Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 24, Pages 10182-10189Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.10.061
Keywords
Lycorine; Alkaloid; Lycoris; Antitrypanosomal activity; Antimalarial activity; Structure elucidation; Structure-activity relationship
Funding
- Japan Society for the Promotion of Science
- Astellas Foundation for Research on Metabolic Disorders
- Drugs for Neglected Diseases initiative (DNDi)
- All Kitasato Project Study (AKPS)
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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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