冷蒿中五种倍半萜内酯化合物抑制人肿瘤细胞增殖活性及构效关系研究  

Studies of sesquiterpenoids from Artemisia frigida on the anti-growth activity of human tumor cell lines

作　　者：陈进军[1] 王思明[2] 李存芳[2] 张嫚丽[2] 董玫[3] 史清文[2] 

机构地区：[1]河北医科大学第一医院肝胆外科,石家庄050031 [2]河北医科大学药学院,石家庄050017 [3]河北医科大学基础医学院法医学系河北省法医学重点实验室,石家庄050017

出　　处：《中药药理与临床》2011年第2期24-26,共3页Pharmacology and Clinics of Chinese Materia Medica

基　　金：国家自然科学基金(81072551);河北省自然科学基金(C2010000489)

摘　　要：目的:通过观察冷蒿中分离纯化的五种倍半萜内酯化合物对人子宫颈肿瘤细胞、人脑神经胶质瘤细胞、人肝癌细胞和人黑色素瘤细胞生长的影响,探讨这五种倍半萜内酯化合物的体外抑制人肿瘤细胞增殖作用,以及化合物结构与活性之间的构效关系。方法:利用四唑盐(MTT)比色法检测五种倍半萜内酯化合物对人肿瘤细胞增殖活性的影响。结果:去氢-姜黄烯(1)对子宫颈肿瘤细胞、人脑神经胶质瘤细胞、人肝癌细胞和人和色素瘤细胞的增殖均有明显的抑制作用,IC50分别为7.90 mol/L、37.78mol/L、22.50 mol/L和20.76 mol/L。二氢去氢木香内酯对各种实验用肿瘤细胞的增殖显示中等程度的抑制活性,其他三种试验用倍半萜内酯即使在100 mol/L的高浓度下,对四种肿瘤细胞的增殖不显示抑制活性。结论:实验结果初步推测,不饱和内酯是抑制肿瘤细胞增殖活性的必需基团,而环上的取代基对于抑制人肿瘤细胞增殖活性也有一定的影响。Objective： To detect the anti-human tumor cancer cells effect of five sesquiterpenoids from isolated from Artemisia frigida,and to explore the primary relationship between structure and activity of tested sesquiterpenoids.Methods： Using MTT assay to evaluate the anti-tumor activities of 5 sesquiterpenoids to the cell lines of HeLa,T-98,HLE and HMV-1.Results： Dehydrocostuslactone（1） exhibited significant activities against HeLa,T-98,HLE and HMV-1 cells,with the IC50（50% inhibition concentration） of 7.09 μmol/L,37.78 μmol/L,22.50 μmol/L and 20.76μmol/L respectively. dihydrodehydrocostuslactone（3） demonstrated moderate activities against human humor cell lines only in high concentration,while others did not showed activities against tested cell lines.Conclusions： This experimental result primarily demonstrated that,unsaturated lactone group is necessary for the anti-growth of human humor cell lines,and substitutions on the skeleton were also exerted somewhat anti-growth activity of human humor cell lines.

关 键 词：冷蒿 倍半萜内酯化合物 肿瘤细胞 增殖活性 构-效关系 

分 类 号：R285[医药卫生—中药学]