摘要
小檗红碱属于异喹啉类生物碱,是小檗碱的主要代谢产物,小檗碱在一定的加热条件下可以大量转化为小檗红碱。小檗红碱在中药材黄连和黄柏中含量较低,具有抗肿瘤、抗炎、抗菌、降糖、降脂等作用。小檗红碱在体内吸收迅速,可广泛分布于各种组织中,以肝脏代谢为主。随着小檗红碱的药理活性和用药安全受到广泛关注,本文作者在参考最新最全面的文献基础上,对小檗红碱的化学合成方法、药理作用、药代动力学研究、毒理作用等方面研究进展进行综述,为小檗红碱的药理研究和安全用药提供参考依据。
Berberrubine belongs to the group of isoquinoline alkaloids, and its content is relatively low in Chinese herbs of Coptidis rhizoma and Phellodendron Chinese Sohneid.Berberrubine is the main metabolite of berberine.Berberine can be transformed into berberrubine significantly under the certain heating conditions.Berberrubine has various pharmacological effects, such as anti-tumor, anti-inflammatory, antibacterial, hypoglycemic and hypolipidemic bioactivities.Berberrubine is rapidly absorbed in the body, widely distributed in various tissues, and mainly metabolized in the liver.With the development of berberrubine, more and more attention has been paid to its pharmacological activity and safety.In order to provide theoretical basis for the pharmacological study and medication safety of berberrubine, this article summarized the research progress in the chemical synthesis methods, pharmacological effects, pharmacokinetics research, toxicological effects of berberrubine based on the most advanced literatures.
作者
饶近秋
王凯
张婷婷
邱峰
RAO Jin-qiu;WANG Kai;ZHANG Ting-ting;QIU Feng(School of Chinese Materia Medica,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;State Key Laboratory of Component-based Chinese Medicine,Tianjin 301617,China)
出处
《中国药物化学杂志》
CAS
CSCD
2021年第5期369-377,共9页
Chinese Journal of Medicinal Chemistry
基金
国家科技重大专项(2017ZX09301012)
国家自然科学基金重点项目(81430095)
973计划前期研究专项课题(SQ2015CB050405)。
关键词
小檗红碱
合成
药理作用
药代动力学
体内代谢
毒性作用
berberrubine
chemical synthesis
pharmacological effects
pharmacokinetics
metabolism in vivo
toxic effects