Apigenin inhibits STAT3/CD36 signaling axis and reduces visceral obesity

Su, Tao; Huang, Chunhua; Yang, Chunfang; Jiang, Ting; Su, Junfang; Chen, Minting; Fatima, Sarwat; Gong, Rui-Hong; Hu, Xianjing; Bian, Zhaoxiang; Liu, Zhongqiu; Kwan, Hiu Yee

doi:10.1016/j.phrs.2019.104586

Cited by 103 publications

(74 citation statements)

References 48 publications

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“…Besides its reduction of the inflammatory phenotype in adipose tissue, apigenin administration to diet-induced obese mice ameliorated the body weight increment, reduced the visceral adiposity by inhibiting the adipogenesis via a STAT3/CD36 signaling pathway [ 361 ], decreased leptin and increased adiponectin [ 362 ] and induced energy expenditure mainly by promoting lipolysis and FAO as well as browning of WAT [ 363 ]. In scWAT, apigenin-treated mice exhibited a downregulation of adipogenic genes ( Pparγ, Lpl and aP2) and of genes involved in lipogenesis ( Fasn and Scd1 ) and a promotion of lipolysis by increasing the mRNA levels of Atgl, Hsl, Forkhead box protein O1 (FoxO1) and Sirt1.…”

Section: Flavonesmentioning

confidence: 99%

Metabolic Impact of Flavonoids Consumption in Obesity: From Central to Peripheral

et al. 2020

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The prevention and treatment of obesity is primary based on the follow-up of a healthy lifestyle, which includes a healthy diet with an important presence of bioactive compounds such as polyphenols. For many years, the health benefits of polyphenols have been attributed to their anti-oxidant capacity as free radical scavengers. More recently it has been described that polyphenols activate other cell-signaling pathways that are not related to ROS production but rather involved in metabolic regulation. In this review, we have summarized the current knowledge in this field by focusing on the metabolic effects of flavonoids. Flavonoids are widely distributed in the plant kingdom where they are used for growing and defensing. They are structurally characterized by two benzene rings and a heterocyclic pyrone ring and based on the oxidation and saturation status of the heterocyclic ring flavonoids are grouped in seven different subclasses. The present work is focused on describing the molecular mechanisms underlying the metabolic impact of flavonoids in obesity and obesity-related diseases. We described the effects of each group of flavonoids in liver, white and brown adipose tissue and central nervous system and the metabolic and signaling pathways involved on them.

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Section: Flavonesmentioning

confidence: 99%

Metabolic Impact of Flavonoids Consumption in Obesity: From Central to Peripheral

et al. 2020

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“…Baicalin (20 mg/kg/day), luteolin (5 mg/kg/day), apigenin (50 mg/kg/day), and vitexin (5 mg/kg/day) repress the expression of transcription factors associated with adipose differentiation, attenuate adiposity, and mitigate lipogenesis in WAT of HFD-fed C57BL/6J mice [128,134,139,145]. Apigenin (15-30 mg/kg) inhibit preadipocyte differentiation and visceral obesity in HFD-fed mice, by directly interacting with STAT3, hence inhibiting STAT3 transcriptional activity and reducing the expression of CD36 and PPARγ [129]. These results further support that flavones can exert their biological activities through direct binding to proteins.…”

Section: Role Of Flavones In Obesity-induced Inflammationmentioning

confidence: 99%

The Targeted Impact of Flavones on Obesity-Induced Inflammation and the Potential Synergistic Role in Cancer and the Gut Microbiota

