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. 2016 Feb 16;8(2):90. doi: 10.3390/nu8020090

Table 2.

Anticancer activity of myricetin towards various cancer cell lines.

Cell line/Enzyme Effect of Myricetin Reference
Activity on Cell Lines
Brain
U251, NCH89 and LN229 cells No effect when alone, since the IC50 value for each cell line was found to be >200 µM. A combination of myricetin (150 µM) and TRAIL (50 ng/mL) yielded a synergistic activity and increased cell death in U251, NCH89 and LN229 by 59%, 65% and 52%, respectively. [78]
Breast
MCF-7 IC50 2.70 μg/mL compared to vinblastine (IC50 45.6 μg/mL) [79]
Increased GSH content of cells and also increased the EROD reaction 2-fold at a concentration of 25 μM [80]
Cervix
HeLa cells Cytotoxic with IC50 18.9 µg/mL [81]
Colon
Epithelial adenocarcinoma cells Proliferation of cells inhibited at 50 μM by decreasing COX-2 and cyclin D1 expression [82]
HCT116 Inhibited the proliferation of human colon carcinoma cells by halting the cell cycle in G2/M phase and inducing apoptosis; LD50 28.2 μM [83]
COLO 205, COLO 320HSR, COLO 320DM, HT 29 and COLO 205-X Inhibited the activation of MMP-2 enzyme in the cells with IC50 values of 7.82, 11.18, 11.56, 13.25 and 23.51 μM, respectively. It also suppressed TPA-induced MMP-2 protein expression in COLO 205 cells by blocking the translocation of PKCα from cytosol to membrane, phosphorylation of ERK1/2 protein and induction of c-Jun protein expression activated by TPA. [84]
Leukemia
HL-60 Alone, and in combination with piceatannol, induced apoptotic cell death through a ROS-independent cell death pathway. The effect was greater with the combined treatment [85]
Anti-proliferative activity and the effect was enhanced with increasing concentration [70]
Prostate
LNCaP IC50 value 2.10 μg/mL while taxol (IC50 0.08 μg/mL) used as standard [79]
22Rv1 Inhibition of TCDD-induced EROD activity in cancer cells; IC50 value 3.0 μM [86]
Uterus
RL95-2 endometrial cancer cells Inhibition of CYP1 activity of cancer cells; IC50 values 3 μM and lower [87]
Inhibition of enzyme/protein activity
Thioredoxin reductase (TrxR) from mammals Inhibitory effect on enzyme, which is overexpressed in many aggressive tumours; IC50 value 0.62 μM. Attacks the reduced COOH-terminal of -Cys-Sec-Gly, the active site of TrxR [88]
TrxR At 50 μM, inhibited growth of A549 (human lung carcinoma) cells and reduced TrxR activity in the cell lysates, corresponding with the oxidization of thioredoxin [88]
Mammalian DNA polymerases IC50 values ranged from 21.3 to 40.9 μM. Human DNA topoisomerase II activity inhibited; IC50 27.5 μM [83]
Phosphatidylinositol 3-kinase (PI3K) Inhibited this enzyme (IC50 1.8 μM) that plays an important role in signal transduction and cell transformation. Also inhibited PKC and tyrosine kinase activity of EGF-R [89,90]
E6, a primary oncoprotein of human papillomaviruses Inhibited E6, responsible for cervical cancer by inhibiting GST-E6 and His-caspase 8 binding [91]
CCAAT-enhancer-binding proteins-α, peroxisome proliferator-activated receptor-γ, lipoprotein lipase, fatty acid binding aP2 protein and adiponectin At 30 μM, myricetin decreased mRNA levels of these enzymes. Inhibited adipogenesis in human adipose tissue-derived mesenchymal stem cells. [92]
Multidrug resistance-associated protein MRP1 and MRP2 mediated vincristine efflux in MDCKII cells Inhibitory effects with IC50 30.5 and 24.6 μM, respectively. At a concentration of 25 μM, it increased the sensitivity of the cells towards vincristine toxicity towards MRP1 and MRP2 cells with IC50 values of 7.6 and 5.8 μM, respectively [93]