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3'-Hydroxy-3,4'-dimethoxyflavone-induced Cell Death in Human Leukaemia Cells Is Dependent on Caspases and Reactive Oxygen Species and Attenuated by the Inhibition of JNK/SAPK

3'-Hydroxy-3,4'-dimethoxyflavone-induced Cell Death in Human Leukaemia Cells Is Dependent on Caspases and Reactive Oxygen Species and Attenuated by the Inhibition of JNK/SAPK

Francisco Estévez-Sarmiento, Elisa Hernández, Ignacio Brouard, Francisco León, Celina García, José Quintana, Francisco Estévez

Chem Biol Interact. 2018 May 25;288:1-11.

PMID: 29630880

Abstract:

Flavonoids are phenolic substances that appear to exert beneficial effects in several chronic diseases, including cancer. Structure-activity relationships of the cytotoxic activity of a series of flavonols and their 3-methyl ether derivatives established that 3'-hydroxy-3,4'-dimethoxyflavone (flavonoid 11) displayed strong cytotoxicity against human leukaemia cell lines (HL-60, U-937 and MOLT-3), and cells that over-express the anti-apoptotic proteins, Bcl-2 and Bcl-xL, and against P-glycoprotein-overexpressing K-562/ADR cells. This compound induced G2-M cell cycle arrest and it was a potent apoptotic inducer on HL-60, MOLT-3, U-937 and U-937/Bcl-2 cell lines. Cell death was (i) mediated by caspase activation, since it was prevented by the non-specific caspase inhibitor z-VAD-fmk and reduced by a selective caspase-9 inhibitor, (ii) associated with cytochrome c release, the dissipation of the inner mitochondrial membrane potential (ΔΨm) and the activation of the mitogen-activated protein kinase pathway and (iii) partially blocked by the inhibition of c-jun NH2 terminal kinases/stress activated protein kinases (JNK/SAPK) signalling and by the free-radical scavenger N-acetyl-l-cysteine.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP4143628	3′,4′-Dimethoxyflavone		4143-62-8	Price

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