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学科主题: 药学
题名:
Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent
作者: 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
发表日期: 2007-10-01
DOI: 10.1111/j.1745-7254.2005.00179.x
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53171
Appears in Collections:北京大学深圳医院_药学部_期刊论文

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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

Recommended Citation:
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.
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