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Rationalizing the therapeutic potential of apigenin against cancer

Semim Akhtar Ahmed¹, Dey Parama², Enush Daimari¹

¹Cell and Molecular Biology Laboratory, Department of Zoology, Cotton University, Pan Bazar, Guwahati, Assam 781001, India.

|December 17, 2020

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.

Insights

Apigenin, a natural compound, shows promise in cancer prevention and treatment by targeting key molecular pathways. Further clinical studies are needed to explore its full therapeutic potential and safety.

Area of Science:

Natural product chemistry
Cancer biology
Pharmacology

Background:

Cancer remains a leading cause of mortality globally, with challenges in advanced stages including chemoresistance and high treatment costs.
Natural products, like apigenin, are increasingly recognized for their potential cancer-preventive and therapeutic properties.
Apigenin is a safe compound with demonstrated potential in cancer prevention and therapy.

Purpose of the Study:

To review the literature on apigenin and its analogs for their role in cancer prevention and treatment.
To assess the modulation of key molecular targets by apigenin in various cancers.

Main Methods:

Comprehensive literature search on PubMed.
Information gathered on sources, analogs, chemistry, biosynthesis, properties, biological activities, bioavailability, and toxicity of apigenin.

Main Results:

Apigenin and its analogs modulate crucial cancer signaling pathways (e.g., PI3K/AKT/mTOR, JAK/STAT, NF-κB, MAPK/ERK, Wnt/β-catenin).
Apigenin demonstrates effectiveness in vitro, in vivo, and in cohort studies.
The compound inhibits chemoresistance and radioresistance, enhancing sensitivity to cancer treatments.
Apigenin is safe, and nanotechnology can improve its bioavailability.

Conclusions:

Apigenin exhibits significant pharmacological activities against various cancers.
Its properties and efficacy warrant further investigation in clinical trials.
Apigenin represents a promising natural compound for cancer therapy.

Read full analysis

Keywords:

Apigenin Bioavailability Cancer Chemoresistance Molecular targets

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