Apoptotic effects of chrysin in human cancer cell lines

Abstract

Chrysin is a natural flavonoid currently under investigation due to its important biological anti-cancer properties. In most of the cancer cells tested, chrysin has shown to inhibit proliferation and induce apoptosis, and is more potent than other tested flavonoids in leukemia cells, where chrysin is likely to act via activation of caspases and inactivation of Akt signaling in the cells. Moreover, structure-activity relationships have revealed that the chemical structure of chrysin meets the key structural requirements of flavonoids for potent cytotoxicity in leukemia cells. It is possible that combination therapy or modified chrysin could be more potent than single-agent use or administration of unmodified chrysin. This study may help to develop ways of improving the effectiveness of chrysin in the treatment of leukemia and other human cancers in vitro.

Keywords: apoptotic effect; chrysin; human cancers; in vitro.

Figure 1.

(A) Common chemical structure of flavones. Flavones have a common chemical structure consisting of fused A and C rings, and a phenyl B ring attached to position 2 of the C ring. (B) Chrysin is in the flavone subgroup of flavonoids and shares a common flavone structure with hydroxyls at position 5 and 7 of the A ring. Replacing the hydroxyl with a phosphate group at position 7, such as in diethyl chrysin-7-yl phosphate (CPE). (C) or at positions 5 and 7, such as in tetraethyl bis-phosphoric ester of chrysin (CP). (D), enhances the anti-cancer potential of the chrysin.

Figure 2.

The PI3K/Akt signaling pathway. Chrysin is likely to act via activation of caspases and inactivation of Akt signaling in leukemia cells. (•) depicts chrysin.