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[藜芦酮-胆汁酸盐的制备及其镇咳、祛痰和平喘活性]

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

作者信息

Xu Fang-Zhou, Zhang Yong-Hui, Ruan Han-Li, Pi Hui-Fang, Chen Chang, Wu Ji-Zhou

机构信息

Faculty of Pharmaceutical Sciences, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China.

出版信息

Yao Xue Xue Bao. 2007 Mar;42(3):274-8.

Abstract

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.

摘要

为了寻找具有强效镇咳、祛痰、平喘活性且低毒的潜在药物,基于明确阐明的浙贝母中浙贝母碱的镇咳、祛痰和平喘活性以及蛇胆中不同胆汁酸的活性,制备了一系列浙贝母碱-胆汁酸盐。然后用不同的动物模型筛选这些浙贝母碱-胆汁酸盐的镇咳、祛痰和平喘活性。浙贝母碱-胆酸盐(Ver-CA)和浙贝母碱-鹅去氧胆酸盐(Ver-CDCA)显示出比其他化合物更强的活性。Ver-CA和Ver-CDCA的生物活性值得深入研究,而且它们比磷酸可待因具有更强的镇咳作用也值得高度关注。为了阐明它们是否具有协同作用以及毒性是否降低,将在不同动物模型上以相同剂量将它们的活性与单一的浙贝母碱、胆酸和鹅去氧胆酸持续进行比较。中药方剂中“配伍原则”的应用可能是中药研究与发现的一种新途径。

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