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西番莲作为抗溃疡饮食的益处:通过体外和计算机 H+/K+ATP 酶抑制活性评估的科学证据。

The Benefit of Passion Fruit as an Anti-ulcerogenic Diet: Scientific Evidence by In vitro and In silico H+/K+ATPase Inhibitory Activity Assessment.

机构信息

Department of Pharmacology, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Science Campus, Kochi, India

出版信息

Curr Comput Aided Drug Des. 2020;16(5):555-563. doi: 10.2174/1573409915666191025121005.

Abstract

BACKGROUND

H+/K+ ATPase a protein present in the gastric parietal cells is a better target for the prevention and treatment of gastric ulcer. Plant flavonoids have been reported to elicit anti-ulcer activity by inhibiting the proton pump as well as by antioxidant defense mechanism.

METHODS

Chloroform fraction of hydro-alcoholic extract of passion fruit was screened for proton pump inhibitory assay using goat parietal cell. In-silico computational docking studies were carried out using Glide program in order to validate the inhibitory action of selected constituents.

RESULTS

The flavonoid rich fruit possess a promising radical scavenging activity against DPPH. 10.41μg/mL is sufficient to inhibit 50% of ATPase enzyme activity. A synergistic activity was also achieved by the fruit with sub-effective doses of lansoprazole. Fenton's oxidation induced by H2O2 was also blunted by the fruit extract.

CONCLUSION

The in-vitro and in-silico findings indicated that, passion fruit can be a good dietary supplement for the prevention and management of ulcer.

摘要

背景

胃壁细胞中存在的 H+/K+ATPase 蛋白是预防和治疗胃溃疡的更好靶点。植物类黄酮已被报道通过抑制质子泵以及抗氧化防御机制发挥抗溃疡活性。

方法

使用山羊壁细胞对西番莲的水醇提取物的氯仿级分进行质子泵抑制测定。使用 Glide 程序进行基于计算机的计算对接研究,以验证所选成分的抑制作用。

结果

富含类黄酮的水果具有针对 DPPH 的有前途的自由基清除活性。足以抑制 50%的 ATP 酶活性的浓度为 10.41μg/mL。水果与亚有效剂量的兰索拉唑联合使用也可实现协同作用。水果提取物还可减弱由 H2O2 诱导的 Fenton 氧化。

结论

体外和计算机研究结果表明,西番莲可以作为预防和治疗溃疡的良好膳食补充剂。

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