摘要
为了明确密蒙花抗肿瘤药效物质基础,对密蒙花的4种不同溶剂提取物(乙酸乙酯提取物、正丁醇提取物、石油醚提取物、水提取物)进行了抗肿瘤活性的初筛;接着,对具有抗肿瘤活性的提取物进行了分离和纯化,通过NMR、MS、FTIR、UV对所得单体化合物进行了结构鉴定;随后,探讨了单体化合物对体外肿瘤细胞(MCF-7细胞、SGC-7901细胞、BEL-7404细胞)增殖和凋亡的影响;最后,在无细胞体系中检测了单体化合物对DNA TopoisomeraseⅠ(简称DNA TopoⅠ)的活力影响及对DNA的直接切割作用。结果表明,密蒙花4种不同溶剂的提取物均能在一定程度上抑制肿瘤细胞的增殖,分离得到单体化合物为芹菜素、蒙花苷、毛蕊花糖苷和芹菜素-7-O-葡萄糖醛酸苷,其对3种肿瘤细胞均具有较好的抗肿瘤活性,可能是密蒙花抗肿瘤的主要活性成分。其中,芹菜素可显著抑制BEL-7404肿瘤细胞的增殖;芹菜素-7-O-葡萄糖醛酸苷在促进细胞凋亡方面效果较为显著。4种单体化合物均可抑制DNA TopoⅠ。
The antitumor activity of 4 different solvent extracts(ethyl acetate extract,n-butanol extract,petroleum ether extract,water extract)was screened in order to clarify the anti-tumor substance basis of Buddleja officinalis Maxim.The extract with anti-tumor activity was then isolated and purified,while the structures of the monomer compounds were identified by NMR,MS,FTIR and UV.The effects of monomer compounds on the in vitro proliferation and apoptosis of tumor cells(MCF-7 cells,SGC-7901 cells,BEL-7404 cells)were analyzed,while the influence of monomer compounds on DNA TopoisomeraseⅠ(DNA TopoⅠ)Iactivity and the direct cleavage of DNA were evaluated in cell-free system.The results showed that all the 4 different solvent extracts could inhibit the proliferation of tumor cells to a certain extent.The isolated monomer compounds,apigenin,linarin,verbascoside and apigeninpigenin-7-O-glucuronide,displayed good anti-tumor activity against all the three type of tumor cells,and might be the main anti-tumor active ingredient of Buddleja officinalis Maxim.Among them,apigenin could significantly inhibit the proliferation of BEL-7404 tumor cells,while apigenin-7-O-glucuronide showed a significant effect on promoting cell apoptosis.All the four monomer compounds could inhibit DNA TopoⅠ.
作者
李童
李丽媛
李爱鹏
谢欣
何婷婷
莫斯锐
黄上峰
黄锁义
LI Tong;LI Liyuan;LI Aipeng;XIE Xin;HE Tingting;MO Sirui;HUANG Shangfeng;HUANG Suoyi(School of Basic Medical Sciences,Youjiang Medical University for Nationalities,Baise 533000,Guangxi,China;Guangxi Colleges and Universities Key Laboratory of Characteristic Ethnic Medicine of Youjiang Valley,Baise 533000,Guangxi,China;School of Pharmacy,Youjiang Medical University for Nationalities,Baise 533000,Guangxi,China;Key Laboratory of Molecular Pathology(Hepatobiliary Diseases),Youjiang Medical University for Nationalities,Baise 533000,Guangxi,China)
出处
《精细化工》
北大核心
2025年第9期2005-2013,共9页
Fine Chemicals
基金
广西重点研发计划项目(桂科AB18221095)
广西肝胆疾病分子病理学重点实验室资助项目(GXZDSYS-005)
2021年百色市科学研究与技术开发计划课题(百科20211810)
右江民族医学院高层次人才科研项目(01002018079)。
关键词
密蒙花
肿瘤细胞
抗肿瘤
活性筛选
活性单体化合物
中药现代化技术
Buddleja officinalis Maxim
tumor cells
anti-tumor
activity screening
active monomer compounds
modern technology of Chinese medicine
