Table 7.
Antitumoral effects of quercetin in colorectal cancer.
| QUERCETIN | ||||
|---|---|---|---|---|
| Experimental Models |
Concentration Range | Biological Response | Pathway/Genes/Proteins Involved |
Refs. |
| Cells and cell lines | ||||
| HT-29 | 25, 50, 100 µM | Apoptosis | ↓ Bcl-2, ↑ cleaved caspase-3, ↑ cleaved PARP, ↓ p-Akt, ↓ ErbB2/ErbB3 proteins | [117] |
| 5–30 µg/mL (with resveratrol, 1:1 ratio) |
↓ Oncogenic µmicroRNA-27a |
↓ Sp1, ↓ Sp3, ↓ Sp4, ↓ survivin mRNA and proteins |
[118] | |
| 50, 100, 200 µM | Apoptosis S-phase arrest |
↓ p-Akt, ↓ CSN6, ↓ Myc, ↓ Bcl-2, ↑ p53, ↑ Bax proteins | [119] | |
| 50 μM (with cisplatin: 10 mg/L) | ↑ Cisplatin-induced Apoptosis | ↓ Activation of NF-κB protein expression | [120] | |
| 30 µM | ↑ TRAIL-induced Apoptosis | Redistribution of death receptors DR4 and DR5 into lipid rafts ↑ cleaved caspase-3 and ↑ cleaved Bid proteins,↑ release Cyt-C |
[121] | |
| 50, 100 μM | Apoptosis G1-phase arrest |
↑ AMPK, ↑ p53, ↑ p21 proteins | [122] | |
| 50 µM (with dox: 250 nM) |
↑ Doxorubicin-induced cytotoxicity | ↓ Proliferation, ↑ apoptosis, and G2/M arrest for lower IC50 of Dox | [123] | |
| Caco-2 | 5–50 µM | ↓ Cell proliferation | ↓ CDC6, ↓ CDK4, ↓ cyclin D1 mRNA | [124] |
| 5–20 μM | Anti-migration Anti-invasion |
↓ MMP-2, ↓ MMP-9, ↓ TLR4, ↓ NF-κB, ↑ E-cadherin proteins ↓ TNF-α, ↓ COX-2, ↓ IL-6 production |
[125] | |
| Caco-2 and SW-620 |
25–100 µM | Apoptosis | ↑ IκB-α, ↓ p-IκB-α, ↓ Bcl-2, ↑ Bax proteins |
[126] |
| SW480 | 20–80 µM | Apoptosis | ↓ Cyclin D1, ↓ survivin mRNA, and proteins | [127] |
| 10 µM | Apoptosis S-phase arrest |
↓ EGF receptor phosphorylation | [128] | |
| Colo-320 and Colo-741 |
25 μg/mL | Apoptosis Senescence | ↑ p16, ↑ Lamin B1, ↑ cyclin B1, ↑ Bax, ↓ Bcl-2 proteins | [129] |
| CT26 and MC38 |
1–10 µM | Anti-metastasis | ↑ E-cadherin, ↓ N-cadherin, ↓ β-catenin, ↓ snail proteins ↓ MMP-2, ↓ MMP-9 activities |
[130] |
| DLD-1 | 10.5 µM | Anticarcinogenesis | ↓ COX-2 transcription | [131] |
| CO115 and HCT15 |
12 µM (with 5-FU: 1 µM) |
↑ Fluorouracil-induced apoptosis | ↑ p53, ↑ cleaved caspase-9, ↑ cleaved caspase-3, ↑ cleaved PARP, ↓ Bcl-2 proteins |
[132] |
| HCT8-β8 | 50 µM | ↓ Cell proliferation | ↑ ERβ mRNA, ↑ ER-responsive luciferase activity | [133] |
| Animal models | ||||
| HT-29 xenograft in Balb/C nude mice | 10 mg/kg/day (SC; 4 weeks) |
↑ Radiosensitivity | ↓ Jagged-1, ↓ Notch-1, ↓ Hes-1, ↓ Presenilin 1, ↓ Nicastrin proteins |
[134] |