Table 2.
Summary of in vitro biochemical effects of emodin in breast cancer cell lines.
| Cell Line | Concentration | Mechanism | Reference |
|---|---|---|---|
| MDA-MB453 BT-483 AU-565 |
40 µM | Suppressing the autophosphorylation and transphosphorylation activities of HER-2/neu tyrosine kinase |
[17] |
| MDA-MB453 MCF-7 B104-1-1 |
40 µM emodin 20 µM potent derivative: 10-(4-acetamidobenzylidene)-9-anthrone) |
Suppressing the tyrosine phosphorylation of p185neu, inhibiting the proliferation and transformation of HER-2/neu-overexpressing human breast cancer cells Cell cycle arrest at G0/G1 phase in MDA-MB 453 |
[84] |
| MDA-MB-231 MCF-7 | 110 µM emodin 5 µM doxorubicin |
Increased γH2Ax expression and the DNA damage Decreased expression of the AKT1, p53, PARP1, RAD51, and XRCC1 signaling pathway |
[80] |
| ZR-75-1 MCF-7 |
60 µM emodin 4 µM tamoxifen |
Up-regulation of cyclin D1 and p-ERK | [85] |
| MDA-MB-231 | 10–40 µM | Inhibition of TPA-stimulated MMP-9 activity Reduced transcriptional activity of AP-1 and NF-kB |
[86] |
| BCap-37 | 50 µM | Increased the percentage of cells in the sub-G0/1 phase Decreased Bcl-2, Increased Bax level, and cytosolic cyt c level |
[87] |
| BCap-37 | 50 µM | Up-regulation of P21 Down-regulation of IGF-2 Induced gene expression of p53 and caspase 3 |
[88] |
| SKBR3 | 25 and 50 μM | Increased caspase 3, 8, and 9 mRNA levels Increased Bax level Reduced Bcl 2 level |
[89] |
| MDA-MB-453 MCF-7/ADR MCF-7 | 2.3 to 9.2 µg/mL emodin azide methyl anthraquinone derivative |
Lowered the Her2/neu protein Inhibited the downstream MAPK and PI3K-Akt signaling pathway by inhibiting p-Akt, and p-ERK1/2 in the MDA-MB-453 | [90] |
| MDA-MB-453 | Arrested the cell cylce in the G0/G1 phase Inhibited the expressions of: Cyclin D1, c/Myc, CDK4, and p-Rb |
[91] | |
| MCF-7/Adr | 20 μg/mL | DecreasedERCC1 expression | [92] |
| MCF-7 MDA-MB-453 |
25 μM | Effect on nuclear ERα distribution | [93] |
| MCF-7 | 35 µM | Single-stranded DNA breaking, DNA fragmentation, up-regulation of FASL gene expression Down-regulation of the expression of CCND1, C-MYC, and MCL1 |
[94] |
| MDA-MB-435s | 1 to 10 µM | Inhibition of ATP-induced increase in [Ca2+] | [73] |
| MCF-7 | 20 and 40 µM | Arrested the cell cycle in the G0/G1 phase Blocking the effect of estrogen on ERα expression and transcriptional activity Down-regulation of cyclin D1 and Bcl-2 protein expression, decreased PI3K/Akt protein expression |
[95] |
| EO771-GFP | 10 µM and 30 µM | Reduced adhesion between macrophages and cancer cells | [99] |
| 4T1 | 100 µM | Decreased macrophage migration | [97] |
| EO771 4T1 |
0 to 50 μmol/L | Inhibition of the adherence of macrophages to the monolayer of tumor cells |
[100] |
| 4T1 | 25 µM | Decreased TGF- β1 production Inhibited the formation of EMT and CSC |
[101] |
| MDA-MB-231 MDA-MB-453 | 25 μM | Inhibition ofcell migration and invasion Decreased CCL5 levels Inhibition of the phosphorylation of AKT, activation of GSK3β, downregulation of the expression of β-catenin, Vimentin and snail Increased expression ofE-cadherin |
[102] |
| MCF-7 | 20 μM emodin 40 μM 5-FU |
Up-regulation of p21, p16, p27 protein Down-regulation of E2F1 and NRARP protein |
[103] |
| MCF-10A MCF-7 MDA-MB-231 |
Berberine + emodin (5, 10, 20 μM) |
Suppressed SIK3 activity Cell cycle arrest (G0/G1) |
[104] |
| MCF-7 T47D |
Emodin 10 µg/mL and thymoquinone 2 µg/mL |
Cell arrest in the sub G0/G1 phase, an increase in p53, Bax, and cleaved caspase 3 expression levels, a decrease in Bcl-2 protein, induction of ROS formation, and Cyt C releasein MCF7 cells Inhibition of cell migration and FAK, pFAK, and integrin β1 proteins were down-regulated in both cell lines |
[105] |
| MCF7 | 25–100 µmol/L | Increase in CYP1A1 expression Regulating the expression of AhR and CYP1A1 proteins |
[106] |