Apigenin (4’,5,7-trihydroxyflavone), found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally occurring glycosides. It is a yellow crystalline solid that has been used to dye wool.
In in vitro experiments and animal studies, a variety of potential biological activities of apigenin have been identified, but its effects on human health are unknown.
Apigenin induces autophagy (a kind of cellular waste-recycling system) in leukemia cells, which may support a possible chemopreventive role, but that induction of autophagy simultaneously induces resistance against the chemotherapy drug vincristine. Apigenin is a potent inhibitor of CYP2C9, an enzyme responsible for the metabolism of many pharmaceutical drugs in the body.
Apigenin has been shown to prevent renal damage caused by cyclosporin in rats, associated with reduced expression of the cell death mediator bcl-2 in histopathological sections. Cyclosporine A enhances the expression of transforming growth factor-β in the rat kidney, which signifies accelerated apoptosis. Therefore, transforming growth factor-β and apoptotic index may be used to assess apigenin and its effect on cyclosporine A-induced renal damage.
In vitro studies have shown that apigenin may be toxic to red blood cells.
Apigenin may also stimulate adult neurogenesis, with at least one study claiming that apigenin "stimulate[s] adult neurogenesis in vivo and in vitro, by promoting neuronal differentiation" and may be useful "for stimulating adult neurogenesis and for the treatment of neurological diseases, disorders and injuries, by stimulating the generation of neuronal cells in the adult brain." While potentially promising, the study used rats and its effects have yet to be demonstrated in humans.
^Chong FW, Srikumar Chakravarthi, HS Nagaraja, PM Thanikachalam, Nagarajah Lee (2009). "Expression of Transforming Growth factor-β and determination of Apoptotic Index in histopathological sections for assessment of the effects of Apigenin (4',5',7'- trihydroxyflavone) on Cyclosporine A induced renal damage". Malaysian Journal of Pathology31 (1): 35–43. PMID19694312.
^Zhao, G; Qin, GW; Wang, J; Chu, WJ; Guo, LH (2010). "Functional activation of monoamine transporters by luteolin and apigenin isolated from the fruit of Perilla frutescens (L.) Britt". Neurochemistry international56 (1): 168–76. doi:10.1016/j.neuint.2009.09.015. PMID19815045.
^Viola, H; Wasowski, C; Levi De Stein, M; Wolfman, C; Silveira, R; Dajas, F; Medina, JH; Paladini, AC (1995). "Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects". Planta medica61 (3): 213–6. doi:10.1055/s-2006-958058. PMID7617761.
^Campbell EL, Chebib M, Johnston GAR (2004): "The dietary flavonoids apigenin and (−)-epigallocatechin gallate enhance the positive modulation by diazepam of the activation by GABA of recombinant GABAA receptors", Biochemical Pharmacology, Vol. 68, 1631
^Jacobson KA et al. (2002): "Interactions of flavones and other phytochemicals with adenosine receptors.", Adv. Exp. Med. Biol., Vol. 505, 163
^Losi G et al. (2004): "Apigenin modulates GABAergic and glutamatergic transmission in cultured cortical neurons." Eur. J. Pharmacol., Vol. 502, 41
^Zbidah, M; Lupescu, A; Jilani, K; Fajol, A; Michael, D; Qadri, SM; Lang, F (2012). "Apigenin-induced suicidal erythrocyte death". Journal of agricultural and food chemistry60 (1): 533–8. doi:10.1021/jf204107f. PMID22132906.
^Taupin, P (2009). "Apigenin and related compounds stimulate adult neurogenesis. Mars, Inc., the Salk Institute for Biological Studies: WO2008147483". Expert opinion on therapeutic patents19 (4): 523–7. doi:10.1517/13543770902721279. PMID19441930.
^Meyer, Hellen; Bolarinwa, Adrian; Wolfram, Guenther; Linseisen, Jakob (2006). "Bioavailability of Apigenin from Apiin-Rich Parsley in Humans". Annals of Nutrition and Metabolism50 (3): 167–72. doi:10.1159/000090736. PMID16407641.