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. 2021 May 31;13(11):2733. doi: 10.3390/cancers13112733

Table 1.

Summary of biochemical effects of emodin in lung cancer cell lines.

Cell Line Cell Type Concentration Mechanism Reference
A549 Lung adenocarcinoma 50 µM Increased cyt c, activation of caspase-2, -3, -9, and mitochondrial Bax
Inactivation of ERK and AKT, formation of ROS, disruption of ∆Ψm, reduction of
mitochondrial Bcl-2
[14]
CH27 Lung squamous cell
carcinoma
50 µM Morphological change, sub-G1 formation,
disruption of focal adhesion kinase
Increased expression of Bak and Bax proteins, activation of caspase-3, -8, -9
[25]
CH27 Lung squamous cell
carcinoma
50 µM Internucleosomal DNA fragmentation
Increase in cyt c, activation of caspase-3,
expression of PKCa
Decreased expression of PKCδ and ε
[58]
H460 Non-small human lung
carcinoma
NCI-H446 Small cell lung cancer 20 μmol/L Increased caspase-3 activation
Up-regulated NACA, p8, and PQBP1 genes
Downregulated B2M, HLA-E, and CD1D genes
[62]
A549
H1650
Lung adenocarcinoma 2–10 μM (Emodin)
2 μM (Gefitinib)
Triggered Rad51 protein instability
Decrease in phospho-ERK1/2 and Rad51
protein levels
[63]
A549 Lung adenocarcinoma 50 µM Activation of the ATM-p53-Bax signaling
pathway, ROS formation
[64]
H1650
A549
Lung adenocarcinoma 25–100 µM Inactivation of ERK1/2
Down-regulation of Rad51 and ERCC1
[65]
H520 Human bronchioloalveolar cell carcinoma
H1703 Lung squamous cell
carcinoma
H1650
A549
Lung adenocarcinoma 25–200 µM (capecitabine)
50 µM (emodin)
Inactivation of ERK1/2
Down-regulation of Rad51 and ERCC1
Increased mRNA and protein expression of TP
[66]
H520 Human bronchioloalveolar cell carcinoma
H1703 Lung squamous cell
carcinoma
H1703
A549
Lung squamous cell
carcinoma
Lung adenocarcinoma
1 µg/mL
(cisplatin)
8.1; 16.2; 24.3 µg/mL (emodin)
Instability of the ERCC1 protein
Inactivation of ERK1/2
[67]
SK-MES Lung squamous cell
carcinoma
40 μmol/L (SK-MES)
70 μmol/L (A549)
Decreased expression of ERCC1 and Rad51
protein and mRNA
[68]
A549 Lung adenocarcinoma
A549 Lung adenocarcinoma 100 μM Decreased expression of CXCR4 and HER2 [69]
A549
PC9
Lung adenocarcinoma 50 μM Increase in the phosphorylation of AMPKα and ERK1/2
Decrease in the expression of ILK
[71]
H1299
H1650
H1975
Non-small cell lung
carcinoma
A549
Lung adenocarcinoma
5 to 50 μM (emodin)
50 to 2000 nM (daunorubicin)
Inhibition of anthracycline reductase
enzymes
Sensitized cells to daunorubicin
[70]
A549 Lung adenocarcinoma 50 μM Arrest in G2/M phase
Invasion inhibition
Increased PPARγ protein and luciferase
reporter activity
[72]
H1975 Non-small cell lung
carcinoma
A549 Lung adenocarcinoma 1 nM to 10 µM Prevention of ATP-induced increases in P2X7
Invasion inhibition
[73]
A549
H1299
Lung adenocarcinoma 80 µmol/L Increased caspase 3 activation, TRIB3
expression
[74]
A549 Lung adenocarcinoma 30 to 100 µM/mL Arrest in G1 and G2/M phase
Loss of ∆Ψm
Increased release of cyt c
[75]
A549 Lung adenocarcinoma 10,15, and 20 µM Inhibition of p53 protein aggregates [76]
A549 Lung adenocarcinoma Emodin 10 μM
Paclitaxel 4 μM
Increased Bax and active caspase 3
expressions
Decreased Bcl-2, p-Akt, and p-ERK levels
[77]
A549 Lung adenocarcinoma 5 µM emodin, 5–10 µM cisplatin (A549)
2.5 µM emodin,
5–10 µM cisplatin (H460)
Increased DNA damage
Decreased Pgp expression
[79]
H460 Non-small human lung
carcinoma
NCI-H-520 Human bronchioloalveolar cell carcinoma 50 µM Inhibition of MTH1, arrest in G2/M
Increased expression of Bax, survivin, P-21, cleaved caspase 3, cleaved PARP (A549)
Decreased Bcl-2, p-65 NFκβ (A549)
Reduced integrin β1 and vimentin protein
expression (A549)
[81]
NCI-H-460 Non-small human lung
carcinoma
A-549 Lung adenocarcinoma
H1703 Lung squamous cell
carcinoma
60 μM Decreased levels of mitomycin C-derived Rad51 mRNA and protein [82]
A549 Lung adenocarcinoma
A549 Lung adenocarcinoma 30 µM Suppressed the secretion of HA
Augmented cells in G1/G0 phase and reduced cells in S and G2/M phase (A549)
Decreased cyclin A and B, increased cyclin C,D,E (A549)
[83]
H520 Human bronchioloalveolar cell carcinoma
H1975 Non-small cell lung
carcinoma
H1299 Lung adenocarcinoma
H460 Non-small human lung
carcinoma