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Effect of phenolic compounds from the rind of Punica granatum on the activity of three metabolism-related enzymes.
Biotechnology and Applied Biochemistry ( IF 3.2 ) Pub Date : 2019-11-25 , DOI: 10.1002/bab.1866 Mohamed H Ahmed 1 , Hala M Aldesouki 1 , Farid A Badria 2
Biotechnology and Applied Biochemistry ( IF 3.2 ) Pub Date : 2019-11-25 , DOI: 10.1002/bab.1866 Mohamed H Ahmed 1 , Hala M Aldesouki 1 , Farid A Badria 2
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Enzyme activity modulation by synthetic compounds provide strategies combining the inhibitory and therapeutic mode of action of the confirmed inhibitors. However, natural modulators could offer a valuable alternative for synthetic ones for the treatment of different chronic diseases (diabetes, hypertension, cancer) due to the numerous side effects of the latter. In vitro screening assays were conducted for Punica granatum rind methanolic extract against three metabolism‐related enzymes: α‐amylase, tyrosinase, and hyaluronidase. The obtained results showed that the examined extract retained high multitarget inhibition with inhibition percentages 31.5 ± 1.3%, 75.9 ± 4.7%, and 68.5 ± 5.3% against α‐amylase, tyrosinase, and hyaluronidase, respectively. Bioguided fractionation of P. granatum rind extract revealed that quercetin is the major active compound with inhibitory activities: 54.3 ± 2.7%, 94.2 ± 3.5%, and 90.9 ± 2.7% against α‐amylase, tyrosinase, and hyaluronidase, respectively. Kinetic studies of enzymes showed that quercetin inhibition was noncompetitive, uncompetitive, and competitive for α‐amylase, tyrosinase, and hyaluronidase, respectively. The molecular docking of quercetin with α‐amylase and hyaluronidase showed high binding energy with different bonds stabilizing the ligand–protein complex. Compiling all obtained results led to conclude that both P. granatum rind extract and quercetin have multitarget activities with potential therapeutic applications in many metabolic disorders.
中文翻译：
石榴皮中酚类化合物对三种代谢相关酶活性的影响。
合成化合物对酶活性的调节提供了结合已证实的抑制剂的抑制作用和治疗作用方式的策略。然而，由于天然调节剂的许多副作用，它可以为合成的调节剂提供有价值的替代品，以治疗不同的慢性疾病（糖尿病，高血压，癌症）。针对石榴皮中的甲醇提取物进行了针对三种代谢相关酶的体外筛选测定：α-淀粉酶，酪氨酸酶和透明质酸酶。获得的结果表明，所检测的提取物保留了较高的多靶点抑制率，分别对α-淀粉酶，酪氨酸酶和透明质酸酶的抑制率分别为31.5±1.3％，75.9±4.7％和68.5±5.3％。生物引导分离石榴皮提取物显示槲皮素是具有抑制活性的主要活性化合物：对α-淀粉酶，酪氨酸酶和透明质酸酶的抑制活性分别为54.3±2.7％，94.2±3.5％和90.9±2.7％。酶的动力学研究表明，槲皮素抑制作用分别对α-淀粉酶，酪氨酸酶和透明质酸酶无竞争性，无竞争性和竞争性。槲皮素与α-淀粉酶和透明质酸酶的分子对接显示出高结合能，且具有不同的键，可稳定配体-蛋白质复合物。汇总所有获得的结果可得出结论，认为体育颗粒提取物和槲皮素均具有多靶标活性，在许多代谢性疾病中均具有潜在的治疗应用价值。
更新日期：2019-11-25
中文翻译：
石榴皮中酚类化合物对三种代谢相关酶活性的影响。
合成化合物对酶活性的调节提供了结合已证实的抑制剂的抑制作用和治疗作用方式的策略。然而，由于天然调节剂的许多副作用，它可以为合成的调节剂提供有价值的替代品，以治疗不同的慢性疾病（糖尿病，高血压，癌症）。针对石榴皮中的甲醇提取物进行了针对三种代谢相关酶的体外筛选测定：α-淀粉酶，酪氨酸酶和透明质酸酶。获得的结果表明，所检测的提取物保留了较高的多靶点抑制率，分别对α-淀粉酶，酪氨酸酶和透明质酸酶的抑制率分别为31.5±1.3％，75.9±4.7％和68.5±5.3％。生物引导分离石榴皮提取物显示槲皮素是具有抑制活性的主要活性化合物：对α-淀粉酶，酪氨酸酶和透明质酸酶的抑制活性分别为54.3±2.7％，94.2±3.5％和90.9±2.7％。酶的动力学研究表明，槲皮素抑制作用分别对α-淀粉酶，酪氨酸酶和透明质酸酶无竞争性，无竞争性和竞争性。槲皮素与α-淀粉酶和透明质酸酶的分子对接显示出高结合能，且具有不同的键，可稳定配体-蛋白质复合物。汇总所有获得的结果可得出结论，认为体育颗粒提取物和槲皮素均具有多靶标活性，在许多代谢性疾病中均具有潜在的治疗应用价值。
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