4.7 Article

New lycorine-type alkaloid from Lycoris traubii and evaluation of antitrypanosomal and antimalarial activities of lycorine derivatives

期刊

BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 24, 页码 10182-10189

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.10.061

关键词

Lycorine; Alkaloid; Lycoris; Antitrypanosomal activity; Antimalarial activity; Structure elucidation; Structure-activity relationship

资金

  1. Japan Society for the Promotion of Science
  2. Astellas Foundation for Research on Metabolic Disorders
  3. Drugs for Neglected Diseases initiative (DNDi)
  4. All Kitasato Project Study (AKPS)

向作者/读者索取更多资源

A new lycorine derivative LT1 (4) was isolated from the aerial part and bulbs of Lycoris traubii Hayward (Amaryllidaceae). Its structure including absolute con. guration was established by spectroscopic analysis and semi-synthesis to be 1-O-(3'S)-hydroxybutanoyllycorine. Some lycorine ester derivatives including LT1 were examined for their inhibitory activity against Trypanosoma brucei brucei, the parasite associated with sleeping sickness, and against Plasmodium falciparum, the causative agent of malaria. Among them, 2-O-acetyllycorine (6) showed the most potent activity against parasitic T. b. brucei, and LT1 (4), 1-O-(3'R)-hydroxybutanoyllycorine (8), 1,2-di-O-butanoyllycorine (11), and 1-O-propanoyllycorine (12) showed significant activity against P. falciparum in an in vitro experiment. (C) 2008 Elsevier Ltd. All rights reserved.

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