小檗碱作用靶点及其吸收特点——老药如何新用  

Berberine action targets and its absorption behavior:how to use old drug for new mechanisms

作　　者：袁梽漪[1] 王玉刚[1] 柴玉爽[1] 胡珺[1] 姜敬非[1] 严孝金[1] 杜力军[1] 

机构地区：[1]清华大学生命科学学院药物药理实验室,北京100084

出　　处：《中国中药杂志》2016年第12期2362-2370,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金面上项目(81374006;81073092)

摘　　要：随着研究的不断深入,小檗碱的多种药理作用不断被发现。随之而来的是如何针对小檗碱的这些新的药理作用来合理用药。由于小檗碱具有一定的心肌毒性、且其口服吸收较差,因此导致了在如何提高生物利用度与控制其可能产生的毒性之间的矛盾。同时一些新的用途如调血脂、降血糖以及防治神经退行性病变等都需要长期给药,从而形成了长期口服与对肠道菌群失调及其对机体其他生理功能影响可能产生潜在的风险之间的矛盾。该文在阐明小檗碱作用靶点及其相关药学特性的基础上,就这方面议题进行了综合讨论分析。最后提出建议:长期口服给药对机体尤其是肠道菌群的影响尚需进一步考察;通过改变制剂提高口服药物的吸收率时应考虑由此带来的风险;对于药物浓度需求较高的治疗用药(如肿瘤),靶向给药值得考虑。A variety of pharmacological effects of berberine（ BBR） are constantly being discovered with the deepening of BBR research. What followed is how to rationally use the drug according to these new pharmacological effects. Because of some cardiac toxicity and poor oral absorption,conflicts may arise between improving the bioavailability and controlling the toxicity of BBR. Meanwhile some new therapeutic uses of BBR,such as hypolipidemia,hypoglycemia as well as prevention and treatment of neurodegenerative diseases,need long-termoral administration,thereby may lead to alteration of intestinal flora and potentially affect body＇s other physiological functions. Based on the stated targets of BBR and related pharmaceutical properties,comprehensive analysis of these issues was conducted in this study. Some suggestions were presented below： the effect of long-term oral administration on body function,especially the intestinal flora,needs to be further investigated; risks shall be considered in changing the composition of the formulation to improve the absorption rate of oral administration; for the medication with higher concentration demand（ such as anti-cancer）,targeted drug-delivery is worthy to be considered.

关 键 词：小檗碱 药理 吸收 毒性 应用 

分 类 号：R285.5[医药卫生—中药学]