Current Status and Future Perspectives on Therapeutic Potential of Apigenin: Focus on Metabolic-Syndrome-Dependent Organ Dysfunction

Alam, Waqas; Rocca, Carmine; Khan, Haroon; Hussain, Yaseen; Aschner, Michael; Bartolo, Anna De; Amodio, Nicola; Angelone, Tommaso; Cheang, Wai San

doi:10.3390/antiox10101643

Cited by 32 publications

(21 citation statements)

References 192 publications

(222 reference statements)

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“…Apigenin was also found to lower the plasma levels of free fatty acids, total cholesterol, apolipoprotein B and hepatic injury markers and ameliorated the progression of hepatic steatosis and hepatomegaly. The reduction in endothelial dysfunction along with improvement in insulin resistance further strengthens its therapeutic implications in metabolic disorders [ 6 ].…”

Section: Pharmacological Actions Of Apigeninmentioning

confidence: 99%

“…However, extensive regulatory toxicology studies are yet needed to establish its safety in human studies. Apigenin has been reported to induce hepatocyte degeneration and toxicity, mild sedation, and muscle relaxation in murine models at very high doses (100 and 200 mg/kg) [ 6 ]. However, chamomile, a rich source of apigenin on widespread use, has not been linked to clinically apparent liver injury.…”

Section: Pharmacokinetics and Toxicity Of Apigeninmentioning

confidence: 99%

“…Considering the health benefits and dietary availability, efforts have been made in the past few years to promote its nutraceutical usage. Regarding the biopharmaceutic characteristics, it has been classified as a Class II molecule in the Biopharmaceutics Classification System (BCS) owing to the high membrane permeability and poor solubility [ 6 ]. BCS plays a role in signifying oral drug absorption, solubility, and intestinal permeability, and is thus considered useful in drug discovery, development and regulatory concerns.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacological and Molecular Insight on the Cardioprotective Role of Apigenin

Thomas

Jha

et al. 2023

Nutrients

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Apigenin is a naturally occurring dietary flavonoid found abundantly in fruits and vegetables. It possesses a wide range of biological properties that exert antioxidant, anti-inflammatory, anticancer, and antibacterial effects. These effects have been reported to be beneficial in the treatment of atherosclerosis, stroke, hypertension, ischemia/reperfusion-induced myocardial injury, and diabetic cardiomyopathy, and provide protection against drug-induced cardiotoxicity. These potential therapeutic effects advocate the exploration of the cardioprotective actions of apigenin. This review focuses on apigenin, and the possible pharmacological mechanisms involved in the protection against cardiovascular diseases. We further discuss its therapeutic uses and highlight its potential applications in the treatment of various cardiovascular disorders. Apigenin displays encouraging results, which may have implications in the development of novel strategies for the treatment of cardiovascular diseases. With the commercial availability of apigenin as a dietary supplement, the outcomes of preclinical studies may provide the investigational basis for future translational strategies evaluating the potential of apigenin in the treatment of cardiovascular disorders. Further preclinical and clinical investigations are required to characterize the safety and efficacy of apigenin and establish it as a nutraceutical as well as a therapeutic agent to be used alone or as an adjuvant with current drugs.

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Section: Pharmacological Actions Of Apigeninmentioning

confidence: 99%

Section: Pharmacokinetics and Toxicity Of Apigeninmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Pharmacological and Molecular Insight on the Cardioprotective Role of Apigenin

Thomas

Jha

et al. 2023

Nutrients

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“…T2DM is a heterogeneous metabolic disorder, characterized by insulin tolerance and cell dysfunction, resulting in persistent hyperglycemia. Hyperglycemia is thought to be the primary cause of metabolic disorders, which not only reduce living standard and longevity, but also place a financial strain on health-care systems [112].…”

