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菊苣叶香茶菜中的 3,5-二(1-丙烯基)-4-羟基苯乙酮的镇痛作用及其胃保护机制。

Antinociceptive effect and gastroprotective mechanisms of 3,5-diprenyl-4-hydroxyacetophenone from Ageratina pichinchensis.

机构信息

Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, Colonia Santo Tomás, Delegación Miguel Hidalgo, México, D F Mexico.

出版信息

Fitoterapia. 2013 Jun;87:11-9. doi: 10.1016/j.fitote.2013.03.015. Epub 2013 Mar 22.

Abstract

The present study aimed to evaluate the antinociceptive activity (in inflammatory and neuropathic pain models) and gastroprotective effect of the 3,5-diprenyl-4-hydroxyacetophenone (HYDP), isolated from Ageratina pichinchensis. The gastroprotective activity of this plant was previously reported by our workgroup, finding encesanescin to be one active compound. The present results show that HYDP reduced nociception in a dose-dependent manner in carrageenan and L5/L6 spinal nerve ligation, with efficacies of 72.6 and 57.1%, respectively, at doses of 100 and 562 mg/kg. HYDP also showed gastroprotective activity in the model of ethanol-induced gastric lesion, with a 75.59% maximum inhibition of ulcers at a dose of 100mg/kg. This gastroprotective effect was attenuated by N(G)-nitro-L-arginine methyl ester, indomethacin and N-ethylmaleimide, indicating that NO, prostaglandins and sulfhydryl groups are involved in the mechanisms of action. This is the first evidence, to our knowledge, of the antinociceptive and gastroprotective activities of HYDP.

摘要

本研究旨在评估从 Ageratina pichinchensis 中分离得到的 3,5-二烯丙基-4-羟基苯乙酮(HYDP)的抗伤害活性(在炎症和神经病理性疼痛模型中)和胃保护作用。我们的研究小组之前已经报道了该植物的胃保护活性,发现 encesanescin 是一种活性化合物。目前的结果表明,HYDP 以剂量依赖性方式降低角叉菜胶和 L5/L6 脊神经结扎引起的疼痛,在 100 和 562mg/kg 剂量下的效力分别为 72.6%和 57.1%。HYDP 还在乙醇诱导的胃损伤模型中表现出胃保护活性,在 100mg/kg 剂量下最大抑制溃疡率为 75.59%。这种胃保护作用被 N(G)-硝基-L-精氨酸甲酯、吲哚美辛和 N-乙基马来酰亚胺减弱,表明 NO、前列腺素和巯基参与了作用机制。这是迄今为止首次证明 HYDP 具有抗伤害和胃保护活性。

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