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HIV/AIDS Drug Development: Sulfonated naphthyl porphyrins active against HIV-1

AIDSWEEKLY Plus; Monday, May 9, 2005
Staff Medical Writers


NewsRx -- Sulfonated naphthyl porphyrins active against HIV-1.

"Sulfonated 5,10,15,20-tetra(1-naphthyl)porphyrin (T1NapS) and 5,10,15,20-tetra(2-naphthyl)porphyrin (T2NapS) and their copper and iron chelates show activity against the human immunodeficiency virus (HIV-1).

"The porphyrins were prepared by sulfonation of the parent structures with sulfuric acid. More highly sulfonated structures were prepared by sulfonation for longer times," researchers in the United States report.

"Matrix-assisted laser desorption/ionization (MALDI) mass spectrometry showed species with as many as eight sulfonates.

"Some of the mass spectral peaks for the copper chelates were consistent with loss of water, apparently from intramolecular sulfone formation between two adjacent naphthalene rings that took place during copper insertion," wrote D.W. Dixon and colleagues at Georgia State University in Atlanta.

"The compounds could be separated using capillary electrophoresis; addition of beta- or gamma-cyclodextrin gave substantially better separation of the components. Activity against HIV was evaluated using an epithelial HeLa-CD4-CCR5 cell line; EC50 values for HIV-1 IIIB and HIV-1 JR-FL ranged from 1 to 15 mcg/ml," scientists said.

The authors concluded, "The compounds exhibit low toxicity for human epithelial cells and have potential as microbicides which might be used to provide protection against sexual transmission of HIV."

Dixon and colleagues published their study in the Journal of Inorganic Biochemistry (Sulfonated naphthyl porphyrins as agents against HIV-1. J Inorg Biochem. 2005 Mar;99(3):813-21.

For additional information, contact D.W. Dixon, Georgia State University, Department Chemical, Box 4098, Atlanta, GA 30303, USA.

Publisher contact information for the Journal of Inorganic Biochemistry is: Elsevier Science Inc., 360 Park Avenue South, New York, NY 10010-1710, USA.

Keywords: Atlanta, Georgia, United States, Sulfonated Naphthyl Porphyrin, HIV/AIDS, Anti-HIV Activity, Microbicide, Transmission Prevention.

This article was prepared by AIDS Weekly editors from staff and other reports.

Reference

Dixon DW, Gill AF, Giribabu L, et al., Sulfonated naphthyl porphyrins as agents against HIV-1, J Inorg Biochem. 2005 Mar;99(3):813-21.

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