Wong Jack Ho, Liu Zhaokun, Law Kenneth Wai Kit, Liu Fang, Xia Lixin, Wan David Chi Cheong, Ng Tzi Bun
Peptides. 2014 Dec;62:183-8. doi: 10.1016/j.peptides.2014.07.006.
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.
本研究旨在检测人乳铁蛋白片段和牛乳铁蛋白片段，包括乳铁蛋白（1-11）、乳铁素和乳铁杀菌肽，这些片段在1 mM浓度下对兔红细胞均未表现出溶血活性，以探究其对HIV-1逆转录酶、蛋白酶和整合酶活性可能的抑制作用。数据表明，人乳铁素对HIV-1逆转录酶的抑制作用最强（IC50 = 2 μM）。牛乳铁素（IC50 = 10 μM）和牛乳铁杀菌肽（IC50 = 150 μM）的抑制作用较弱。人乳铁杀菌肽以及1 mM浓度的人乳铁蛋白和牛乳铁蛋白（1-11）对HIV-1逆转录酶均未表现出任何抑制作用。所有肽段对HIV-1蛋白酶仅表现出轻微的抑制作用（抑制率略低于2%至6%）。人乳铁杀菌肽和牛乳铁杀菌肽分别在37 μM和18.5 μM时对HIV-1整合酶表现出明显的抑制作用。人乳铁杀菌肽和牛乳铁杀菌肽对HIV-1整合酶的抑制活性呈剂量依赖性。其他肽段则没有HIV-1整合酶抑制活性。因此，可以得出结论，一些乳铁蛋白片段对HIV-1逆转录酶和HIV-1整合酶具有抑制作用。
