Apigenin in cancer therapy: anti-cancer effects and mechanisms of action

Abstract

Apigenin is a common dietary flavonoid that is abundantly present in many fruits, vegetables and Chinese medicinal herbs and serves multiple physiological functions, such as strong anti-inflammatory, antioxidant, antibacterial and antiviral activities and blood pressure reduction. Therefore, apigenin has been used as a traditional medicine for centuries. Recently, apigenin has been widely investigated for its anti-cancer activities and low toxicity. Apigenin was reported to suppress various human cancers in vitro and in vivo by multiple biological effects, such as triggering cell apoptosis and autophagy, inducing cell cycle arrest, suppressing cell migration and invasion, and stimulating an immune response. In this review, we focus on the most recent advances in the anti-cancer effects of apigenin and their underlying mechanisms, and we summarize the signaling pathways modulated by apigenin, including the PI3K/AKT, MAPK/ERK, JAK/STAT, NF-κB and Wnt/β-catenin pathways. We also discuss combinatorial strategies to enhance the anti-cancer effect of apigenin on various cancers and its use as an adjuvant chemotherapeutic agent to overcome cancer drug resistance or to alleviate other adverse effects of chemotherapy. The functions of apigenin against cancer stem cells are also summarized and discussed. These data demonstrate that apigenin is a promising reagent for cancer therapy. Apigenin appears to have the potential to be developed either as a dietary supplement or as an adjuvant chemotherapeutic agent for cancer therapy.

Therapeutic Potential of Flavonoids in Pain and Inflammation: Mechanisms of Action, Pre-Clinical and Clinical Data, and Pharmaceutical Development

“…Apigenin (4 ,5,6-trihydroxyflavone) is abundantly present in vegetables, fruits, and medicinal herbs, including parsley, apples, grape, and Matricaria chamomilla [99,100]. It was demonstrated that this flavone possesses anti-inflammatory effects by blocking NF-κB activation in a model of LPS-induced apoptosis.…”

A review of molecular mechanisms involved in anticancer and antiangiogenic effects of natural polyphenolic compounds

“…Apigenin (5,7,4′‐trihydroxyflavone) is one of the most common dietary flavonoids, which is widely found in many fruits and vegetables such as parsley, grapes, and apples (X. Yan, Qi, Li, Zhan, & Shao, ). This flavone has been reported to possess antitumor activity against many types of cancers, including colorectal cancer, breast cancer, liver cancer, lung cancer, prostate cancer, melanoma, and osteosarcoma (Madunić, Madunić, Gajski, Popić, & Garaj‐Vrhovac, ; X. Yan et al, ). Apigenin has been shown to have modest antitumor effects on animal models (Q. R. Wang et al, ).…”

CDK4 as a phytochemical based anticancer drug target

“…), mangiferin (Núñez Selles, Daglia, and Rastrelli 2016), voacangine (Y. Kim, Jung, and Kwon 2012), quinic acid (Singh, Chauhan, and Tripathi 2018), andrographolide (Peng et al 2018), luteolin (Cook 2018), apigenin (Yan et al 2017), rutin (Khan et al 2019), and gallic acid (Liu et al 2012) are already reported for their anticancer activities. This suggests that the screening process from the traditionally used medicinal plants contain both potential anticancer properties.…”