浙贝乙素胆汁酸盐的制备及其镇咳、祛痰和平喘活性的筛选  

Preparation and antitussive,expectorant and antiasthmatic activities of verticinone-bile acids salts

作　　者：徐仿周[1] 张勇慧[1] 阮汉利[1] 皮慧芳[1] 陈昶[1] 吴继洲[1] 

机构地区：[1]华中科技大学同济药学院,湖北武汉430030

出　　处：《药学学报》2007年第3期274-278,共5页Acta Pharmaceutica Sinica

基　　金：2006年高等学校科技创新工程重大项目培养基金

摘　　要：为了寻找具有优良镇咳、祛痰和平喘活性且毒性较低的药物,将贝母中的主要药效成分之一浙贝乙素和蛇胆中各主要药效成分进行酸碱反应,得到一系列浙贝乙素胆汁酸盐并对所得的盐进行镇咳、祛痰和平喘活性的筛选。活性筛选结果显示,浙贝乙素胆酸盐和浙贝乙素鹅去氧胆酸盐的镇咳、祛痰和平喘活性较强,尤其是二者显示出比磷酸可待因还强的镇咳活性值得关注。借鉴药物化学中的结构拼合思路有望在中药复方的研究开发中开辟出一条新的途径。To search for potential drugs with potent antitussive, expectorant, antiasthmatic activities and low toxicity, a series of verticinone-bile acids salts were prepared based on the clearly elucidated antitussive, expectorant and antiasthmatic activities of verticinone in bulbs of Fritillaria and different bile acids in Snake Bile. The antitussive, expectorant and antiasthmatic activities of these verticinone-bile acid salts were then screened with different animal models. Ver-CA （verticinone-cholic acid salt） and Ver- CDCA （verticinone-chenodeoxycholic acid salt ） showed much more potent activities than other compounds. The bioactivities of Ver-CA and Ver-CDCA are worthy to be intensively studied, and it is also deserved to pay much attention to their much more potent antitussive effects than codeine phosphate. In order to elucidate whether they have synergistic effect and attenuated toxicity, their activities will be continuously compared with single verticinone, cholic acid and chenodeoxycholic acid at the same doses on different animal models. The application of ＂ combination principles＂ in traditional Chinese medicinal formulations may be a novel way in triditional Chinese medicine research and discovery.

关 键 词：浙贝乙素胆汁酸盐 浙贝乙素胆酸盐 浙贝乙素鹅去氧胆酸盐 镇咳 祛痰 平喘 

分 类 号：R916[医药卫生—药学]