摘要
【目的】基于王三虎教授的"燥湿相混致癌说"探讨半边莲治疗癌症的作用及物质基础,分析中药半边莲提取物的化学成分,为进一步研究其抗癌的活性成分提供依据。【方法】运用硅胶柱层析、硅胶薄层层析、反相RP-C18柱层析、MCI柱层析、高效液相等多种色谱手段对半边莲展开系统的化学成分研究,并通过各种波谱、光谱手段鉴定各化合物的结构。对分离所得的化合物,采用人乳腺癌细胞MCF-7和人胃癌细胞MGC-803模型进行抗癌活性评价。【结果】从半边莲中分离鉴定得到6个化合物,分别为:matairesino(1)、(8S,9S,8’S)-4,4’-Dihydroxy-3,3’,9-trimetoxy-9,9’-epoxylignan(2)、3β-hydroxyhop-22(29)-ene(3)、parietin(4)、chrysophanol(5)、gaultheriadiolide(6)。木脂素类化合物1、2在20μmol/L时,细胞抑制率大于50%。【结论】木脂素类化合物1、2具有潜在的抗胃癌和乳腺癌活性,其中化合物2活性最好,对MGC-803细胞增殖活性的半数抑制浓度(IC50)为9.2μmol/L。
Objective To explore the effect and material basis of Lobelia chinensis Lour. in the treatment of cancer based on professor WANG San-Hu’s interweaved dryness and dampness caused carcinogenesis theory, and analyze the chemical constituents of Lobelia chinensis Lour. extracts,so as to provide basis for further study of its anticancer active ingredients. Methods The chemical constituents of Lobelia chinensis Lour. were systematically studied by silica-gel column chromatography,silica-gel thin-layer chromatography(TLC),RP-C18 reversedphase column chromatography,MCI gel column chromatography and high-performance liquid chromatography,and the structures of each compound were identified by various spectrum and spectral methods. The antitumor activity of the isolated compounds was evaluated by MCF-7 human breast cancer cell and MGC-803 human gastric cancer cell models. Results Six compounds were isolated and identified from Lobelia chinensis Lour.,which were as follows:matairesino(1),(8 S,9 S,8’S)-4,4’-Dihydroxy-3,3’,9-trimetoxy-9,9’-epoxylignan(2),3β-hydroxyhop-22(29)-ene(3),parietin(4),chrysophanol(5),gaultheriadiolide(6),When lignans compounds1 and 2 were 20 μmol/L,the cell inhibition rate was more than 50%. Conclusion Lignans compounds 1 and 2 show potential antitumor activity against gastric cancer and breast cancer, and compound 2 shows the best antiproliferative activity against MGC-803 cell line with a half-maximal inhibitory concentration(IC50)of 9.2 μmol/L.
作者
王雪梅
吴凡伟
李彦荣
WANG Xue-Mei;WU Fan-Wei;LI Yan-Rong(Guangzhou University of Chinese Medicine,Guangzhou 510405 Guangdong,China;Shenzhen Bao’an Traditional Chinese Medicine Hospital(Group),Shenzhen 518100 Guangdong,China)
出处
《广州中医药大学学报》
CAS
2022年第1期171-176,共6页
Journal of Guangzhou University of Traditional Chinese Medicine
基金
深圳市宝安区基础研究项目(编号:2019JD293)
广东省中医药局科研项目(编号:20182129)
深圳市科创委资助项目(编号:JCYJ20180302144457509)。
关键词
燥湿相混致癌说
半边莲
本脂素类
抗癌
胃癌
乳腺癌
王三虎
化合物鉴定
interweaved dryness and dampness caused carcinogenesis theroy
Lobelia chinensis Lour.
lignans
anticancer
gastric cancer
breast cancer
WANG San-Hu
compound indentification