Antidiabetic Potential of Ruthenium(III) hydroxamate Complexes:Spectrophotometric Investigations.

Q4 Pharmacology, Toxicology and Pharmaceutics Current Enzyme Inhibition Pub Date : 2022-08-25 DOI:10.2174/1573408018666220825152849
R. Kaushal, Mandeep Kaur
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Abstract

The potential antidiabetic and antioxidant properties of four ruthenium(III) hydroxamate complexes [RuCl(H2O)(LI-III)2] (1-3) and [RuCl3(H2O)(HLIV)2] (4) were investigated on α-cell enzymes (α-amylase and α-glucosidase). In the instance of -amylase inhibition investigations, the antidiabetic studies of the complexes revealed that they are more active than even the Acarbose as standard, with complex 4 having an IC50 value of 52.31 g/ml. For α-glucosidase inhibition, complex 4 was observed to be the best inhibitor with a remarkable 0.35g/ml IC50 value, which may be attributed to the size and superior lipophilicity of this complex, enabling it to interact with the biological system more effectively than complexes 1-3.The complexes with the best IC50 values were studied further for enzyme kinetics. Molecular docking studies were performed as well to investigate the interactions between the synthesized complexes and target enzymes viz., α glucosidase and α-amylase. The obtained in-vitro results have also been supported by the results of the in-silico docking studies. Furthermore, the antiradical activity of Ru(III) complexes was assessed for its effectiveness in reducing oxidative stress. All the complexes (except complex 3) exhibited remarkable antiradical activity.
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钌(III)羟酸酯配合物的抗糖尿病潜能:分光光度法研究。
研究了四种氢草酸钌(III)配合物[RuCl(H2O)(LI-III)2](1-3)和[RuCl3(H2O),其中复合物4的IC50值为52.31g/ml。对于α-葡萄糖苷酶的抑制,观察到复合物4是最好的抑制剂,具有显著的0.35g/ml IC50值,这可能归因于该复合物的大小和优越的亲脂性,使其能够比复合物1-3更有效地与生物系统相互作用。对具有最佳IC50值的复合物的酶动力学进行了进一步研究。还进行了分子对接研究,以研究合成的复合物与目标酶(即α-葡萄糖苷酶和α-淀粉酶)之间的相互作用。所获得的体外结果也得到了计算机对接研究结果的支持。此外,评估了Ru(III)配合物在减少氧化应激方面的抗自由基活性。除配合物3外,所有配合物均表现出显著的抗自由基活性。
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来源期刊
Current Enzyme Inhibition
Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
1.30
自引率
0.00%
发文量
30
期刊介绍: Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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