Ocete M A, Gálvez J, Crespo M E, Cruz T, González M, Torres M I, Zarzuelo A
Department of Pharmacology, School of Pharmacy, University of Granada, Spain.
Pharmacology. 1998 Nov;57(5):261-70. doi: 10.1159/000028250.
The flavonoid morin was tested for anti-inflammatory activity in trinitrobenzenesulfonic acid (TNBS)-induced rat colitis. Rats were pretreated orally with several doses of the flavonoid (5, 10, 25, 100 and 200 mg/kg) 48, 24 and 1 h before and 24 h after colitis induction and examined for colonic damage 48 h after colitis induction. Colonic inflammation was characterized by diffuse hemorrhagic necrosis of the mucosa, bowel wall thickening, impairment of fluid absorption, increase in myeloperoxidase (MPO) activity, enhanced leukotriene B4 (LTB4) synthesis, glutathione depletion and increased levels of malonyldialdehyde (MDA). Morin treatment, at doses ranging from 10 to 200 mg/kg, significantly reduced colonic macroscopic damage. This beneficial effect was also confirmed by inhibition of colonic MPO activity. Several mechanisms may contribute to the protective effect exerted by morin. First, inhibition of colonic LTB4 synthesis is a common feature for all the active doses of the flavonoid. Second, the antioxidant properties of morin, which partially prevented colonic glutathione depletion (at doses of 10 and 25 mg/kg) or inhibited colonic MDA production (at doses of 100 and 200 mg/kg), can collaborate in preventing TNBS-induced inflammation.
研究了黄酮类化合物桑色素对三硝基苯磺酸（TNBS）诱导的大鼠结肠炎的抗炎活性。在诱导结肠炎前48小时、24小时和1小时以及诱导后24小时，给大鼠口服几种剂量的该黄酮类化合物（5、10、25、100和200毫克/千克），并在诱导结肠炎48小时后检查结肠损伤情况。结肠炎症的特征为黏膜弥漫性出血坏死、肠壁增厚、液体吸收受损、髓过氧化物酶（MPO）活性增加、白三烯B4（LTB4）合成增强、谷胱甘肽耗竭以及丙二醛（MDA）水平升高。桑色素以10至200毫克/千克的剂量治疗，可显著减轻结肠的宏观损伤。结肠MPO活性的抑制也证实了这种有益作用。桑色素发挥保护作用可能有几种机制。首先，抑制结肠LTB4合成是该黄酮类化合物所有活性剂量的共同特征。其次，桑色素的抗氧化特性，可部分防止结肠谷胱甘肽耗竭（剂量为10和25毫克/千克）或抑制结肠MDA生成（剂量为100和200毫克/千克），有助于预防TNBS诱导的炎症。
