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马拉巴酮C是从中药肉豆蔻(Myristica fragrans Houtt.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NCIN87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NCIN87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NCIN87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。
Malabarone C is a class of diaryl nononanes unique to nutmeg plants extracted from the Chinese herbal nutmeg (the seed of Myristica fragrans Houtt.). In this study, the first study of the use of rat liver microsomes biotransformation study, clear its main biotransformation product of malabarone. In vitro evaluation of the cytotoxic activity of human gastric cancer cell lines NCIN87 and MGC803 found that the prototype compound malabarone C and its biotransformation product of malabarone B have a positive drug vinorelbine comparable cytotoxic activity. The half inhibitory concentration (NC) of NCIN87 cells were (42.62 ± 3.10) and (19.80 ± 1.70) μg / mL respectively, and were 22.94 ± 1.33 and 19.60 ± 2.21 μg / mL for MGC803 cells, respectively. Statistical analysis showed that the cytotoxic activity of the transformant Marabaraben B was significantly stronger than that of the malabarone C (P <0.01 for NCIN87 cells and P <0.05 for MGC803 cells), suggesting that the effect of liver microsome on malabarone C Activation. Malabarone C in the liver microsomal biotransformation pathway is more single.Maladaban B and C have the potential to develop gastric cancer.