中国药物警戒 ›› 2022, Vol. 19 ›› Issue (7): 728-732.
DOI: 10.19803/j.1672-8629.2022.07.07

• 基础与临床研究 • 上一篇    下一篇

何首乌醇提物及单体体外肝细胞毒性研究

陈子涵1, 杨建波2, 陈智伟1, 马双成2#, 魏锋2, 孙华1,*   

  1. 1中国医学科学院北京协和医学院药物研究所,北京100032;
    2中国食品药品检定研究院,北京100050
  • 收稿日期:2021-08-04 出版日期:2022-07-15 发布日期:2022-07-12
  • 通讯作者: *孙华,女,副研究员,肝脏病药理学。E-mail：sunhua@imm.ac.cn。#为共同通信作者。
  • 作者简介:陈子涵,女,在读硕士,肝脏病药理学。
  • 基金资助:
    国家自然科学基金资助项目（81773874; 81973476）; 国家重点研发计划（2019YFC1708901）; 中国医学科学院医学与健康科技创新工程重大协同创新项目（2017-I2M-1-013）

Hepatotoxicity of alcohol extract Polygoni Multiflori Radix and related monomer compositions in liver cells

CHEN Zihan1, YANG Jianbo2, CHEN Zhiwei1, MA Shuangcheng2#, WEI Feng2, SUN Hua1,*   

  1. 1Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100032, China;
    2China Institute for Food and Drug Control, National Institutes for Food and Drug Control, State Food and Drug Administration, Beijing 100050, China
  • Received:2021-08-04 Online:2022-07-15 Published:2022-07-12

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摘要： 目的 利用体外实验研究何首乌70% 醇提物、不同洗脱组分及从组分中分离获得的部分单体化合物的肝细胞毒性作用。方法 培养人肝癌细胞（HepG2细胞）及正常人肝细胞（L02细胞）,MTT比色法检测细胞存活率,流式细胞术分析肝细胞凋亡及细胞周期情况。结果 何首乌70% 醇提物的95%乙醇洗脱组分（HSW-D）及从该组分中分离获得的单体化合物芦荟大黄素,作用HepG2细胞48 h,表现显著肝细胞毒性作用;作用L02细胞48 h,HSW-D仍表现肝细胞毒性活性,芦荟大黄素有降低L02细胞存活率的趋势;流式细胞术结果显示,HSW-D 能够引起肝细胞S期阻滞。何首乌70%醇提物、其他洗脱组分、从组分中获得的2个二苯乙烯苷类成分、2个酚类成分及大黄素甲醚、大黄酸、大黄素单蒽酮等10个单体化合物,未表现明显的肝细胞毒性作用。结论 何首乌醇提物中的脂溶性成分含有其毒性物质,芦荟大黄素是其毒性物质基础之一。

关键词: 何首乌, 肝毒性, 芦荟大黄素, 细胞周期, 肝细胞

Abstract: Objective To investigate the hepatotoxicity of 70% alcohol extract of Polygonum multiflorum, different eluted components and some monomer compounds isolated from the components in vitro. Methods The cell viability of HepG2 and L02 cells were detected by MTT colorimetry. Hepatocyte apoptosis and cell cycle were analyzed by flow cytometry. Results Significant toxicity in HepG2 cells was observed in 95% ethanol-eluted component (HSW-D) of 70% alcohol extract of Polygonum multiflorum and the monomer compound aloe emodin obtained from the component with 48 h treatment. Furthermore, significant toxicity of HSW-D was also presented in L02 cells after 48 h treatment. In addition, cell proliferation of HepG2 and L02 cells were inhibited through S-phase arrest. In comparison, little toxicity in HepG2 and L02 cells were observed in the 70% alcohol extract, other eluted components, two stilbene glycosides, two phenols and 10 monomer compounds such as chrysophanol, emodin methyl ether, rhein acid and emodin monanthrone of Polygonum polygonum. Conclusion The toxic substances were presented in the liposoluble constituent of alcohol extract of Polygonum multiflorum, by which aloe emodin is one of the essential toxic elements .

Key words: Polygoni Multiflori Radix, hepatotoxicity, Aloe emodin, cell cycle, liver cells

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