Table 5.
Summary of in vitro and in vivo biochemical effects of emodin in hepatocellular cancer cell lines.
| In Vitro (Cell Line)/ In Vivo Studies |
Concentration and/or Method of Application | Mechanism | Reference |
|---|---|---|---|
| SMMC-7721 | Dose-dependent manner (<50 µmol/L emodin) |
Block the proliferation Stimulation of apoptosis Induction of phosphorylation of ERK and p38 Supression of AKT activation and expression of JNK |
[122] |
| SMMC-7721 | 20, 40, and 80 µmol/L | Antiproliferation activity | [124] |
| HepG2 | Different emodin doses (79.01, 51.39, 33.13 µM) |
Trigger intracellular ROS formation, reduction of the expression of proteins and genes involved in glycolysis, and disruption of cell cycle progression |
[117] |
| HepG2 | Dose-dependent manner (50, 100 µM emodin) |
Stimulation of mitochondrial dysfunction Stimulation of apoptosis by up-regulation of cyclophilin D Trigger ERK and ROS-associated cyclophilin D expression |
[121] |
| HepG2 | 120 µM emodin | Induction of apoptosis and cause cell accumulation in the G1 phase Enhance release of cytochrome c Up-regulation caspase-8 and 9 expressions |
[11] |
| PLC/PRF/5, HepG2/C3A, SK-HEP-1 |
60 µM emodin | Stimulation of apoptosis Arrest in the G2/M phase Increase in caspase-3, p53, Fas, and p21 signals |
[27] |
| HCC (Bel-7402) with SREBP1 targeting |
100 μmol/Lemodin | Stimulation of apoptosis Decrease in mitochondrial membrane potential Activation of the expression of cytochrome C, caspases 9 and 3, endonuclease G, Bax, and Bcl-2 related proteins |
[116] |
| HCC (PLC/PRF5, SK-HEP-1, HepG2, Huh7, and Hep3B) |
Emodin and sorafenib | Inhibition of transcriptional activity of SREBP-2 Stimulation of cell cycle arrest in G1 phase |
[118] |
| HepaRG | 80 µM emodin | Inhibition of cell cycle progression in G2/M and S phases Stimulation apoptosis Up-regulation of cyclin E, p21, p53, Bax, cleaved PARP, cleaved caspase-3, 8, and 9 Down-regulation of protein expression of Bcl-2 |
[119] |
| HepG2/PLC mouse model |
GalNAc-PLGA-sTPGS nanoparticles with emodin |
Increase the antitumoral effect | [120] |
| BALB/c nude mice model |
Dose-dependent manner (1 mg/kg or 10 mg/kg emodin) |
Up-regulation miR-34a Inhibition of ERK1/2, AKT, and VEGFR2 Supression of SMAD2 and SMAD4 expression |
[115] |
| HepG2 /Orthotopic mouse model |
Dose-dependent manner (max. inhibition occurring at around 50 μM) |
Inhibition of c-Src, JAK1 and JAK2 protein kinases | [125] |