO Jia-rong, ZHANG Xiao-fei, ZOU Jun-bo, JIA Yan-zhuo, WANG Wen-fei, SHI Ya-jun
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (6): 1032-1044.   DOI: 10.16333/j.1001-6880.2021.6.018
    Abstract859)      PDF(pc) (3194KB)(118)       Save
    To explore the mechanism of ginger volatile oil in the treatment of head wind disease by the method of network pharmacology and molecular docking.The chemical composition of ginger volatile oil was determined by GC-MS.The targets of ginger volatile oil were predicted by TCMSP and Swiss Target Prediction on-line analysis tools,and the targets of head wind disease were predicted by Drugbank,OMIM and DisGeNET database.Venn diagram was drawn to obtain the intersection of the two.The protein-protein interaction (PPI) network was constructed by using String database,and the intersection targets were visually analyzed by Cytoscape 3.7.2.The R language ClusterProfiler package was used for GO and KEGG enrichment analyses.Finally,the molecular docking of the core targets related to head wind disease was carried out by using Discovery Studio 4.0.53 chemical constituents of ginger volatile oil were detected and 130 targets related to the treatment of head wind disease were predicted.1 361 enrichment items which may be related to the mechanism and 77 enrichment items which may be the pathway of ginger volatile oil in the treatment of head wind disease were obtained by GO and KEGG enrichment analyses respectively.The results of molecular docking showed that the core targets had strong affinity with 2,6,10-dodecatrienal,3,7,11-trimethyl-,(E, E)-,copaene and nerolidol.Ginger volatile oil may play a role in the treatment of head wind disease through APP,OPRM1,ADRA2A and other key targets,and through the regulation of Neuroactive ligand-receptor interaction,Ca2+ signaling pathway,Serotonergic synapse and other signal pathways.The treatment of head wind disease with ginger volatile oil is the result of multi-component,multi-target and multi-pathway,which provides a theoretical basis for further research on the treatment of head wind disease with ginger volatile oil.

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    Study on the chemical constituents from the aerial parts of Blumea balsamifera DC. and their antioxidant and tyrosinase inhibitory activities
    ZHOU Li-qiang, XIONG Yan, CHEN Jun-lei, ZHANG Jia-yu, HAO Xiao-jiang, GU Wei
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1112-1120.   DOI: 10.16333/j.1001-6880.2021.7.005
    Abstract343)      PDF(pc) (800KB)(116)       Save
    To study the chemical constituents from the aerial parts of Blumea balsamifera DC. and their antioxidant and tyrosinase inhibitory activities. Eighteen compounds were isolated and identified from the aerial part of Blumea balsamifera DC. with various chromatographic techniques and spectroscopy methods,which were identified as 7,3′,4′-trimethylquercetin (1),4′,5-dihydroxy-3′,7-dimethoxyflavone (2),luteolin-7-methyl ether (3),rhamnetin (4),(2R,3R)-(+)-3,3′,5,7-tetrahydroxy-4′-methoxydihydroflavone (5),(2R,3R)-(+)-7′-O-methyldihydroquercetin (6),quercetin (7),luteolin (8),eriodictyol (9),isohemiphloin (10),isoquercetin (11),3-methoxyquercetin (12),ursolic acid (13),ursolic acid lactone (14),peroxyergosterol (15),2-hydroxy-4,6-dimethoxyacetophenone (16),2,4-dihydroxy-6-methoxyacetophenone (17),and methyl 3,4-dihydroxyphenyl lactate (18). Among them,compounds 10,14 and 18 were isolated from genus Blumea for the first time,and compound 13 was isolated from B. balsamifera for the first time. The antioxidant and anti-tyrosinase activities of these compounds were screened by using the DPPH free radical method and colorimetric method with L-tyrosine as substrat. The results showed that compounds 3-5,7-12 and 18 have strong antioxidant activities,and compounds 7,13,14,16,17 possessed certain tyrosinase inhibitory effects.

