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. 2022 May 16;18(8):3498–3527. doi: 10.7150/ijbs.70447

Table 1.

Antitumor potentials of emodin

Cancers Mechanisms Cell lines/Animals Dose/Concentration Potential targets References
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Lung cancer
Cytotoxicity PTK inhibition NCI-H1435, NCI-H226, NCI-H460 30 μM HER-2 neu 39
Suppression of ERCC1 and Rad 51 via ERK1/2 inactivation H1650, A549, H520, H1703 25-100 μM ERCC1, Rad51, p-ERK1/2, MKK1/2 40
Down-regulation of ERCC1 and Rad51 SK-MES-1, A549 40 μM, 70 μM ERCC1, Rad51 41
ERCC1 down-regulation and ERK1/2 inactivation H520, H1703 8.1-24.3 μg/mL ERCC1, p-ERK1/2 42
Inhibition of ILK expression via increase of phosphorylation of AMPKα & ERK1/2 and suppression of Sp1 and c-Jun. A549, PC9, H1299, H1650, H1975 50 μM p-AMPKα ILK, Sp1, c-Jun, p-ERK1/2 43
Inhibition of cell growth and induction of cell cycle arrest at G2/M phase via activation of PPARγ & AMPKα/MEK/ERK, down-regulation of Sp1 and up-regulation of IGFBP1 A549, H1975
Nude mice (A549)		 50 μM for cell;
25,50 mg/kg for mice		 p-PPARγ, p-AMPKα, MEK, IGFBP1 Sp1, p-ERK1/2 44
By inhibiting hyaluronan secretion and regulating the expression of cyclin, G1/G0 phase arrest was induced A549, H520, H1975, H1299, H460 30 μM Cyclin C, Cyclin D, Cyclin E HAS2, Cyclin A, Cyclin B 45
Apoptosis Emodin-induced cell death is closely associated with the mitochondria- dependent apoptosis CH27 10, 50 μM c-Caspase 3, c-Caspase 8, c-Caspase 9, Bak, Bax, Cyto C 46
Induction of apoptosis via up-regulation of FASL and down-regulation of C-MYC A549 16.85 μg/ml FASL c-Myc 47
Induction of apoptosis via activation of ER stress and the TRIB3/NF-κB pathway A549, H1299; BALB/c nu/nu nude mice (A549) 80 μM for cell; 50 mg/kg c-Caspase 3, CHOP, TRIB3, GRP78 48
Induction of mitochondria-dependent apoptosis via activating a
ROS-elicited ATM-p53-Bax signaling pathway		 A549 50 μM p-ATM, p53, Bax, Cyct C Survivin 15
Induction of apoptosis via ROS generation and reduced ∆Ψm A549, H460, CH27, WI38 50 μM c-Caspase 2, c-Caspase 3, c-Caspase 8, c-Caspase 9, Bax, ROS, Cyto C Bcl-2, p-Akt, p-ERK1/2 49
Induce tumor cell apoptosis A549 9.31 μg/ml 50
Inhibition of MTH1 promotes DNA damage and apoptosis of tumor cells NCI-H-520, NCI-H-460, A549 25, 50, 75 μM ROS, Cyclin B1, PARP, c-Caspase 3, Bax, CDK4, Bcl-2, MTH1, CDK2, Cyclin D1, Survivin, VIM 52
Inhibition of proliferation of non-small cell lung cancer in vitro and in vivo A549, H1650, H460, H1975, PC9, H1299
C57 mice (LLC cells)		 20, 40, 60 μM for cell; 25, 50 mg/kg ROS, Bax, P27, p-AMPK sPLA2-IIa, NF-κB P65, IKKβ, IκBα, p-mTOR, p-ACC, p-PKM2, p-AKT, Cyclin D1, Cyclin B1, Bcl2 53
Increase ROS, reduce autophagy, induce lung cancer cell apoptosis in vivo and in vitro LLC cell; ICR mice (urethane-induced lung carcinogenesis) 20 μM for cell; 10 mg/kg for mice IFN-γ, IL-12, ROS, P62 IL-6, TNF-α, TGF-β1, LC3-B 60
Autophagy Induction of autophagy via the mutation independent p53 aggregation. A549 10, 15, 20 μM/70 μM p53, LC3 ERCC1, Rad51 16,41
Inhibition of metastasis and invasion Down-regulation of CXCR4 and HER2 A549 100 μM CXCR4, HER-2 neu 54
Inhibition of ATP-induced proliferation and migration by suppression of P2Y receptor and Ca2+ dependent NF-κB pathway A549 1, 5 μM Bax, Claudin-1, E-cadherin Bcl-2, Fibronectin, SNAIL, NF-κB p65 55
Suppressing expressions of Twist, SNAIL & Slug, and inhibiting activation of NF-κB H69, H69AR 10,20,50 μM Twist, SNAIL, Slug, NF-κB p65 56
Chemotherapy resistance Inhibition of drug efflux enhances cisplatin-induced apoptosis and DNA damage A549, H460 2.5, 5, 10 μM Pgp 57
It synergistically inhibited the proliferation of A549 cells with paclitaxel in vivo and in vitro, and exerted anti-tumor effect A549; BALB/nude mice (A549) 10 μM for cell; 50 mg/kg for mice Bax, c-Caspase 3 Bcl-2, p-Akt, p-ERK1/2 58
