Mugaranja Kirana P, Kulal Ananda
Biological Sciences Division, Poornaprajna Institute of Scientific Research, Bidalur Post, Devanahalli, Bangalore Rural, 562110, India.
Manipal Academy of Higher Education, Manipal, 576104, India.
Heliyon. 2020 Jul 8;6(7):e04392. doi: 10.1016/j.heliyon.2020.e04392. eCollection 2020 Jul.
A phenolic rich fraction purified from leaves was effective in alpha glucosidase inhibition. The purified fraction named 'fraction-14' had shown significant inhibition of yeast alpha glucosidase enzyme activity (IC = 2.4 ± 0.4 μg/mL) when compared to anti-diabetic drug acarbose (IC = 2450 ± 24 μg/mL). The purified fraction also had reasonable DPPH (IC = 14.4 ± 0.1 μg/mL) and ABTS (IC = 7.6 ± 0.5 μg/mL) free radical scavenging activity when compared to the standard ascorbic acid. The LC-MS analysis of bioactive 'fraction-14' revealed four compounds, eclalbasaponin-v (), cyanidin-3-O-(2'galloyl)-galactoside (), kaempferol-3-O-glucoside () and kaempferol-3-O-pentoside () for the first time in in this study. The kinetic study of the 'fraction-14' indicates a mixed type of inhibition on the alpha glucosidase enzyme with , 6.2 μg/mL. Docking studies showed promising binding energy for the compounds (-7.769 kJ/mol), (-7.04 kJ/mol) and (-7.127 kJ/mol) against yeast alpha glucosidase which was better than acarbose (-6.867 kJ/mol). In conclusion, the phenolic rich fraction from possessing good antioxidant property and alpha glucosidase enzyme inhibition potential along with mixed inhibition kinetics. Also, better binding energy of compounds () appears to contain potential lead-molecule for antidiabetic therapy.
从树叶中纯化得到的富含酚类的组分对α-葡萄糖苷酶具有抑制作用。与抗糖尿病药物阿卡波糖(IC = 2450±24μg/mL)相比,名为“组分14”的纯化组分对酵母α-葡萄糖苷酶活性表现出显著抑制作用(IC = 2.4±0.4μg/mL)。与标准抗坏血酸相比,该纯化组分还具有合理的DPPH(IC = 14.4±0.1μg/mL)和ABTS(IC = 7.6±0.5μg/mL)自由基清除活性。本研究首次通过LC-MS分析生物活性“组分14”,鉴定出四种化合物,分别为刺蒺藜皂甙V()、矢车菊素-3-O-(2'-没食子酰基)-半乳糖苷()、山奈酚-3-O-葡萄糖苷()和山奈酚-3-O-戊糖苷()。“组分14”的动力学研究表明其对α-葡萄糖苷酶的抑制作用为混合型,Ki为6.2μg/mL。对接研究表明,化合物(-7.769 kJ/mol)、(-7.04 kJ/mol)和(-7.127 kJ/mol)与酵母α-葡萄糖苷酶的结合能前景良好,优于阿卡波糖(-6.867 kJ/mol)。总之,来自[植物名称未给出]的富含酚类的组分具有良好的抗氧化性能和α-葡萄糖苷酶抑制潜力,以及混合型抑制动力学。此外,化合物()的更好结合能似乎包含抗糖尿病治疗的潜在先导分子。