Sood Shailja, Muthuraman Arunachalam
Rayat Institute of Pharmacy, Nawanshahr District, Railmajra, Punjab, India.
Yakugaku Zasshi. 2009 Dec;129(12):1523-8. doi: 10.1248/yakushi.129.1523.
The effect of tacrolimus (FK506) on peptic ulcer was evaluated using pyloric ligation (PL) model in rats. Tacrolimus was administered orally at different doses (1, 2 and 3 mg/kg) and it showed a gastric ulcer healing effect in a dose dependent manner. Gastric volume, total and free acidity and ulcerative index parameters were reduced in the tacrolimus treated rats as compared to pyloric ligated rats. The higher dose (3 mg/kg) treated group produced significant results similar to that of the ranitidine (50 mg/kg) treated group. Pretreatment with tacrolimus also produced significant (p<0.05) reduction in TBARS, total calcium, TNF-alpha, IL-8 and MPO whereas it showed an increase in GSH level at higher dose. The anti-secretory and anti-ulcerative effect of tacrolimus may be due to immunosuppressive actions by inhibition of calcineurin and the oxidative pathway. It can be concluded that tacrolimus can play an important role in the treatment of peptic ulcer disorder to improve the quality of life.
采用大鼠幽门结扎（PL）模型评估他克莫司（FK506）对消化性溃疡的作用。他克莫司以不同剂量（1、2和3毫克/千克）口服给药，呈剂量依赖性地显示出胃溃疡愈合作用。与幽门结扎大鼠相比，他克莫司治疗的大鼠胃体积、总酸度和游离酸度以及溃疡指数参数均降低。高剂量（3毫克/千克）治疗组产生的显著结果与雷尼替丁（50毫克/千克）治疗组相似。他克莫司预处理还使丙二醛、总钙、肿瘤坏死因子-α、白细胞介素-8和髓过氧化物酶显著降低（p<0.05），而在高剂量时谷胱甘肽水平升高。他克莫司的抗分泌和抗溃疡作用可能归因于通过抑制钙调神经磷酸酶和氧化途径产生的免疫抑制作用。可以得出结论，他克莫司在消化性溃疡疾病的治疗中可发挥重要作用，以改善生活质量。
