α-Glucosidase-IN-16

α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin-induced diabetic rats. Antidiabetic activity[1].

Research Areas >> Metabolic Disease

IC50: 3.28 μM (α-Glucosidase)[1]

α-Glucosidase-IN-16 (compound 13B) (10 and 20 mg/kg; PO; once daily for 28 days) significantly reduces the level of blood glucose in diabetic rats[1]. α-Glucosidase-IN-16 (2000 mg/kg; PO; single dosage) exhibits no toxic effects in mice[1]. α-Glucosidase-IN-16 (10 and 20 mg/kg; PO; single dosage) significantly reduces serum glucose level after glucose administration in rats[1]. Animal Model: Wistar rats (170-200 g, 8-10 weeks; induced diabetes by intraperitoneal injection of Streptozotocin (HY-13753))[1] Dosage: 10 and 20 mg/kg Administration: PO; once daily for 28 days Result: Caused a significant reduction in the level of blood glucose compared to diabetic control. Lowered the total cholesterol level. Effect of α-Glucosidase-IN-16 on blood glucose (mg/dL) in Streptozotocin-induced diabetes[1]. dose (mg/kg) day 1 day 7 day 14 day 21 day 28 10 370.81 ± 4.79 289.89 ± 4.33 200.33 ± 4.57 149.30 ± 4.56 132.98 ± 4.33 20 375.31 ± 5.01 230.71 ± 4.88 163.68 ± 4.37 120.72 ± 4.11 108.42 ± 3.98 Animal Model: Balb/C mice[1] Dosage: 2000 mg/kg Administration: PO; single dosage (acute toxicity study) Result: Exhibited no toxic effects (via observing signs of diarrhea, convulsions, lethargy, sleeping, salivation, and tremor). Animal Model: Wistar rats (oral administration with 3 g/kg glucose)[1] Dosage: 10 and 20 mg/kg Administration: PO; single dosage (oral glucose tolerance test) Result: Significantly reduced serum glucose level (110-113 mg/dL) compared to the control group (128 mg/dL) after 2 hours of glucose administration.

[1]. Rabia Mehmood, et al. Synthesis of Novel 2,3-Dihydro-1,5-Benzothiazepines as α-Glucosidase Inhibitors: In Vitro, In Vivo, Kinetic, SAR, Molecular Docking, and QSAR Studies. ACS Omega 2022 Aug.