Open AccessNaturally Occurring Pyrrolizidines: Inhibition of α-Glucosidase 1 and Anti-HIV Activity of One Stereoisomer
Author(s) -
D.L. Taylor,
Robert J. Nash,
Linda E. Fellows,
M.S. Kang,
A.S. Tyms
Publication year - 1992
Publication title -
antiviral chemistry and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.919
H-Index - 51
eISSN - 2040-2066
pISSN - 0956-3202
DOI - 10.1177/095632029200300504
Subject(s) - castanospermine , indolizidine , alkaloid , pyrrolizidine , stereochemistry , biology , swainsonine , pyrrolizidine alkaloid , enzyme , ic50 , pharmacognosy , biological activity , biochemistry , chemistry , in vitro
Alexine, a naturally occurring pyrrolizidine alkaloid, isolated from Alexa leiopetala, and four stereoisomers, isolated from Castanospermum australe, were investigated for inhibitory activity against the growth of HIV-1. Only treatment with the 7,7a-diepialexine restricted virus growth (IC 50 0.38 mm) although it was less active than the indolizidine alkaloid castanospermine (IC50 0.02 mm). The antiviral effects of 7,7a-diepialexine, like castanospermine, correlated with the inhibitory activity against purified pig kidney α-glucosidase 1 of the glycoprotein processing enzymes and the reduced cleavage of the precursor HIV-1 glycoprotein gp160.
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