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4'-O-methyl Quercetin is a flavonoid isolated from C. ordata with anticancer and antiplasmodial activity.1,2,3 4'-O-methyl Quercetin is a major metabolite of quercetin (Item No.10005169) that inhibits the viability of HL-60, U937, MOLT-3, Raji, K562, MCF-7, SK-MEL-1, and A549 human tumor cell lines with IC50 values ranging from 5.5-24.1 μM.1 It induces G2-M arrest and inhibits tubulin polymerization in vitro in a dose-dependent manner. 4'-O-methyl Quercetin inhibits breast cancer resistance protein (BCRP/ABCG2; IC50 = 40 nM in a vesicular transport assay) with no cellular toxicity indicating potential for use in overcoming multidrug resistance in chemotherapy.2 4'-O-methyl Quercetin also reduces in vitro proliferation of chloroquine-resistant P. falciparum (IC50 = 4.8 μM) and suppresses infection in mice (65-81% suppression at 2.5-5 mg/kg dose).3
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1. Induction of G2/M phase arrest and apoptosis by the flavonoid tamarixetin on human leukemia cells. mol. Carcinog. 53(12), 939-950 (2014).
2. Identification of novel dietary phytochemicals inhibiting the efflux transporter breast cancer resistance protein (BCRP/ABCG2). Food Chem. 138(4), 2267-2274 (2013).
3. Antiplasmodial activity-