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    Antitumor secondary metabolites of an endophytic fungus Aspergillus terreus TZS-201607 from Pseudostellaria heterophylla
    HU Xiao-feng, CHAI Hai-quan, JIA Lin-chuan, SHAO Lu, LIU Xiao-xiao, CHEN Ye
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1156-1164.   DOI: 10.16333/j.1001-6880.2021.7.010
    Abstract335)      PDF(pc) (708KB)(115)       Save
    The secondary metabolites of the endophytic fungus Aspergillus terreus TZS-201607 isolated from Pseudostellaria heterophyllawere fully studied.A total of 16 compounds were isolated from the EtOAc extracts of the PDB culture broth by means of chromatographic techniques,including silica gel,Sephadex LH-20 gel,reversed-phase and semi-preparative HPLC column chromatography.Their structures were identified as sterigmatocystin (1),5-methoxysterigmatocystin (2),variecoxanthone A(3),chryxanthone A(4),6,8-di-O-methylaverufin(5),6,8-di-O-methylnidurufin(6),6,8,1′-tri-O-methyl averantin(7),(22E,24R)-ergosta-7,9(11),22-trien-3β-ol(8),(22E,24R)-ergosta-4,6,8(14),22-trtraen-3-one(9),(22E,24R)-3β,5α-dihydroxy-ergosta-7,22-dien-6-one(10),(22E,24R)-3β,5α,9α-trihydroxy-ergosta-7,22-diene-6-one(11),(22E,24R)-3α-ureido-ergosta-4,6,8(14),22-tetraene(12),(22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol(13),(22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol(14),demethylincisterol A315)and (17R)-17-methylincisterol(16,by spectroscopic analysis and by comparison with previously reported literatures.Compounds 1-7,12,and 14-16 were isolated from the fungus A. terreus for the first time.The cytotoxicity of compounds 1-16 against A549,BT-549,HeLa,HepG2,MCF-7,and THP-1 cell lines was evaluated.Compounds 6,7,and 14 showed strong inhibitory activity against A549,BT-549,HeLa,and THP-1 cell lines,respectively (IC50<10 μM).

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    Diterpenoids from the Tripterygium wilfordii stems and their biological activities
    ZHOU Xiao-qiong, RAO Kai-rui, CHEN Xuan-qin
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (7): 1137-1146.   DOI: 10.16333/j.1001-6880.2021.7.008
    Abstract435)      PDF(pc) (825KB)(114)       Save
    A new diterpene quinone wiltriptobenzene (1) and nineteen known ones,including triptoquinone H (2),triptoquinone B (3),hinokione (4),triptonoterpene (5),triptonediol (6),triptobenzene A (7),wilforol F (8),triptobenzene B (9),abietatrien-3β-ol (10),triptobenzene S (11),hypoglicin B (12),triregelin H (13),triptophenolide (14),neotriptophenolide (15),16α-hydroxy-19,20-epoxy-19R*-methoxy-kaurane (16),16α-hydroxy-19,20-epoxy-20R*-ethoxy-kaurane (17),16α-hydroxy-19,20-epoxy-19R*-ethoxy-kaurane (18),fischericin D (19),and ent-pimara -8(14),15-diene-19-ol (20) were isolated from the ethyl acetate extract of Tripterygium wilfordii by silica gel,medium pressure liquid chromatography (MPLC),Sephadex LH-20,and HPLC chromatograph.The structures of them were established by extensive spectroscopic methods and comparing the data with those in the literature.Compounds 10,19,and 20 were isolated from T. wilfordii for the first time.The anti-inflammatory of activity of 1~20 was evaluated in LPS-induced RAW 264.7 cells.Anti-tumor activity of 1-20 in vitro against HeLa cell line was examined by MTT method.Compounds 2,3,and 20 exhibited significant activity to inhibit NO production with IC50 values of 2.01,1.70 and 1.77 μmol/L.Compound 11 exhibited weak anti-tumor activity (IC50 = 18.41 μmol/L).

