Table 2.
Molecular targets of flavones in obesity and cancer.
| Target | Flavone | Dose | Activity | Model System | Ref. |
|---|---|---|---|---|---|
| 10, 30, 50 mg/kg/day i.p. | Systemic TNFα, IL-6, IL-1β, IL-12 ↓ * |
C57Bl/6j male mice fed with HFD | [194] | ||
| 25 mg/kg/day i.p. | TNFα, IL-6, IFNγ, MCP-1 ↓ | Pancreatic cancer in C57Bl/6j mice | [195] | ||
| Apigenin | 300 mg/kg/day i.p. | Nuclear NF-κB ↓ | Human hepatocellular carcinoma xenografts in Balb/c nu/nu mice | [196] | |
| 20 and 50 μg/mouse/day p.o. | Phospho-IκBα, IKKα, NF-κB p65 and p50, COX-2 ↓ | Prostate cancer in C57Bl/6j mice | [197] | ||
| 40 μM | IKBKε, IL-1α, IL-6, MCP-1, GM-CSF ↓ |
Human MDA-MB-231 breast cancer cells |
[198] | ||
| Acacetin | 3–100 μM | Phospho-IκB, nuclear p65, COX-2, TNFα, IL-6, MCP-1 ↓ | Murine RAW264.7 macrophages cultured with 3T3-L1 adipocytes | [199] | |
| Baicalin | 50 mg/kg/day i.p. | TNFα, MCP-1 mRNA ↓ | WAT from HFD-fed C57Bl/6j male mice | [200] | |
| Baicalein | 200, 400 mg/kg/day p.o. | NF-κB ↓ | Murine melanoma B16-F10 xenografts in C57Bl/6j mice |
[201] | |
| NF-κB | Chrysin | 25, 30 mg/kg/day i.p. | Systemic TNFα, IL-1β ↓ | C57Bl/6j male mice fed with HFD | [202] |
| Luteolin | 0.005% w/w in HFD chow | Systemic TNFα, IL-1β, IL-6, MIP-1β ↓ |
C57Bl/6j male mice fed with HFD | [203] | |
| 0.005% w/w in HFD chow | TNFα, IL-6, MCP-1 ↓ | WAT from OVXed C57Bl/6j female mice fed with HFD * | [180] | ||
| Nobiletin | 10–100 μM | TNFα, MCP-1 ↓ | Murine RAW264.7 macrophages cultured with 3T3-L1 adipocytes | [204] | |
| Tangeretin | 20 mg/kg/day p.o. | TNFα, IL-6, IL-1β, MCP-1 ↓ | WAT from HFD-fed C57Bl/6j male mice |
[205] | |
| 20, 40 μM | TNFα, IL-6, IL-1β, MCP-1 ↓ | Murine bone marrow-derived macrophages cultured with adipocytes |
[205] | ||
| Vitexin | 30, 60 mg/kg/day p.o. | Phospho-IκB, NF-κB p65, TNFα, IL-6, IL-1β ↓ | C57Bl/6j male mice fed with HFD |
[47] | |
| 40, 160 mg/kg/day p.o. | Phospho-IκBα, nuclear p65, TNFα ↑ | M1 macrophages from colon cancers in Balb/c mice |
[206] | ||
| STAT | Apigenin | 5–60 μM | Phospho-STAT1, IFNγ- induced PD-L1 expression ↓ |
Human melanoma A375, A2058, RPMI-7951 cell lines |
[207] |
| 10–50 μM | Phospho-STAT1 and STAT3, PD-L1 expression ↓ | Human NSCLC H460, H538, A549 cell lines |
[208] | ||
| Luteolin | 50–100 μM | Phospho-JAK1 and STAT1, IL-8 ↓ |
Human colon cancer HT-29 cells | [209] | |
| 0.3–10 μM | IL-6-induced STAT3 phosphorylation ↓ |
Human cholangiosarcoma KKU-M156 cells |
[210] | ||
| Nrf2 | Apigenin | 1.56–6.25 μM | ARE-luciferase reporter, Nrf2-dependent gene HO-1 ↑ |
Human hepatocellular carcinoma HepG2 cells |
[211] |
| Nobiletin | 10–100 μM | Nrf2-dependent gene HO-1 ↑ |
Murine RAW264.7 macrophages cultured with 3T3-L1 adipocytes | [204] | |
| Scutellarin | 25, 50, 100 mg/kg/day p.o. | Nrf2 ↑ GSK, IL-1β, IL-2 ↓ |
Db/db diabetic mice | [212] | |
| Tangeretin | 20–60 μM | Nrf2 ↓ Overcomes drug resistance |
Human lung cancer A549/T cells | [213] | |
| Wogonin | 20–60 μM | Nrf2 ↓ Overcomes drug resistance |
Human breast cancer MCF7 cells | [214] | |
| NLRP3 | 0.005% w/w in HFD chow | NLRP3, caspase-1, IL-1β ↓ | WAT from OVXed C57Bl/6j female mice fed with HFD * |
[215] | |
| Luteolin | 50–150 μM | NLRP3, caspase-1, IL-1β ↑ | Human colon cancer HT-29 cells | [216] | |
| 50 mg/kg/day i.p. | NLRP3, caspase-1, IL-1β ↑ | Human colon cancer cells xenografts in Balb/c nude mice |
[216] |
↓—decrease, ↑—increase, * OVXed—ovariectomized.