Alfeqy Marwah M, El-Hawary Seham S, El-Halawany Ali M, Rabeh Mohamed A, Alshehri Saad A, Serry Aya M, Fahmy Heba A, Ezzat Marwa I
Pharmacognosy Department, Faculty of Pharmacy, Modern University for Technology & Information, Cairo 11571, Egypt.
Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr El Aini, Cairo 11562, Egypt.
Pharmaceutics. 2023 Oct 27;15(11):2541. doi: 10.3390/pharmaceutics15112541.
Metabolic syndrome (MetS) is a global issue affecting over a billion people, raising the risk of diabetes, cardiovascular disorders, and other ailments. It is often characterized by hypertension, dyslipidemia and/or obesity, and hyperglycemia. Chemical investigation of (L.) Webb & Berthel led to the isolation of six compounds, viz. β-sitosterol, β-sitosterol glucoside, myricetin galactoside, quercetin rhamnoside, kaempferol rhamnoside, and myricetin glucoside. Interestingly, 's dichloromethane (DCM), 100 and 50% MeOH Diaion fractions and the isolated compound (quercetin-3-rhamnoside) revealed potent α-glucosidase inhibitory activity, especially 50% Diaion fraction. In addition, they also showed very potent antioxidant potential, especially the polar fractions, using DPPH, ABTS, FRAP, ORAC, and metal chelation assays. Notably, the 50% Diaion fraction had the highest antioxidant potential using DPPH and ORAC assays, while the 100% Diaion fraction and quercetin-3-rhamnoside showed the highest activity using ABTS, FRAP, and metal chelation assays. Also, quercetin-3-rhamnoside showed a good docking score of -5.82 kcal/mol in comparison to acarbose. In addition, molecular dynamic stimulation studies illustrated high stability of compound binding to pocket of protein. Such potent activities present as a complementary safe approach for the management of diabetes mellitus as well as MetS.
代谢综合征(MetS)是一个全球性问题,影响着超过10亿人,增加了患糖尿病、心血管疾病和其他疾病的风险。它通常表现为高血压、血脂异常和/或肥胖以及高血糖。对(L.)Webb & Berthel进行化学研究后,分离出了六种化合物,即β-谷甾醇、β-谷甾醇葡萄糖苷、杨梅素半乳糖苷、槲皮素鼠李糖苷、山奈酚鼠李糖苷和杨梅素葡萄糖苷。有趣的是,其二氯甲烷(DCM)、100%和50%甲醇的Diaion馏分以及分离出的化合物(槲皮素-3-鼠李糖苷)显示出强大的α-葡萄糖苷酶抑制活性,尤其是50%的Diaion馏分。此外,使用DPPH、ABTS、FRAP、ORAC和金属螯合试验,它们还表现出非常强的抗氧化潜力,尤其是极性馏分。值得注意的是,使用DPPH和ORAC试验时,50%的Diaion馏分具有最高的抗氧化潜力,而使用ABTS、FRAP和金属螯合试验时,100%的Diaion馏分和槲皮素-3-鼠李糖苷表现出最高的活性。此外,与阿卡波糖相比,槲皮素-3-鼠李糖苷的对接分数为-5.82 kcal/mol,表现良好。此外,分子动力学模拟研究表明化合物与蛋白质口袋结合具有高稳定性。这些强大的活性表明其可作为治疗糖尿病以及代谢综合征的一种补充性安全方法。