海南哥纳香醇甲(GHM10)对体外L1210细胞的抗肿瘤活性  

ANTITUMOR ACTIVITY OF HOWIINOL(GHM10) ON L1210 CELLS IN VITRO

作　　者：何剑华[1] 叶玉梅[1] 徐承熊[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所

出　　处：《药学学报》1998年第8期566-570,共5页Acta Pharmaceutica Sinica

摘　　要：用体外培养法研究ＧＨＭ１０对Ｌ１２１０细胞生长的抑制作用和作用机制。结果表明，Ｌ１２１０细胞在用ＧＨＭ１０处理１ｈ，２４ｈ和７ｄ后，ＩＣ５０依次为６８５，３３２和１５９μｇ·ｍｌ－１，提示ＧＨＭ１０有非时相特异性细胞毒药物的特性。在用ＧＨＭ１０１～２μｇ·ｍｌ－１作用２４ｈ后，Ｌ１２１０细胞的增长率和有丝分裂指数下降，细胞核形态发生变化，但活细胞率仍保持在９６％以上，提示ＧＨＭ１０主要抑制细胞的增殖。用流式细胞计对Ｌ１２１０细胞进行细胞周期动力学的分析表明，ＧＨＭ１０可在一定程度上阻断Ｇ１期细胞向Ｓ期移行。Howiinol(GHM10) is a new compound isolated from Goniothalamus howii. Previous studies showed that GHM10 significantly inhibited the growth of cancer cells both in vitro and in vivo. In the present study, the characteristics of the inhibitory effect of GHM10 on L1210 cells was investigated. The results showed that the IC50 of L1210 cells treated with GHM10 for 1　h, 24　h, and 7　d was 685, 332 and 159 μg·ml-1, respectively. This outcome is in compliance with the hypothesis that GHM10 is a cell cycle nonspecific cytotoxic drug. When L1210 cells were treated with 1～2 μg·ml-1 of GHM10 for 24 h, the growth rate and mitotic index were decreased and the morphology of cell nuclei changed, but the cell viability remained at the level of 96% or more, indicating that GHM10 mainly inhibited cell proliferation. The cell cycle kinetics of L1210 cells were studied by using a flow cytometer. The results showed that the transition of cells from G1 phase to S phase was blocked to certain extent by the treatment of GHM10 4 μg·ml-1 for 12 h. The fluidity of cell membrane was also increased when the L1210 cells were exposed to 2～3 μg·ml-1 of GHM10 for 24 h.

关 键 词：抗肿瘤药 海南哥纳香醇甲 细胞毒性 

分 类 号：R979.1[医药卫生—药品]