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甜瓜变种苦瓜作为一种有效的抗糖尿病、抗氧化和可能的抗新冠替代物的研究:通过实验和计算方法的调查。

Cucumis melo var. momordica as a Potent Antidiabetic, Antioxidant and Possible Anticovid Alternative: Investigation through Experimental and Computational Methods.

机构信息

Department of Pharmacology, United Institute of Pharmacy, Industrial area, Naini, Prayagraj, 211010, India.

Department of Pharmacology, Kamla Nehru Institute of Management and Technology, Sultanpur, 228118, India.

出版信息

Chem Biodivers. 2022 Sep;19(9):e202200200. doi: 10.1002/cbdv.202200200. Epub 2022 Aug 25.

Abstract

Diabetes mellitus is a typical life threatening of disease, which generate due to the dysfunction of β cells of pancreas. In 2014, WHO stated that 422 million people were infected with DM. The current pattern of management of diabetes included synthetic or plant based oral hypoglycemic drugs and insulin but drug resentence is become a very big issues in antidiabetic therapy. Thus, it's very earnest to discover now medication for this disease. Now the days, it is well acknowledged that diabetic patients are more prone towards covid and related complications. Thus, medical practitioners reformed the methodology of prescribing medication for covid infected antidiabetic therapy and encouraging the medication contains dual pharmacological properties. It is also well know that polyphenols specifically hold a significant role in oxidative stress and reduced the severity of many inflammatory diseases. Cucumis melo has rich history as ethano-pharmacological use in Indian subcontinent. The fruit and seed are well-known for the treatment of various diseases due to the presence of phenolics. Therefore, in this study, the combined mixture of flower and seeds were used for the extraction of polyphenolic rich extract and tested for antidiabetic activity through the antioxidant and in vivo experiments. The antioxidant potential measurement exhibited that the selected plant extract has the significant competence to down-regulate oxidative stress (DPPH scavenging IC at 60.7±1.05 μg/mL, ABTS IC at 62.15±0.50 μg/mL). Furthermore, the major polyphenolic phyto-compounds derived from the Cucumis melo were used for in silico anticovid activity, docking, and complementarity studies. The anticovid activity prognosis reflected that selected phyto-compounds amentoflavone and vanillic acid have optimal possibility to interact with 3C-like protease and through this moderate anticovid activity can be exhibit. The docking experiments established that the selected compounds have propensity to interact with protein tyrosine phosphatase 1B, 11β-Hydroxysteroid dehydrogenase, superoxide dismutase, glutathione peroxidase, and catalase β-glucuronidase receptor. In vivo experiments showed that 500 mg/kg, Cucumis melo extract ominously amplified body weight, plasma insulin, high-density lipoprotein levels, and biochemical markers. Furthermore, extract significantly downregulate the blood glucose, total cholesterol, triglycerides, low-density lipoprotein, and very low-density lipoprotein.

摘要

糖尿病是一种典型的危及生命的疾病,它是由于胰腺β细胞功能障碍引起的。2014 年,世界卫生组织表示,全球有 4.22 亿人患有糖尿病。目前糖尿病的治疗模式包括合成或植物来源的口服降糖药和胰岛素,但药物耐药性已成为抗糖尿病治疗中的一个大问题。因此,发现治疗这种疾病的新药迫在眉睫。如今,人们已经认识到,糖尿病患者更容易感染新冠病毒并出现相关并发症。因此,医疗从业者改变了治疗新冠病毒感染的糖尿病患者的用药方法,鼓励使用具有双重药理作用的药物。众所周知,多酚类物质在氧化应激中具有显著作用,并能减轻许多炎症性疾病的严重程度。在印度次大陆,苦瓜作为乙醇药理学用途有着悠久的历史。由于含有酚类物质,苦瓜的果实和种子被广泛用于治疗各种疾病。因此,在这项研究中,我们使用花和种子的混合物来提取富含多酚的提取物,并通过抗氧化和体内实验来测试其抗糖尿病活性。抗氧化潜力测量结果表明,所选植物提取物具有显著的下调氧化应激能力(DPPH 清除 IC 值为 60.7±1.05μg/mL,ABTS IC 值为 62.15±0.50μg/mL)。此外,苦瓜中提取的主要多酚类植物化合物被用于计算机模拟抗新冠病毒活性、对接和互补性研究。抗新冠病毒活性预测结果表明,所选植物化合物芹菜素和香草酸与 3C 样蛋白酶相互作用的可能性最大,通过这种方式可以表现出适度的抗新冠病毒活性。对接实验表明,所选化合物有与蛋白酪氨酸磷酸酶 1B、11β-羟类固醇脱氢酶、超氧化物歧化酶、谷胱甘肽过氧化物酶和β-葡萄糖醛酸酶受体相互作用的倾向。体内实验表明,500mg/kg 的苦瓜提取物显著增加了体重、血浆胰岛素、高密度脂蛋白水平和生化标志物。此外,提取物还显著降低了血糖、总胆固醇、甘油三酯、低密度脂蛋白和极低密度脂蛋白。

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