Reverse cisplatin resistance, promote lung cancer cell apoptosis, inhibit cell migration and invasion A549 Not mentioned NF-κB, P-gp, MDR-1, GST 59
Hepatocellular carcinoma
Cycle arrest G2/M phase arrest of tumor cells Huh7, Hep3B, HepG2 50 μM Cyclin B, Chk2, Cdk2, P27, CYP1A1, CYP1B1, CHAC1, TIPARP, GDF15, SOS1, RASD1, SLC7A11, CYR61, MRAS, SERPINE1 Cdc25c, P21, NR1H4, PALMD, TXNIP, IGFBP3, Cyclin A, Cdk1 65
Results in G1 phase arrest, increased intracellular ROS level and DNA fragmentation HepG2 30, 60, 90, 120 μM c-Caspase 8, c-Caspase 9, Cyto C, p53 Bcl-2, NF-kB p65, p-Caspase 3 66
It can cause G1 phase arrest and cytotoxicity, increase ROS level and inhibit cell glycolysis HepG2 10, 20, 40 μM PKM2, HK11, LDHA 67
Apoptosis ROS production is increased, G2/M phase arrest occurs, and the mitochondrial transmembrane potential (∆Ψm) decreases, leading to DNA fragmentation and inducing cell apoptosis Mahlavu, PLC/PRF/5, HepG2 Mahlavu (5, 10, 30 μg/ml), PLC/PRF/5 (40, 80, 160 μM), HepG2 (20, 40, 80 μM) Cyt c, P53, P21, Bax, Cyclin E, c-Caspase 3, c-Caspase 9, c-PARP Bcl2, Cyclin A, CDK2 68-70
Decreased mitochondrial membrane potential (∆Ψm) and induced apoptosis HepG2 50, 100 μM CypD, Cyt c p-ERK1/2 71
Induce tumor cell apoptosis and inhibit tumor growth HepG2, PLC/PRF/5, Hep3B, C3A;
Athymic nu/nu female mice (HCCLM3)		 10, 50 μM for cell;
25, 50 mg/kg for mice		 SHP-1, c-Caspase 3; PARP CD31, p-STAT3, Bcl2, Bcl-xL, survivin, Mcl-1, VEGF, p-JAK2, p-JAK1, p-AKT, p-Src, cyclin D1 76
Inhibit cell viability and promote tumor cell apoptosis through death receptor and mitochondrial pathways HepG2, HL-7702 20, 40, 80 μM PARP, BAX, Cyt c, Fas, Fas-L, tBid, p-p38 p-Caspase 3, Bcl2, Bid, p-Caspase 8, p-Akt, p-ERK1/2, p-JNK 77
Decrease cell viability and induce apoptosis in vitro. Inhibit tumor growth in vivo, induce apoptosis of tumor cells, improve liver and kidney function of tumor mice SMMC-7721
male BALB/c-nu nude mice (SMMC-7721)		 25, 50, 100 μM for cell; 25, 50 mg/kg for mice p-p38, c-Caspase 3, c-Caspase 9 p-AKT, p-Caspase 9, p-JNK, p-ERK1/2, p-Caspase 3 78
Induce tumor cell apoptosis and inhibit tumor growth HepG2; BALB/c nude mice (HepG2) 10, 100 nM for cell; 1, 10 mg/kg for mice mir-34a SMAD2, SMAD4, p-VEGFR2, p-AKT, p-ERK1/2 79
Inhibit lipid metabolism of tumor cells, promote apoptosis and inhibit tumor growth BALB/C mice (Be L-7402) 20, 40, 80 mg/kg Bax, c-Caspase 9, c-Ccaspase 3, APAF1, Cyt c, AIF Bcl2, SREBP1, FASN, ACACA, ACLY, SCD1, SIP, SCAP、Caspase 2 80
It inhibited tumor cell viability, reduced mitochondrial membrane potential, inhibited triglyceride level and fatty acid desaturation, and induced apoptosis Bel-7402 100 μM c-Caspase 3, c-Caspase 9, APAF1, Cyt c, ENDOG, AIF, Bax Bcl2, SCD, FASN, ACACA, ACLY, SREBP1 81
Inhibition of metastasis and invasion Inhibit the migration and invasion of tumor cells and inhibit lung metastasis in vivo HepG2, Hep3B, PLC/PRF5, HUH7
female Balb/c nude mouse (HCCLM3)		 50 μM for cell;
25, 50 mg/kg for mice		 CXCR4, HER2, NF-kB 84
Inhibit tumor cell viability, induce a small amount of apoptosis, inhibit cell migration and invasion MHCC-97H 100 μg/kg p-p38 p-ERK1/2, p-Akt, MMP-2, MMP-9 85
Chemotherapy resistance Reversal of cisplatin resistance increases DNA damage HepG2 10 μM FGFR2, p-ERK1/2, ERCC1 89
Enhanced irradiation induces cytotoxicity G2/M block was induced and apoptosis was induced HepG2 10 μM c-PARP1 JMJD1A, HIF-1α, JMJD2B 90
It can induce G1 phase arrest and apoptosis, reduce cholesterol synthesis, inhibit tumor growth, and improve Sorafenib resistance HepG2, Hep3B, Huh7, SK-HEP-1, PLC/PRF5; BALB/c-nude mice (HepG2 or SK-HEP-1) 20 μM for cell;
10 mg/kg for mice		 c-Caspase 3 HMGCS1, HMGCR, FDPS, p-AKT, p-4E-BP1, p-STAT3 91
