中国药物警戒 ›› 2023, Vol. 20 ›› Issue (10): 1099-1107.
DOI: 10.19803/j.1672-8629.20230194

• 基础与临床研究 • 上一篇    下一篇

基于弱键化学探究姜黄素-槟榔碱分子互作的“减毒存效”

林晓钰, 项嘉伟, 姚舒畅, 谭森丽, 魏吉昌, 陈子瑜, 陈思宇, 雷海民#, 王鹏龙*   

  1. 北京中医药大学中药学院,北京 102488
  • 收稿日期:2023-03-01 出版日期:2023-10-15 发布日期:2023-10-16
  • 通讯作者: *王鹏龙,男,博士,教授·博导,中药物质基础与复方配伍机制研究。E-mail: wpl581@126.com。#为共同通信作者。
  • 作者简介:林晓钰,女,在读硕士,中药复方物质基础。
  • 基金资助:
    国家自然科学基金资助项目(82073974、82274072); 北京市科技新星计划(Z201100006820026); 中央高校基金科研业务项目(2022-XJ-KYQD-008); 国家级高层次青年人才支持计划; 国家药品监督管理局课题资助

The mechanism of “reducing toxicity and preserving effect” of curcumin - arecoline interaction based on weak bond chemistry

LIN Xiaoyu, XIANG Jiawei, YAO Shuchang, TAN Senli, WEI Jichang, CHEN Ziyu, CHEN Siyu, LEI Haimin#, WANG Penglong*   

  1. School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China
  • Received:2023-03-01 Online:2023-10-15 Published:2023-10-16

摘要: 目的 基于中医临床常用配伍药对,观察姜黄素与槟榔碱分子间相互作用以及聚集体的形成,探究中药配伍过程中的“减毒存效”机制,为临床安全使用槟榔的复方制剂提供参考。方法 应用UV-vis、IR、1H-NMR、PXRD、ITC与电导滴定技术,解析聚集体的形成过程并对其结构表征。通过小鼠急性毒性实验、HepG2细胞模型,观察聚集体形成前后的毒效作用变化。结果 槟榔碱与姜黄素能够在水溶液中,通过弱键作用力以1:1比例聚集形成聚集体。该聚集体能够显著缓和大剂量氢溴酸槟榔碱的刺激作用,同时能够保持姜黄素原有的抗HepG2增殖的活性。结论 本实验从中医药配伍理论和中医临床用药经验实践出发,为中药配伍“减毒存效”研究提供了新的思路。

关键词: 槟榔碱, 姜黄素, 弱键化学, 减毒存效, 中药配伍

Abstract: Objective The interaction between curcumin and arecoline and the formation of aggregates were observed on the basis of the commonly used matching drug pairs of traditional Chinese medicine, so as to explore the mechanism of “attenuating toxicity and preserving effect” during the matching process of traditional Chinese medicine and provide references for the safe use of arecoline compound preparations in clinical practice. Methods UV-vis, IR, 1H-NMR, PXRD, ITC and conductance titration were used to analyze the formation process of the aggregation and characterize its structure. Acute toxicity test in mice and HepG2 cell model were used to observe the changes of toxicity and effect of the aggregation before and after formation. Results The results showed that arecoline and curcumin could form aggregation in 1:1 ratio by weak bond force in aqueous solution. This aggregate can significantly alleviate the stimulative effect of high-dose arecoline hydrobromide while maintaining the original anti-HepG2 proliferation activity of curcumin. Conclusion Based on the theory of TCM compatibility and the experience and practice of TCM clinical medication, this experiment provided a new idea for the study of “reducing toxicity and preserving effect” of TCM compatibility.

Key words: arecoline, curcumin, weak bond chemistry, reducing toxicity and preserving effect, the matching process of traditional Chinese medicine

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