Aur, Auranofin: Click to Expand ⟱
Features:
Auranofin is a synthetic gold(I) complex originally developed for the treatment of rheumatoid arthritis. Its structure features a gold atom coordinated with triethylphosphine and a thiolate ligand derived from a sugar (often referred to as a thiosugar).

Pathways:
1.Thioredoxin Reductase (TrxR) Inhibition.
- Most widely recognized for potently inhibiting TrxR.
2.Induction of Reactive Oxygen Species (ROS) and Oxidative Stress.
3.MMP depolarization, release of cytochrome c
4.Endoplasmic Reticulum (ER) Stress and Unfolded Protein Response (UPR)
5.Inhibition of Pro-survival Pathways (e.g., NF-κB Signaling)

-ic50 for cancer typically 1-3uM, normal cell 5-10uM or higher.
-Several studies animal testing antitumor efficacy have used doses in the region of 5–8 mg/kg via intraperitoneal injection or oral administration.

-Auranofin’s anticancer activity is often linked to its inhibition of thioredoxin reductase, leading to increased oxidative stress.
Scientific Papers found: Click to Expand⟱
1900- Aur,    Potential Anticancer Activity of Auranofin
- Review, Var, NA
TrxR↓, Auranofin inhibits the activity of thioredoxin reductase (TrxR
ROS↑, TrxR inhibition leads to an increase in cellular oxidative stress and induces apoptosis
Apoptosis↓,
TumCP↓, TrxR1 knockdown also inhibits cancer cell proliferation and DNA replication
eff↑, cytotoxicity of cisplatin is increased in cells expressing high levels of TrxR1 compared with cells expressing low levels

2951- PL,  Aur,    Synergistic Dual Targeting of Thioredoxin and Glutathione Systems Irrespective of p53 in Glioblastoma Stem Cells
- in-vitro, GBM, U87MG
GSH↓, natural product piperlongumine (PPL) inhibit the GSH system.
eff↑, subsequent efficacy of PLL in combination with Au within a nanomolar range in GSCs. Auranofin (Au), a known TrxR1 inhibitor
GSTP1/GSTπ↓, PPL is a natural alkaloid found in the plant Piper longum Linn that directly inhibits GSTP-1 and exhibits anti-cancer properties

1459- SFN,  Aur,    Auranofin Enhances Sulforaphane-Mediated Apoptosis in Hepatocellular Carcinoma Hep3B Cells through Inactivation of the PI3K/Akt Signaling Pathway
- in-vitro, Liver, Hep3B - in-vitro, Liver, HepG2
eff↑, sulforaphane significantly enhanced auranofin-induced apoptosis by inhibiting TrxR activity and cell proliferation compared to either single treatment
TumCCA↑, Sub-G1 cells
Apoptosis↑,
MMP↓,
BAX↑,
cl‑PARP↑,
Casp3↑,
Casp8↑,
Casp9↑,
ROS↑, combined treatment induced excessive generation of reactive oxygen species (ROS)
eff↓, treatment with N-acetyl-L-cysteine, a ROS scavenger, reduced combined treatment-induced ROS production and apoptosis.
PI3K↓,
Akt↓,
TrxR↓, treatment with either sulforaphane or auranofin alone at low concentrations weakly inhibit TrxR activity Combined treatment significantly reduced TrxR activity and cell viability
BAX↑,
Bcl-2∅,


* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 3

Results for Effect on Cancer/Diseased Cells:
Akt↓,1,   Apoptosis↓,1,   Apoptosis↑,1,   BAX↑,2,   Bcl-2∅,1,   Casp3↑,1,   Casp8↑,1,   Casp9↑,1,   eff↓,1,   eff↑,3,   GSH↓,1,   GSTP1/GSTπ↓,1,   MMP↓,1,   cl‑PARP↑,1,   PI3K↓,1,   ROS↑,2,   TrxR↓,2,   TumCCA↑,1,   TumCP↓,1,  
Total Targets: 19

Results for Effect on Normal Cells:

Total Targets: 0

Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:273  Target#:%  State#:%  Dir#:%
  wNotes=on  sortOrder:rid,rpid

 

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