Enhance the toxicity of cisplatin and inhibit the migration and invasion of tumor cells HepG2 cell 25, 50 μg/ml E-cadherin 92
Colon cancer
Cell cycle Intracellular ROS production and Ca2+ release were induced, and G0/G1 phase arrest was induced in tumor cells LS1034; Athymic BALB/c nu/nu mice (LS1034) 10, 20, 30, 40, 50 μM for cell; 40 mg/kg for mice c-Caspase 3, c-Caspase 9, Bax, AIF, Cyt c Bcl2 96
Apoptosis Increase intracellular ROS production and induce tumor cell apoptosis HCT116 20, 40, 80 μM Bax, Cyt c, P53 Bcl2 97
Inducing tumor cell apoptosis through mitochondrial pathway LOVO 10, 20, 40 μM Bax, Cyt c, Bcl2 98
Increase intracellular ROS level, inhibit tumor cell proliferation and induce apoptosis. SW480, SW620 20, 40, 60, 80 μM p-P38, P53, Puma 99
Inhibition of fatty acid synthesis of tumor cells plays an anti-proliferation and pro-apoptotic role HCT116, SW480 25 μM FASN, p-AKT, p-PI3K 100
Regulation of PI3K/AKT pathway induces G2/M cycle arrest and apoptosis of human colon cancer cells CACO-2 15, 30, 60 μM Bax Bcl2, p-PI3K, p-Akt 101
Induce cell apoptosis, inhibit migration and invasion, inhibit tumor growth, and reverse 5-FU resistance SW480, SW480/5-Fu
BALB/c nude mice (SW480/5-Fu)		 9 μM for cell;
40 mg/kg for mice		 Bax, c-Caspase 3 Bcl2, p-ERK1/2, p-AKT 102
Autophagy Increase intracellular ROS accumulation, induce cell apoptosis and autophagy HCT116, LOVO 20 μM c-Caspase 9, c-Caspase 3, c-PARP, LC3-2, Beclin 1, LC3-1, Cyt c, Bax P62, Bcl2 103
Inhibition of metastasis and invasion Inhibit the migration and invasion of tumor cells DLD-1 10, 20, 30, 40 μM α- ERM pThr567 PRL-3 104
The ROS level in tumor cells was increased, G2/M phase arrest occurred, and the migration and invasion of tumor cells were inhibited SW480, SW620 50 μM CDH1, EP300 β-catenin, TCF, LEF,
hbp1, PCNA, Cyclin D1, c-Myc, SNAIL, VIM, MMP-2, MMP-9		 105
Blocking EMT, and inhibits the invasion and migration of tumor cells in vivo and in vitro HT29, RKO
Balb.c nude mice (RKO)		 5, 10, 20 μM for cell; 40 mg/kg for mice E-cadherin VEGF, MMP-7, MMP-9, N-cadherin, SNAIL, N-catenin, TCF4, Cyclin D1, c-Myc 106
Inhibit the growth, adhesion and migration of HCT116 cells, and inhibit the growth of xenograft tumor HCT116; BALB/c nude mice (HCT116 cells) 15, 30, 60 μg/ml for cell; 20, 40, 80 mg/kg for mice VEGFR2, p-PI3K, p-AKT 107
Anti-inflammatory Inhibit intestinal inflammation related to cancer and prevent the occurrence and progression of intestinal tumors SW620, HCT116
AOM/DSS model mice		 10, 20 ,40 μM for cell; 50 mg/kg for mice TNFa, IL1a/b, IL6, CCL2, CXCL5, COX-2, iNOS 108
Breast cancer
Cytotoxicity Inhibit the growth of cancer cells, induce the production of lipid droplets, and promote the mature differentiation of BC cells MDA-MB453, BT-483, MDA-MB231, MCF-7 40 μM HER-2/neu 111
Apoptosis Apoptosis is induced by mitochondrial signaling pathway BCap-37 20, 50 μM Bax, Cyt-c Bcl2 115
Apoptosis is induced by the destruction of mitochondrial signaling pathways in cells BCap-37 20, 50 μM P21, P53 IGF-2 116
Induce DNA breakage and DNA fragmentation, and induce tumor cell apoptosis and cycle arrest through internal and external pathways MCF-7 30 μg/ml Fasl Mcl-1, Cyclin D, c-MYC 117
Inhibition of ERα pathway and PI3K/Akt pathway inhibited the proliferation of tumor cells and induced apoptosis MCF-7, MDA-MB-231 20, 40 μM ERα, Cyclin D1, BCL2, p-MAPK, p-AKT 118
Induce growth inhibition and apoptosis of human breast cancer cells Bcap-37, ZR-75-30 10, 40 μM c-Caspase 3, PARP, p53, Bax Bcl-2 119
It exerts anti-tumor activity by activating AhR-CYP1A1 signaling pathway MCF-7 25, 50, 100 μM AHR, CYP1A1 120
Chemotherapy resistance Increase tumor sensitivity to paclitaxel and improve tumor drug resistance MDA-MB-361, MDA-MB-453, BT-483, SKBr-, BT474, MDA-MB-231, MCF-7;
