Rationalizing the therapeutic potential of apigenin against cancer.

Abstract

BACKGROUND:

Despite the remarkable advances made in the diagnosis and treatment of cancer during the past couple of decades, it remains the second largest cause of mortality in the world, killing approximately 9.6 million people annually. The major challenges in the treatment of the advanced stage of this disease are the development of chemoresistance, severe adverse effects of the drugs, and high treatment cost. Therefore, the development of drugs that are safe, efficacious, and cost-effective remains a 'Holy Grail' in cancer research. However, the research over the past four decades shed light on the cancer-preventive and therapeutic potential of natural products and their underlying mechanism of action. Apigenin is one such compound, which is known to be safe and has significant potential in the prevention and therapy of this disease.

AIM:

To assess the literature available on the potential of apigenin and its analogs in modulating the key molecular targets leading to the prevention and treatment of different types of cancer.

METHOD:

A comprehensive literature search has been carried out on PubMed for obtaining information related to the sources and analogs, chemistry and biosynthesis, physicochemical properties, biological activities, bioavailability and toxicity of apigenin.

KEY FINDINGS:

The literature search resulted in many in vitro, in vivo and a few cohort studies that evidenced the effectiveness of apigenin and its analogs in modulating important molecular targets and signaling pathways such as PI3K/AKT/mTOR, JAK/STAT, NF-κB, MAPK/ERK, Wnt/β-catenin, etc., which play a crucial role in the development and progression of cancer. In addition, apigenin was also shown to inhibit chemoresistance and radioresistance and make cancer cells sensitive to these agents. Reports have further revealed the safety of the compound and the adaptation of nanotechnological approaches for improving its bioavailability.

SIGNIFICANCE:

Hence, the present review recapitulates the properties of apigenin and its pharmacological activities against different types of cancer, which warrant further investigation in clinical settings.

• Authors: Semim Akhtar Ahmed, Dey Parama, Enush Daimari, Sosmitha Girisa, Kishore Banik, Choudhary Harsha, Uma Dutta, Ajaikumar B Kunnumakkara
• Journal: Life sciences (Life Sci) Vol. 267 Pg. 118814 (Feb 15 2021) ISSN: 1879-0631 [Electronic] Netherlands
• PMID: 33333052 (Publication Type: Journal Article, Review)
• Copyright: Copyright © 2020 Elsevier Inc. All rights reserved.

Chemical References

• Biological Products
• NF-kappa B
• Apigenin
• Proto-Oncogene Proteins c-akt
• TOR Serine-Threonine Kinases

Topics

• Apigenin (metabolism, pharmacology)
• Biological Availability
• Biological Products (pharmacology)
• Humans
• NF-kappa B (metabolism)
• Neoplasms (drug therapy, metabolism)
• Phosphatidylinositol 3-Kinases (metabolism)
• Proto-Oncogene Proteins c-akt (metabolism)
• Signal Transduction (drug effects)
• TOR Serine-Threonine Kinases (metabolism)