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Plant flavone apigenin: An emerging anticancer agent
Eswar Shankar1,2, Aditi Goel3, Karishma Gupta1,2
1Department of Urology, The James and Eilleen Dicke Laboratory, Case Western Reserve University, Cleveland, OH 44106, USA.
Abstract:
Research in cancer chemoprevention provides convincing evidence that increased intake of vegetables and fruits may reduce the risk of several human malignancies. Phytochemicals present therein provide beneficial anti-inflammatory and antioxidant properties that serve to improve the cellular microenvironment. Compounds known as flavonoids categorized anthocyanidins, flavonols, flavanones, flavonols, flavones, and isoflavones have shown considerable promise as chemopreventive agents. Apigenin (4', 5, 7-trihydroxyflavone), a major plant flavone, possessing antioxidant, anti-inflammatory, and anticancer properties affecting several molecular and cellular targets used to treat various human diseases. Epidemiologic and case-control studies have suggested apigenin reduces the risk of certain cancers. Studies demonstrate that apigenin retain potent therapeutic properties alone and/or increases the efficacy of several chemotherapeutic drugs in combination on a variety of human cancers. Apigenin's anticancer effects could also be due to its differential effects in causing minimal toxicity to normal cells with delayed plasma clearance and slow decomposition in liver increasing the systemic bioavailability in pharmacokinetic studies. Here we discuss the anticancer role of apigenin highlighting its potential activity as a chemopreventive and therapeutic agent. We also highlight the current caveats that preclude apigenin for its use in the human trials.
Insights
Apigenin, a plant flavone, shows promise in cancer prevention and treatment due to its antioxidant and anti-inflammatory effects. Further research is needed to address limitations for human trials.
Area of Science:
- Oncology
- Pharmacology
- Nutritional Science
Background:
- Fruits and vegetables contain phytochemicals with anti-inflammatory and antioxidant properties.
- Flavonoids, a class of phytochemicals, show potential as cancer chemopreventive agents.
- Apigenin is a prominent flavone with demonstrated antioxidant, anti-inflammatory, and anticancer activities.
Purpose of the Study:
- To review the anticancer role of apigenin.
- To highlight apigenin's potential as a chemopreventive and therapeutic agent.
- To discuss current limitations for apigenin's use in human trials.
Main Methods:
- Review of epidemiological and case-control studies on apigenin.
- Analysis of preclinical studies on apigenin's mechanisms of action.
- Pharmacokinetic evaluation of apigenin's bioavailability and metabolism.
Main Results:
- Apigenin intake is associated with reduced risk of certain cancers.
- Apigenin exhibits potent therapeutic effects alone and enhances chemotherapy efficacy.
- Apigenin shows minimal toxicity to normal cells with favorable pharmacokinetic properties.
Conclusions:
- Apigenin possesses significant anticancer potential as both a preventive and therapeutic agent.
- Apigenin's unique properties contribute to its anticancer effects and bioavailability.
- Caveats currently limit the direct application of apigenin in human clinical trials.
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