S-腺苷-L-甲硫氨酸抑制剂δ(24)-甾醇甲基转移酶和δ(24(28))-甾醇甲基还原酶作为抗巴西副球孢子菌的潜在药物。
S-Adenosyl-L-methionine inhibitors delta(24)-sterol methyltransferase and delta(24(28))-sterol methylreductase as possible agents against Paracoccidioides brasiliensis.
作者信息
Visbal Gonzalo, Alvarez Alvaro, Moreno Belisario, San-Blas Gioconda
机构信息
Laboratorio de Síntesis Orgánica y Productos Naturales, Instituto Venezolano de Investigaciones Científicas, Caracas 1020A, Venezuela.
出版信息
Antimicrob Agents Chemother. 2003 Sep;47(9):2966-70. doi: 10.1128/AAC.47.9.2966-2970.2003.
Abstract
We studied the antiproliferative effects of three azasterol analogs [piperidyl-2-yl-5alpha-pregnan-3beta,20(R)-diol (AZA-1), 22-piperidin-2-yl-pregnan-22(S),3beta-diol (AZA-2), and 22-piperidin-3-yl-pregnan-22(S),3beta-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 microM, 62% for AZA-2 at 10 microM, and 100% for AZA-3 at 0.5 microM. The analogs inhibited different stages of the sterol biosynthesis pathway.
摘要
我们研究了三种氮杂甾醇类似物[哌啶基-2-基-5α-孕烷-3β,20(R)-二醇(AZA-1)、22-哌啶基-2-基-孕烷-22(S),3β-二醇(AZA-2)和22-哌啶基-3-基-孕烷-22(S),3β-二醇(AZA-3)]的抗增殖作用及其对双态真菌巴西副球孢子菌致病酵母样相脂质组成的影响。AZA-1在5微摩尔时抑制率为100%，AZA-2在10微摩尔时抑制率为62%，AZA-3在0.5微摩尔时抑制率为100%。这些类似物抑制了甾醇生物合成途径的不同阶段。
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