- Sep 21, 2011
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 ...
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AbstractApigenin 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.
Conclusions and Future PerspectivesApigenin is a multimodal nutraceutical with therapeutic applications in several chronic diseases, such as cancer, Alzheimer’s disease, depression, diabetes, and cardiovascular disorders. Apigenin as a naturally derived bioactive molecule is greatly supported by preclinical studies to provide a powerful cardioprotective effect, supporting its development as a drug product for clinical translation. Its availability as a nutraceutical and utilization as a non-prescription dietary supplement also supports its safety profile in humans. However, extensive clinical trials are required before making recommendations for human usage. Studies standardizing these therapeutically beneficial effects, especially with respect to establishing a reproducible dose–response and dose–safety profile, are currently lacking and require further investigations.
Furthermore, apigenin has been shown to be unstable and poorly absorbed in the GI tract on oral administration. Thus, formulating an oral dosage form enhancing its stability and bioavailability, and supporting its therapeutic advantages in vivo are also necessary before being evaluated in clinical studies and for its translation into a clinically acceptable option for therapy.