雷公藤提取物中主要物质基础及其抗肿瘤活性研究  

Main material basis and anti-tumor activities of Tripterygium wilfordii extract

作　　者：胡丹 丁同同 李江[1,2] 邓璐璐[1,2] 吴树燕 穆淑珍[1,2] HU Dan;DING Tongtong;LI Jiang;DENG Lulu;WU Shuyan;MU Shuzhen(State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang 550014,China;Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550014,China;School of Pharmaceutical Sciences,Guizhou Medical University,Guiyang 550025,China)

机构地区：[1]贵州医科大学省部共建药用植物功效与利用国家重点实验室,贵阳550014 [2]贵州省中国科学院天然产物化学重点实验室,贵阳550014 [3]贵州医科大学药学院,贵阳550025

出　　处：《广西植物》2022年第9期1514-1521,共8页Guihaia

基　　金：贵州省科技计划项目(黔科合基础-ZK[2021]一般516);贵阳市科技计划项目([20151001]药14号)。

摘　　要：为进一步阐明雷公藤中的主要物质基础,并评价其抗肿瘤活性。该研究采用柱层析、HPLC等技术,对雷公藤提取物进行研究。结果表明:(1)从雷公藤95%乙醇提取物中分离得到12个化合物,根据理化性质及波谱数据鉴定各化合物的结构分别为α,β-amyrenone(1)、3β-acetoxyolean-12-en-28-oic acid(2)、antriptolactone(3)、ω-hydroxypropioquaiacone(4)、3-(4-hydroxy-3-methoxyphenyl)-propenal(5)、3-methoxy-4-hydroxy phenylethanol(6)、vanillin(7)、3,4,5-三甲氧基苯酚(8)、对羟基苯甲酸(9)、对羟基苯甲醛(10)、vanillyl alcohol(11)、2,6-dimethxy-1,4-benzoquinone(12)。其中,化合物1、2、5、12为首次在该属植物中分离得到。(2)采用噻唑蓝(MTT)法对12个化合物进行抗SH-SY5Y细胞株、K562细胞株和Hel细胞株3种肿瘤细胞系细胞增殖活性的筛选,并对活性较好的化合物12进行Hoechst荧光染色和促凋亡作用的检测发现,化合物2、3、5、12具有一定的抗肿瘤活性,其中化合物12的抗肿瘤活性最为显著(SH-SY5Y细胞、Hel细胞、K562细胞的IC_(50)值分别为35.6、14.3、28.8μmol·L^(-1))。该研究结果进一步丰富了雷公藤的化学成分,发现了1个具有明显抗肿瘤活性的单体物质,为雷公藤的进一步开发提供了科学依据。In order to clarify the main material basis of Tripterygium wilfordii and evaluate its anti-tumor activity.This study used column chromatography,HPLC and other separation materials and techniques.The results were as follows:(1)A total of 12 compounds were isolated from 95%ethanol extract of T.wilfordii,and according to the physicochemical properties and spectral data,the structures of the compounds were identified asα,β-amyrenone(1),3β-acetoxyolean-12-en-28-oic acid(2),antriptolactone(3),ω-hydroxypropioquaiacone(4),3-(4-hydroxy-3-methoxyphenyl)-propenal(5),3-methoxy-4-hydroxy phenylethanol(6),vanillin(7),3,4,5-trimethoxyphenol(8),p-hydroxybenzoic acid(9),p-hydroxybenzaldehyde(10),vanillyl alcohol(11)and 2,6-dimethxy-1,4-benzoquinone(12).Among them,compounds 1,2,5 and 12 were isolated from this genus for the first time.(2)In terms of biological activity,their anti-tumor activities in vitro were screened for the SH-SY5Y cell line,K562 cell line and Hel cell line by MTT method,and Compound 12 with better activity was subjected to Hoechst fluorescent staining to detect its pro-apoptotic effect.The results showed that compounds 2,3,5 and 12 had certain anti-tumor activity,of which Compound 12 had the most significant anti-tumor activity(IC_(50) values of SH-SY5Y,Hel,K562 were 35.6,14.3,28.8μmol·L^(-1)).This study further enriches the chemical components of T.wilfordii,and discoveres a monomer substance with obvious anti-tumor activity,which provides a scientific basis for the further development of T.wilfordii.

关 键 词：雷公藤 物质基础 分离纯化 结构鉴定 抗肿瘤活性 

分 类 号：Q946[生物学—植物学]