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首页> 外文期刊>RSC Advances >Antiulcer secondary metabolites fromElaeocarpus grandis, family Elaeocarpaceae, supported byin silicostudies
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Antiulcer secondary metabolites fromElaeocarpus grandis, family Elaeocarpaceae, supported byin silicostudies

机译：Bulercarpus grandis，Familara的副代谢物，伊斯兰氏菌属（Silicostudies）支持

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摘要

Elaeocarpus grandishas a very potent analgesic effect, especially to a delta-opioid receptor, but its antiulcer activity has not yet been validated. Therefore, the present study was carried out to evaluate the antiulcer potential of the total methanolic extract and its derived fractions of the aerial parts of the plant using an indomethacin-induced gastric ulcer method. One new compound, grandisine H (1), and five known compounds,P-methoxy benzaldehyde, methyl gallate, kaempferol, quercetin and heterophyllin A (2-6), were isolated from the ethyl acetate fraction, which was the most potent one with an ulcer index value of 5 +/- 1.95 (mm) ** (*P< 0.05, **P< 0.01) and a preventive index of 92.9%, following a bioassay-guided fractionation. The isolated compounds were subjected to a molecular docking study in an attempt to explain their significant antiulcer potential, and the results revealed that kaempferol and quercetin bind to the active site of the M3 receptor with a strong binding affinityviastrong hydrogen bonds of -6.081 kcal mol(-1)and -6.013 kcal mol(-1), respectively. Also, quercetin and heterophyllin A showed a binding affinity with the gastric proton pump receptor and a strong hydrogen bond interaction with the amino acid active sites in the case of an H-2-modeled receptor. These results clarify the effectiveness and importance of the ethyl acetate fraction as a natural anti-ulcer remedy.
机译：Elaeocarpus Grandishas是一个非常有效的镇痛作用，尤其是δ-阿片受体，但其抗菌活动尚未得到验证。因此，使用吲哚美辛诱导的胃溃疡方法进行本研究以评估植物的总甲醇提取物及其衍生级分的抗燃烧剂。从乙酸乙酯级分中分离出一种新的化合物，祖母H（1）和五种已知的化合物，对甲氧基苯甲醛，甲酸甲酯，kaempferol，槲皮素和异丙肾（2-6），这是最有效的溃疡指数值5 +/- 1.95（mm）**（* p <0.05，** p <0.01），并在生物测定引导的分馏之后的预防指数为92.9％。进行分离的化合物进行分子对接研究，以试图解释其显着的抗燃烧潜力，结果表明，Kaempferol和槲皮素与M3受体的活性位点与-6.081 kcal摩尔的强粘结亲和透视氢键合结合-1）和-6.013 kcal摩尔（-1）分别。此外，槲皮素和Heterophyllin A与胃质子泵受体的结合亲和力和与氨基酸活性位点的强氢键相互作用在H-2模拟的受体的情况下。这些结果阐明了乙酸乙酯馏分作为天然抗溃疡补救措施的有效性和重要性。

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