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    Study on the chemical composition and tyrosinase inhibitory activity of Castanopsis ceratacantha
    WANG Ya-feng, LI Si-wen, HE Rui-jie, YANG Bing-yuan, HUANG Yong-lin
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (9): 1499-1505.   DOI: 10.16333/j.1001-6880.2021.9.007
    Abstract354)      PDF(pc) (490KB)(112)       Save
    Study the chemical constituents and their tyrosinase inhibitory activity in the leaves of Castanopsis ceratacantha.The compounds were isolated and purified by Sephadex LH-20,Toyopearl HW-40F,Diaion HP20SS and other column chromatography and HPLC.The structures of compounds were elucidated by spectroscopic data and comparison with literatures.The characteristic compounds in the leaves of C. ceratacantha were screened for tyrosinase inhibitory activity.In the previous research,our group had isolated 11 compounds from the 80% ethanol extract of C. ceratacantha. On the basis of this research,17 compounds were obtained and their structures were identified as protocatechuic acid (1),6-O-galloylarbutin (2),3-methoxy-4-hydroxyphenol 1-O-β-D-(6′-O-galloyl) glucopyranoside (3),valoneic acid dilactone (4),1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (5),pedunculagin (6),casuarictin (7),praecoxin A (8),castalin (9),vescalin (10),chinquapinic acid (11),vescalagin (12),castalagin (13),castacrenin D (14),kaempferol (15),isoquercitrin (16),aviculin (17).All the compounds were isolated from this plant for the first time.Experimental results show that compound 14 has strong tyrosinase inhibitory activity,and other compounds also have better inhibitory activity.
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    Panax notoginseng saponins inhibited the formation of atherosclerotic foam cells in ApoE knockout mice by regulating TLR4/SYK signaling
    ZHAO Pei, LI Yong-hui, GAO Wei, MA Qian, YU Yue-qing, WANG Jie, LU Yong-gang, TIE Yan-qing
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (8): 1267-1273.   DOI: 10.16333/j.1001-6880.2021.8.001
    Abstract334)      PDF(pc) (1390KB)(111)       Save
    Panax notoginseng saponins (PNS) is an active ingredient extracted from the roots of Panax notoginseng,which is widely used in the treatment of atherosclerotic diseases.However,its related mechanism is not completely clear.In this study,we found that PNS has the function of improving blood lipid and inhibiting the formation of atherosclerotic plaque in ApoE-/- mice.Its molecular mechanism is related to TLR4/SYK signaling pathway.Furthermore,in vitro cell experiments showed that PNS could inhibit macrophage phagocytosis and CD36 expression in mouse plaques.Therefore,we believe that PNS can inhibit the formation of foam cells in ApoE-/- mice by inhibiting TLR4/SYK signaling so as to inhibiting the progression of atherosclerosis.

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    Ionones from the “nine steaming nine sun-drying” Rehmanniae Radix Praeparata
    ZHANG Jing-ke, LYU Jin-jin, LI Meng, WEI Jun-jun, ZHENG Xiao-ke, FENG Wei-sheng
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 767-772.   DOI: 10.16333/j.1001-6880.2021.5.007
    Abstract489)      PDF(pc) (687KB)(110)       Save
    Three ionones were isolated from the Rehmanniae Radix Praeparata,which were processed by the traditionally-adopted nine cycles of steaming and sun-drying,by using multiple chromatographic methods and their structures were elucidated as sec-hydroxyaegineticacid-2-O-β-D-glucopyranoside,frehmaglutin A,dihydroxy-β-ionone,from their spectral data and physicochemical properties.Among them,compound 1 is a new ionone glycoside.Compounds 2 and 3 were isolated from the Rehmanniae Radix Praeparata for the first time.The effect of compounds 1-3 on Human malignant melanoma A375 cell was investigated by MTT.The results showed that compounds 1-3 (25 μM) significantly inhibited the cell activities of A375 cells.

