Anti-5-hydroxytryptamine_3 Effect of Galanolactone, Diterpenoid Isolated from Ginger

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概要

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• It has been reported that an acetone extract of ginger and its fractions have anti-5-HT (5-hydroxytryptamine; serotonin) effects. In the present study, guinea pig ileum, rat stomach fundus and rabbit aortic strips are used in order to determined the constituents of fraction 2 which are responsible for anti-5-HT effect and to examine their pharmacological properties.The analysis of fraction 2-3 indicated that galanolactone, a diterpenoid, is one of the active constituents. In guinea pig ileum, galanolactone inhibited contractile responses to 5-HT with a pIC_<50> value 4.93. pIC_<50> value of galanolactone against the response to 2-methyl-5-HT, a selective 5-HT_3 agonist, in the presence of methysergide at 1×10^<-5>M was 5.10. pIC_<50> values of ICS 205-930,a selective 5-HT_3 antagonist, were 5.30 and 7.49,respectively. The concentration-response curve of 5-HT was shown as a biphasic curve and galanolactone caused a selective shift to the right of the second phase.In the same preparations, the pIC_<50> value of galanolactone and ICS 205-930 against the response to carbamylcholine (CCh) was 4.45 and 4.46.The inhibitory effect of galanolactone on the 5-HT response in the stomach fundus and aortic strips was less than that in the ileum.In addition, in the thoracic aorta precontracted with 50 mM K^+, the relaxing effect of galanolactone was about 1/10 of that of papaverine.These results suggest that the anti-5-HT effect of galanolactone, a diterpenoid isolated from ginger, is related to antagonism of 5-HT_3 receptors.

• 社団法人日本薬学会の論文
• 1991-02-25

著者

• 富松 利明

  徳島大学薬学部

• 富松 利明

  Faculty of Pharmaceutical Sciences of Kyushu University

• 田中 直美

  Kyoto Pharmaceutical University

• 高石 喜久

  Faculty of Pharmaceutical Sciences, The University of Tokushima

• 山原 條二

  Kyoto Pharmaceutical University

• 高石 喜久

  Faculty Of Pharmaceutical Science Tokushima University

• 山原 條二

  (株)クラレnic研究開発室

• 玉井 洋進

  (株)クラレNIC研究開発室

• HUANG Qirong

  Kyoto Pharmaceutical University

• 岩本 真承

  Kyoto Pharmaceutical University

• 青木 俊二

  Kyoto Pharmaceutical University

• 田嶋 清子

  Kyoto Pharmaceutical University

• 吉田 雅昭

  Faculty of Pharmaceutical Science, Tokushima University

• 玉井 洋進

  Kuraray Co., Ltd.,

• 富松 利明

  徳島大薬

• 山原 絛二

  Kyoto Pharmaceutical University

• Huang Q

  Toyama Medical And Pharmaceutical Univ. Toyama Jpn

• 吉田 雅昭

  Faculty Of Pharmaceutical Science Tokushima University

• 富松 利明

  Faculty Of Pharmaceutical Sciences Tokushima University

• 高石 喜久

  Faculty of Integrated Arts and Sciences, University of Tokushima

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