Camuesco Desiree, Comalada Monica, Rodríguez-Cabezas M Elena, Nieto Ana, Lorente Maria D, Concha Angel, Zarzuelo Antonio, Gálvez Julio
Department of Pharmacology, School of Pharmacy, University of Granada, Granada, Spain.
Br J Pharmacol. 2004 Dec;143(7):908-18. doi: 10.1038/sj.bjp.0705941. Epub 2004 Nov 8.
Quercitrin, 3-rhamnosylquercetin, is a bioflavonoid with antioxidant properties, which exerts anti-inflammatory activity in experimental colitis. In the present study, different in vivo experiments were performed in order to evaluate the mechanisms of action involved in this effect, with special attention to its effects on proinflammatory mediators, including nitric oxide (NO). Experimental colitis was induced in female Wistar rats by incorporation of dextran sodium sulfate (DSS) in drinking water. Oral treatment of quercitrin (1 or 5 mg kg(-1) day(-1)) to colitic rats ameliorated the evolution of the inflammatory process induced when administered in a preventative dosing protocol. When quercitrin (1 mg kg(-1) day(-1)) was administered on established colitis, it facilitated the recovery of the inflamed mucosa. The beneficial effects exerted by quercitrin were evidenced both histologically and biochemically, and were associated with an improvement in the colonic oxidative status, altered as a consequence of the colonic insult induced by DSS. In addition, a reduction of colonic NO synthase activity was observed, probably related to a decreased expression in the inducible form of the enzyme via downregulation in the colonic activity of the nuclear factor-kappaB. Immunohistochemical studies showed that quercitrin treatment reduced macrophage and granulocyte infiltration in the inflamed tissue.
槲皮苷,即3 - 鼠李糖基槲皮素,是一种具有抗氧化特性的生物类黄酮,在实验性结肠炎中发挥抗炎活性。在本研究中,进行了不同的体内实验以评估这种作用所涉及的作用机制,特别关注其对包括一氧化氮(NO)在内的促炎介质的影响。通过在饮用水中加入葡聚糖硫酸钠(DSS)诱导雌性Wistar大鼠发生实验性结肠炎。对结肠炎大鼠口服给予槲皮苷(1或5 mg kg⁻¹ 天⁻¹),在预防性给药方案中给药时可改善诱导的炎症过程的进展。当对已确诊的结肠炎给予槲皮苷(1 mg kg⁻¹ 天⁻¹)时,它促进了炎症黏膜的恢复。槲皮苷所发挥的有益作用在组织学和生化方面均得到证实,并且与结肠氧化状态的改善有关,结肠氧化状态因DSS诱导的结肠损伤而改变。此外,观察到结肠一氧化氮合酶活性降低,这可能与通过下调核因子 - κB的结肠活性而导致该酶诱导形式的表达减少有关。免疫组织化学研究表明,槲皮苷治疗减少了炎症组织中的巨噬细胞和粒细胞浸润。