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黄芪甲苷IV的胃保护作用:前列腺素、巯基和一氧化氮的作用

Gastroprotective effect of Astragaloside IV: role of prostaglandins, sulfhydryls and nitric oxide.

作者信息

Navarrete Andrés, Arrieta Jesús, Terrones Liliana, Abou-Gazar Hassan, Calis Ihsan

机构信息

Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria Coyoacan 04510, México D.F., México.

出版信息

J Pharm Pharmacol. 2005 Aug;57(8):1059-64. doi: 10.1211/0022357056659.

Abstract

This investigation evaluated the gastroprotective activity of Astragaloside IV, a cycloartane-type triterpene glycoside isolated from Astragalus zahlbruckneri. Gastric mucosal damage was induced in rats by intragastric ethanol (1 mL/rat). Rats treated orally with Astragaloside IV suspended in Tween 80 at 3, 10 and 30 mg kg(-1), showed 15, 37 and 52% gastroprotection, respectively. The gastroprotection observed at 30 mg kg(-1) for this compound was attenuated in rats pretreated with N(G)-nitro-L arginine methyl ester (70 mg kg(-1), i.p), a nitric oxide (NO)-synthase inhibitor, suggesting that the gastroprotective mechanism of this glycoside involves, at least in part, the participation of NO. The gastroprotective effect of Astragaloside IV was not affected by the inhibition of prostaglandin synthesis with indometacin (10 mg kg(-1), s.c.) nor by the block of endogenous sulfhydryls with N-ethylmaleimide (NEM, 10 mg kg(-1), s.c.). Carbenoxolone was used as a gastroprotective model drug and showed a dose-dependent gastroprotective effect (25, 43 and 88% of gastroprotection, at 3, 10 and 30 mg kg(-1), respectively). The partial participation of prostaglandins, sulfhydryls and NO was observed in the gastroprotective mechanism of carbenoxolone.

摘要

本研究评估了黄芪甲苷IV的胃保护活性,黄芪甲苷IV是从梭果黄芪中分离得到的一种环阿尔廷型三萜糖苷。通过给大鼠灌胃乙醇(1 mL/只)诱导胃黏膜损伤。用吐温80悬浮的黄芪甲苷IV分别以3、10和30 mg kg⁻¹的剂量口服给药的大鼠,胃保护率分别为15%、37%和52%。用一氧化氮(NO)合酶抑制剂N⁻硝基⁻L⁻精氨酸甲酯(70 mg kg⁻¹,腹腔注射)预处理的大鼠,该化合物在30 mg kg⁻¹剂量下观察到的胃保护作用减弱,这表明该糖苷的胃保护机制至少部分涉及NO的参与。黄芪甲苷IV的胃保护作用不受吲哚美辛(10 mg kg⁻¹,皮下注射)抑制前列腺素合成或N⁻乙基马来酰亚胺(NEM,10 mg kg⁻¹,皮下注射)阻断内源性巯基的影响。甘珀酸用作胃保护模型药物,显示出剂量依赖性的胃保护作用(在3、10和30 mg kg⁻¹时,胃保护率分别为25%、43%和88%)。在甘珀酸的胃保护机制中观察到前列腺素、巯基和NO的部分参与。

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