From: Apigenin in cancer therapy: anti-cancer effects and mechanisms of action
Tumor type | Cell lines (concentration) | Mice (dosages) | Therapeutic effects | Mechanisms | Citations |
---|---|---|---|---|---|
Colorectal cancer | SW480 (40 μM) |  | Inhibited proliferation, invasion and migration | Inhibited Wnt/β-catenin signaling | [11] |
HCT116 (25 μM) |  | Inhibited proliferation; autophagy; apoptosis | Suppressed the expression of cyclin B1, Cdc2 and Cdc25c; induced PARP cleavage; induced LC3-II | [28] | |
DLD1 and SW480 (40 μM) | 20 mg/kg (athymic nude mice, intraperitoneally) | Inhibited proliferation, invasion and migration | Attenuated NEDD9; reduced phosphorylations of FAK, Src, and Akt | [48] | |
SW480, DLD-1, and LS174T (40 μM) | 50 mg/kg (BALB/c-nude mice, orthotopically implanted) | Inhibited proliferation, invasion and migration | Up-regulated TAGLN; down-regulated MMP-9 expression; decreasing phosphorylation of Akt | [50] | |
Breast cancer | BT-474 (40 μM) |  | Inhibited cell proliferation; apoptosis | Reduced the p-JAK1, p-JAK2 and p-STAT3; up-regulated the levels of cleaved caspase-8, cleaved caspase-3 and the cleavage of PARP | [25] |
MDA-MD-231 (40 μM) | 5, 25 mg/kg (BALB/c-nude mice, orthotopically injected) | Cell cycle arrest | Suppressed cyclin A, cyclin B, and CDK1; upregulated p21WAF1/CIP1; inhibited HDAC activity; induced histone H3 acetylation | [29] | |
MDA-MB-231 and T47D (40 μM) |  | Inhibited cell proliferation; apoptosis | Increased levels of caspase3, PARP cleavage and Bax/Bcl-2 ratios | [41] | |
MDA-MB-468 and 4T1 (30 μM) |  | Enhanced the immune responses | Inhibited IFN-γ-induced PD-L1 expression; inhibited STAT1 | [58] | |
SKBR3 (40 μM) |  | Apoptosis | Reduced the expression of p-JAK2 and p-STAT3; inhibited VEGF | [98] | |
MDA-MB-453 (60 μM) |  | Inhibited cell proliferation; apoptosis | Up-regulated caspase-8, caspase-3 and the cleavage of PARP; inactivation of JAK2 and STAT3 | [99] | |
Lung cancer | H1299 and H460 (20 μM) |  | Inhibited cell proliferation; apoptosis | Suppressed GLUT1 | [13] |
A549 (40 μM) |  | Inhibited cell proliferation, migration, invasion | Decreased the PI3K/Akt signaling pathway | [47] | |
Prostate cancer | LNCaP (20 μM) |  | Inhibited cell proliferation; apoptosis | Decreased cyclin D1, D2 and E; upregulated WAF1/p21 | [15] |
PC-3 and DU145 (20 μM) | 20, 50 μg/mouse/day (athymic nude mice, oral gavage) | Cell cycle arret; apoptosis | Suppression of XIAP, c-IAP1, c-IAP2 and survivin; decreased Bcl-xL and Bcl-2 and increase in Bax protein | [22] | |
DU145 (20 μM) |  | Inhibited migration and invasion; cell cycle arrest | Increased E-cadherin; decreased snail and vimentin | [46] | |
 | 20 and 50 μg/mouse/day (TRAMP mice, oral gavage) | Inhibited tumorigenesis | Inhibited IKK activation and restored the expression of IκBα | [89] | |
PC-3 and 22Rv1 (20 μM) | 20 and 50 μg/mouse/day (athymic nude mice, oral gavage) | Inhibited cell proliferation, invasivion | Inactivation of IKKα; suppressed NF-ĸB/p65 activation | [90] | |
