A Convenient Synthesis of Short α-/β-Mixed Peptides as Potential α-Amylase Inhibitors
Naeem Ahmed, Fakhira Razzaq, Muhammad Arfan, Mansour K. Gatasheh, Hammad Nasir, Joham Sarfraz Ali, Hamna Hafeez
TL;DR
This paper describes a new method to synthesize short peptides that may help control blood sugar by inhibiting the α-amylase enzyme.
Contribution
A novel synthesis method for α-/β-mixed peptides with potential α-amylase inhibition is introduced.
Findings
Three novel α-/β-mixed peptides were successfully synthesized and characterized.
Peptide 16 showed the highest α-amylase inhibition at 45.22%.
The synthesis method avoids racemization and retains configuration.
Abstract
Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. Inhibition of the α-amylase enzyme is one therapeutic approach in lowering glucose levels in the blood to manage diabetes mellitus. The objective of this study was to synthesize short α-/β-mixed peptides in the solution phase. The Boc-protected α-L-leucine was converted to β-analogue by using Arndt–Eistert synthesis with the advantage of no racemization and retention of configuration. Three novel short peptides were successfully synthesized: N(Boc)-Gly-β-Leu–OCH3(14), N(Boc)-O(Bz)α-Ser-β-Leu–OCH3(16), and N(Boc)-O(Bz)-α-Tyr-α-Gly-β-Leu–OCH3(17), characterized by FTIR and 1H NMR analysis. The synthesized peptide 16 showed highest inhibitory activity (45.22%) followed by peptide 14 (18.51%) and peptide 17 (17.05%),…
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Taxonomy
TopicsProtein Hydrolysis and Bioactive Peptides · Enzyme Production and Characterization · Carbohydrate Chemistry and Synthesis