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Extraction and identification of two flavonoids in Phlomoides hyoscyamoides as endemic plant of Iran: The role of quercetin in the activation of the glutathione peroxidase, the improvement of the hydroxyproline and protein oxidation in bile duct-ligated rats.
Current Computer-Aided Drug Design ( IF 1.5 ) Pub Date : 2020-09-30 , DOI: 10.2174/1573409915666190903163335
Amir H Doustimotlagh 1, 2 , Salman Taheri 3 , Mahboubeh Mansourian 1, 4 , Mahdieh Eftekhari 5
Affiliation  

Background: Cholestatic liver disease, a serious chronic condition that develops progressive hepatic degeneration through free radicals.

Objective: The present study was designed to extract and identify two flavonoids in Phlomoides hyoscyamoides plant, native to Iran and evaluate the role of quercetin identified on the liver injury among bile ductligated rats.

Methods: This study was conducted on 25 male Wistar rats within three groups of sham control, mere bile duct-ligated, and bile duct-ligated with quercetin. The bile duct-ligated animals received quercetin at a dose of 50 mg/kg/day for 10 days, followed by biochemical tests, oxidative stress markers, activity of antioxidant enzymes and hematoxylin and eosin staining. Molecular docking was used to explore the interactive behavior of quercetin with glutathione peroxidase.

Results: According to analyses of the obtained extract, two main active ingredients of P. hyoscyamoides were rutin and quercetin. Bile duct-ligated group showed a significant liver necrosis, a clear increase in plasma and tissue oxidative stress parameters, and a decrease in glutathione peroxidase activity as compared to sham control group. Quercetin injection in bile duct-ligated rats resulted in significant decrease in hydroxyproline, protein carbonyl and histopathologic indexes and significant increase in glutathione peroxidase activity (P-value≤0.05). Based on the molecular docking, the quercetin was able to regulate the glutathione peroxidase activity.

Conclusion: The quercetin acts as an enzyme inducer by renewing the glutathione peroxidase activity and inhibiting the oxidation of proteins and hence decreases the oxidative stress. These results could be a sign of confirming the positive role of quercetin in attenuating the liver damage and degeneration.



中文翻译:

伊朗特有植物木瓜中两种黄酮类化合物的提取鉴定:槲皮素在激活谷胱甘肽过氧化物酶、改善胆管结扎大鼠羟脯氨酸和蛋白质氧化中的作用。

背景:胆汁淤积性肝病,一种严重的慢性病,​​通过自由基发展为进行性肝变性。

目的:本研究旨在提取和鉴定原产于伊朗的 Phlomoides hyoscyamoides 植物中的两种黄酮类化合物,并评估槲皮素对胆管结扎大鼠肝损伤的作用。

方法:本研究对 25 只雄性 Wistar 大鼠进行,它们分为三组假对照、单纯胆管结扎组和用槲皮素结扎胆管组。胆管结扎动物以 50 毫克/公斤/天的剂量接受槲皮素治疗 10 天,然后进行生化测试、氧化应激标记、抗氧化酶活性以及苏木精和伊红染色。分子对接用于探索槲皮素与谷胱甘肽过氧化物酶的相互作用。

结果:对所得提取物进行分析,凤仙花的两种主要活性成分为芦丁和槲皮素。与假对照组相比,胆管结扎组显示出明显的肝坏死,血浆和组织氧化应激参数明显增加,谷胱甘肽过氧化物酶活性降低。胆管结扎大鼠注射槲皮素后羟脯氨酸、蛋白羰基和组织病理学指标显着降低,谷胱甘肽过氧化物酶活性显着升高(P值≤0.05)。基于分子对接,槲皮素能够调节谷胱甘肽过氧化物酶活性。

结论:槲皮素通过更新谷胱甘肽过氧化物酶活性和抑制蛋白质氧化而起到酶诱导剂的作用,从而降低氧化应激。这些结果可能是确认槲皮素在减轻肝损伤和变性方面的积极作用的标志。

更新日期:2020-11-09
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