PC3-M and LNCaP C4-2B (25 μM) |  | Inhibited cell proliferation and metastases | Inhibited the Smad2/3 and Src/FAK/ Akt pathways | [110] | |
PC3 (25 μM) |  | Apoptosis; cell cycle arrest; suppressed stem cell migration | Increased p21 and p27; upregulated caspases-8, -3 and TNF-α; downregulation of PI3K/Akt and NF-κB signaling | [65] | |
Melanoma | A375, C8161 (40 μM) |  | Inhibited proliferation and invasion; apoptosis; cell cycle arrest | Activation of cleaved caspase-3 and cleaved PARP; decreased ERK1/2 proteins, p-AKT and p-mTOR | [14] |
A2058, A375 (20 μM) |  | Inhibited metastasis | Inhibited the phosphorylation of FAK/ERK1/2 | [82] | |
A375, G361 (20 μM) |  150 mg/kg (C57BL/6 mice, oral gavage) | Inhibited metastasis | Suppressed STAT3 phosphorylation; down-regulated MMP-2, MMP-9, VEGF and Twist1 | [97] | |
Leukemia | HL60 (60 μM) |  | Apoptosis | Activation of caspase-9 and caspase-3 | [23] |
HL60 (50 μM); TF1 (30 μM) |  | Cell cycle arrest | Inhibited JAK/STAT pathway | [37] | |
U937 (40 μM) | 20, 40 mg/kg (athymic nude mice, intraperitoneally) | Apoptosis | Inactivation of Akt; activation of JNK; downregulated Mcl-1 and Bcl-2 | [112] | |
Ovarian cancer | A2780 (20, 40 μM) | 5 mg/kg (BALB/c nude mice, intraperitoneally) | Inhibited adhesion, migration and invasion | Inhibited FAK expression | [49] |
SKOV3 (20, 40 μM) |  | Inhibited the self-renewal capacity | Downregulated Gli1; inhibition of CK2α | [66] | |
Glioblastoma | GL-15 (50 μM) |  | Inhibited angiogenic | Reduced TGF-b1 production | [111] |
U87MG and U373MG (25 μM) |  | Inhibited self-renewal capacity | Blocked the activation of c-Met signaling | [64] | |
Renal cell carcinoma | ACHN, 786-0, and Caki-1 (20 μM) | 30 mg/kg (BALB/c-nude mice intraperitoneally) | Cell cycle arrest | p53 accumulation; modulated ATM signalling | [30] |
Adenoid cystic carcinoma | ACC-2 (40 μM) |  | Inhibited proliferation; apoptosis | Suppressed the expression of GLUT-1 | [31] |
Papillary thyroid carcinoma | BCPAP (25 μM) |  | Cell cycle arrest; autophagy | Down-regulation of Cdc25C expression | [32] |
Oral squamous cell carcinoma | SCC-25, HaCaT (100 μM) |  | Inhibited proliferation; apoptosis | Decreased expression of cyclin D-1 and E; inactivation of CDK1 | [33] |
Pancreatic cancer |  Murine Panc02 (20 μM) | 25 mg/kg (female C57BL/6N mice, intraperitoneally) | Maintain T cell homeostasis | Stabilizing Ikaros expression | [60] |
Mesothelioma | Malignant mesothelioma (MM) cells (50 μM) | 20 mg/kg (C57BL/6 mice, oral gavage) | Apoptosis | Inhibited AKT and c-Jun phosphorylation, and inhibited NF-κB nuclear translocation | [91] |
Osteosarcoma | U2OS and MG63 (50 μg/ml) |  | Inhibited proliferation and invasion | Inactivated Wnt/β-catenin signaling | [108] |
Head and neck squamous cell carcinoma | HSC-3, HN-8, and HN- 30 (40 μM) |  | Suppressed cancer stem cell marker expression | Downregulated the stem cell markers of CD44,NANOG, and CD105, and abolished the hypoxia-induced increase | [63] |
Cervical cancer | HeLa (40 μM) |  | Inhibited cell self-renewal capacity | Downregulation of CK2α expression | [67] |