Nu/nu mice (MDA-MB-361 or MDA-MB-231)		 20 μM for cells;
40 mg/kg for mice		 HER-2/neu 113
Inhibit DNA damage repair and reverse multidrug resistance of tumor cells MCF-7/Adr
MCF-7		 20 μg/ml ERCC1 123
Enhance apoptosis of breast cancer cells, resulting in cell senescence MCF-7 20 μM P21, P16, P27, ROS E2F1, NRARP, GSH 124
It increased the sensitivity of BC cells to doxorubicin, inhibited cell proliferation and induced DNA damage MDA-MB-231, MCF-7 110 μM γH2A, P53 AKT1, XRCC1, PARP1, RAD51 125
Inhibition of metastasis and invasion Inhibition of tumor cell metastasis by targeting HER-2/ neu MDA-MB453, MCF-7 20 μM HER-2/neu 112
Inhibits the invasion of breast cancer cells in vivo and in vitro MDA-MB-435s, MDA-MB-468 1, 10 μM P2X7R 126
It can reduce the infiltration of macrophages, reduce the migration of macrophages to tumor environment, inhibit the polarization of macrophages M2, and inhibit the lung metastasis of tumor 4T1 cell, EO771
BALB/c or C57BL/6 mice (4T1 cell and EO771 cell)		 10, 100 μM fo cells; 40 mg/kg for mice p-STAT6, C/EBPβ 129
Inhibit the EMT of breast cancer cells and the formation of cancer stem cells, and prevent the recurrence of lung metastasis after breast cancer EO771, 4T1, MCF7, MDA-MB-231
C57BL/6, BALB/c, NOD-SCID mice (EO771, 4T1, MCF7, MDA-MB-231)		 40 mg/kg TGF-β1 130
Inhibit macrophage infiltration and m2-like polarization, block their migration and adhesion to the tumor site, inhibit tumor growth, increase T cell activation, and reduce tumor angiogenesis 4T1, EO771
C57BL/6 and BALB/c mice (4T1 cells, EO771 cells)		 0-100 μM for cells; 40 mg/kg for mice iNOS MMP 2, MMP 9, JMJD3, Arg1, p-STAT6, C/EBPβ, CSF-1, MCP-1, ICAM1, Thy1 131
Inhibit TGF-β and inhibit the EMT and migration of cancer-associated fibroblasts BT20 30 μM E-cadherin β-catenin, VIM, MMP-2 132
Inhibit tumor cell migration in vivo and in vitro, and inhibit lung metastasis of breast cancer in nude mice MDA-MB-231
athymic nude mice (MDA-MB-231)		 10, 20, 40, 80 μM for cells; 40 mg/kg for mice MMP 2, MMP 9, uPA, uPAR, p38, p-ERK1/2 133
Inhibit CCL5 secretion of adipocytes, inhibit EMT of tumor cells, inhibit tumor growth and lung liver metastasis MDA-MB-231, MDA-MB-453
Balb/C nude mice (MDA-MB-231)		 50 μM for cells;
40 mg/kg for mice		 GSK3, E-cadherin CCL5, p-AKT, β-catenin, vimentin, SNAIL, p-CCR5, MMP2, MMP9 134
Anti-angiogenesis Tumor cell - induced metastasis and angiogenesis were inhibited in vitro and in vivo EA.hy 926; NOD/SCID mice/ SD rats (MDA-MB-231) 10, 20, 40 μM for cells; 40, 80 mg/kg for mice MMP9, MMP13, p-Runx2, p-VEGFR-2 135
Inhibit angiogenesis and tumor growth MDA-MB-231, 4T1; BALB/c NOD-SCID mice; and, BALB/c mice 5, 10, 20 μM for cells; 10 mg/kg SerRS, HOXB1, PCK1, UCP1, NCOR2, HDAC3 VEGFA 136
Pancreatic cancer
Cytotoxicity Promote the demethylation of tumor suppressor genes and inhibit the growth of pancreatic cancer cells PANC-1 10,20,40μM P16, RASSF1A, ppENK 5mC, DNMT1, DNMT3a 145, 146
Inhibit tumor cell growth, angiogenesis and glycolysis, reduce cancer cachexia AsPC-1, BxPC-3, HPAF-2, MiaPaCa2, Panc-1; Male athymic Balb/c mice (MiaPaCa2) 100 μM for cells; 50 mg/kg for mice HIF-1α, Glut1, HK-II, PFK- 1, VEGF, caveolin-1, p-Akt, p-ERK1/2, PHD-2 148
Apoptosis It plays anti-tumor proliferative role by inducing apoptosis Mia Paca-2, BxPC-3, panc -1, L3.6pl 12.5, 25, 50 μM PARP 149
Induced apoptosis of pancreatic cancer cells and increased sensitivity of pancreatic cancer to gilotrif PANC-1, BxPC-3
BALB/c nude mice (PANC-1)		 30, 60, 90 μM for cells; 50 mg/kg for mice c-Caspase 3, bax p-STAT3, Bcl2, EGFR 153
Chemotherapy resistance Enhanced the antitumor activity of gemcitabine Mia Paca-2, BxPC-3, panc -1, L3.6pl 40, 80 μM c-Caspase 3, PPAR Survivin, b-catenin 154
Enhanced the antitumor activity of gemcitabine SW1990, SW1990/GZ 20 μM NF-κB 155
