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

Molecules

Xiao Liu¹  Maoluo Gan¹  Biao Dong¹  Tian Zhang¹  Yongzhen Li¹  Yuqin Zhang¹  Xiuyong Fan¹  Yexiang Wu¹  Shuoke Bai¹  Minghua Chen¹  Liyan Yu¹  Peizhen Tao¹  Wei Jiang¹ 

[1] ¹Institute of Medicinal Biotechnology, Peking Union Medical College, Chinese Academy of Medical Sciences, Tiantanxili No.1, Beijing 100050, China ²National Institute of Biological Sciences, 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China

关键词: Streptomyces albosporus;    structure elucidation;    HIV-1 protease inhibitor;   

DOI  :  10.3390/molecules18010236

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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