Pharmacokinetic properties and drug interactions of apigenin, a natural flavone

ABSTRACT

Introduction: Apigenin, a natural flavone, is widely distributed in plants such as celery, parsley and chamomile. It is present principally as glycosylated in nature. Higher intake of apigenin could reduce the risk of chronic diseases. It has gained particular interest in recent years as a beneficial, health-promoting agent with low intrinsic toxicity.

Areas covered: This review summarizes and the absorption, distribution, metabolism and excretion (ADME) properties of apigenin, and drug-drug interaction of apigenin.

Expert opinion: Since apigenin is a bioactive plant flavone and is widely distributed in common food, its consumption through the diet is recommended. Apigenin-enriched drugs are better for some chronic diseases, but may affect animal and human health if present in the daily diet. Dietary or therapeutic apigenin has value as a good cellular regulator in cancer, especially cancers of the gastrointestinal tract. Due to apigenin’s limitations on absorption and bioavailability, novel carriers would need to be developed to enhance the oral bioavailability of apigenin. Further research about its ADME properties and drug-drug interactions are needed before apigenin can be brought to clinical trials.

KEYWORDS:

• Apigenin
• pharmacokinetic
• ADME
• interaction

Article highlights

• Apigenin is present in food as glycosides, glycosides are absorbed and distributed as aglycone.

• Oral bioavailability of apigenin is poor, the ingested apigenin was either excreted unabsorbed or was rapidly metabolized after absorption.

• The absorbed apigenin in blood circulation and tissues is in the form of glucuronide, sulfate conjugates or luteolin.

• An accumulation in tissues seems possible, due to its slow elimination.

• Apigenin possesses the ability to inhibit P-gp and CYP3A4, and thus it may be involved drug-drug interactions.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Additional information

Funding

This work was supported by the Natural Science Foundation project [30470193], the Scientific Research Foundation Project of the Education Department of Hubei Province [Q20142007], and the Young Plan Project of Hubei University of Chinese Medicine [XJ2014KJ008].