Ferroptosis-centered Drug Response Information

General Information of the Drug (ID: ferrodrug0266)
Name
Erianin
Synonyms
Erianin; 95041-90-0; 2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)ethyl]phenol; 2-methoxy-5-(3,4,5-trimethoxyphenethyl)phenol; Phenol, 2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)ethyl]-; CHEMBL10557; 2-Methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-ethyl]-phenol; NSC613744; Dendrobium chrysotoxum; SCHEMBL1535646; DTXSID40326751; UXDFUVFNIAJEGM-UHFFFAOYSA-N; B817373-K388, same as; BCP07974; EX-A7098; HY-N0517; BDBM50005478; MFCD06795132; s9137; AKOS025401669; CCG-267683; NSC-613744; AC-24234; AS-78334; 3'-Hydroxy-3,4,4',5-tetramethoxybibenzyl; CS-0009056; FT-0686606; B817373-K346; 5-(3,4,5-trimethoxyphenethyl)-2-methoxyphenol; A851725; Q-100898; 7BA

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Structure
Formula
C18H22O5
IUPAC Name
2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)ethyl]phenol
Canonical SMILES
COC1=C(C=C(C=C1)CCC2=CC(=C(C(=C2)OC)OC)OC)O
InChI
InChI=1S/C18H22O5/c1-20-15-8-7-12(9-14(15)19)5-6-13-10-16(21-2)18(23-4)17(11-13)22-3/h7-11,19H,5-6H2,1-4H3
InChIKey
UXDFUVFNIAJEGM-UHFFFAOYSA-N
PubChem CID
356759
Full List of Ferroptosis Target Related to This Drug
Nuclear factor erythroid 2-related factor 2 (NFE2L2)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [1]
Target for Ferroptosis Marker/Suppressor
Responsed Disease Bladder cancer ICD-11: 2C94
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Glutathione metabolism hsa00480
Cell Process Cell ferroptosis
Cell proliferation
In Vitro Model RT4 cells Bladder carcinoma Homo sapiens CVCL_0036
KU-19-19 cells Bladder carcinoma Homo sapiens CVCL_1344
In Vivo Model
4-weeks-old female BALB/c nude mice aged were injected into 5 x 105 cells. Every 2 days mice weight and tumor size were assessed, and the tumor volume (V) was calculated with the formula: (maximum length) x (maximum width)2/2. Once tumors were found, the mice were stochastically divided into 2 groups: the control (PBS) group and the treatment (erianin 100 mg/kg) group. For 14 days, mice were injected intraperitoneally with drugs once a day, then puting the mice to death, after that tumors were taken for IHC (immunohistochemical) analysis.

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Response regulation Erianin inhibited cell proliferation and triggered cell death in bladder cancer cells. Mechanistically, we showed NRF2 was a key determinant for erianin-triggered ferroptosis. NRF2 activation by TBHQ treatment protected against erianin-induced cell death and increased the expression of GPX4, ferritin, xCT and glutaminase.
Unspecific Target
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [2]
Responsed Disease Lung cancer ICD-11: 2C25
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
Cell proliferation
Cell migration
In Vitro Model NCI-H460 cells Lung large cell carcinoma Homo sapiens CVCL_0459
NCI-H1299 cells Lung large cell carcinoma Homo sapiens CVCL_0060
In Vivo Model
H460-luc cells (2 x 106 cells in 0.1 ml phosphate-buffered saline) were subcutaneously injected into the right dorsal flank of 6-week-old female BALB/c nude mice; for the orthotopic xenograft lung tumor mouse model, a volume of 100 ul of cell suspension was injected into the right side of the lung. Tumor volume was assessed every 2 days.

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Response regulation Erianin could inhibit cell proliferation, promote G2/M-phase arrest, trigger ferroptosis, and suppress migration in lung cancer cells.
References
Ref 1 Natural Product Erianin Inhibits Bladder Cancer Cell Growth by Inducing Ferroptosis via NRF2 Inactivation. Front Pharmacol. 2021 Oct 29;12:775506. doi: 10.3389/fphar.2021.775506. eCollection 2021.
Ref 2 Erianin, a novel dibenzyl compound in Dendrobium extract, inhibits lung cancer cell growth and migration via calcium/calmodulin-dependent ferroptosis. Signal Transduct Target Ther. 2020 May 8;5(1):51. doi: 10.1038/s41392-020-0149-3.