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    Mechanism of olibanum in the treatment of acute kidney injury based on network pharmacology and in vitro cell experiment verification
    BAI Juan, ZHANG Yan, HONG Shu-xia, SHI Jin-ping, XU Li-ting, WANG Fang
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2023, 35 (9): 1613-1623.   DOI: 10.16333/j.1001-6880.2023.9.015
    Abstract308)      PDF(pc) (2101KB)(110)       Save
    To study the mechanism of olibanum on acute kidney injury (AKI) based on network pharmacology,and establish an in vitro model of human renal tubular epithelial cells (HK-2) according to the results.To search 223 drug targets through the TCMSP database and the Swiss Target Prediction database,then using the OMIM,DisGeNet,DrugBank and GeneCards database to collect 1 245 disease targets,72 drug-disease targets were obtained through the Venn diagram tool.Protein interaction PPI network was constructed by String database;GO analysis and KEGG pathway analysis were performed using DAVID database;Cytoscape 3.7.2 software was used to construct the network diagram;Molecular docking was performed by Autodock.Involving Toll-like receptor、TNF、NF-kappa B and other signaling pathways.Based on this,the proliferation of HK-2 was detected by cell counting kit-8 (CCK-8) method,and the grouping was determined.The rate of cell apoptosis was detected by Hoechst33258 fluorescent staining,and the quantitative real time polymerase chain reaction (Q-PCR) was used to detect the relative expression of MAPK3 and PPARG mRNA.The experimental results showed that in CCK-8 experiment,compared with the model group,the cell viability in low,medium and high dose groups decreased gradually (P <0.05);Hoechst33258 experiment,ELISA experiment and Q-PCR experiment,compared with the model group,the cell apoptosis rate,the capacity of cellular inflammatory factors and the molecular weight and mRNA expression of MAPK3 and PPARG protein decreased significantly (P <0.05).In conclusion,olibanum has the characteristics of multi-target and multi-pathway,which provides a basis for the clinical application of this drug.
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    Study on UHPLC fingerprint and chemical pattern recognition of Uncariae Ramulus Cum Uncis
    HUANG Wen-wen, WANG Xiao-ming, GUO Ya-qing, HAN Li-feng, HUANG Yu-hong, PAN Gui-xiang
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (5): 727-733.   DOI: 10.16333/j.1001-6880.2021.5.002
    Abstract309)      PDF(pc) (1316KB)(109)       Save
    The UHPLC fingerprints and chemical pattern recognition were studied to evaluate the quality of Uncariae Ramulus Cum Uncis(URCU).The chromatographic separation was performed on an ACQUITY UPLC HSS T3 column (2.1 mm × 100 mm,1.8 μm).Acetonitrile-0.1% formic acid solution was used as mobile phase with gradient elution.The detection wavelength was set at 254 nm,the flow rate was 0.3 mL/min,the injection volume was 2 μL,and the column temperature was 30 ℃.The chemical pattern recognition of similarity evaluation,cluster analysis,principal component analysis and orthogonal partial least squares analysis were used to analyze and evaluate the quality of URCU.The established URCU UHPLC fingerprint identified 15 common peaks and 7 common peaks could be identified using standards,including chlorogenic acid, isomitraphylline, isorhynchophylline,rhynchophylline, geissoschizine methylether,hirsuteine and hirsutine.The results about the chemical pattern recognition showed that the similarities of those fingerprints were between 0.850 and 0.995.Furthermore,the quality difference of those URCU was mainly caused by 5 common peaks according to the results of orthogonal partial least squares discriminant analysis.In conclusion,the fingerprints combined with chemical pattern recognition provide a simple and accurate analytical method for the quality evaluation of URCU.
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    Study on the mechanism of artesunatum-puerarin combination in interventing COVID-19 cardiovascular complications based on network pharmacology
    DENG Shuo-qiu, TIAN Ya, CHEN Li-na, SHEN Shuo, YANG Yuan-min, ZHANG Yu, QU Shui-qing, ZHENG Zhong-yuan, LIU Hui, WANG Xi, LI Hong-mei, LI Yu-jie
    NATURAL PRODUCT RESEARCH AND DEVELOPMENT    2021, 33 (增刊1): 70-80.   DOI: 10.16333/j.1001-6880.2021.S.009
    Abstract917)      PDF(pc) (2665KB)(109)       Save
    More than 50 million confirmed coronavirus disease 2019 (COVID-19)-related cases have been reported across the world.There is high incidence of cardiovascular complication and a high mortality rate among patients.This study aims to predict and explore the potential pathways and mechanistic targets of artesunate-puerarin combination in the intervention of COVID-19 cardiovascular injury through network pharmacology and molecular docking.Firstly,the related targets of SARS-CoV 2 were collected from GenCards and UniProt.And the related targets of Artesunate and Puerarin were collected and predicted from TCMSP and Swiss target prediction.Secondly,protein-protein interaction of common targets was analyzed by STRING.GO and KEGG enrichment analysis were performed by DAVID.At last,Vina was used for molecular docking of compounds and key targets including ACE2,TMPRSS2,SARS-CoV-2 3CL hydrolase and S protein.A total of 16 key targets were collected.GO enrichment analysis collected 100 biological processes,14 cell compounds and 32 molecular functions (P<0.05).According to the results,Artesunate and Puerarin may regulate the body processes through multiple targets and pathways.We predicted that,on the one hand,two monomer compositions may prevent the process of virus invasion and proliferation.On the other hand,they can also inhibit cytokine storm and protect cardiovascular from injury.Two compositions play a role on protection of COVID-19 cardiovascular damage.Based on these results,we obtained the potential protection mechanisms of Artesunate-Puerarin combination,which would laid a solid foundation for the subsequent development and research,and provide the basis for expanding clinical existing treatments and reference.

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