Abstract
Diabetes mellitus is a severe health problem in Mexico, and its prevalence is increasing exponentially every year. Recently, DPP-4 (dipeptidyl peptidase-4) inhibitors have become attractive oral anti-hyperglycemic agents to reduce the pathology of diabetes. Gliptin’s family, such as sitagliptin, vildagliptin, and alogliptin, are in clinical use to treat diabetes mellitus but possess side effects. Therefore, there is a specific need to look for new therapeutic scaffolds (biomolecules). Garlic bulb is widely used as a traditional remedy for the treatment of diabetes. The garlic extracts are scientifically proven to control glucose levels in patients with diabetes, despite the unknown mechanism of action. The aim of the study is to investigate the antidiabetic effects of ultrasonication assisted garlic bulb extract. To achieve this, in-vitro assays such as DPP-4 inhibitory and antioxidant activities were investigated. Further, functional group analysis using FTIR and identification of phytochemicals using mass spectrometry analysis was performed. The results showed that 70.9 µg/mL of garlic bulb extract inhibited 50% DPP-4 activity. On top of that, the garlic extract exhibited a 20% scavenging activity, equivalent to 10 µg/mL of ascorbic acid. Molecular docking simulations on identified phytochemicals using mass spectrometry revealed their potential binding at the DPP-4 druggable region, and therefore the possible DPP-4 inhibition mechanism. These results suggest that prepared garlic extract contains phytochemicals that inhibit DPP-4 and have antioxidant activity. Also, the prepared extract induces skeletal muscle cell proliferation that demonstrates the antidiabetic effect and its possible mechanism of action.
Highlights
Diabetes mellitus (DM) is a condition in people with elevated levels of blood glucose and is a common and major health concern in Mexico [1] and around the world [2]
Dipeptidyl peptidase 4 (DPP-4) has emerged as an important therapeutic drug target to treat diabetes mellitus, and great effort by academics and the pharmaceutical industry have naturally led to the development of DPP-4 inhibitors with few side effects in comparison to current FDA approved therapeutics
The DPP-4 inhibitory activity of prepared garlic bulb extract in this study is shown in Figure 3 It is observed that the garlic extract showed 60.5% DPP-4 inhibition at 100 μg/mL and the inhibition capacity is concentration-dependent
Summary
Diabetes mellitus (DM) is a condition in people with elevated levels of blood glucose and is a common and major health concern in Mexico [1] and around the world [2]. Recent developments in the pharmacology of diabetes mellitus have led to the discovery of more than one therapeutic drug target to adequately reduce glucose levels and, among these, dipeptidyl peptidase-4 was found to be more effective [4]. DPP-4 rapidly degrades glucagon-like peptide (GLP-1 and GLP-2), glucose-dependent insulin releasing polypeptide GIP [5], stromal-cell derived factor (SDF-2) [6], chemokine (C-C motif) ligand 5 (RANTES) [7], and eotaxin [8]. Among these specific substrates, incretin hormones secreted by intestinal cells are responsible for adequately controlling blood glucose levels [9]. DPP-4 inhibitors are scientifically proven to prolong the incretin effect for the successful treatment of diabetes mellitus
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