MEDIATORS INVOLVED IN INFLAMMATION - EFFECTS OF DAFLON 500MG ON THEIR RELEASE
MEDIATORS INVOLVED IN INFLAMMATION - EFFECTS OF DAFLON 500MG ON THEIR RELEASE
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DOI：
10.1177/000331979404500610
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发表时间：
1994-06-01
期刊：
影响因子：
2.8
通讯作者：
BODINIER, MC
中科院分区：
文献类型：
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作者：
JEAN, T;BODINIER, MC
炎症反应的每一步都是由一种或几种化学或生物介质触发的，如花生四烯酸衍生物(前列腺素[PG]、白三烯[LT]或血栓烷[TX])、血管活性胺(组胺或5-羟色胺)和氧自由基(超氧阴离子，O2-或过氧化氢，过氧化氢)。在周围静脉炎症中，这些介质在促进血管扩张(组胺)，增加膜通透性(PGE_2，组胺，自由基)和为特殊细胞，如中性粒细胞，巨噬细胞，淋巴细胞(LTB_4，自由基)提供趋化信号方面发挥着重要作用。达富隆500 mg，一种微粉化的精制黄酮组分(90%地奥司明，10%橙皮苷)，在不同的体内和体外模型中，研究了达富隆500 mg的抗炎作用。在大鼠炎性肉芽肿模型中，达氟隆500 mg(100 mg/kg，口服)减少了水肿的形成，并抑制了PGE2(78.5%)的合成。PGF_2α(45.2%)和TXB_2(59.5%)(Damon et al，Arzneim-Forsch/Drug Res 37：1149-1153,1987)。静脉注射达富隆500 mg(25和50 mg/kg)可降低四氧嘧啶所致的大鼠高血糖。Daflon 500 mg的这种作用与其清除活性氧自由基的能力有关，该能力是通过酵母多糖刺激的人中性粒细胞(LonChampt等，Arzneim-Forsch/Drug Res 39：882-885,1989)或小鼠腹膜巨噬细胞(Bodinier等，手稿正在准备中)在体外演示的。达富龙500 mg在10(-7)~10(-4)M的浓度范围内具有清除自由基的作用，在10(-6)M至10(-5)M之间有半极大的清除作用。因此，达富龙500 mg是一种有效的抗炎性疾病保护剂。这些特性，在体内和体外都证明了它的合理性
Each step of an inflammatory reaction is triggered by one or several chemical or biological mediators such as arachidonic acid derivatives (prostaglandins [PG], leukotrienes [LT], or thromboxanes [TX]), vasoactive amines (histamine or serotonin), and oxygen free radicals (superoxide ion, O2-, or hydrogen peroxide, H2O2). In perivenous inflammation, these mediators play a prominent role in favoring vasodilatation (histamine), increasing membrane permeability (PGE2, histamine, free radicals) and providing a chemotactic signal for specialized cells, ie, neutrophil polynuclears, macrophages, lymphocytes (LTB4, free radicals).The antinflammatory effects of Daflon 500 mg,* a micronized purified flavonoid fraction (90% diosmin, 10% hesperidin), were studied in different in vivo and in vitro models.In a model of inflammatory granuloma in the rat, Daflon 500 mg (100 mg/kg, orally) reduced edema formation and inhibited the synthesis for PGE2 (78.5%), PGF2alpha (45.2%) and TXB2 (59.5%) (Damon et al, Arzneim-Forsch/Drug Res 37:1149-1153, 1987).Intravenous injection of Daflon 500 mg (25 and 50 mg/kg) reduced the hyperglycemia induced by injection of alloxan in rat. This effect of Daflon 500 mg was linked to its ability to scavenge active oxygen radicals, demonstrated in vitro using human neutrophils (Lonchampt et al, Arzneim-forsch/Drug Res 39:882-885, 1989) or mouse peritoneal macrophages (Bodinier et al, manuscript in preparation) stimulated by zymosan. The free radical scavenger effect of Daflon 500 mg is observed at concentrations ranging from 10(-7)M to 10(-4)M, with half-maximal effect between 10(-6)M and 10(-5)M.Thus, Daflon 500 mg behaves as a potent protective agent against inflammatory disorders. These properties, demonstrated both in vivo and in vitro, justify its