Drug Metabolism & Toxicology Research Laboratories, Department of Biochemistry, College of Medicine, University of Ibadan, Ibadan, Nigeria.
Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):49-55. doi: 10.1111/bcpt.12050. Epub 2013 Mar 21.
The beneficial effects of kolaviron, a natural biflavonoid from the seeds of Garcinia kola, have been attributed mainly to its antioxidant and anti-inflammatory effects. This study investigated these effects on dextran sulphate sodium (DSS)-induced ulcerative colitis in rats. Sulfasalazine served as standard reference in this study. Kolaviron and sulfasalazine were separately co-administered orally at 200 mg/kg and 500 mg/kg, respectively, to dextran sulphate sodium-exposed rats for 5 days. The result indicated that kolaviron or sulfasalazine significantly prevented DSS-induced body weight loss as well as the incidence of diarrhoea and bleeding in DSS-exposed rats. Kolaviron suppressed the DSS-mediated increase in colonic nitric oxide concentration and myeloperoxidase activity and significantly prevented the increase in inflammatory mediators, interleukin-1β and tumour necrosis factor alpha, in the colon of DSS-treated rats. The significant depletion in colonic antioxidant status in rats exposed to DSS alone was evident by marked reduction in colonic catalase and glutathione S-transferase activities as well as glutathione content, leading to elevated hydrogen peroxide and lipid peroxidation levels. Histopathologically, DSS alone resulted in severe epithelial erosion, total absence of goblet cells, destruction of the crypts, necrotic and distorted glands, accompanied by marked cellular mononuclear cells infiltration. However, administration of kolaviron and sulfasalazine ameliorated DSS-induced colitis by increasing the antioxidant status decreased hydrogen peroxide and lipid peroxidation levels and attenuated the adverse effect of DSS on colon architecture. In conclusion, the anti-colitis effect of kolaviron is related to its intrinsic anti-inflammatory and anti-oxidative properties.
科拉维酮是从可乐果种子中提取的一种天然双黄酮，其有益作用主要归因于其抗氧化和抗炎作用。本研究探讨了其对葡聚糖硫酸钠（DSS）诱导的大鼠溃疡性结肠炎的影响。本研究以柳氮磺胺吡啶为标准参考。分别以 200mg/kg 和 500mg/kg 的剂量将科拉维酮和柳氮磺胺吡啶口服给予 DSS 暴露的大鼠，共 5 天。结果表明，科拉维酮或柳氮磺胺吡啶可显著预防 DSS 诱导的体重减轻以及 DSS 暴露大鼠腹泻和出血的发生率。科拉维酮抑制了 DSS 介导的结肠中一氧化氮浓度和髓过氧化物酶活性的增加，并显著防止了 DSS 处理大鼠结肠中炎症介质白细胞介素-1β和肿瘤坏死因子-α的增加。单独用 DSS 处理的大鼠结肠抗氧化状态显著耗尽，表现在结肠过氧化氢酶和谷胱甘肽 S-转移酶活性以及谷胱甘肽含量明显降低，导致过氧化氢和脂质过氧化水平升高。组织病理学上，单独的 DSS 导致严重的上皮侵蚀，杯状细胞完全缺失，隐窝破坏，坏死和扭曲的腺体，伴有明显的单核细胞浸润。然而，科拉维酮和柳氮磺胺吡啶的给药通过增加抗氧化状态，降低过氧化氢和脂质过氧化水平，减轻 DSS 对结肠结构的不良影响，改善了 DSS 诱导的结肠炎。总之，科拉维酮的抗结肠炎作用与其内在的抗炎和抗氧化特性有关。
