Abstract

Diabetes mellitus is a chronic degenerative disease that causes long-term complications and represents a serious public health problem. Turnera diffusa (damiana) is a shrub that grows throughout Mexico and is traditionally used for many illnesses including diabetes. Although a large number of plant metabolites are known, there are no reports indicating which of these are responsible for this activity, and this identification was the objective of the present work. Through bioassay-guided fractionation of a methanolic extract obtained from the aerial part of T. diffusa, teuhetenone A was isolated and identified as the main metabolite responsible for the plant’s hypoglycemic activity. Alpha-glucosidase inhibitory activity and cytotoxicity of this metabolite were determined. Hypoglycemic and antidiabetic activities were evaluated in a murine model of diabetes in vivo, by monitoring glucose levels for six hours and comparing them with levels after administering various controls. Teuhetenone A was not cytotoxic at the tested concentrations, and did not show inhibitory activity in the glucosidase test, and the in vivo assays showed a gradual reduction in glucose levels in normoglycemic and diabetic mice. Considering these results, we suggest that teuhetenone A has potential as an antidiabetic compound, which could be further submitted to preclinical assays.

Highlights

  • Type 2 diabetes mellitus (T2DM) is a chronic degenerative disease characterized by hyperglycemia, mainly due to defects of insulin secretion and/or action

  • In the first pharmacological approach to T. diffusa derivatives, the hypoglycemic activity of methanolic extracts of the plant was investigated in normoglycemic mice, as described in the Materials and Methods section (Figure 1)

  • By means of a bioassay-guided fractionation, we determined that the terpenoid-rich fraction was responsible for the activity

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Summary

Introduction

Type 2 diabetes mellitus (T2DM) is a chronic degenerative disease characterized by hyperglycemia, mainly due to defects of insulin secretion and/or action. The disorder is associated with an imbalance of the glycemic index and glucose intolerance, which increases the risk of individuals progressing to. Complications from diabetes, such as coronary artery and peripheral vascular disease, stroke, diabetic neuropathy, risk of ulcers and amputations, renal failure, sexual dysfunction, and blindness are resulting in increasing disability, reduced life expectancy, and enormous health costs for virtually every society [1,2]. T2DM is a leading cause of morbidity and mortality in industrialized and developing countries, resulting in part from high-carbohydrate and high-fat diets that lead to excess weight and/or obesity, Molecules 2017, 22, 599; doi:10.3390/molecules22040599 www.mdpi.com/journal/molecules. The consequences of high-carbohydrate and high-fat diets are most severe in communities in developing countries, where poverty represents an additional problem [3,4]

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