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

关键词:  雷公藤, 物质基础, 分离纯化, 结构鉴定, 抗肿瘤活性

Key words:  Tripterygium wilfordii, material basis, separation and purification, structure identification, anti-tumor activity

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 IC₅₀值分别为35.6、14.3、28.8 μmol·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。

Abstract:

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 as 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-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(IC₅₀ values of SH-SY5Y,Hel,K562 were 35.6,14.3,28.8 μmol·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.