Diosgenin from Dioscorea bulbifera: Novel Hit for Treatment of Type II Diabetes Mellitus with Inhibitory Activity against α-Amylase and α-Glucosidase

Abstract

Diabetes mellitus is a multifactorial metabolic disease characterized by post-prandial hyperglycemia (PPHG). α-amylase and α-glucosidase inhibitors aim to explore novel therapeutic agents. Herein we report the promises of Dioscorea bulbifera and its bioactive principle, diosgenin as novel α-amylase and α-glucosidase inhibitor. Among petroleum ether, ethyl acetate, methanol and 70% ethanol (v/v) extracts of bulbs of D. bulbifera, ethyl acetate extract showed highest inhibition upto 72.06 ± 0.51% and 82.64 ± 2.32% against α-amylase and α-glucosidase respectively. GC-TOF-MS analysis of ethyl acetate extract indicated presence of high diosgenin content. Diosgenin was isolated and identified by FTIR, 1H NMR and 13C NMR and confirmed by HPLC which showed an α-amylase and α-glucosidase inhibition upto 70.94 ± 1.24% and 81.71 ± 3.39%, respectively. Kinetic studies confirmed the uncompetitive mode of binding of diosgenin to α-amylase indicated by lowering of both Km and Vm. Interaction studies revealed the quenching of intrinsic fluorescence of α-amylase in presence of diosgenin. Similarly, circular dichroism spectrometry showed diminished negative humped peaks at 208 nm and 222 nm. Molecular docking indicated hydrogen bonding between carboxyl group of Asp300, while hydrophobic interactions between Tyr62, Trp58, Trp59, Val163, His305 and Gln63 residues of α-amylase. Diosgenin interacted with two catalytic residues (Asp352 and Glu411) from α-glucosidase. This is the first report of its kind that provides an intense scientific rationale for use of diosgenin as novel drug candidate for type II diabetes mellitus.

Novel platinum–palladium bimetallic nanoparticles synthesized by Dioscorea bulbifera: anticancer and antioxidant activities

“…[24][25][26][27] Similarly, it has been extensively used for synthesis of metal nanoparticles like gold, silver, and gold core silver shell (Au core Ag shell NPs) bimetallic nanoparticles. [28][29][30] Hereby, as a part of our growing interest in nanobiotechnology, herein we report for the first time, the synthesis of Pt-PdNPs by a medicinal plant, D. bulbifera.…”

Biochemical Evaluation of the Effects of Hydromethanolic Extracts of Dioscorea bulbifera in Wistar Rats

“…It is also possible that the extract stimulated insulin secretion from the β-cells of the islets of Langerhans [23,24]. Dioscorea bulbifera has also be shown to have a potent hypoglycaemicactivity [21,[24][25][26].…”

PENETAPAN KADAR DIOSGENIN DALAM EKSTRAK AIR Costus speciosus SECARA HPLC

“…Struktur kimia diosgenin Diosgenin (Gambar 2) adalah konstituen bioaktif yang sangat penting dalam herba pacing. Diosgenin berperan penting dalam aktivitas farmakologi seperti antihiperlipidemi (Son et al, 2007), antidiabetes (Ghosh et al., 2014), anti kanker (Selim and Al Jouni, 2015). Oleh karena itu, ada kebutuhan mendesak untuk mengembangkan metode sederhana untuk estimasi senyawa ini menggunakan instrumen canggih seperti kromatografi cair kinerja tinggi (HPLC).…”