Apigenin

Catalogue number C107957
Chemical nameApigenin
CAS Number520-36-5
Synonyms5,7-dihydroxy-2-(4-hydroxyphenyl)-1-benzopyran-4-one
Molecular WeightC15H10O5
Formula270.2
Purity98%
Physical DescriptionYellow powder
SolventChloroform, Dichloromethane,DMSO
StorageStored at 2-8°C, Protected from air and light, refrigerate or freeze
Applications

Apigenin was recently shown that apigenin induces a process called autophagia (a kind of cellular dormancy) that may well explain its chemopreventive properties, but at the same time it induces resistance against chemotherapy. 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 reverse the adverse effects of cyclosporin. Research has been conducted to study the effects of apigenin on reversal of cyclosporin-induced damage, and this was assessed by immunohistochemical estimation of expression of bcl-2, and estimation of apoptosis 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 and even evaluate apigenin as anti-cancer agent.


Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.


Zbidah and colleagues have shown that apigenin may be toxic to red blood cells in vitro.
Apigenin may also stimulate adult neurogenesis, with at least one study claiming that apigenin "stimulate 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.
Apigenin has significant chemopreventive activity against UV-radiation. It may reduce DNA oxidative damage; inhibit the growth of human leukemia cells and induced these cells to differentiate; inhibit cancer cell signal transduction and induce apoptosis; act as an anti-inflammatory; and as an anti-spasmodic or spasmolytic.

References1. Magnetic Resonance in Chemistry, 1986, 24(10), 879-882.
2. J. Org. Chem., 1991, 56(16), 4884-4887.
3. Journal of Pharmaceutical Sciences, 1997, 86(6), 721-725.
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Apigenin
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