a-葡萄糖苷酶抑制剂RadicamineA的初步研究.docVIP

文章编号： ?-葡萄糖苷酶抑制剂Radicamine A?的初步研究 刘春艳1,2,*，孟爱国3，张卫国2 （1. 天津大学药物科学与技术学院，天津，300072；2. 华北煤炭医学院药学系；3. 华北煤炭医学院附属医院，河北唐山，063000）Radicamine A对?-葡萄糖苷酶?-葡萄糖苷酶抑制实验和体外小肠外翻肠囊模型Radicamine A的抑制作用。结果 Radicamine A对??-葡萄糖苷酶抑制作用呈剂量依赖性，其IC50为2.27mg/L；其能明显抑制小肠对葡萄糖的吸收（p0.01）,其IC50为0.10 mg/mL。与拜糖平(P0.05)。结论Radicamine A能显著抑制小肠葡萄糖的吸收，有望成为一种治疗糖尿病的药物。 关键词：Radicamine A；?-葡萄糖苷酶抑制剂抑制作用拜糖平Study on Radicamine A as ???glucosidase inhibitor Liu Chunyan1,2,*, Meng Aiguo3, Zhang Weiguo (1.School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, 2. Department of Pharmacy, North China Coal Medical University, 3. Affiliated Hospital of North China Coal Medical University Tangshan 063000) Abstract Objective: To evaluate the inhibitory effect on ?-glucosidase and the glucose’s absorption in the small intestine by Radicamine A. Mothods: The inhibitiory effect induced by Radicamine A was obtained by both the ?-glucosidase inhibitory test and the rat’s intestinal glucose’s absorption model. Results: Radicamine A showed an inhibitory effect on ?-glucosidase in a dose-dependent manner, and IC50 value was 2.27mg/L. Furthermore the glucose’s absorption in the small intestine was obviously inhibited in a dose-dependent manner by Radicamine A and IC50 value was 0.10 mg/mL. Moreover there was no significant difference between acarbose’s group and Radicamine A’s. Conclusion: Radicamine A inhibited clearly the glucose’s absorption in the small intestine, suggesting that Radicamine A might be a novel therapeutic drug for diabetes. Key words：Radicamine A; ?-glucosidase inhibitor; inhibitory effect; acarbose; glucose’s absorption ??葡萄糖苷酶抑制剂是一类新型口服降血糖药物，能竞争性抑制小肠内??葡萄糖苷酶的活性，延缓或抑制葡萄糖在肠道吸收，有效降低餐后高血糖。近年来研究发现??葡萄糖苷酶抑制剂参与蛋白糖基化和脂类糖基化等过程，具有抗肿瘤、抗病毒、免疫刺激活性和抗动脉粥样硬化等作用[1]，这引起了国内外学者极大的兴趣。天然产物Radicamines A和B是日本植物学家Kusano等从半边莲中分离到的两个新型吡刘春艳，女，1974年生，博士，副教授，主要从事新药的设计、合成和活性研究。E-mail:tangshan2002@yahoo.cn咯烷型生物碱，发现他们是有效的?-葡萄糖苷酶抑制剂，根据各种光谱数据推断他们为全反式取代的吡咯烷结构，绝对构型为(2S,3S,4S,5S)[2]。后来，本课题组[3]和其他课题组[4]分别采用不同的全合成方法纠正了