title: 3-hydroxyphthalic anhydride-modified chicken ovalbumin exhibits potent and broad anti-HIV-1 activity: a potential microbicide for preventing sexual transmission of HIV-1.
abstract: Heterosexual transmission is the primary route by which women acquire human immunodeficiency virus (HIV)/AIDS. Thus, development of woman-controlled topical microbicides for prevention of sexual transmission of HIV is urgently needed. Here we report that 3-hydroxyphthalic anhydride-modified chicken ovalbumin (HP-OVA) exhibits potent antiviral activity against a broad spectrum of human immunodeficiency virus type 1 (HIV-1) isolates with different genotypes and biotypes. Its antiviral activity is correlated with the percentages of the chemically modified and unmodified lysines and arginines in OVA. HP-OVA inhibits HIV-1 fusion and entry through multiple mechanisms of action, including (i) blocking gp120 binding to CD4 and (ii) interfering with gp41 six-helix bundle formation. Because of the widespread availability and established safety profile of OVA, HP-OVA has good potential to be developed as an effective, safe, and affordable microbicide for prevention of HIV sexual transmission.
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong, China.
authors.forename: Lin
authors.initials: L
authors.lastname: Li
authors.forename: Lili
authors.initials: L
authors.lastname: He
authors.forename: Suiyi
authors.initials: S
authors.lastname: Tan
authors.forename: Xinhua
authors.initials: X
authors.lastname: Guo
authors.forename: Hong
authors.initials: H
authors.lastname: Lu
authors.forename: Zhi
authors.initials: Z
authors.lastname: Qi
authors.forename: Chungen
authors.initials: C
authors.lastname: Pan
authors.forename: Xiuli
authors.initials: X
authors.lastname: An
authors.forename: Shibo
authors.initials: S
authors.lastname: Jiang
authors.forename: Shuwen
authors.initials: S
authors.lastname: Liu
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000494:pharmacology*; D001120:Arginine / Q000737:chemistry; D016466:CHO Cells; D002645:Chickens; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D004847:Epithelial Cells / Q000166:cytology / Q000821:virology; D005260:Female; D015700:HIV Envelope Protein gp41 / Q000737:chemistry; D015658:HIV Infections / Q000517:prevention & control* / Q000635:transmission; D015497:HIV-1 / Q000187:drug effects*; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D007371:Interferon-gamma / Q000378:metabolism; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000378:metabolism / Q000821:virology; D008239:Lysine / Q000737:chemistry; D008561:Membrane Fusion / Q000187:drug effects; D008970:Molecular Weight; D010047:Ovalbumin / Q000737:chemistry / Q000494:pharmacology*; D010796:Phthalic Anhydrides / Q000737:chemistry / Q000494:pharmacology*; D017433:Protein Structure, Secondary; D015229:Sexually Transmitted Diseases, Viral / Q000517:prevention & control / Q000635:transmission; D015302:Simian Immunodeficiency Virus / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D015700:HIV Envelope Protein gp41; D010796:Phthalic Anhydrides; C478070:3-hydroxyphthalic anhydride; D007371:Interferon-gamma; D010047:Ovalbumin; D001120:Arginine; D008239:Lysine