S -Adenosyl- l -Methionine Inhibitors Δ 24 -Sterol Methyltransferase and Δ 24(28) -Sterol Methylreductase as Possible Agents against Paracoccidioides brasiliensis

Author:

Visbal Gonzalo1,Alvarez Alvaro1,Moreno Belisario2,San-Blas Gioconda2

Affiliation:

1. Laboratorio de Síntesis Orgánica y Productos Naturales, Centro de Química

2. Laboratorio de Micología, Centro de Microbiología y Biología Celular, Instituto Venezolano de Investigaciones Científicas, Caracas 1020A, Venezuela

Abstract

ABSTRACT We studied the antiproliferative effects of three azasterol analogs [piperidyl-2-yl-5α-pregnan-3β,20( R )-diol (AZA-1), 22-piperidin-2-yl-pregnan-22( S ),3β-diol (AZA-2), and 22-piperidin-3-yl-pregnan-22( S ),3β-diol (AZA-3)] and their effects on the lipid composition of the pathogenic yeastlike phase of the dimorphic fungus Paracoccidioides brasiliensis . Inhibition was 100% for AZA-1 at 5 μM, 62% for AZA-2 at 10 μM, and 100% for AZA-3 at 0.5 μM. The analogs inhibited different stages of the sterol biosynthesis pathway.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

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