Increased sensitivity of tumor cells to gemcitabine SW1990; BALB/c female mice (SW1990) 40 μM for cells; 40 mg/kg for mice Bax, CytC, c-Caspase 3 Bcl-2 156
Improve chemotherapy resistance of tumor cells to Gemcitabine BALB/c female mice (SW1990) 40 mg/kg for mice Bax, c-Caspase 9, c-Caspase 3, CytC p-AKT, Bcl-2, NF-κB p65 157
Enhanced the antitumor activity of gemcitabine SW1990; Female BALB/c nude mice (SW1990) 40 μM for cells; 40 mg/kg for mice XIAP, NF-Κb p65 158
Enhanced the antitumor activity of gemcitabine BaLB/c male mice (Panc-1) 40 mg/kg c-Caspase 9, c-Caspase 3 XIAP, NF-κb p65, Survivin 159
Increased sensitivity of tumor cells to gemcitabine SW1990, SW1990/GZ 10, 20, 40, 80, 160 μM Bax, Cytc, c-Caspase 9, c-Caspase 3 MDR-1 (P-gp), NF-κB p65, Bcl-2 160
Increased sensitivity of resistant cells to gemcitabine treatment Bxpc-3/Gem 40 μM MDR-1 (P-gp), NF-κB p65, XIAP, survivin 161
To enhance the therapeutic effect of gemcitabine and improve the drug resistance of tumor cells to gemcitabine BALB/c mice (PANC‑1) 40 mg/kg MDR-1(P-gp), MRP1, MRP5 162
Reversal of gemcitabine resistance in pancreatic cancer cell lines pan -1/Gem, MIAPaCa-2/Gem 40 μM c-Caspase 3, c-Caspase 9, IκB-α Survivin, XIAP, NF-κB p65, IKKβ, P-gp 163
Inhibition of metastasis and invasion Inhibit metastasis of pancreatic cancer SW1990; BALB/c nu/nu mice (SW1990) 10, 20, 40 μM for cells; 20, 40 mg/kg for mice c-Caspase-3 MMP9, NF-κB p65, survivin 164
Inhibit EMT and invasion of pancreatic cancer cells, and inhibit hepatic metastasis of pancreatic cancer SW1990; Nude mice (SW1990) 20, 40 μM for cells; 50 mg/kg for mice miR-1271, E-cadherin ZEB1, TWIST1 166
Anti-angiogenesis Regulating the expression of angiogenesis related factors can promote apoptosis and inhibit angiogenesis SW1990, Panc-1, ECs
Female athymic BALB/c nu/nu mice (Panc-1 cells)		 40 μM for cells;
1 mg/mouse for mice		 NF-κB p65, VEGF, MMP 2, MMP 9, p-eNOS 167
Inhibits angiogenesis in pancreatic cancer SW1990; Female athymic BALB/c nu/nu mice 20, 40, 80 mg/kg for mice miR-20b, Smad4, TβRI, TβRII TGF-β1, Angptl 4, miR-155, miR-210 168
Leukemia
Cytotoxicity Induction of ROS production, improve the sensitivity of tumor cells to arsenic trioxide C8166 cells, MT2, II85, LAF, Jurkat 10 μM PARP, ROS Akt, Jun D, JAB 1 171
Apoptosis Apoptosis of HL-60 cells was induced by ROS independent method HL-60 40 μM Caspase3, PARP, D4-GD1, Mcl-1, 172
G0/G1 phase arrest was induced and apoptosis was induced K562 20, 40, 80, 100 μM c-myc 173
Apoptosis of tumor cells was induced by caspase signaling pathway K562 20, 30, 40 μM c-Caspase 3, c-Caspase 9, c-Caspase 8 174
Inhibit the growth of tumor cells in vivo and in vitro and induce their apoptosis BALB/c nude mice (K562) 25, 50, 100 mg/kg Bax Bcl2 175
Cause tumor regression and induce cell apoptosis K562; Male BALB/c nude mice (K562) 25, 50, 100 μM for cells; 20, 50 mg/kg for mice Bax, c-Caspase 3, c-Caspase 8, c-Caspase 9 Bcl2 176
Induce G0/G1 phase arrest and apoptosis U937 30, 60, 90 μM Bax Bcl2, CPP32 177
Apoptosis of human myeloma cells was significantly induced by inhibition of McL-1 RPMI8226, U266, IM-9 10, 20, 50 μM c-Caspase 3, c-Caspase 9 p-JAK2, p-STAT3, Mcl-1, Histone H2 178
Inhibit hL-60 cell proliferation, induce G0/G1 phase arrest, and induce apoptosis HL-60 10, 20, 40 μM p-AKT, p-IκB-α, p-p65, p-mTOR 179
Decreased cell mitochondrial membrane potential, caused cell G0/G1 phase arrest, induced apoptosis, improved doxorubicin resistance HL-60 (ADR) 10, 20, 40 μM c-Caspase-3 Bcl-2, c-myc、 180
Induction of tumor cell apoptosis, overcoming all-trans retinoic acid resistance NB4, MR2, primary AML 10, 30, 60 μM c-Caspase 9, c-caspase 3, PARP Bcl-2, RARα, p-Akt, p-mTOR, 4E-BP1, p70S6K 181
