新型碳水化合物修饰的小檗碱衍生物：合成与抗糖尿病研究。
Novel carbohydrate modified berberine derivatives: synthesis and anti-diabetic investigation.
作者信息
Han Liwen, Sheng Wenlong, Li Xiaobin, Sik Attila, Lin Houwen, Liu Kechun, Wang Lizhen
机构信息
Biology Institute , Qilu University of Technology (Shandong Academy of Sciences) , Jinan 250014 , Shandong Province , China . Email:
Institute of Transdisciplinary Discoveries , University of Pecs , Ifjúság útja 20 , Pécs , 7624 , Hungary.
出版信息
Medchemcomm. 2019 Feb 8;10(4):598-605. doi: 10.1039/c9md00036d. eCollection 2019 Apr 1.
Berberine is a bioactive alkaloid used in Chinese medicine and has numerous positive effects on biological systems. This paper describes the facile and highly efficient synthesis of some carbohydrate modified berberine derivatives, and conjugation of the carbohydrate moiety with berberine was finished by "click" chemistry. The cytotoxicity and anti-diabetic measurements of all berberine derivatives were accomplished on HepG2 cell lines, and the results indicated that most of the derivatives exhibit higher anti-diabetic activity than berberine. The mannose modified berberine derivative has significantly lower cytotoxicity than berberine, and the induced IC value of this derivative is nearly 1.5 times that of berberine. Furthermore, this mannose modified berberine derivative exhibits high anti-diabetic activity at both high and low drug concentrations, thereby indicating its potential application for the development of novel anti-diabetic drugs.
黄连素是一种用于中药的生物活性生物碱，对生物系统有许多积极作用。本文描述了一些碳水化合物修饰的黄连素衍生物的简便高效合成方法，并且通过“点击”化学完成了碳水化合物部分与黄连素的共轭。所有黄连素衍生物的细胞毒性和抗糖尿病活性测定均在肝癌细胞系HepG2上进行，结果表明大多数衍生物表现出比黄连素更高的抗糖尿病活性。甘露糖修饰的黄连素衍生物的细胞毒性明显低于黄连素，该衍生物的诱导半数抑制浓度值几乎是黄连素的1.5倍。此外，这种甘露糖修饰的黄连素衍生物在高、低药物浓度下均表现出高抗糖尿病活性，从而表明其在新型抗糖尿病药物开发中的潜在应用价值。
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