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Differential inhibition of fungal oxidosqualene cyclase by 6E and 6Z isomers of 2,3-epoxy-10-aza-10,11-dihydrosqualene
Authors:Gianni Balliano  Paola Milla  Maurizio Ceruti  Franca Viola  Lcia Carrano  Luigi Cattel
Institution:Gianni Balliano, Paola Milla, Maurizio Ceruti, Franca Viola, Lùcia Carrano,Luigi Cattel,
Abstract:Inhibitory properties of 6E (compound 1) and 6Z (compound 2) isomers of 2,3-epoxy-10-aza-10,11-dihydrosqualene against oxidosqualene-lanosterol cyclase were assayed on microsomes and whole cells of Saccharomyces cerevisiae and Candida albicans. Only the 6E isomer (compound 1), bearing a correct substrate-like configuration, strongly inhibited the enzyme both in microsomes and cell cultures. The difference between compounds 1 and 2 (which had an unfavorable geometry) was especially evident when measuring 14C]acetate incorporation into non-saponifiable lipids extracted from treated cells. While isomer Z was totally ineffective at up to 30 μM, in cells treated with 5 μM isomer E, labelled oxidosqualene, the level of which was negligible in the control, rose to over 60% of the non-saponifiable lipids.
Keywords:Oxidosqualene cyclase  Sterol biosynthesis inhibitor  Saccharomyces cerevisiae  Candida albicans
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