Table 1.
Anti-cancer effects and mechanisms investigated with luteolin.
| Target | Effect of luteolin | Publication source(s) |
|---|---|---|
| Tumor cell proliferation | Inhibits proliferation of various tumor cell lines in vitro | [12,13,14,15,16,17,18,19,20,21,22,23,25,27,28,30,31,32,34,35] |
| Cell cycle arrest | Induces cell cycle arrest in G2/M, S, or G0/1 phase | [19,22,23,24,25,26] |
| Angiogenesis | Inhibits bFGF and VEGF induced in vitro angiogenesis of BBE cells | [12] |
| Tumor growth in vivo | Inhibits growth of tumors from different organs when applied p.o. or i.p. | [21,33,34,35,36,37,38,40,50,68] |
| Anti-oxidant enzymes and compounds | Increases levels of SOD, CAT, GPx, Vit A, Vit C, ß-Carotene | [29,49,50,51] |
| NAT | Inhibits N-acetyltransferase in cancer cell lines | [54,56,57] |
| MMP | Inhibits secretion of MMP-2 and MMP-9 release | [20] |
| IGF / IFR | Inhibits tyrosin phosphorylation of IGFR | [36] |
| EGF / EGFR | Inhibits EGF or IGF-1 induced activation of EGFR | [20,36,66] |
| HGF / c-Met | Inhibits phosphorylation of hepatocyte growth factor receptor c-Met | [58] |
| AR | Downregulates androgen receptor | [35] |
| PI-3-Kinase / Akt | Inhibits Akt phosphorylation | [36,65,66,67] |
| PI-3-Kinase / Akt | Suppresses Akt expression | [21] |
| Mitochondria | Reduces mitochondrial membrane potential | [21,70] |
| Cytochrome C | Induces cytochrome C release into cytosol | [21,70,71] |
| Bcl-2 family | Increases Bax, Bad, Bax / Bcl2 ratio; decreases Bcl2, increases Bax / Bak translocation | [21,23,25,34,70] |
| AI-P | Induces expression of apoptose-inducing factor | [26] |
| Caspase 9 | Activates caspase 9 | [21,23,70,72,73] |
| Caspase 3 / 6 / 7 | Activates caspase 3 | [21,23,25,26,70,73] |
| Caspase 8 / 10 | Activates Caspase 8 / 10 via death receptors | [68,72] |
| PARP | Cleaves poly (ADP-ribose) polymerase | [21,26,70] |
| DFF-45 | Activates DNA fragmentation factor | [70] |
| Topoisomerase | Inhibits topoisomerase I and II | [60,61,64] |
| MAPK / ERK | Inhibits IGF induced activation of signaling; suppresses ERK expression | [21,36] |
| JNK / p38 | Activates JNK | [68,71] |
| p21 | Increases expression of p21 in p53 knockout cells | [36] |
| p21 | low doses induce, high doses suppress p21 expression | [23,33] |
| p53 | Stabilizes p53 via JNK activation; Accumulates p53 |
[68] [24] |
| Cyclin | Inhibits expression of cyclin D1 induced by IGFR or pSTAT3 | [34,36] |
| survivin | Downregulates survivin | [23,34] |
| PCNA | Reduces expression of proliferating cell nuclear antigen | [21] |
| Fas/CD95 | Increases Fas/CD95 expression | [34] |
| TRAIL | Sensitizes TRAIL-induced apoptosis | [68] |
| XIAP | Reduces X-linked inhibitor of apoptosis protein | [74] |
| FASN | Inhibits fatty acid synthesis in cancer cells | [75] |