5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. The treatment with 5-methoxyflavone (5-MF） at various times (3, 6, 12, 18 and 24 h) in MOLT-4 cells results in a time dependent reduction in the levels of antiapoptotic proteins cFLIP, Mcl-1 and an increase in the proapoptotic protein BAX. 5-MF induces both TRAIL-R1(DR4) and TRAIL-R2 (DR5) in a time-dependent manner.
|Cell lines||human leukemic MOLT-4, U937 cell lines and PBMCs|
|Preparation method||MOLT-4 or U937 or PBMC cells are treated with DMF or TMF or PMF, 5-MF or 2'-MF at various concentrations for 24 h, then the cell viability is determined by the MTT assay.|
|Incubation time||24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity.
Merlo S, et al. J Nat Prod. 2015 Nov 25;78(11):2704-11. PMID: 26517378.
Methoxyflavone derivatives modulate the effect of TRAIL-induced apoptosis in human leukemic cell lines.
Wudtiwai B, et al. J Hematol Oncol. 2011 Dec 21;4:52. PMID: 22185222.
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