Antitussive Indole Alkaloids from Kopsia hainanensis

 

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Abstract

Three new indole alkaloids, named kopsihainins A–C (1–3), and two known compounds, kopsinine (4) and methyl demethoxycarbonylchanofruticosinate (5), were isolated from the stems of Kopsia hainanensis. Their structures were determined using extensive spectroscopic methods. The two main constituents 4 and 5 exhibited significant antitussive activity in a citric acid induced guinea pig cough model. The antitussive effect of 4 was demonstrated to interact with the δ-opioid receptor. This is the first report of antitussive effects of aspidofractinine type and chanofruticosinate type alkaloids.

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Prof. Yang Ye

State Key Laboratory of Drug Research & Natural Products Chemistry Department
Shanghai Institute of Materia Medica
Chinese Academy of Sciences

555 Zu-Chong-Zhi Road, Zhangjiang Hightech Park

Shanghai 201203

P. R. China

Phone: +86 21 50 80 67 26

Fax: +86 21 50 80 67 26

Email: yye@mail.shcnc.ac.cn

Prof. Ge Lin

School of Biomedical Sciences
The Chinese University of Hong Kong

Shatin, N. T.

Hong Kong SAR

P. R. China

Phone: +85 2 26 09 68 24

Fax: +85 2 26 03 51 39

Email: linge@cuhk.edu.hk

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