Inducing apoptosis of tumor cells in vivo and in vitro K562; BALB/c nude mice (K562) 25, 50, 100 μM for cells; 25, 50, 100, 120 mg/kg for mice PTEN PI3K, AKT, BCR-ABL 182
Decreased cell viability, induced DNA damage, decreased ΔΨm levels, and induced apoptosis through endoplasmic reticulum stress (ER) and mitochondrial pathways WEHI-3;Male BALB/c mice (WEHI-3) 25, 50, 100 μM for cells; 5, 10 mg/kg for mice ROS, c-Caspase 8, c-Caspase 9, Cyt-c, c-Caspase 7, c-Caspase 12, c-Caspase 3, PARP, Apaf-1, AIF, Endo G, GADD153, GRP78, ATF-6α, Bax, Bad Bcl2, Bcl-xl 183
Chemotherapy resistance Increase the sensitivity of resistant cells to chemotherapeutic drugs K562/ADM 6.1, 17.6, 33.2 μM MDR1, P-gp 187
The doxorubicin resistance of K562/ADM cells was reversed K562/ADM 50, 100, 200 μM P-gp 188
Increased cytotoxicity of 3'-azido-3'-deoxythymidine to tumor cells K562 8, 16, 32 μM EGR1 β-catenin 189
The chemosensitivity of AML cells to ARA-C was increased, and the survival rate of AML transplanted tumor mice was improved. HL-60/ADR;
BALB/C-nude mice (HL-60/H3)		 5, 10 μM for cells; 20, 40 mg/kg for mice PARP, c-Caspase 9, c-Caspase 3, Bax Bid, p-Akt, p-mTOR, p-4E-BP1, p-ERK1/2, p-P70S6K, Bcl2 190
Enhanced the sensitivity of drug-resistant cells to imatinib, inhibited cell proliferation and induced cell apoptosis K562, G01 20, 40 μM c-Caspase-3, c-PARP p-Bcr-Abl, c-MYC, MCL-1, Bcl-2, p-STAT5, Src, p-Src 191
Cervical cancer
Cytotoxicity It inhibited the proliferation of HeLa cells and reduced the tumor growth of tumor-bearing mice HeLa; Female old athymic nude mice (HeLa) 1, 10, 25 μM for cells; 25 mg/kg for mice p-STAT1, p-STAT2, IFNAR1, p-TYK2 p-STAT3 193
Apoptosis Inhibits DNA synthesis and induces apoptosis through the mitochondrial pathway HeLa, Ca Ski, ME-180, Bu 25TK 25, 50 μM c-Caspase 3, c-Caspase 9 194
Induce tumor cell apoptosis HeLa 40 μM p-JUN p-AKT, mTPR, p-PTEN, P-MAPK 195
Apoptosis is induced by internal mitochondrial and external death receptor pathways HeLa 20, 40, 80 μM caspase-3, caspase-9, caspase-8, Fas, Fasl, FADD, Cyt-c, Apaf-1 JAK2, STAT3, Mcl-1 196
Induce apoptosis and autophagy, inhibit cell cycle, inhibit angiogenesis Hela, JAR, HO-8910 5, 10, 15 μM Atg12-Atg5, Beclin-1, c-Caspase-9, c-Caspase-3 Cyclin D1, Cyclin E1, VEGF, VEGFR-2, Bcl2, Mcl-1, MAPLC3 197
Autophagy By increasing the number of lysosome, the number of autophagic vacuoles and the activity of lysosome hydrolase can induce lysosome membrane damage and promote the death of tumor cells HeLa 1, 15, 30, 60, 100 μM Cathepsin D, Cathepsin L 198
To improve the toxicity of photodynamic therapy to cervical cancer cells and increase the activity of caspase-3 and autophagy SiHa, CaSki 30 μM c-Caspase 2, ROS, ATF2, AURKA, AURKC, BIRC5, CDK1, CDK7, GSTP1,
HDAC4, HIF1A, HSP90AA1, MDM4, MTOR, PARP4, PIK3C2A, PIK3C3, PIK3CA, PLK2, PLK4, RHOA, RHOB, TNKS, TOP2B		 CTSS, ESR1 199
Inhibition of metastasis and invasion Inhibit the invasion, migration and stem cell characteristics of tumor cells and reverse EMT SiHa, Hela 20 μM Bax TGFRII, Smad2, Smad3, Smad4, CyclinD1, p21, Pin1, p15, p16, CDK6, p27, SNAIL, Slug, Bcl 2, β-catenin 200
Ovarian cancer
Cytotoxicity Induced DNA damage and inhibited cell proliferation A2780 1 μM 202
Inhibit cell viability, and reduce cell viability and colony formation of A2780 cells A2780 20 μM FOXD3, miR-199a TGF-β2 203
Apoptosis Inhibit tumor cell proliferation, induce apoptosis and inhibit invasion SKOV3, HO8910 20, 60 μM surviving 204
Inhibition of metastasis and invasion Inhibit EMT, migration and invasion of tumor cells, and inhibit metastasis of ovarian cancer A2780, SK-OV-3 20, 40, 80 μM E-cadherin, Claudin N-cadherin, vimentin, p-GSK-3β, ILK, β-Catenin, and Slug 205
Inhibit EMT and invasion of tumor cells A2780, SK-OV-3 10, 20, 40 μM E-cadherin, keratin N-cadherin, Vimentfin, MMP 9, MMP 2, ZEB1, p-GSK-3β, β-Catenin 206
