H<sub>2</sub>‐receptor antagonists are scavengers of oxygen radicals

European Journal of Clinical Investigation - Tập 24 Số 7 - Trang 476-481 - 1994
Domenico Lapenna1, Sergio de Gioia1, Andrea Mezzetti1, L. Grossi1, Davide Festi1, Leonardo Marzio1, Franco Cuccurullo1
1Cattedra di Patologia Speciale Medica, Universitá degli Studi ‘G. D'Annunzio’, Facoltá di Medicina e Chirurgia, Chieti, Italy

Tóm tắt

Abstract. Potential oxygen radical scavenging properties of the H2‐receptor antagonists cimetidine, ranitidine and famotidine were investigated. These drugs, although ineffective against superoxide anion and hydrogen peroxide, can scavenge hydroxyl radical (OH·) with a very high rate constant, which is about tenfold higher than that of the specific scavenger mannitol for famotidine (1·7 × 1010 mol−1 s−1) and cimetidine (1·6 × 1010 mol−1 s−1), ranitidine displaying a rate constant of 7·5 × 109 mol−1 s−1. These OH· scavenging effects are significant beginning from 10, 28 and 100 μmol 1−1 concentration for famotidine, cimetidine and ranitidine, respectively, thus suggesting that the drugs may effectively act as OH· scavengers in vivo especially in the gastric lumen. Only cimetidine can apparently bind and inactivate iron, which further emphasizes its antioxidant capacity. Moreover, all drugs, even at 10 μmol 1−1 concentration, show powerful scavenging effects on hypochlorous acid and monochloramine, which are cytotoxic oxidants arising from inflammatory cells, such as neutrophils. These data suggest that some therapeutical effects of H2‐receptor antagonists in peptic ulcer may also be related to their antiradical‐antioxidant capacity, and that these drugs could potentially be used in other disease entities characterized by free radical‐mediated oxidative stress in vivo.

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Thông tin xuất bản

European Journal of Clinical Investigation

Tập 24 Số 7

476-481

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