Sansenya Sompong, Winyakul Chankan, Nanok Kesinee, Phutdhawong Waya S
Department of Chemistry, Faculty of Science and Technology, Rajamangala University of Technology Thanyaburi, Pathum Thani, 12110, Thailand.
Deparment of Chemistry, Faculty of Science and Technology, Phetchabun Rajabhat University, Phetchabun, 67000, Thailand.
Res Pharm Sci. 2020 Feb 20;15(1):14-25. doi: 10.4103/1735-5362.278711. eCollection 2020 Feb.
Carbohydrate hydrolysis enzymes including α-glucosidase and α-amylase are related to type 2 diabetes mellitus. The inhibiting of these enzymes might use for type 2 diabetes mellitus treatment.
-substituted-acetylpyrrolidine linked with -benzyl- (-(benzyl)-2-acetylpyrrolidine ()) and -tosyl- (-(tosyl)-2-acetylpyrrolidine ()) were synthesized and evaluated for their pharmaceutical properties against α-glucosidase and α-amylase and free radical scavenging activity. The structures of and were determined through spectral studies (H-NMR).
FINDINGS / RESULTS: Both compounds and had highest inhibitory potential on α-glucosidase with the IC50 values of 0.52 ± 0.02 and 1.64 ± 0.08 mM, respectively. The kinetic investigation of and against α-glucosidase and α-amylase were functioned in mixed type inhibition. Moreover, both compounds are more likely to bind with the free enzyme than the enzyme-substrate complex based on the i < i on the α-glucosidase and α-amylase enzymes. Regarding the free radical scavenging, had a higher capacity than with IC50 values of 1.01 ± 0.010 mM for and 1.82 ± 0.048 mM for .
Our results indicated that a derivative of -substitute-acetylpyrrolidine had high potential to inhibit α-glucosidase and α-amylase, and their free radical scavenging properties might be applied to the therapeutic care of patients with type 2 diabetes mellitus.
包括α-葡萄糖苷酶和α-淀粉酶在内的碳水化合物水解酶与2型糖尿病有关。抑制这些酶可能用于2型糖尿病的治疗。
合成了与苄基相连的-N-取代-乙酰基吡咯烷（-（苄基）-2-乙酰基吡咯烷（））和与对甲苯磺酰基相连的-N-取代-乙酰基吡咯烷（-（对甲苯磺酰基）-2-乙酰基吡咯烷（）），并评估了它们对α-葡萄糖苷酶和α-淀粉酶的药学性质以及自由基清除活性。通过光谱研究（氢核磁共振）确定了和的结构。
两种化合物和对α-葡萄糖苷酶均具有最高的抑制潜力，IC50值分别为0.52±0.02和1.64±0.08 mM。和对α-葡萄糖苷酶和α-淀粉酶的动力学研究表现为混合型抑制。此外，基于α-葡萄糖苷酶和α-淀粉酶上的i < i，两种化合物与游离酶结合的可能性大于与酶-底物复合物结合的可能性。关于自由基清除，的清除能力高于，的IC50值为1.01±0.010 mM，的IC50值为1.82±0.048 mM。
我们的结果表明，-N-取代-乙酰基吡咯烷衍生物具有抑制α-葡萄糖苷酶和α-淀粉酶的高潜力，其自由基清除特性可能应用于2型糖尿病患者的治疗护理。
