Lonchampt M, Guardiola B, Sicot N, Bertrand M, Perdrix L, Duhault J
Institut de Recherches Servier, Suresnes, France.
Arzneimittelforschung. 1989 Aug;39(8):882-5.
S 5682 is a purified flavonoid fraction containing 90% diosmin (flavone derivative) and 10% hesperidin (flavanone derivative). In this study the scavenging properties of S 5682 on active oxygen radicals were demonstrated in vivo and in vitro. The activity of intravenous S 5682 was evaluated in the rat by measuring the degree of hyperglycemia provoked by an intravenous injection of alloxan, the metabolism of which produces active oxygen radicals which are toxic to B cells of the pancreas. S 5682 produced a decrease in the hyperglycemia in a dose-dependent manner (25 mg/kg and 50 mg/kg). The production in vitro of active oxygen radicals during phagocytosis by polymorphonuclear cells and macrophages is accompanied by emission of photons which can be amplified in the presence of luminol. Measurement of this chemiluminescence is a way of determining the quantity of active oxygen radicals generated in the medium, this may be reduced either by a decrease in production or by an increase in neutralisation through a reducing effect. Results demonstrated that S 5682 had a scavenging effect on active oxygen radicals for concentrations between 2 x 10(-8) mol/l and 2 x 10(-4) mol/l. The concentration of S 5682 reducing the chemiluminescence by 50% was 1.6 x 10(-5) mol/l. These scavenging properties imply that S 5682 has a pharmacological action on capillary hyperpermeability as well as an anti-inflammatory and anti-oedematous action.
S 5682是一种纯化的类黄酮组分，含有90%的地奥司明（黄酮衍生物）和10%的橙皮苷（黄烷酮衍生物）。在本研究中，S 5682对活性氧自由基的清除特性在体内和体外均得到了证实。通过测量静脉注射四氧嘧啶诱发的高血糖程度来评估大鼠体内静脉注射S 5682的活性，四氧嘧啶的代谢会产生对胰腺B细胞有毒性的活性氧自由基。S 5682以剂量依赖的方式（25毫克/千克和50毫克/千克）降低了高血糖水平。多形核细胞和巨噬细胞吞噬过程中活性氧自由基的体外产生伴随着光子发射，在鲁米诺存在的情况下这种发射可以被放大。测量这种化学发光是确定培养基中产生的活性氧自由基数量的一种方法，活性氧自由基数量可以通过产生减少或通过还原作用增加中和作用而降低。结果表明，S 5682在2×10⁻⁸摩尔/升至2×10⁻⁴摩尔/升的浓度范围内对活性氧自由基具有清除作用。使化学发光降低50%的S 5682浓度为1.6×10⁻⁵摩尔/升。这些清除特性意味着S 5682对毛细血管通透性具有药理作用以及抗炎和抗水肿作用。
