Abstract
A wide group of natural compounds (flavonoids, stilbenes, neolignans and others) has been identified as Peroxisome Proliferator-Activated Receptor (PPAR) agonists, with a large variety of chemical structure and different activity versus the three PPAR subtypes. These receptors are transcription factors controlling metabolic pathways in the organism, involved in lipid and glucose metabolism, cell differentiation and energy homeostasis. Otherwise, very little is known about natural compounds able to inhibit PPARs. A number of studies demonstrate that PPARγ repression has a beneficial effect in reducing body weight and improving insulin sensitivity, suggesting a potential clinical role in obesity and type 2 diabetes. This review analyzes natural compounds able to repress PPAR activity and their potential use in metabolic disorders.
Highlights
Obesity is considered one of the major metabolic disease in industrialized countries, being the number of obese always increasing worldwide
Very little is known about natural compounds able to inhibit Peroxisome ProliferatorActivated Receptor (PPAR)
A recent study examined a possible connection between Foenumoside B and Lysimachia foenum-graecum extract with PPARγ, a master regulator of adipocyte differentiation [50]
Summary
Obesity is considered one of the major metabolic disease in industrialized countries, being the number of obese always increasing worldwide. Incorrect lifestyles and high-fat diet contribute to the weight gain, in addition to hereditary and medical factors This disease is strongly linked to concomitant medical situations, as dyslipidemia, hypertension, coronary heart disease, type 2 diabetes and metabolic syndrome. The Thiazolidinediones (TZDs), PPARγ agonists, have been used as antidiabetic drugs, being able to improve insulin sensitivity [7] Despite their beneficial effects in the treatment of diabetic patients, major safety problems emerged during the treatment with TZDs, including hepatic dysfunction, hypoglycemia, weight gain, cardiovascular failure and edema; for these reasons, some compounds of this class were withdrawn from the pharmaceutical market or discontinued from clinical studies [8, 9]. PPARγ antagonists from natural sources will be the focus of this review, with special attention to their promising activities as antiobesity and antidiabetic agents
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