Plant Flavone Apigenin: an Emerging Anticancer Agent

Abstract

Research in cancer chemoprevention provides convincing evidence that increased intake of vegetables and fruits may reduce the risk of several human malignancies. Phytochemicals present therein provide beneficial anti-inflammatory and antioxidant properties that serve to improve the cellular microenvironment. Compounds known as flavonoids categorized anthocyanidins, flavonols, flavanones, flavonols, flavones, and isoflavones have shown considerable promise as chemopreventive agents. Apigenin (4′, 5, 7-trihydroxyflavone), a major plant flavone, possessing antioxidant, anti-inflammatory, and anticancer properties affecting several molecular and cellular targets used to treat various human diseases. Epidemiologic and case-control studies have suggested apigenin reduces the risk of certain cancers. Studies demonstrate that apigenin retain potent therapeutic properties alone and/or increases the efficacy of several chemotherapeutic drugs in combination on a variety of human cancers. Apigenin’s anticancer effects could also be due to its differential effects in causing minimal toxicity to normal cells with delayed plasma clearance and slow decomposition in liver increasing the systemic bioavailability in pharmacokinetic studies. Here we discuss the anticancer role of apigenin highlighting its potential activity as a chemopreventive and therapeutic agent. We also highlight the current caveats that preclude apigenin for its use in the human trials.

Flavones Produced by Mulberry Flavone Synthase Type I Constitute a Defense Line against the Ultraviolet-B Stress

“…Other significant properties of certain flavones are their nutritional value and bioactivities in humans, including antioxidant and putative anticancer activity [1,13]. For example, apigenin, a major plant flavone, has antioxidant, anti-inflammatory, and anti-cancer properties, and has potential activity as a chemopreventive and therapeutic agent [14].…”

Modulation of the formation of active forms of nitrogen by ingredients of plant products in the inhibition of carcinogenesis

“…Растительный флавоноид, содержащийся в сельдерее, красном сладком перце, траве пустырника и др.,апигенин (4 1 ,5,7-триоксифлавон), антиоксидант, тормозил рост опухолей различных локализаций, включая легкие, предстательную, поджелудочную и щитовидную железы, толстую кишку, кожу; опухоли головы и шеи и др., действуя на многие критические белки и онкогенные сигнальные пути. На культуре андроген-нечувствительных опухолевых клеток предстательной железы апигенин инициировал апоптоз, ингибировал NF-κB и экспрессию генов, контролируемых NF-κB: Bcl-2, циклина D1, COX-2, iNOS и VEGF [78,79]. Апигенин способен усиливать цитотоксический эффект 5-фторурацила через ингибирование лекарственной резистентности и активацию апоптоза [79].…”

The beneficial and deleterious role of dietary polyphenols on chronic degenerative diseases by regulating gene expression

“…Apigenin (4',5,7-trihydroxyflavone), a major plant flavone, has shown anticancer properties reducing the risk of certain cancers alone and/or increasing the efficacy of several chemotherapeutic drugs. It could affect several molecular and cellular targets related to a variety of human cancers, in particular, inducing differential effects in causing minimal toxicity to normal cells (37). However, the underlying mechanisms are still unclear.…”