Abstract
We have isolated an extraordinary pentapeptide, called 4862F, from the culture broth of Streptomyces albosporus I03A-04862 by Diaion HP-20 macroporous adsorbent resin column, ODS-A and Sephadex LH-20 chromatography, followed by preparative HPLC. This peptide shows inhibitory activity against HIV-1 protease. The structure was elucidated by spectroscopic approaches, including ESI-MS and various NMR methods. Absolute configuration of the amino acid residues in 4862F was defined using Marfey’s method, and the structure was identified as N,N,N-(trimethylated)-Tyr-L-Leu-L-Val-L-Leu-(dehydrated)-His. The peptide 4862F displays inhibitory activity against HIV-1 protease, with IC50 values of 15.26 nM, using a fluorescence-based assay.
Highlights
The protease of human immunodeficiency virus type 1 is an essential enzyme in the viral life cycle where it cleaves the viral Gag-Pol polyprotein precursor into Gag proteins and two enzymes, integrase and protease [1]
We are interested in the isolation of new inhibitors of HIV-1 protease, and the microbial products from an actinomycete strain Streptomyces albosporus I03A04862 exhibited promising activity
We found that 1 mg·mL−1 of fermentation product from I03A-04862 could inhibit 50.2% of the activity of HIV-1 protease
Summary
The protease of human immunodeficiency virus type 1 is an essential enzyme in the viral life cycle where it cleaves the viral Gag-Pol polyprotein precursor into Gag proteins and two enzymes, integrase and protease [1] Inhibition of this enzyme has been used successfully for the treatment of HIV-1-. We are interested in the isolation of new inhibitors of HIV-1 protease, and the microbial products from an actinomycete strain Streptomyces albosporus I03A04862 exhibited promising activity. We found that 1 mg·mL−1 of fermentation product (dried powder) from I03A-04862 could inhibit 50.2% of the activity of HIV-1 protease This strain was classified as a member of the Streptomyces genus on the basis of 16S rRNA sequence analysis. We provide evidence for the demonstration of its inhibitory activity against HIV-1 protease in vitro
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