七种天然二萜类化合物的体外细胞毒活性及其构效关系  

Ann-,tumor Activity and Structure-activity Relationship of Seven Natural Diterpenoids in Vitro

作　　者：史祥[1] 闫福林[2] 葛峰[1] 蒲丽平[1] 赵晶[1] 高清祥[1] 王春明[1] 

机构地区：[1]兰州大学生命科学学院生物物理研究所,兰州730000 [2]新乡医学院药学院,新乡453003

出　　处：《天然产物研究与开发》2011年第B12期39-42,共4页Natural Product Research and Development

摘　　要：应用SRB法测定七种二萜类化合物对人急性早幼粒白血病细胞系HL-60、人肝癌细胞系SMMC-7721和人宫颈癌细胞系HeLa的细胞毒活性。化合物1和6对三种细胞的GI卯值均小于4μg／mL，显示出很强的毒性；化合物2—4对三种细胞的GI50值介于2—33μg／mL之间；化合物5和7对三种细胞的G150值介于26～126μg／mL之间，毒性相对较弱。分析构效关系支持仪一亚甲基环戊酮结构为该类化合物毒性中心的观点。羟基在此类化合物的细胞毒作用中起抑制作用，羟基数越多，化合物的毒性越小，而羟基的位置变化对毒性影响比羟基数目的影响小。化合物1和6最具进一步研究的价值。Sulforhodamine B （SRB） stained method was used to evaluate the cytotoxicity of seven natural diterpenoids in three cancer cell lines, human promyelocytic leukemia cell line HL-60, human hepatocelhtlar carcinoma cell line SMMC- 7721 and human cervical cancer cell line HeLa. The GI50 values against three cell lines of lsodocarpin （1） and Serrin B （6） were less than 4 μg/mL ;the GIs0 values of the Enmein （2）, Nodosin （3）, and Epinodosin （4） were between 2 - 33 μg/mL; and the values of epinodosinol （5;） and 15α, 20β-dihydroxy-6β-methoxy-6,7-seco-6,20-epoxy -1,7-olideent-kaur-16-ene （71） were between 26 - 126 μg/mL. The structure-activity analysis indicated that a-methylene cyclo- pentanone in the molecule structures was cytotoxicity center, and hydroxyl group seemed to exhibit a negative effect on the cytotoxicity, the more hydroxyls the less cytotoxicity. However, the position of hydroxyl group has very little effect on cytotoxicity. Based on these analyses, it was suggested that compound Isodocarpin （1） and Serrin B （6） were deserved to further research.

关 键 词：二萜化合物 细胞毒性 SRB 构效关系 α-亚甲基环戊酮结构 

分 类 号：R962[医药卫生—药理学]