Bourinbaiar A S, Fruhstorfer E C
Metatron, Inc., New York, NY 10003, USA.
Life Sci. 1996;59(23):PL 365-70. doi: 10.1016/s0024-3205(96)00553-x.
The suppression of human immunodeficiency virus (HIV) replication by histamine type 2 (H2) receptor antagonists, cimetidine, ranitidine, and famotidine was examined in vitro. The 50% reduction (IC50) in p24 antigen expression caused by the anti-ulcer agent, cimetidine, was observed at 26.8 nM with IC100 at 10 microM. Unlike azidothymidine-a reverse transcriptase inhibitor-cimetidine blocked HIV infection without affecting cell growth, as no cytotoxicity was observed even at the highest 1 mM dose. Ranitidine and famotidine were less potent than cimetidine. H1 antagonists, cyproheptadine and diphenhydramine, had no effect on HIV replication. Although the activity of cimetidine was observed at concentrations attainable by oral administration, the mechanism of anti-HIV action is unknown. This is the first report on antiretroviral action of H2 blockers. Further studies are warranted to establish the potential of a new class of anti-HIV agents with immunomodulating properties.
在体外研究了2型组胺（H2）受体拮抗剂西咪替丁、雷尼替丁和法莫替丁对人类免疫缺陷病毒（HIV）复制的抑制作用。抗溃疡药西咪替丁导致p24抗原表达降低50%（IC50）时的浓度为26.8 nM，IC100为10 μM。与逆转录酶抑制剂叠氮胸苷不同，西咪替丁可阻断HIV感染而不影响细胞生长，因为即使在最高1 mM剂量下也未观察到细胞毒性。雷尼替丁和法莫替丁的效力低于西咪替丁。H1拮抗剂赛庚啶和苯海拉明对HIV复制无影响。虽然在口服可达到的浓度下观察到了西咪替丁的活性，但其抗HIV作用机制尚不清楚。这是关于H2阻滞剂抗逆转录病毒作用的首次报道。有必要进一步研究以确定具有免疫调节特性的新型抗HIV药物的潜力。
