4''-O-methyl Quercetin is a flavonoid isolated from
C. ordata with anticancer and antiplasmodial activity. 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 IC
50 values ranging from 5.5-24.1 μM.
1 It induces G
2-M arrest and inhibits tubulin polymerization
in vitro in a dose-dependent manner. 4''-O-methyl Quercetin inhibits breast cancer resistance protein (BCRP/ABCG2; IC
50 = 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 (IC
50 = 4.8 μM) and suppresses infection in mice (65-81% suppression at 2.5-5 mg/kg dose).
3