Inhibit the proliferation, migration and invasion of ovarian cancer cells A2780, SK-OV-3;
Female BALB/C nude mice (SK-OV-3)		 20 μM for cells; 50 mg/kg for mice E-cadherin Slug, MMP 9, Vimentin, ILK 207
Chemotherapy resistance Induced apoptosis and increased sensitivity of drug-resistant cells to paclitaxel A2780 10 μM c-Caspase 3 P-gp, XIAP, MDR-1, surviving 208
Increase the sensitivity of drug-resistant cancer cells to cisplatin COC1 50 μM ROS MRP1 209
Inhibit the growth of cancer cells and enhance the sensitivity of drug-resistant cells to cisplatin therapy SKOV3, OVCAR3, MDH2774, and ES2 0-50 μM AURKA 220
Head and neck neoplasm
Cytotoxicity Induced cell DNA damage SCC-4 25, 50, 100 μM ATM, ATR, 14-3-3σ, BRCA1, DNA-PK, MGMT 212
Inhibit the growth, proliferation and cell division cycle of human oral squamous cell carcinoma cells Tca8113 10, 20, 40, 80 μM CDK2, Cyclin E, P21 216
Inhibition of cell cycle markers play an anti-proliferation role Buccal mucosa of hamsters treated with DMBA 50 mg/kg Cyclin D1, PCNA, CDK4, CDK6, survivin 217
Prevention of DMBA - induced hamster buccal pouch carcinogenesis by proapoptotic and antioxidant effects Buccal mucosa of hamsters treated with DMBA 50 mg/kg P53, Bid, Bax, c-Caspase 3, c-Caspase 9 Bcl-xl 218
Apoptosis Increased ROS level leads to DNA damage, endoplasmic reticulum stress and apoptosis of tumor cells SCC-4 30 μM ROS, c-Caspase 9, c-Caspase 3, P21, Chk2, Cyto c, AIF, GADD153, GRP78, Bax Cyclin B1, Cdc2, Bcl2 211
Apoptosis was induced by the production of ROS and the decrease of pH EC-109 2.5, 5, 10, 20 μM ROS Intracellular PH 214
Tumor cell death was induced by apoptosis and necrosis HSC-3 46.3, 92.5, 185 μM Bax, c-Caspase-9, c-Caspase-3 Bcl2, p-AKT 219
Induce cell cycle arrest and apoptosis Human nasopharyngeal carcinoma cells (CNE-2Z) 50 μM chloride channel 220
Inhibit the proliferation of thyroid papillary carcinoma cells, induce cell cycle arrest and apoptosis TPC‑1;
Balb/c female nude mice (TPC‑1 cells)		 10, 25, 50 μM for cells; 40 mg/kg for mice p-AMPK, c-Caspase 3, Cyclin D1 PCNA, p-MEK, p-ERK1/2 222
Inhibition of metastasis and invasion Inhibit tumor cell migration and invasion SCC-4 15,30μM TIMP-1 MMP 2, u-PA, FAK, NF-κB p65, p-AKT, p-P38, p-JNK, p-ERK1/2 213
Inhibit EMT of tumor cells and inhibit migration and invasion FaDu, HEK-293T, OECM-1; Severe combined immunodeficient (SCID) mice 5 μM for cells; 50 mg/kg for mice E-cadherin, p-GSK-3β TEIST1, Vimentin, p-AKT 215
Inhibit tumor angiogenesis and lung metastasis 8505c, SW1736
Balb/c nude mice (SW1736)		 10, 15, 20, 25 μM for cells; 100 mg/kg for mice TRAF6, HIF1α, VEGF, CD147, MMP 9 221
Glioma
Inhibition of metastasis and invasion The invasion of hyaluronic acid (HA) induced glioma cells was inhibited Hyaluronic acid (HA)-induced invasion of human glioma cells. 40 μM MMP2, MMP9, p-FAK, p-ERK1/2, p-Akt, p-PKB, AP-1, NF-kB-p65 223
Inhibit cell migration and intracellular glycolysis U-87 MG or ΔFBP1 U-87 MG
male BALB/c athymic nude mice (U-87 MG or ΔFBP1 U-87 MG)		 20, 40 μM for cells; 40 mg/kg for mice E-cadherin FBP1, Vimentin, Fibronectin 224
Apoptosis Apoptosis of glioma stem cells was induced, the invasiveness of glioma stem cells was decreased, and the sensitivity of glioma stem cells to ionizing radiation was increased X01 and X03, and CSC2 5 μM Hsp90 b-catenin, p-STAT3, p-Akt, SNAIL, slug, p-EGFR 225
The proliferation of U251 cells was inhibited and apoptosis and necrosis were induced U251;
BALB/C nude mice (U251)		 10, 20, 40 μM for cells; 20, 40, 80 mg/kg for mice TNF-α, RIP 1, RIP 3, MLKL, c-Caspase-3 Caspase 8 226
Neuroblastoma Inhibit the migration and invasion of tumor cells in vitro SH-SY5Y 10, 25 μM GRB2, RhoA, NF-kB p65, HIF-1a, VEGF, FAK, Ras, COX2, p-p38, p-JNK, MMP2, MMP9, MMP7 227
