右美沙芬
化学
药理学
豚鼠
敌手
辣椒素
生物碱
天然产物
柠檬酸
立体化学
吗啡
一氧化氮
右旋糖酐孤儿
羟甲基
受体
生物化学
医学
内科学
有机化学
作者
Hiroko Tani,Masayuki Yamaga,Tomoki Sekiya,Yoichiro Isohama,Hiroyuki Koshino,Toshihiko Nogawa,Ayanori Yamaki,Syouki Takahashi
标识
DOI:10.1021/acs.jafc.3c03864
摘要
The cough-suppressing effect of honey was demonstrated for the first time using a guinea pig model whereby cough was induced by citric acid and capsaicin, and a new pyrrolyl pyridoindole, 1-(5-(hydroxymethyl)-1H-pyrrol-2-yl)-9H-pyrido[3,4-b]indole-3-carboxylic acid (1), named melpyrrole, and flazin (2) were identified as the active principle components. The structures of 1 and 2 were estimated using a combination approach of an activity-guided survey and LC-MS/MS multivariate analysis and were finally established by total synthesis of 1 and comparison with an authentic standard for 2. Both compounds showed antitussive activity comparable to that of dextromethorphan in guinea pigs. Their antitussive effects were unaffected by an opioid antagonist and reversed by a nitric oxide (NO) synthase inhibitor, indicating that these natural products do not act directly on opiate receptors but through the NO signaling pathway.
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