Flavonoids as antiobesity agents: A review

Abstract

Obesity is a global health problem that affects all age groups in both developing and developed countries. In recent years, the prevalence of overweight and obesity has reached pandemic levels, resulting in a dramatic increase in the incidence of various comorbidities, such as cardiovascular diseases, type 2 diabetes, and cancer, consequently leading to massive health and socioeconomic burdens. Together with lifestyle changes, antiobesity pharmacotherapy is gaining momentum as an adjunctive treatment. However, the available pharmacological approaches have limited use owing to either significant adverse effects or low efficacy. Over the years, natural products have been an important source of lead compounds for drug discovery. Among these, flavonoids are associated with important biological effects and health‐promoting activities. In this review, we discuss the modulatory effects of flavonoids on obesity and their potential mechanisms of action. The literature strongly suggests that most common flavonoids demonstrate a pronounced effect on obesity as shown by their ability to lower body weight, fat mass, and plasma triglycerides/cholesterol, both in in vitro and in vivo models. The impact of flavonoids on obesity can be observed through different mechanisms: reducing food intake and fat absorption, increasing energy expenditure, modulating lipid metabolism, or regulating gut microbiota profile. A better understanding of the known antiobesity mechanisms of flavonoids will enable their potential use to treat this medical condition. Therefore, this review focuses on the putative biological mechanisms through which flavonoids may prevent or treat obesity and highlights new perspectives on future pharmacological use.

A review of the lipolytic effects and the reduction of abdominal fat from bioactive compounds and moro orange extracts

“…Further in vitro investigations have revealed that 3T3-L1 preadipocytes treated with the flavonoid aglycosides naringenin and hesperetin inhibited adipogenesis by suppressing transcription factors including C/EBPα, PPARγ and SREBP-1c, in addition, to inducing lipolysis mechanisms in these adipocytes. Additionally, in another study also carried out on 3T3-L1 preadipocytes treated with naringenin inhibited adipogenesis through the molecular markers PPARγ, a P2, adiponutrin (ADPN) and STAT5s ( Rufino et al., 2021 ).…”

“…To date, a variety of studies have shown in the literature that the combined use of these flavonoids or isolates can suppress adipogenic and adipocyte differentiation markers through especially the modulation of PPARγ, C/EBPα, C/EBPβ, SREBP-1 and even stimulating thermogenesis through the expression of UCP-2 ( Rufino et al., 2021 ).…”

“…Furthermore, it has been shown in Huh7 hepatic cells human treated with naringenin that these bioactive agents promote significant increased target genes that control fatty acid oxidation, such as CYP4A11, ACOX, ApoAI and UCP1 while concurrently, inhibiting LXRα-regulated lipogenesis genes, such FAS, ABCA1, ABCG1, and HMG CoA reductase (HMGR) ( Rufino et al., 2021 ).…”

“… Inhibits adipogenesis → decrease of C/EBP-α, PPARγ, SREBP-1c, PAGC-1α, FAS, and aP2 mRNA expression ( Lim et al, 2019 ). [( Rufino et al, 2021 )] II. In vitro, Adipocytes derived from human MSCs II.…”

“…To date, a variety of studies have shown in the literature that the combined use of these flavonoids or isolates can suppress adipogenic and adipocyte differentiation markers through especially the modulation of PPARγ, C/EBPα, C/EBPβ, SREBP-1 and even stimulating thermogenesis through the expression of UCP-2 (Rufino et al, 2021). Interestingly, naringenin supplementation reduced adipose tissue weight gain and triacylglycerol content in rats by increasing the expression PPARα, CPT-1, and UCP-2 in the liver which are target genes for fatty acid oxidation.…”