Pan Guo-yu, Wang Guang-ji, Sun Jian-guo, Huang Zhi-jiang, Zhao Xiao-chen, Gu Yi, Liu Xiao-dong
Drug Metabolism and Pharmacokinetics Research Center, China Pharmaceutical University, Nanjing 210009, China.
Yao Xue Xue Bao. 2003 Dec;38(12):911-4.
To study the absorption characteristics of berberine and its influence on glucose absorption.
Rat recirculating perfusion model was used to study berberine absorption characteristics and Caco-2 cell model was used to explore the influence of berberine on disaccharidase, using HPLC to assay the appearance of glucose to indicate enzyme activities.
Berberine was found to be hardly absorbed in the intestine (less than 5% in 2.5 h). However, sucrase and maltase activities were found to be inhibited by berberine, its ID50 to sucrase is 1.830 mg.L-1, and showed no dose dependent influence on maltase activity. Berberine also showed influence on glucose absorption. However, this effect is not significant.
Berberine may act as an alpha-glucosidase inhibitor, which is its main mechanism in diabetes treatment.
研究小檗碱的吸收特性及其对葡萄糖吸收的影响。
采用大鼠循环灌注模型研究小檗碱的吸收特性,采用Caco-2细胞模型探讨小檗碱对双糖酶的影响,用高效液相色谱法测定葡萄糖的出现以指示酶活性。
发现小檗碱在肠道中几乎不被吸收(2.5小时内低于5%)。然而,发现小檗碱可抑制蔗糖酶和麦芽糖酶的活性,其对蔗糖酶的半数抑制浓度为1.830mg.L-1,对麦芽糖酶活性无剂量依赖性影响。小檗碱对葡萄糖吸收也有影响。然而,这种作用不显著。
小檗碱可能作为一种α-葡萄糖苷酶抑制剂,这是其治疗糖尿病的主要机制。