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Table 1 Effects of apigenin treatment alone on cancer cells

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]