Adzu Bulus, Balogun Sikiru Olaitan, Pavan Eduarda, Ascêncio Sérgio Donizeti, Soares Ilsamar Mendes, Aguiar Raimundo Wagner Souza, Ribeiro Reginaldo Vicente, Beserra Ângela Márcia Selhorst e Silva, de Oliveira Ruberlei Godinho, da Silva Larissa Irene, Damazo Amílcar Sabino, Martins Domingos Tabajara de Oliveira
Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil; Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development (NIPRD), Abuja, Nigeria.
Área de Farmacologia, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.
J Ethnopharmacol. 2015 Dec 4;175:378-89. doi: 10.1016/j.jep.2015.09.027. Epub 2015 Sep 25.
ETHNOPHARMACOLOGICAL RELEVANCE: Copaifera malmei Harms (Fabaceae) is a plant that occurs in the central region of Brazil, where the plant's leaves infusion is popularly used to treat gastric ulcer and inflammatory diseases. This study was aimed to investigate the gastroprotective activity and mode of action of the plants' leaves infusion in order to establish the scientific basis for such usage, and to assess its potential as a source of an anti-ulcer agent. MATERIALS AND METHODS: Leaves infusion extract of the plant (SIECm) was prepared, freeze dried and lyophilised. Its qualitative and quantitative phytochemical constituents were investigated using TLC and HPLC techniques. The safety profile was evaluated on CHO-k1 epithelial cells viability using the Alamar blue assay, and by acute toxicity test in mice. The gastroprotection and anti-ulcer efficacy of the SIECm (25, 100 and 400mg/kg, p.o.) were tested using acute (acidified ethanol, piroxicam and water restrain stress), and chronic (acetic acid) experimental ulcer models. The plausible mode of action of the SIECm was assessed using gastric secretion, gastric barrier mucus, nitric oxide, and its antioxidant (myeloperoxidase and catalase) effects in mice and rats. The histopathological analyses of the ulcerated tissues as well as the extract's activity on Helicobacter pylori were also investigated. RESULTS: Phytochemical tests indicated the presence of mainly phytosterols, phenolics and flavonoids. The SIECm exhibited no cytotoxic effects on the CHO-k1 cells, and no oral acute toxicity in mice. It prevented against the acute induced ulcerations by enhancing gastroprotection through gastric mucus production, NO modulation, antioxidant, reduced gastric secretion and enhanced chronic ulcers healing process, as shown by reduction/prevention of epithelial and vascular damage, in addition to reduction in leucocyte infiltration. The SIECm however did not exhibit activity against H. pylori. CONCLUSION: The SIECm is safe, contain useful phytochemicals and exhibited significant gastroprotective/anti-ulcer effects. The results justify its folkloric usage, and provided scientific evidence of its potential as a source of new phytodrug to treat gastric ulcers.
民族药理学相关性：马尔梅 Copaifera malmei Harms（豆科）是一种生长在巴西中部地区的植物，该植物的叶浸剂在当地普遍用于治疗胃溃疡和炎症性疾病。本研究旨在调查该植物叶浸剂的胃保护活性及作用机制，以便为这种用法建立科学依据，并评估其作为抗溃疡药物来源的潜力。 材料与方法：制备该植物的叶浸剂提取物（SIECm），进行冷冻干燥和冻干处理。采用薄层色谱（TLC）和高效液相色谱（HPLC）技术对其定性和定量的植物化学成分进行研究。使用阿拉玛蓝测定法在CHO-k1上皮细胞活力上评估其安全性，并通过小鼠急性毒性试验进行评估。采用急性（酸化乙醇、吡罗昔康和水束缚应激）和慢性（乙酸）实验性溃疡模型测试SIECm（25、100和400mg/kg，口服）的胃保护和抗溃疡功效。通过检测小鼠和大鼠的胃分泌、胃屏障黏液、一氧化氮及其抗氧化（髓过氧化物酶和过氧化氢酶）作用，评估SIECm可能的作用方式。还研究了溃疡组织的组织病理学分析以及提取物对幽门螺杆菌的活性。 结果：植物化学测试表明主要存在植物甾醇、酚类和黄酮类化合物。SIECm对CHO-kl细胞无细胞毒性作用，对小鼠无经口急性毒性。它通过增加胃黏液分泌、调节一氧化氮、抗氧化、减少胃分泌以及促进慢性溃疡愈合过程来预防急性诱导的溃疡，表现为上皮和血管损伤的减轻/预防，以及白细胞浸润的减少。然而，SIECm对幽门螺杆菌没有活性。 结论：SIECm是安全的，含有有用的植物化学成分，并表现出显著的胃保护/抗溃疡作用。这些结果证明了其民间用法的合理性，并为其作为治疗胃溃疡的新植物药来源的潜力提供了科学证据。
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