Sudhakaran

Doseff

2020

Molecules

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Obesity is an inflammatory disease that is approaching pandemic levels, affecting nearly 30% of the world’s total population. Obesity increases the risk of diabetes, cardiovascular disorders, and cancer, consequentially impacting the quality of life and imposing a serious socioeconomic burden. Hence, reducing obesity and related life-threatening conditions has become a paramount health challenge. The chronic systemic inflammation characteristic of obesity promotes adipose tissue remodeling and metabolic changes. Macrophages, the major culprits in obesity-induced inflammation, contribute to sustaining a dysregulated immune function, which creates a vicious adipocyte–macrophage crosstalk, leading to insulin resistance and metabolic disorders. Therefore, targeting regulatory inflammatory pathways has attracted great attention to overcome obesity and its related conditions. However, the lack of clinical efficacy and the undesirable side-effects of available therapeutic options for obesity provide compelling reasons for the need to identify additional approaches for the prevention and treatment of obesity-induced inflammation. Plant-based active metabolites or nutraceuticals and diets with an increased content of these compounds are emerging as subjects of intense scientific investigation, due to their ability to ameliorate inflammatory conditions and offer safe and cost-effective opportunities to improve health. Flavones are a class of flavonoids with anti-obesogenic, anti-inflammatory and anti-carcinogenic properties. Preclinical studies have laid foundations by establishing the potential role of flavones in suppressing adipogenesis, inducing browning, modulating immune responses in the adipose tissues, and hindering obesity-induced inflammation. Nonetheless, the understanding of the molecular mechanisms responsible for the anti-obesogenic activity of flavones remains scarce and requires further investigations. This review recapitulates the molecular aspects of obesity-induced inflammation and the crosstalk between adipocytes and macrophages, while focusing on the current evidence on the health benefits of flavones against obesity and chronic inflammation, which has been positively correlated with an enhanced cancer incidence. We conclude the review by highlighting the areas of research warranting a deeper investigation, with an emphasis on flavones and their potential impact on the crosstalk between adipocytes, the immune system, the gut microbiome, and their role in the regulation of obesity.

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“…3T3-L1 preadipocytes (ATCC) were induced to differentiate into mature white adipocytes with differentiation-inducing medium containing 1 mM dexamethasone, 0.5 mM isobutylmethylxanthine, and 1.67 mM insulin in Dulbecco's modified Eagle's medium with 10% FBS for 4 days before switching to Dulbecco's modified Eagle's medium with only 10% FBS and 10 μg/mL insulin for an additional 3 days (Su et al, 2020).…”

Section: T3-l1 Preadipocyte Differentiationmentioning

confidence: 99%

“…The apoptotic effect of ZBM was first validated in vitro. We first examined the effect of ZBM on the viability of 3T3-L1 adipocytes, which are the commonly used adipocyte models (Su et al, 2020). Figure 6A showed that ZBM significantly reduced the viability of 3T3-L1 cells after 24 or 48 h treatments.…”

Section: Experimental Validation In Vitromentioning

confidence: 99%

Network Pharmacology-Based Strategy for the Investigation of the Anti-Obesity Effects of an Ethanolic Extract of Zanthoxylum bungeanum Maxim

et al. 2020

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Network pharmacology is considered as the next paradigm in drug discovery. In an era when obesity has become global epidemic, network pharmacology becomes an ideal tool to discover novel herbal-based therapeutics with effective anti-obesity effects. Zanthoxylum bungeanum Maxim (ZBM) is a medicinal herb. The mature pericarp of ZBM is used for disease treatments and as spice for cooking. Here, we used the network pharmacology approach to investigate whether ZBM possesses anti-obesity effects and reveal the underlying mechanism of action. We first built up drug–ingredient–gene symbol–disease network and protein–protein interaction network of the ZBM-related obesity targets, followed by Gene Ontology and Kyoto Encyclopedia of Genes and Genomes pathway enrichment analyses. The results highlight apoptosis as a promising signaling pathway that mediates the anti-obesity effects of ZBM. Molecular docking also reveals quercetin, a compound in ZBM has the highest degree of connections in the compound-target network and has direct bindings with the apoptotic markers. Furthermore, the apoptotic effects of ZBM are further validated in 3T3-L1 adipocytes and in the high-fat diet–induced obesity mouse model. These findings not only suggest ZBM can be developed as potential anti-obesity therapeutics but also demonstrate the application of network pharmacology for the discovery of herbal-based therapeutics for disease treatments.

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Apigenin inhibits STAT3/CD36 signaling axis and reduces visceral obesity

Cited by 103 publications

References 48 publications

Metabolic Impact of Flavonoids Consumption in Obesity: From Central to Peripheral

Metabolic Impact of Flavonoids Consumption in Obesity: From Central to Peripheral

The Targeted Impact of Flavones on Obesity-Induced Inflammation and the Potential Synergistic Role in Cancer and the Gut Microbiota

Network Pharmacology-Based Strategy for the Investigation of the Anti-Obesity Effects of an Ethanolic Extract of Zanthoxylum bungeanum Maxim

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