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3',?4',?5',?5,?7-?Pentamethoxyflavone

CAS No.: 53350-26-8

3',4',5',5,7-Pentamethoxyflavone is a naturally occurring brassinosteroid compound from the Rutaceae family that exhibit
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Description 3',4',5',5,7-Pentamethoxyflavone is a naturally occurring brassinosteroid compound from the Rutaceae family that exhibits resistance to cancer cells by inhibiting the Nrf2 pathway to overcome chemotherapeutically active molecules.
In vitro 3',4',5',5,7-Pentamethoxyflavone (PMF), a natural flavonoid extracted from Rutaceae plants, sensitized A549/CDDP to CDDP and substantially induced apoptosis compared with that of CDDP alone treated group, and this reversal effect decreased when Nrf2 was downregulated by siRNA. Mechanistically, PMF reduced Nrf2 expression leading to a reduction of Nrf2 downstream genes, and in contrast, this effect was decreased by blocking Nrf2 with siRNA. Taken together, these results demonstrated that PMF could be used as an effective adjuvant sensitizer to increase the efficacy of chemotherapeutic drugs by downregulating Nrf2 signaling pathway.[1]
In vivo The flavones tricin (4',5,7-trihydroxy-3',5'-dimethoxyflavone) and 3',4',5',5,7-Pentamethoxyflavone (PMF) are under development as potential colorectal cancer chemopreventive agents as they reduced adenoma development in the Apc(Min) mouse model of intestinal carcinogenesis. Plasma concentrations and area under the plasma concentration versus time curve for PMF were higher than those for tricin. A mono-O-desmethyl PMF and several isomeric mono-O-desmethyl PMF glucuronides and sulfonates were major PMF metabolites in murine plasma, liver and intestinal tissue. In murine and human liver fractions, in vitro metabolic removal of tricin was faster than that of PMF[1].
Synonyms 5,7,3',4',5'-Pentamethoxyflavone
molecular weight 372.37
Molecular formula C20H20O7
CAS 53350-26-8
Storage store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 22.5 mg/mL (60.4 mM), Sonication is recommended.
References 1. Hou X, et al. 3',4',5',5,7-pentamethoxyflavone sensitizes Cisplatin-resistant A549 cells to Cisplatin by inhibition of Nrf2 pathway. Mol Cells. 2015;38(5):396-401. 2. Cai H, et al. Pharmacokinetics in mice and metabolism in murine and human liver fractions of the putative cancer chemopreventive agents 3',4',5',5,7-pentamethoxyflavone and tricin (4',5,7-trihydroxy-3',5'-dimethoxyflavone). Cancer Chemother Pharmacol. 2011;67(2):255-263. 3. Cai H, et al. Determination of 3',4',5',5,7-pentamethoxyflavone in the plasma and intestinal mucosa of mice by HPLC with UV detection. Biomed Chromatogr. 2009;23(4):335-339.