Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, Colonia Casco de Santo Tomás, Miguel Hidalgo, Ciudad de México 11340, Mexico.
Facultad de Estudios Superiores Zaragoza, UNAM. Av. Guelatao No. 66, Colonia Ejército de Oriente, Iztapalapa, Ciudad de México 09230, Ciudad de Mexico.
Molecules. 2020 May 10;25(9):2246. doi: 10.3390/molecules25092246.
Peptic ulcer disease, the most common gastrointestinal disorder, is currently treated with several types of drugs, but all have severe side effects. The aim of the present study was to evaluate the gastroprotective activity of juanislamin, isolated from , in a rat model of ethanol-induced gastric lesions. Thirty minutes after orally administering a given dose of juanislamin (from 1 to 30 mg/kg) or carbenoxolone (the reference drug, at 1-100 mg/kg) to rats, 1 mL of ethanol was applied, and the animals were sacrificed 2 h later. The stomachs were removed and opened to measure the total area of lesions in each. To examine the possible participation of prostaglandins, nitric oxide and/or sulfhydryl groups in the mechanism of action of juanislamin, the rats received indomethacin, NG-Nitro-l-arginine methyl ester hydrochloride (l-NAME) or -ethylmaleimide pretreatment, respectively, before being given juanislamin and undergoing the rest of the methodology. Juanislamin inhibited gastric lesions produced by ethanol in a non-dose-dependent manner, showing the maximum gastroprotective effect (100%) at 10 mg/kg. The activity of juanislamin was not modified by pretreatment with indomethacin, l-NAME or -ethylmaleimide. In conclusion, juanislamin protected the gastric mucosa from ethanol-induced damage, and its mechanism of action apparently does not involve prostaglandins, nitric oxide or sulfhydryl groups.
消化性溃疡病是最常见的胃肠道疾病，目前有多种类型的药物治疗，但都有严重的副作用。本研究旨在评估从 中分离得到的 Juanislamin 在乙醇诱导的大鼠胃损伤模型中的胃保护活性。大鼠口服给予一定剂量的 Juanislamin（1-30mg/kg）或 carbenoxolone（参考药物，1-100mg/kg）30 分钟后，给予 1ml 乙醇，2 小时后处死动物。取出胃并打开以测量每个胃的总损伤面积。为了研究 Juanislamin 作用机制中前列腺素、一氧化氮和/或巯基基团的可能参与，大鼠在给予 Juanislamin 并进行其余方法之前分别接受吲哚美辛、NG-硝基-L-精氨酸甲酯盐酸盐（l-NAME）或 -乙基马来酰亚胺预处理。Juanislamin 以非剂量依赖性方式抑制乙醇引起的胃损伤，在 10mg/kg 时表现出最大胃保护作用（100%）。吲哚美辛、l-NAME 或 -乙基马来酰亚胺预处理不改变 Juanislamin 的活性。综上所述，Juanislamin 保护胃黏膜免受乙醇诱导的损伤，其作用机制显然不涉及前列腺素、一氧化氮或巯基基团。
