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首页> 外文期刊>International Journal of Phytopharmacy >IN VITRO SOLUBLE EPOXIDE HYDROLASE ENZYME INHIBITORY ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES
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IN VITRO SOLUBLE EPOXIDE HYDROLASE ENZYME INHIBITORY ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES

机译：某些新型查尔酮衍生物的体外可溶性环氧酶水解酶抑制活性

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Objective Soluble epoxide hydrolase ( sEH) belongs to the α/β -hydrolase superfamily, a subclass of α/β proteins. Chalcones are chemical compounds that show hopeful obliging efficacy in controlling numerous diseases. The main objective of the study is to evaluate the sEH inhibitory activity of some synthesized chalcone derivatives and identification of its mode of inhibition. Methods Four different chalcone derivatives (PC-1 to PC-4) were selected for synthesis by Claisen-Schmidt method. The in vitro sEH inhibitory activity was performed for the synthesized compounds by fluorimetric assay. The percentage of sEH activity and IC 50 values were calculated for the synthesized compounds. Dissociation constant were determined by following the method described by Lineweaver-Burks plot. Results and Conclusions The IC 50 value obtained for PC-1, PC-2, PC-3, and PC-4 were found to be 0.8213 μg/mL, 2.64 μg/mL, 0.2490 μg/mL and 0.5238 μg/mL respectively. The order of potency (IC 50 ) of the chalcone and chalcone oxide in sEH inhibition assay was PC-3 > PC-4 > PC-1 >PC-2. All the compounds (PC-1, PC-2, PC-3) showed mixed type of inhibition except PC-4 which showed non-competitive type of inhibition. Further in vivo studies are to be carried out for these compounds to confirm their activity and explore the mechanism by which these compounds act and rationalize their use.
机译：目的可溶性环氧化物水解酶（sEH）属于α/β水解酶超家族，是α/β蛋白的一个亚类。查尔酮是在控制多种疾病方面显示出希望的强制功效的化合物。该研究的主要目的是评估某些合成查尔酮衍生物的sEH抑制活性并确定其抑制方式。方法采用克莱森-施密特方法选择四种不同的查耳酮衍生物（PC-1至PC-4）进行合成。通过荧光测定法对合成的化合物进行了体外sEH抑制活性。计算合成化合物的sEH活性百分比和IC 50值。通过遵循Lineweaver-Burks图描述的方法确定解离常数。结果与结论PC-1，PC-2，PC-3和PC-4的IC 50值分别为0.8213μg/ mL，2.64μg/ mL，0.2490μg/ mL和0.5238μg/ mL。 sEH抑制试验中查耳酮和氧化查尔酮的效价顺序（IC 50）为PC-3> PC-4> PC-1> PC-2。除PC-4表现出非竞争性抑制作用外，所有化合物（PC-1，PC-2，PC-3）均表现出混合抑制作用。将对这些化合物进行进一步的体内研究，以确认其活性并探索这些化合物起作用并合理化其使用的机理。

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