马钱子减毒增效途径及机制研究进展

Research progress on the pathways and mechanisms of reducing toxicity and enhancing efficacy of semen strychni

本文综述马钱子减毒增效的主要途径及其减毒增效的机制研究进展。马钱子减毒增效的主要途径包括炮制、配伍、新剂型与制剂新技术等;减毒增效的机制主要包括生物碱成分含量发生变化、生物碱药代动力学行为改变、影响CYP450酶的mRNA表达和酶活性、诱导血脑屏障上P-糖蛋白外向转运加速生物碱外排、缓释及靶向控制药物浓度梯度等。关于马钱子减毒增效的途径研究较多,但对其减毒增效的机制和原理研究较少且不甚深入,建议后续研究从毒性物质基础、体内暴露和体内过程、分子机制、量-时-毒-效关联性及转化规律等方面对马钱子减毒增效的机制进行深入研究。

This article reviews the research progress on the main pathways and mechanisms of reducing toxicity and enhancing efficacy of semen strychni.The main pathways of reducing toxicity and enhancing efficacy of semen strychni include processing,compatibility,new dosage forms,and new technology of preparations.The mechanisms of reducing toxicity and enhancing efficacy mainly include changes in the content of alkaloid components,changes in the pharmacokinetic behavior of alkaloids,effects on the mRNA expression and enzyme activity of CYP450 enzyme,induction of P-glycoprotein outward transport on the blood-brain barrier to accelerate alkaloid efflux,sustained release,and targeted control of drug concentration gradient.There are many studies on the pathways of reducing toxicity and enhancing efficacy of semen strychni,but researches on the mechanism and principles of reducing toxicity and enhancing efficacy are relatively few and not very in-depth.It is recommended that future research should conduct in-depth research on the mechanism of reducing toxicity and enhancing efficacy of semen strychni from the aspects of toxic substance basis,in vivo exposure and in vivo processes,molecular mechanisms,correlation of dose-time-toxic ity-effect,and transformation patterns.