Zanatta Francielle, Gandolfi Renan Becker, Lemos Marivane, Ticona Juan Carlos, Gimenez Alberto, Clasen Bruna Kurz, Cechinel Filho Valdir, de Andrade Sérgio Faloni
Programa de Mestrado em Ciências Farmacêuticas, Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí-UNIVALI, Itajaí, Santa Catarina, Brazil.
Chem Biol Interact. 2009 Jul 15;180(2):312-7. doi: 10.1016/j.cbi.2009.04.001. Epub 2009 Apr 14.
As part of our continuing search for bioactive natural products from plants, the present study was carried out in order to evaluate the gastroprotective properties of alkaloid extract and 2-phenylquinoline obtained from the bark of Galipea longiflora (Rutaceae). Anti-ulcer assays were performed using the following protocols in mice: nonsteroidal anti-inflammatory drug (NSAID)/bethanecol-induced ulcer, ethanol/HCl-induced ulcer, and stress-induced ulcer. The effects of the extract on gastric content volume, pH and total acidity were also evaluated, using the pylorus ligated model. Treatment using doses of 50, 125 and 250 mg/kg of G. longiflora alkaloid extract and positive controls (omeprazol or cimetidine) significantly diminished the lesion index, total lesion area, and percentage of lesion, in comparison with the negative control groups in all the models evaluated. Regarding the model of gastric secretion, a reduction in volume of gastric juice and total acidity was observed, as well as an increase in gastric pH. The main alkaloid of the plant, 2-phenylquinoline, was also evaluated in the ethanol-induced ulcer model. The results showed that at a dose of 50 mg/kg, it significantly inhibited ulcerative lesions. However, this effect was less than that of the alkaloid extract. All these results taken together show that G. longiflora displays gastroprotective activity, as evidenced by its significant inhibition of the formation of ulcers induced by different models. There are indications that mechanisms involved in anti-ulcer activity are related to a decrease in gastric secretion and an increase in gastric mucus content. Also, there is evidence of involvement of NO in the gastroprotector mechanisms. These effects may be attributed, at least in part, to the presence of some alkaloids, particularly 2-phenylquinoline.
作为我们持续从植物中寻找生物活性天然产物工作的一部分,开展了本研究,以评估从长花加里波木(芸香科)树皮中获得的生物碱提取物和2-苯基喹啉的胃保护特性。在小鼠中使用以下方案进行抗溃疡试验:非甾体抗炎药(NSAID)/氨甲酰甲胆碱诱导的溃疡、乙醇/盐酸诱导的溃疡和应激诱导的溃疡。还使用幽门结扎模型评估了提取物对胃内容物体积、pH值和总酸度的影响。与所有评估模型中的阴性对照组相比,使用50、125和250mg/kg剂量的长花加里波木生物碱提取物及阳性对照(奥美拉唑或西咪替丁)进行治疗,显著降低了损伤指数、总损伤面积和损伤百分比。关于胃分泌模型,观察到胃液体积和总酸度降低,以及胃pH值升高。还在乙醇诱导的溃疡模型中评估了该植物的主要生物碱2-苯基喹啉。结果表明,在50mg/kg剂量下,它能显著抑制溃疡性病变。然而,这种作用小于生物碱提取物。综合所有这些结果表明,长花加里波木具有胃保护活性,不同模型诱导的溃疡形成受到其显著抑制即为明证。有迹象表明,抗溃疡活性涉及的机制与胃分泌减少和胃黏液含量增加有关。此外,有证据表明一氧化氮参与了胃保护机制。这些作用可能至少部分归因于某些生物碱的存在,特别是2-苯基喹啉。
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