Pharmacokinetic properties and drug interactions of apigenin, a natural flavone

Abstract

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.

Absorption Profile of (Poly)Phenolic Compounds after Consumption of Three Food Supplements Containing 36 Different Fruits, Vegetables, and Berries

“…The T max of apigenin (measured as aglycone after enzymatic hydrolysis) has been reported to be around 7 h after consumption of parsley [45]. The few human feeding studies involving flavones available so far reported a low bioavailability for this phytochemical [18,46], which could be ascribable to the low absorption of flavones, as demonstrated in the present investigation. Conversely, several scientific data are available for naringenin and hesperetin absorption, and all studies agree about the importance of colonic microbiota activity on this class of (poly)phenols [47,48,49].…”

Phenolic Compounds Exerting Lipid-Regulatory, Anti-Inflammatory and Epigenetic Effects as Complementary Treatments in Cardiovascular Diseases

“…Oral bioavailability of apigenin is relatively low due to its poor solubility and because the main part of the ingested apigenin is either excreted unabsorbed or is rapidly metabolized after absorption. In vivo, after ingestion, apigenin is subjected to sulfation and glucuronidation, the absorbed apigenin being present in tissues (mainly hepatic and small intestin) as glucuronide, sulfate conjugates or luteolin [182].…”

Improvement of Antioxidative Activity of Apigenin by B12N12 Nanocluster: Antioxidative Mechanism Analysis

“…Apigenin (APG) with three hydroxyl groups in positions 5, 7 and 4 ′ (Figure ) is mainly found in dried flowers of chamomile, parsley, celery, thyme, oregano, olives, onions, kumquats, cherries, oranges, broccoli, tomatoes, barley, carrots, and legumes . In recent years, a lot of research showed that APG have different pharmacological activities, such as anti‐oxidant, anti‐inflammatory, anti‐depressant, anti‐mutagenic, anti‐cancer, anti‐viral, anti‐bacterial, anti‐thrombotic, cardioprotective, hepatoprotective, and immunostimulant effects . The antioxidant activity of APG was previously reported using DFT method .…”