香豆素类化合物药理和毒理作用的研究进展

香豆素类化合物是自然界重要的一类天然有机化合物,存在于不同种属的植物中,具有广泛的用途。实验研究发现香豆素具有抗HIV、抗肿瘤、抗氧化、抗炎等多种药理活性,在临床上广泛用于抗凝血和淋巴管性水肿的治疗。近年来的研究发现,香豆素类化合物在啮齿类动物中存在着明显的毒性作用,且具有种属和位点特异性,这与其代谢途径和CYP2A6酶的多态性有关。另外,毒性作用还与给药剂量和给药途径密切相关,口服和高剂量给药更容易产生毒性反应。该文综述了近年来有关香豆素及其衍生物在药理和毒理方面的研究进展,以期为香豆素类化合物的研发和临床应用提供帮助。

Advances in pharmacology and toxicology of coumarins

Coumarins are an important class of natural compounds found in different species of plants in nature.Experimental studies have found that coumarins have multi-biological activities such as anti-HIV,anti-tumor,anti-oxidation,anti-flammatory and other pharmacological activities,which are widely applied to anti-coagulation and lymphatic edema in clinic.In recent years,studies have found that coumarins have clear toxic effects with species and site-specific in rodents,which is related to metabolic pathways and CYP2A6 polymorphisms.In addition,toxic effects are closely related to dose and route of administration,and oral and high dose are more prone to toxicity.This paper reviews the advances in pharmacology and toxicology of coumarin and its derivatives,with a view to the development of coumarins and clinical applications.