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Molecules 2013, 18(1), 236-243; doi:10.3390/molecules18010236

4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862

1, 1, 1, 1, 1, 1, 1, 1, 1, 1, 1, 1 and 1,*
1 Institute of Medicinal Biotechnology, Peking Union Medical College, Chinese Academy of Medical Sciences, Tiantanxili No.1, Beijing 100050, China 2 National Institute of Biological Sciences, 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China
* Author to whom correspondence should be addressed.
Received: 31 October 2012 / Revised: 14 December 2012 / Accepted: 18 December 2012 / Published: 27 December 2012
(This article belongs to the Section Metabolites)
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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.
Keywords: Streptomyces albosporus; structure elucidation; HIV-1 protease inhibitor Streptomyces albosporus; structure elucidation; HIV-1 protease inhibitor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Liu, X.; Gan, M.; Dong, B.; Zhang, T.; Li, Y.; Zhang, Y.; Fan, X.; Wu, Y.; Bai, S.; Chen, M.; Yu, L.; Tao, P.; Jiang, W.; Si, S. 4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862. Molecules 2013, 18, 236-243.

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