Ben Bacha Abir, Jemel Ikram, Bhat Ramesa Shafi, Onizi Mona Awad
Biochemistry Department, Science College, King Saud University, P.O Box 22452, Riyadh 11495, Saudi Arabia.
Laboratory of Plant Biotechnology Applied to Crop Improvement, Faculty of Science of Sfax, University of Sfax, Sfax 3038, Tunisia.
Cell Mol Biol (Noisy-le-grand). 2018 Oct 30;64(13):55-62.
Many enzymes are involved in numerous pathologies which are related to metabolic reactions and inflammatory diseases such as pancreatic lipase, α-amylase, α-glucosidase and xanthine oxidase and secreted phospholipases A2 (Group IIA, V and X), respectively. Therefore, inhibiting these enzymes offer the potential to block production of more inflammatory substances and decrease the risk factors for cardiovascular diseases. The purpose of this study was to investigate some potent, bioavailable and selective inhibitors of some catalytic proteins implicated to metabolic syndrome and their antioxidant effects from various solvent extracts of R. frangula leaves. The anti-inflammatory, obesity, diabete and XO potentials were evaluated through analyses of inhibition activities of corresponding metabolites.The water extract exhibited an important inhibitory effect on human, dromedary and stingray sPLA2-G IIA achieved an IC50 of 0.16±0.06, 0.19±0.05 and 0.07±0.01 mg/mL, respectively. Likewise, the same fraction demonstrated the highest pancreatic lipase inhibitory activity using two different substrates. Indeed, 50% of dromedary pancreatic lipase inhibition was demonstrated for 5 min and 15 min using olive oil and TC4 substrates, respectively. Besides, it was established that methanolic extract had more effective inhibitory lipase activity than ORLISTAT used as a specific inhibitor of gastric, pancreatic and carboxyl ester lipase for treating obesity, with an IC50 of 5.51±0.27 and 91.46±2.3 µg/mL, respectively. In the case of α-amylase, α-glucosidase and xanthine oxidase, the crude methanolic extract showed a potential inhibitory effect with an IC50 of 45±3.45, 3±0.15 and 27±1.71 µg/mL, respectively. Conclusively, R. frangula leaves extracts showed a potential value of some sPLA2, some metabolic enzymes and XO inhibitors as anti-inflammatory and metabolic syndrome drugs.
许多酶参与了众多与代谢反应和炎症性疾病相关的病理过程，例如胰脂肪酶、α-淀粉酶、α-葡萄糖苷酶和黄嘌呤氧化酶，以及分别为分泌型磷脂酶A2（IIA、V和X组）。因此，抑制这些酶有可能阻止更多炎症物质的产生，并降低心血管疾病的风险因素。本研究的目的是从欧鼠李叶的各种溶剂提取物中研究一些对与代谢综合征相关的某些催化蛋白具有强效、生物可利用性和选择性的抑制剂及其抗氧化作用。通过分析相应代谢物的抑制活性来评估抗炎、抗肥胖、抗糖尿病和抗黄嘌呤氧化酶的潜力。水提取物对人、单峰骆驼和黄貂鱼的分泌型磷脂酶A2 - G IIA表现出重要的抑制作用，IC50分别为0.16±0.06、0.19±0.05和0.07±0.01 mg/mL。同样，同一提取物使用两种不同底物时表现出最高的胰脂肪酶抑制活性。事实上，使用橄榄油和TC4底物时，分别在5分钟和15分钟内实现了对单峰骆驼胰脂肪酶50%的抑制。此外，已确定甲醇提取物的脂肪酶抑制活性比用作治疗肥胖症的胃、胰和羧基酯脂肪酶特异性抑制剂的奥利司他更有效，IC50分别为5.51±0.27和91.46±2.3 µg/mL。对于α-淀粉酶、α-葡萄糖苷酶和黄嘌呤氧化酶，粗甲醇提取物表现出潜在的抑制作用，IC50分别为至45±3.45、3±0.15和27±1.71 µg/mL。总之，欧鼠李叶提取物显示出作为抗炎和代谢综合征药物的一些分泌型磷脂酶A2、一些代谢酶和黄嘌呤氧化酶抑制剂具有潜在价值。