Section: Role Of Curcumin Targeting Inflammation In Diabetes Resistancementioning

confidence: 99%

How Curcumin Targets Inflammatory Mediators in Diabetes: Therapeutic Insights and Possible Solutions

et al. 2022

Self Cite

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Diabetes mellitus is a multifactorial chronic metabolic disorder, characterized by altered metabolism of macro-nutrients, such as fats, proteins, and carbohydrates. Diabetic retinopathy, diabetic cardiomyopathy, diabetic encephalopathy, diabetic periodontitis, and diabetic nephropathy are the prominent complications of diabetes. Inflammatory mediators are primarily responsible for these complications. Curcumin, a polyphenol derived from turmeric, is well known for its anti-oxidant, anti-inflammatory, and anti-apoptotic properties. The regulation of several signaling pathways effectively targets inflammatory mediators in diabetes. Curcumin’s anti-inflammatory and anti-oxidative activities against a wide range of molecular targets have been shown to have therapeutic potential for a variety of chronic inflammatory disorders, including diabetes. Curcumin’s biological examination has shown that it is a powerful anti-oxidant that stops cells from growing by releasing active free thiol groups at the target location. Curcumin is a powerful anti-inflammatory agent that targets inflammatory mediators in diabetes, and its resistant form leads to better therapeutic outcomes in diabetes complications. Moreover, Curcumin is an anti-oxidant and NF-B inhibitor that may be useful in treating diabetes. Curcumin has been shown to inhibit diabetes-related enzymes, such as a-glucosidase, aldose reductase and aldose reductase inhibitors. Through its anti-oxidant and anti-inflammatory effects, and its suppression of vascular endothelial development and nuclear transcription factors, curcumin has the ability to prevent, or reduce, the course of diabetic retinopathy. Curcumin improves insulin sensitivity by suppressing phosphorylation of ERK/JNK in HG-induced insulin-resistant cells and strengthening the PI3K-AKT-GSK3B signaling pathway. In the present article, we aimed to discuss the anti-inflammatory mechanisms of curcumin in diabetes regulated by various molecular signaling pathways.

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“…In the context of oesophageal cancer, IL-6 transcription is inhibited in response to apigenin as an intervention [154], and apigenin also exhibits anti-leukemic activity in vivo and in human cells by inducing apoptosis [155]. Apigenin can further attenuate metabolic complications leading to risk and characteristics of metabolic disorders, such as metabolic syndrome, atherosclerosis, and diabetes [156]. Apigenin reduces the expression of COX2 and can also produce anti-inflammatory effects in the context of cardiovascular disease, neurodegeneration, diabetes, and cancer [157].…”

Section: Betainementioning

confidence: 99%

Potential Synergistic Supplementation of NAD+ Promoting Compounds as a Strategy for Increasing Healthspan

Sharma¹,

Chabloz²,

Roider³

et al. 2022

Preprint

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Disrupted biological function, manifesting through the hallmarks of aging, poses as one of the largest threats to healthspan and risk of disease development, such as metabolic disorders, cardiovascular ailments, and neurodegeneration. In recent years, numerous geroprotectors, senolytics, and other nutraceuticals have emerged as potential disruptors of aging and may be viable interventions in the immediate state of human longevity science. In this review, we focus on the decrease of nicotinamide adenine dinucleotide (NAD+) with age and the supplementation of NAD+ precursors, such as nicotinamide mononucleotide (NMN) or nicotinamide riboside (NR), in combination with other geroprotective compounds to restore youthful NAD+ levels. Furthermore, these geroprotectors may enhance the efficacy of NMN supplementation while concurrently providing their own numerous health benefits. By analyzing the prevention of NAD+ degradation through inhibition of CD38 or supporting protective downstream agents of SIRT1, we provide a potential framework of the CD38/NAD+/SIRT1 axis through which geroprotectors may enhance the efficacy of NMN supplementation and reduce the risk of age-related diseases, thereby potentiating healthspan in humans.

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Current Status and Future Perspectives on Therapeutic Potential of Apigenin: Focus on Metabolic-Syndrome-Dependent Organ Dysfunction

Cited by 32 publications

References 192 publications

Pharmacological and Molecular Insight on the Cardioprotective Role of Apigenin

Pharmacological and Molecular Insight on the Cardioprotective Role of Apigenin

How Curcumin Targets Inflammatory Mediators in Diabetes: Therapeutic Insights and Possible Solutions

Potential Synergistic Supplementation of NAD+ Promoting Compounds as a Strategy for Increasing Healthspan

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