天然产物研究与开发 ›› 2023, Vol. 35 ›› Issue (3): 444-452.doi: 10.16333/j.1001-6880.2023.3.010

• 研究简报 • 上一篇    下一篇

臭牡丹苯乙醇苷类成分的鉴定及体外抗人肺腺癌A549细胞的机制研究

王   芬1,唐   皓2,周厚元1,余湘蓉1,朱克俭2,李顺祥1,余   娜1*,唐   林3*   

  1. 1湖南中医药大学,长沙 410208;2湖南省中医药研究院附属医院,长沙 410006;3湖南中医药大学第一附属医院,长沙 410007
  • 出版日期:2023-03-28 发布日期:2023-03-28
  • 基金资助:
    湖南省自然科学基金(2020JJ5428);湖南省中医药管理局一般项目(201935);中药现代化研究室,湖南中医药大学中药学一流学科项目(校行科字[2018]3号)

Identification of phenylethanoid glycosides from Clerodendrum bungei and its mechanism of anti-human lung adenocarcinoma A549 cell in vitro

WANG Fen1,TANG Hao2,ZHOU Hou-yuan1,YU Xiang-rong1,ZHU Ke-jian2,LI Shun-xiang1,YU Na1 *,TANG Lin3*    

  1. 1School of Pharmacy,Hunan University of Chinese Medicine,Changsha 410208,China;2Hunan Academy of Chinese Medicine,Changsha 410006,China;3The First Affiliated Hospital of Hunan University of Traditional Chinese Medicine,Changsha 410007,China
  • Online:2023-03-28 Published:2023-03-28

摘要:

臭牡丹提取物具有良好的抗肿瘤的作用,为了鉴定臭牡丹提取物的成分及探究其对A549细胞体外抑制的影响,采用超高效液相色谱-质谱联用技术、CCK-8、细胞划痕法、Transwell、Western blot、免疫荧光及流式细胞术等方法进行检测。鉴定了臭牡丹提取物中34个苯乙醇苷类化合物,其中类叶升麻苷含量为32.95%,异类叶升麻苷5.49%。体外实验表明,臭牡丹提取物能抑制A549细胞的增殖、迁移和侵袭,且IC50为0.125 mg/mL,还能下调A549细胞中EphA2、p-AKT、mTOR、p-mTOR、p-GSK-3β和β-catenin的表达,上调EphrinA1的表达,减少EphA2在A549细胞膜与膜质上的表达,并将A549细胞周期阻滞于G1/S期。本研究证实臭牡丹地上部分富含苯乙醇苷类成分,尤以类叶升麻苷和异类叶升麻苷为多,且可通过调控EphA2/Akt/mTOR通路达到抗肺癌作用。

关键词: 臭牡丹, 苯乙醇苷, 肺腺癌细胞, EphA2/AKT/mTOR通路

Abstract:

Clerodendrum bungei extract has a good anti-tumor effect.In order to identify the ingredients of the C. bungei extract and explore its impact on the A549 in vitro,the ultra-high-efficiency liquid chromatography-mass spectrometry technology,CCK-8,cell scratch,Transwell,Western blot,immunofluorescence and flow cytometry methods were used to detect. The 34 phenylethanoid glycosides compounds of the C. bungei extract were identified,of which the content of acteoside was 32.95%,and isoacteoside was 5.49%.The C. bungei extract can inhibit the proliferation,migration and invasion of A549 cellsin vitro,and the IC50 is 0.125 mg/mL.In addition,the C. bungei extract can reduce the expression of EphA2,P-AKT,mTOR,P-mTOR,P-GSK-3β,and β-cateninin in A549 cells,increase the expression of EphrinA1,reducing the expression of EphA2 in A549 cell membrane and membrane quality,and blocke the A549 cell cycle to the G1/S stage.This study has confirmed that the C. bungei is rich in phenylethanoid glycosides,especially acteoside and isoacteoside,and can achieve anti-lung cancer effect by regulating the EphA2/AKT/ mTOR pathway.

Key words: Clerodendrum bungei, phenylethanoid glycosides, A549, EphA2/AKT/mTOR pathway

中图分类号:  R965.2