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学科主题药学
Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent
Fang-zhou Xu1; Chang Chen1; Yong-hui Zhang1; Han-li Ruan1; Hui-fang Pi1; Pong Zhang1; Ji-zhou Wu1
关键词Verticinone-cholic Acid Salt Shedan-chuanbei Powder Cholic Acid Verticinone Antitussive Effect Atp-sensitive K++ Channels
刊名ACTA PHARMACOLOGICA SINICA
2007-10-01
DOI10.1111/j.1745-7254.2005.00179.x
28期:10页:1591-1596
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]GUINEA-PIG ; MOGUISTEINE
英文摘要

Aim: To seek a novel and potent antitussive drug based on Shedan-Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy. Methods: Verticinone-cholic acid (Ver-CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan-Chuanbei powder, was synthesized. We then evaluated the antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver-CA could result in over 50% reduction of a citric acid-induced cough. Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K+ channel blocker, can also significantly reduce the antitussive effect of Ver-CA. A further acute toxicity study showed that the LD50 values of Ver-CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acute toxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver-CA, a potential novel antitussive agent, may exert its antitussive effect via both the peripheral (modulated by ATP-sensitive K+ channels) and central mechanisms (modulated by the opioid receptor).

语种英语
WOS记录号WOS:000249699600011
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/53171
专题北京大学深圳医院_药学部
作者单位1.Huazhong Univ Sci & Technol, Tongji Med Coll, Fac Pharmaceut Sci, Wuhan 430030, Peoples R China
2.Peking Univ, Shenzhen Hosp, Dept Pharm, Shenzhen 518036, Peoples R China
推荐引用方式
GB/T 7714
Fang-zhou Xu,Chang Chen,Yong-hui Zhang,et al. Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent[J]. ACTA PHARMACOLOGICA SINICA,2007,28(10):1591-1596.
APA Fang-zhou Xu.,Chang Chen.,Yong-hui Zhang.,Han-li Ruan.,Hui-fang Pi.,...&Ji-zhou Wu.(2007).Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent.ACTA PHARMACOLOGICA SINICA,28(10),1591-1596.
MLA Fang-zhou Xu,et al."Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent".ACTA PHARMACOLOGICA SINICA 28.10(2007):1591-1596.
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