中文摘要：

马拉巴酮C是从中药肉豆蔻（Myristicafragrans Hour．的种子）中提取到的，肉豆蔻科植物所特有的一类二芳基壬烷类化合物。本文首次利用大鼠肝微粒体对其进行了生物转化研究，明确其主要生物转化产物为马拉巴酮B。在体外对人胃癌细胞株NCI-N87和MGc803细胞毒活性评价试验中发现，原型化合物马拉巴酮C及其生物转化产物马拉巴酮B均具有与阳性药长春瑞滨相当的细胞毒活性。两者的半数抑制浓度，对NCI-N87细胞株分别为（42．62±3．10）和（19．80±1．70）μg／mL；对MGC803细胞株分别为（22．94±1．33）和（19．60±2．21）μg／mL。统计学分析表明，转化产物马拉巴酮B的细胞毒活性显著性强于原型化合物马拉巴酮C（对NCI-N87细胞P〈0．01，对MGC803细胞P〈0．05），提示肝微粒体对马拉巴酮C有活化作用。马拉巴酮C在肝微粒体的生物转化途径较为单一：马拉巴酮B和C具有治疗胃癌的开发潜力。

英文摘要：

Malabaricone C （1）, isolated from the seeds ofMyristicafragrans Houtt., belongs to a kind of diarylnonanoid compounds that are only found in Myristicaceae till now. In this study, biotransformation of 1 was investigated using rat hepatic microsomes for the first time and the main biotransformation product was elucidated as malabaricone B （2） according to the spectroscopic data. Further evaluation on human gastric cancer cell lines showed that the cytotoxic effects of malabaricone C and its metabolite malabaricone B were comparable to those of vinorelbine, with the values of IC50 of （42.62±3.10） and （19.80±1.70） μg/mL on NCI-N87, and （22.94±1.33） and （19.60±2.21） μg/mL on MGC803, respectively. Statistical analysis revealed that malabaricone B had significantly stronger cytotoxicity than the parent compound （P〈0.01 on NCI-N87 and P〈0.05 on MGC803）, which may indicate a bioactivation of malabaricone C by hepatic microsomes. These results suggest that malabaricone C has a simple biotransformation pathway by hepatic microsomes and provide valuable information for further investigation on both the parent compound and its biotransformation product as anti-gastric cancer agents or lead compounds.