4.5 Article

Antitussive Indole Alkaloids from Kopsia hainanensis

Journal

PLANTA MEDICA
Volume 77, Issue 9, Pages 939-944

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/s-0030-1250631

Keywords

Kopsia hainanensis; Apocynaceae; danuphyllin type; aspidofractinine type; chanofruticosinate type; antitussive activity

Funding

  1. National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China [2009ZX09301-001]
  2. Ministry of Science and Technology [2007DFC31030]
  3. Shanghai Commission of Science and Technology [08DZ1971401]

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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 delta-opioid receptor. This is the first report of antitussive effects of aspidofractinine type and chanofruticosinate type alkaloids.

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