钒配合物的生物效应、分子机制和药物发现

Bioactivity,Molecular Mechanism and Drug Discovery of Vanadium Complexes

钒化合物可以通过改善葡萄糖和脂质代谢,促进胰岛素信号转导,发挥降血糖以及胰岛素保护作用;同时,其还能抑制多种肿瘤的增殖和诱导肿瘤细胞凋亡,并通过多种作用方式限制肿瘤细胞的侵袭和转移。钒配合物具有良好的药动学特性,在生理介质中,可以通过复杂的物种变化与各种细胞内靶标相互作用。过去20年,研究者对钒化合物生物活性及其分子机制获得了较为深入的认识,从而推动了该类化合物的理性分子设计和药物发现。综述钒化合物抗糖尿病和抗肿瘤的药理作用及潜在分子机制研究,并简述其药物设计及药物发现的策略。

Vanadium compounds can improve the glucose and lipid metabolism,and promote insulin signal transduction,thus exerting hypoglycemic effects and insulin protection.At the same time,they can inhibit the proliferation of tumors,induce tumor apoptosis,and limit the invasion and metastasis of tumor cells through a variety of ways.With their good pharmacokinetic properties,vanadium complexes in physiological media may interact with a variety of intracellular targets through a complex speciation change.In the past two decades,great progress has been made in the study of the biological activities and molecular mechanisms of vanadium compounds,which accelerated its rational drug design and discovery.This paper reviews the pharmacological action and potential molecular mechanism of vanadium compounds against diabetes and tumors,as well as the strategy for drug design and discovery of vanadium compounds.