title: Anti-HIV-1 activity of a new scorpion venom peptide derivative Kn2-7.
abstract: For over 30 years, HIV/AIDS has wreaked havoc in the world. In the absence of an effective vaccine for HIV, development of new anti-HIV agents is urgently needed. We previously identified the antiviral activities of the scorpion-venom-peptide-derived mucroporin-M1 for three RNA viruses (measles viruses, SARS-CoV, and H5N1). In this investigation, a panel of scorpion venom peptides and their derivatives were designed and chosen for assessment of their anti-HIV activities. A new scorpion venom peptide derivative Kn2-7 was identified as the most potent anti-HIV-1 peptide by screening assays with an EC(50) value of 2.76 µg/ml (1.65 µM) and showed low cytotoxicity to host cells with a selective index (SI) of 13.93. Kn2-7 could inhibit all members of a standard reference panel of HIV-1 subtype B pseudotyped virus (PV) with CCR5-tropic and CXCR4-tropic NL4-3 PV strain. Furthermore, it also inhibited a CXCR4-tropic replication-competent strain of HIV-1 subtype B virus. Binding assay of Kn2-7 to HIV-1 PV by Octet Red system suggested the anti-HIV-1 activity was correlated with a direct interaction between Kn2-7 and HIV-1 envelope. These results demonstrated that peptide Kn2-7 could inhibit HIV-1 by direct interaction with viral particle and may become a promising candidate compound for further development of microbicide against HIV-1.
authors.affiliation: State Key Laboratory of Virology, College of Life Sciences, Wuhan University, Wuhan, People's Republic of China.
authors.forename: Yaoqing
authors.initials: Y
authors.lastname: Chen
authors.forename: Luyang
authors.initials: L
authors.lastname: Cao
authors.forename: Maohua
authors.initials: M
authors.lastname: Zhong
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.forename: Chen
authors.initials: C
authors.lastname: Han
authors.forename: Qiaoli
authors.initials: Q
authors.lastname: Li
authors.forename: Jingyi
authors.initials: J
authors.lastname: Yang
authors.forename: Dihan
authors.initials: D
authors.lastname: Zhou
authors.forename: Wei
authors.initials: W
authors.lastname: Shi
authors.forename: Benxia
authors.initials: B
authors.lastname: He
authors.forename: Fang
authors.initials: F
authors.lastname: Liu
authors.forename: Jie
authors.initials: J
authors.lastname: Yu
authors.forename: Ying
authors.initials: Y
authors.lastname: Sun
authors.forename: Yuan
authors.initials: Y
authors.lastname: Cao
authors.forename: Yaoming
authors.initials: Y
authors.lastname: Li
authors.forename: Wenxin
authors.initials: W
authors.lastname: Li
authors.forename: Deying
authors.initials: D
authors.lastname: Guo
authors.forename: Zhijian
authors.initials: Z
authors.lastname: Cao
authors.forename: Huimin
authors.initials: H
authors.lastname: Yan
mesh_terms: D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008969:Molecular Sequence Data; D011485:Protein Binding; D017433:Protein Structure, Secondary; D012604:Scorpion Venoms / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D019380:Anti-HIV Agents; D023181:Antimicrobial Cationic Peptides; C574603:Kn2-7 peptide; D012604:Scorpion Venoms