Trigger caspase cascade signaling pathway and induce tumor cell apoptosis IMR-32 20 μM Ca2+, ROS, p53, p21, c-Caspase-9, c-Caspase-3 228
Prostatic cancer Inhibit the growth of tumor cells and prolong the survival time of tumor mice LNCaP, PC3, DU-145
Male athymic nude mice (PC3)		 10, 20, 40 μM for cells; 40 mg/kg for mice PARP AR, PSA 229
Inhibit cell proliferation and induce cell apoptosis through mitochondrial pathway LNCaP, PC-3 10, 20, 30, 40 μM p53, p21, Bax, c-Caspase 3, c-Caspase 9 Bcl-2, AR, PSA 230
Enhance anti-tumor effect of cisplatin in vivo and in vitro and reverse drug resistance DU-145; BALB/c-nu/nu mice (DU0145) 50 μM for cells; 50 mg/kg for mice ROS MDR1, HIF-1 231
Inhibit tumor growth LNCaP, PC-3 50 μM ROS, LRP1 AR 232
Inhibit the migration and invasion of tumor cells DU145 100 μM CXCR4, HER2, NF-Κb p65 54
Inhibit the growth of tumor cells and induce cell cycle arrest and apoptosis PC-3 10, 20, 40, 60, 80 μM Notch1 Jagged1, VEGF, bFGF 233
Bladder cancer Reverse the transformation of cancer epigenetics to normal epigenetics, and inhibit the occurrence of tumors T24, TSGH8301, MBT24 40, 80 μM H3K27me3 HBP17, FABP4, pH3Ser10 234
Improve cisplatin resistance of tumor cells in vitro and in vivo T24, J82; BALB/cnu/nu mice (T24) 20 μM for cells; 50 mg/kg for mice ROS MRP1 235
Lymphoma Mitochondrial apoptosis pathway of Dalton's lymphoma (DL) cells was induced in vivo Inbred AKR strain mice (DL cells) 40 mg/kg H2O2, Bax, Cyto c, SOD2, SOD1 Bcl2, GPx 236
It can reduce the survival rate of tumor cells, induce apoptosis and increase the sensitivity of tumor cells to doxorubicin Raji 6.25, 12.5, 25, 50 mg/kg c-Caspase 3, c-Caspase 9, PARP, DNMT3A p53, UHRF1 237
Inhibit cell proliferation and induce cell apoptosis SU-DHL4 10, 20, 40 μM p-PI3K, P53, p-AKT 238
Gallbladder carcinoma Induce apoptosis and improve the sensitivity of tumor cells to chemotherapy SGC996; BALB/c-nu/nu mice (SGC996) 50 μM for cells; 50 mg/kg for mice ROS GSH, MRP1 241
Cisplatin-induced apoptosis of gallbladder carcinoma cells is promoted in a ROS dependent manner SGC996; BALB/c-nu/nu mice (SGC996) 50 μM for cells; 50 mg/kg for mice ROS surviving 242
Osteosarcoma In vitro and in vivo anti-angiogenesis of osteosarcoma SOSP-9607, MG63, SAOS-2; Male BALB/c nude mice (SOSP-9607, MG63, SAOS-) 2.5 μM for cells;
0.3 mg/kg for mice		 SIRT1 VEGF, H4-K16AC 243
Reduce the radiation resistance of tumor cells and promote cell apoptosis MG63 15, 30, 45, 60 μM c-Caspase 3 Shh, bcl2, Gli 1 244
Apoptosis is induced by mitochondrial pathway and endoplasmic reticulum stress U2OS 120 μM ROS, GRP78, CHOP, c-Caspase 4 245
Inhibit tumor cell proliferation and synergistic anti-tumor with cisplatin MG-63 10 μM Nrf2 246
Skin cancer Inhibit skin tumor formation in mice ICR mice skin tumors induced by 7,12-dimethylbenz[a]anthracene as an initiator and 12- O-tetradecanoylphorbol-13-acetate (TPA) / 247
It induced the disorder of cell redox balance and accelerated cell apoptosis B16F10; C57BL6J mice (B16F10) 30 μM for cells; 5 mg/kg for mice 8-OH-dG, MDA, ROS, c-PARP, Drp1, Bax, IDH2, p-4EBP1, p-P38, p-ERK1/2, OPA1 248
Inhibit the proliferation and migration of tumor cells and induce G2/M phase cycle arrest B16-F10; C57BL/6 (B16-F10) 20, 50 μM for cells; 50 mg/kg for mice CD155 249
Inhibit glycolysis of tumor cells and inhibit their proliferation B16F10 4, 8 μM p-AMPK P53, AMPKα, ATP 250
Inhibit the growth, migration and invasion of melanoma cells B16F10, A375 20, 40, 60 μM Bax β-catenin, c-Myc, TCF, Bcl2, MMP2, MMP9 251
Gastric carcinoma Induction of anoikis, a detachment-initiated apoptosis, in tumor cells, and increases the antitumor effect of arsenic trioxide SGC-7901 5 μM ROS, c-Caspase 3 RhoA 252
The proliferation of SGC-7901 cells was inhibited and apoptosis was induced SGC-7901 15, 30, 45, 60 μM PRL-3 253