摘要：为了开发桑叶咀嚼片，本文利用微波烫漂联合微细化处理技术制备桑叶粉，然后在此基础上，建立桑叶咀嚼片的最佳配方，并采用DiscoveryStudio2.1软件对桑叶咀嚼片中的活性物质1-脱氧野尻霉素（1-deoxynojirimycin，DNJ）进行降血糖分子机制研究。结果表明：确定最佳微波烫漂联合微细化处理的条件为微波功率700W，微波烫漂时间2min，微细化处理的料液比50g/L，微细化处理时间2min，微细化处理初始温度70℃，在此条件下，桑叶粉保持着良好的营养成分(黄酮、DNJ、Vc)；确定了桑叶咀嚼片配方为桑叶浓缩粉75％、微晶纤维素23％、甘露醇1.95％、聚乙烯吡咯烷酮醇0.05％。分子对接结果表明，α-葡萄糖苷酶分子中的Gln438、Arg437和Phe455为DNJ的重要结合位点，而异麦芽糖酶分子中的Gln279和Val216为DNJ的重要结合位点。研究结果有助于对DNJ衍生物类降血糖药物的设计与研发。

关键词:桑叶；咀嚼片；降血糖机理；分子对接

Abstract:In order to develop chewable tablets of mulberry leaf, Mulberry leaves powders were prepared by microwave blanching and fine pulverization treatment. On the basis of the study of mulberry leaves powders, optimal formula of chewable tablets of mulberry leaf was studied. Then the hypoglycemic mechanism of 1-deoxynojirimycin (DNJ) from chewable tablets of mulberry leaf was studied by the molecular docking between DNJ and α-glucosidase, as  well as isomaltase using Discovery Studio 2.1 software. The results showed that the optimum conditions of microwave blanching and fine ulverization treatment were as follows: microwave power 700W, microwave time 2min, solid-liquid ratio of fine pulverization treatment 50g / L, treatment time of fine pulverization 2min, the initial temperature of fine pulverization  70  °  C.  Under  this  condition,  mulberry  leaves  powers  maintain  a   good nutrient(Flavonoids、DNJ、Vc). Formula of chewable tablets of mulberry leaf was as follows:75% of mulberry leaves powder, 23% of microcrystalline cellulose, 1.95% of mannitol and 0.05% of polyvinylpyrrolidone (PVP). The results of molecular docking showed that Gln438, Arg437 and Phe455 in α-glucosidase were especially important binding site with DNJ, while Gln279 and Val216 in isomaltase were especially important binding site with DNJ. This study will be helpful for the design and development on DNJ derivatives with hypoglycemic activity.

Keywords: Mulberry leaves; Chewable tablets; Hypoglycemic mechanism; Molecular docking

目录

第一章绪论

1.1引言

1.2咀嚼片的简介

1.2.1咀嚼片的定义

1.2.2咀嚼片的使用优势

1.2.3咀嚼片的研究现状

1.3桑叶的简介

1.4桑叶降血糖成分DNJ

1.5桑叶咀嚼片的研究进展

1.6课题研究意义及内容

1.6.1研究目的和意义

1.6.2研究内容

第二章实验材料与方法

2.1实验仪器和试剂

2.1.1实验药品

2.1.2实验仪器

2.2试验方法

2.2.1桑叶的杀青灭酶

2.2.2桑叶的微细化处理

2.2.3桑叶咀嚼片的制备

2.2.41-脱氧野尻霉素的降血糖机制研究

第三章结果与分析

3.1桑叶的杀青灭酶和微细化处理

3.1.1桑叶的杀青灭酶条件

3.1.2桑叶的微细化处理条件

3.2桑叶咀嚼片的配方

3.31-脱氧野尻霉素降血糖的分子机制研究结果与分析

结论· 25

现有成果·