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Discovery of Galangin as a Potential DPP-4 Inhibitor That Improves Insulin-Stimulated Skeletal Muscle Glucose Uptake: A Combinational Therapy for Diabetes

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Departamento de Biofísica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Prolongación de Carpio y Plan de Ayala S/N, Col. Santo Tomás, C.P. 11340 Ciudad de México, Mexico
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Departamento de Ingeniería Bioquímica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Av. Wilfrido Massieu S/N, Col. Unidad Profesional Adolfo López Mateos, Zacatenco, CP. 07738 Ciudad de México, México
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Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(5), 1228; https://doi.org/10.3390/ijms20051228
Received: 24 January 2019 / Revised: 5 March 2019 / Accepted: 8 March 2019 / Published: 11 March 2019
(This article belongs to the Section Bioactives and Nutraceuticals)
Dipeptidyl peptidase-4 (DPP-4) is a well-known therapeutic drug target proven to reduce blood glucose levels in diabetes mellitus, and clinically, DPP-4 inhibitors are used in combination with other anti-diabetic agents. However, side effects and skeletal muscle health are not considered in the treatment for diabetic patients. Recently, natural compounds have been proven to inhibit DPP-4 with fewer side effects. In this work, initially, molecular docking simulations revealed that a natural compound, Galangin, possess a binding energy of −24 KJ/mol and interaction residues SER 630 and TYR 547, that are responsible for potent DPP-4 inhibition. In vitro studies showed that galangin not only inhibits DPP-4 in a concentration-dependent manner but also regulates glucose levels, enabling the proliferation of rat L6 skeletal muscle cells. The combination of galangin with insulin benefits regulation of glucose levels significantly in comparison to galangin alone (p < 0.05). These findings suggest the beneficial effect of the use of galangin, both alone or in combination with insulin, to reduce glucose levels and improve skeletal muscle health in diabetes mellitus. View Full-Text
Keywords: diabetes mellitus; molecular docking; galangin; DPP-4 inhibitor; combination therapy; skeletal muscle cell health diabetes mellitus; molecular docking; galangin; DPP-4 inhibitor; combination therapy; skeletal muscle cell health
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Kalhotra, P.; Chittepu, V.C.S.R.; Osorio-Revilla, G.; Gallardo-Velázquez, T. Discovery of Galangin as a Potential DPP-4 Inhibitor That Improves Insulin-Stimulated Skeletal Muscle Glucose Uptake: A Combinational Therapy for Diabetes. Int. J. Mol. Sci. 2019, 20, 1228.

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