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

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

Xiao Liu 1,2 email, Maoluo Gan 1 , Biao Dong 1 , Tian Zhang 1 , Yongzhen Li 1 , Yuqin Zhang 1 , Xiuyong Fan 1 , Yexiang Wu 1 , Shuoke Bai 1 , Minghua Chen 1 , Liyan Yu 1 , Peizhen Tao 1 , Wei Jiang 1  and Shuyi Si 1,* email
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; in revised form: 14 December 2012 / Accepted: 18 December 2012 / Published: 27 December 2012
(This article belongs to the Section Natural Products)
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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.
Keywords: Streptomyces albosporus; structure elucidation; HIV-1 protease inhibitor

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Cite This Article

MDPI and ACS Style

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.

AMA Style

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(1):236-243.

Chicago/Turabian Style

Liu, Xiao; Gan, Maoluo; Dong, Biao; Zhang, Tian; Li, Yongzhen; Zhang, Yuqin; Fan, Xiuyong; Wu, Yexiang; Bai, Shuoke; Chen, Minghua; Yu, Liyan; Tao, Peizhen; Jiang, Wei; Si, Shuyi. 2013. "4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862." Molecules 18, no. 1: 236-243.

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