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Antimicrobial Agents and Chemotherapy, September 2003, p. 2966-2970, Vol. 47, No. 9
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.9.2966-2970.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

S-Adenosyl-L-Methionine Inhibitors {Delta}24-Sterol Methyltransferase and {Delta}24(28)-Sterol Methylreductase as Possible Agents against Paracoccidioides brasiliensis

Gonzalo Visbal,1* Alvaro Alvarez,1 Belisario Moreno,2 and Gioconda San-Blas2

Laboratorio de Síntesis Orgánica y Productos Naturales, Centro de Química,1 Laboratorio de Micología, Centro de Microbiología y Biología Celular, Instituto Venezolano de Investigaciones Científicas, Caracas 1020A, Venezuela2

Received 9 October 2002/ Returned for modification 13 November 2002/ Accepted 11 June 2003

We studied the antiproliferative effects of three azasterol analogs [piperidyl-2-yl-5{alpha}-pregnan-3ß,20(R)-diol (AZA-1), 22-piperidin-2-yl-pregnan-22(S),3ß-diol (AZA-2), and 22-piperidin-3-yl-pregnan-22(S),3ß-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.

* Corresponding author. Mailing address: Laboratorio de Síntesis Orgánica y Productos Naturales, Centro de Química, Instituto Venezolano de Investigaciones Científicas, Carretera Panamericana Km 11, Caracas 1020A, Venezuela. Phone: (58-212) 504 1652. Fax: (58-212) 504 1350. E-mail: gvisbal{at}ivic.ve.

Antimicrobial Agents and Chemotherapy, September 2003, p. 2966-2970, Vol. 47, No. 9
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.9.2966-2970.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Serrano-Martin, X., Garcia-Marchan, Y., Fernandez, A., Rodriguez, N., Rojas, H., Visbal, G., Benaim, G. (2009). Amiodarone Destabilizes Intracellular Ca2+ Homeostasis and Biosynthesis of Sterols in Leishmania mexicana. Antimicrob. Agents Chemother. 53: 1403-1410 [Abstract] [Full Text]  


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