SPMG和AOSC对不同性别中国人肝药酶CYP450活性的影响

Effects of SPMG and AOSC on CYP450 enzymatic activity in different sexual Chinese people

目的研究不同结构的海洋新药对人类肝药酶的影响及性别差异,从而对这些新药进行安全性评价,并预测它们与其他药物合用的不良相互作用。方法通过研究肝药酶专属探针药物的体外代谢过程的变化,判断不同结构药物对这些酶有无诱导或抑制作用。结果SPMG和AOSC对CYP3A4均无影响,AOSC可诱导男性CYP2E1但对CYP1A2无影响,SPMG抑制男性CYP1A2但对CYP 2E1无影响。结论结构不同的药物对不同性别人CYP450的影响存在明显差异,此药物在与各种与CYP1A2或CYP 2E1酶代谢有关的药物合用时,应充分考虑其对肝药酶的不同影响,以避免潜在的毒性或不良反应。

[ Objective ] The sexual-based differences between the effects of two novel ocean drugs （SPMG and AOSC） on CYP 450 of Chinese human liver microsome were investigated arid also the safety assessment of these drugs were estimated. [Methods] The metabolic changes in vivo of the probe drug were studied, then the inhibition or induction effects of these different-structure drugs were estimated. [ Results ] Neither SPMG nor AOSC have any effect on CYP3A4. AOSC induced the CYP 2El in men but have no effect on CYP1A2. SPMG inhibit the CYP1A2 also in men but have no effect on CYP2E1. [Conclusion] The effect of SPMG and AOSC on CYP1A2 and CYP2E1 were different because of their different structure. When these two drugs are used combined with other drugs which are related with CYP1A2 and CYP2E1 enzyme, both the effect and the sex difference should be considered totally to avoid the potential adverse reactions.