绿茶多酚在新药设计中的应用研究  

Application of Green Tea Polyphenols in New Drug Design

作　　者：徐斯盛 郭抗萧 臧婧蕾 周羽 XU Sisheng;GUO Kangxiao;ZANG Jinglei;ZHOU Yu(ChangSha Health Vocational College,Hunan Changsha 41000)

机构地区：[1]长沙卫生职业学院,湖南长沙410001

出　　处：《生物化工》2020年第6期92-94,共3页Biological Chemical Engineering

基　　金：湖南省教育科学研究工作者协会“十三五”规划2020年度立项课题(XJKX20B056)。

摘　　要：目的:设计合成基于表没食子儿茶素没食子酸酯(EGCG)这一主要成分的化合药物,以有效抑制癌细胞的活性与增殖。方法:采用绿茶多酚中EGCG作为原成分,经过甲基化、葡萄糖醛酸化和硫酸化等化学反应得到没食子儿茶素(EGC)母体,由药理学机制出发采取药物制备策略合成药物。选用噻唑蓝试验,以4,6-联脒-2-苯基吲哚(DAPI)染色与细胞凋亡(Annexin V-FITC/PI染色)检测验证EGCG合成药物对肝癌HepG2细胞活性及增殖的抑制效果。结果:EGCG合成药物对肝癌HepG2细胞活性及增殖具有显著抑制作用。结论:绿茶多酚的抗癌细胞活性可通过进一步地激发、转移来充分挖掘其性能,目前在转变成治疗药物上仍存在对时间与剂量严重依赖的缺陷,实际中有待于确定其真正用量以及药物学原理。Objective:To design and synthesize a compound drug based on the main component of Epigallocatechin gallate(EGCG)to effectively inhibit the activity and proliferation of cancer cells.Methods:the EGCG in green tea polyphenols was used as the original component,and then methylated,glucuronized and sulfated to obtain the parent of EGC.Based on the pharmacological mechanism,the drug was synthesized by drug preparation strategy.MTT assay,4,6-diamidino-2-phenylindole(DAPI)staining and Apoptosis(Annexin V-FITC/PI staining)detection were used to verify the inhibitory effect of EGCG on the activity and proliferation of HepG2 cells.Results:the results showed that EGCG synthetic drugs could significantly inhibit the activity and proliferation of HepG2 cells.Conclusion:the anticancer activity of green tea polyphenols can be further stimulated and transferred to fully tap its properties.At present,there are still some defects in the transformation of green tea polyphenols into therapeutic drugs,and the actual dosage and pharmacological principle need to be determined.

关 键 词：绿茶多酚 EGCG合成药物 MTT试验 抑制 

分 类 号：R91[医药卫生—药学]