title: A study of effects of peptide fragments of bovine and human lactoferrins on activities of three key HIV-1 enzymes.
abstract: The intent of this study was to examine human and bovine lactoferrin fragments including lactoferrin (1-11), lactoferricin and lactoferrampin, all of which did not demonstrate hemolytic activity toward rabbit erythrocytes at 1 mM concentration, for possible inhibitory effects on the activities of HIV-1 reverse transcriptase, protease and integrase. The data showed that human lactoferricin was the most potent in inhibiting HIV-1 reverse transcriptase (IC50 =2 μM). Bovine lactoferricin (IC50 = 10 μM) and bovine lactoferrampin (IC50 = 150 μM) were less potent. Human lactoferrampin and human and bovine lactoferrin (1-11) at 1 mM concentration did not exhibit any inhibitory effect on HIV-1 reverse transcriptase. All peptides showed only a slight inhibitory effect (from slightly below 2% to 6% inhibition) on HIV-1 protease. Human lactoferrampin and bovine lactoferrampin showed obvious inhibitory effect on HIV-1 integrase at 37 μM and 18.5 μM, respectively. The HIV-1 integrase inhibitory activity of human lactoferrampin and bovine lactoferrampin was dose-dependent. The other peptides were devoid of HIV-1 integrase inhibitory activity. Thus, it is concluded that some lactoferrin fragments exert an inhibitory action on HIV-1 reverse transcriptase and HIV-1 integrase.
authors.forename: Jack Ho
authors.initials: JH
authors.lastname: Wong
authors.forename: Zhaokun
authors.initials: Z
authors.lastname: Liu
authors.forename: Kenneth Wai Kit
authors.initials: KW
authors.lastname: Law
authors.forename: Fang
authors.initials: F
authors.lastname: Liu
authors.forename: Lixin
authors.initials: L
authors.lastname: Xia
authors.forename: David Chi Cheong
authors.initials: DC
authors.lastname: Wan
authors.forename: Tzi Bun
authors.initials: TB
authors.lastname: Ng
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002417:Cattle; D004912:Erythrocytes / Q000187:drug effects; D019427:HIV Integrase / Q000187:drug effects; D016333:HIV Protease / Q000187:drug effects; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D007781:Lactoferrin / Q000008:administration & dosage* / Q000235:genetics; D010446:Peptide Fragments / Q000008:administration & dosage* / Q000235:genetics; D011817:Rabbits
chemical_list: C490098:LTF protein, human; D010446:Peptide Fragments; C502040:lactoferrampin; C082171:lactoferricin B; D019427:HIV Integrase; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; D007781:Lactoferrin; D016333:HIV Protease; C514803:p16 protease, Human immunodeficiency virus 1; C514801:p31 integrase protein, Human immunodeficiency virus 1