Total synthesis and biological evaluation of methylgerambullone
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- 作者：Jong Taik Moon ; Sung Hoon Ha ; So Hyung Lee ; Tae Hui Kwon ; Chun Rim Oh ; Young Deuk Kim ; Jungahn Kim ; Dong Joon Choo ; Jae Yeol Lee
- 关键词：Natural product ; Methylgerambullone ; Guinea-pig ileum ; Relaxation
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：1 January 2010
- 年：2010
- 卷：20
- 期：1
- 页码：52-55
- 全文大小：276 K
文摘
First total synthesis of methylgerambullone (MGB, 1) isolated from Glycosmis angustifolia was completed via a convergent route. The effect of MGB on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine was investigated. As a result, it showed a potent relaxation rate (78.66 ± 4.30 % at 100 mg/L) in a concentration-dependent manner on longitudinal smooth muscle contraction of isolated guinea-pig ileum induced by 1 μM acetylcholine.