Gressier B, Cabanis A, Lebegue S, Brunet C, Dine T, Luyckx M, Cazin M, Cazin J C
Faculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Clinique, Lille, France.
Methods Find Exp Clin Pharmacol. 1994 Jan-Feb;16(1):9-13.
Among reactive oxygen species generated by human neutrophils during inflammatory disorders, hypochlorous acid and hydroxyl radical are especially involved in many diseases such as arteriosclerosis or emphysema. It was shown in vitro that two thiol-containing drugs, mesna and N-acetylcysteine, have antioxidant properties towards these oxidants. The 50% inhibitory concentrations (IC50s) of mesna and N-acetylcysteine for hypochlorous acid production by stimulated neutrophils were 29 and 30 mcM, respectively, and for hydroxyl radical production, IC50s were 520 and 480 mcM, respectively. With this in vitro demonstrated effectiveness, both mesna and N-acetylcysteine have been considered as therapeutic antioxidants to decrease tissue damage inflicted by an excess of activated neutrophils by scavenging hypochlorous acid and hydroxyl radical.
在炎症性疾病中人类中性粒细胞产生的活性氧物种中,次氯酸和羟基自由基尤其与许多疾病有关,如动脉硬化或肺气肿。体外实验表明,两种含硫醇的药物,美司钠和N - 乙酰半胱氨酸,对这些氧化剂具有抗氧化特性。美司钠和N - 乙酰半胱氨酸对受刺激的中性粒细胞产生次氯酸的50%抑制浓度(IC50)分别为29和30 μM,对羟基自由基产生的IC50分别为520和480 μM。鉴于这种体外实验证明的有效性,美司钠和N - 乙酰半胱氨酸都被认为是治疗性抗氧化剂,通过清除次氯酸和羟基自由基来减少过量活化的中性粒细胞造成的组织损伤。