Current Pharmacology Reports

, Volume 3, Issue 6, pp 423–446 | Cite as

Plant Flavone Apigenin: an Emerging Anticancer Agent

  • Eswar Shankar
  • Aditi Goel
  • Karishma Gupta
  • Sanjay GuptaEmail author
Cancer Chemoprevention (R Agarwal, Section Editor)
Part of the following topical collections:
  1. Topical Collection on Cancer Chemoprevention


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 retains 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 the 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.


Cancer chemoprevention Dietary agents Plant flavonoids Health effects Nanoparticle Polyphenols 



N-(4-Hydroxyphenyl) retinamide




Aberrant crypt foci




Adenosine di-phosphate


American Institute for Cancer Research




Adenomatous polyposis coli


Activating transcription factor 3


Breast cancer resistance protein


Casein kinase 2




Death-inducing signaling complex




Death receptor 4


Epidermal growth factor receptor


Extracellular regulated kinase


Focal adhesion kinase


DNA fragmentation factor-45


Glioma-associated oncogene 1


Glucose transporter 1


Glutathione S-transferase A1


Histone deacetylase


Hypoxia-inducible factor 1-alpha


Telomerase reverse transcriptase


Intercellular adhesion molecule-1


Type I interferon receptor 1


Interferon gamma


Insulin-like growth factor




Janus kinase


c-Jun amino-terminal kinase


Krüpple-like factor 4


Mitogen-activated protein kinases


Matrix metalloproteinases


Nicotinamide adenine dinucleotide phosphate


Nuclear factor-kappaB


Na+/I− symporter


Non-small cell lung cancer


Ornithine decarboxylase


Poly (ADP-ribose) polymerase


Programmed death-ligand 1


Proline-directed protein kinase FA


Phosphatidylinositol-4,5-bisphosphate 3-kinase


Protein kinase C




Protein kinase C-activating phorbol ester


Reactive oxygen species


Superoxide dismutase


Signal transducer and activator of transcription


Transforming growth factor-beta


Tumor necrosis factor-related apoptosis-inducing ligands


Transgenic adenocarcinoma of the mouse prostate


UDP-glucuronosyltransferase 1–1


Vascular endothelial growth factor


World Cancer Research Fund



We sincerely apologize to those investigators whose work could not be cited due to space constraints.

Funding information

The original work from author’s laboratory outlined in this review was supported by VA Merit Review 1I01BX002494; United States Public Health Service Grants RO1CA108512, R21CA193080, and R03CA186179 and Department of Defense grant W81XWH-15-1-0558 to SG.

Compliance with Ethical Standards

Conflict of Interest

The authors have no competing interest.

Human and Animal Rights and Informed Consent

This article does not contain any studies with human or animal subjects performed by any of the authors.


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Copyright information

© Springer International Publishing AG 2017

Authors and Affiliations

  1. 1.Department of Urology, The James and Eilleen Dicke LaboratoryCase Western Reserve UniversityClevelandUSA
  2. 2.Department of Urology, The Urology InstituteUniversity Hospitals Cleveland Medical CenterClevelandUSA
  3. 3.Department of Biology, School of Undergraduate StudiesCase Western Reserve UniversityClevelandUSA
  4. 4.Department of NutritionCase Western Reserve UniversityClevelandUSA
  5. 5.Division of General Medical SciencesCase Comprehensive Cancer CenterClevelandUSA
  6. 6.Department of UrologyLouis Stokes Cleveland Veterans Affairs Medical CenterClevelandUSA

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