Curcumol, a pharmacologically active sesquiterpenoid, which is an imperative bioactive constituent of several plants mainly from genus Curcuma. Curcumol has potential to fight against cancer, oxidative stress, neurodegeneration, microbial infections, and inflammation. Curcumol has been documented as potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers[3]. Curcumol reduced the proliferation of CRC (colorectal cancer) cells through PTEN/PI3K/Akt by targeting miR-21 and miR-21 could be a target molecule of curcumol for CRC treatment[4]. Furthermore, curcumol evidently reduced cell proliferation and facilitated cell apoptosis in BGC-823/DDP and BGC-823 cells. Curcumol suppressed the PI3K/AKT pathway dose-dependently in BGC-823/DDP and BGC-823 cells[5]. Curcumol inhibits the expression of PD-L1 (programmed cell death-ligand 1) through crosstalk between HIF-1α and p-STAT3 (T705) signaling pathways in hepatic cancer[6]. Curcumol attenuated melanoma progression and concomitantly suppressed ERK/NF-κB signaling and promoted miR-152-3p expression to inactivate the c-MET/PI3K/AKT signaling pathway[7].
Curcumol/莪术醇 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LO2 cells
15, 30, 60 μM
24 h
Curcumol significantly alleviated PA-induced damage in LO2 cells, reduced lipid accumulation, and inhibited the expression of cellular senescence markers.
Cell Prolif. 2021 Sep;54(9):e13107.
primary microglia
0.1 g/L or 0.3 g/L
72 h
Curcumol treatment reduced the percentage of CD11b+Iba1+CD16+ and CD11b+Iba1+CD86+ M1 microglia and increased the percentage of CD11b+Iba1+CD163+ and CD11b+Iba1+CD206+ M2 microglia, indicating that Curcumol promoted anti-inflammatory M2 microglial polarization.
Cell Death Discov. 2024 Jun 24;10(1):300.
C666-1 cells
100 µg/mL
24 h
To investigate the inhibitory effect of Curcumol on nasopharyngeal carcinoma cells, the results showed that Curcumol significantly inhibited the invasion and migration of C666-1 cells.
Biomolecules. 2024 Sep 9;14(9):1142.
Primary microglia
0.1 g/L or 0.3 g/L
72 h
Curcumol induced anti-inflammatory M2 microglial polarization, reduced the production of pro-inflammatory cytokines, and protected neurons from apoptosis.
Cell Death Discov. 2024 Jun 24;10(1):300.
K7M2 WT cells
0-500 nM
72 h
Curcumol inhibited K7M2 WT cell proliferation in a dose-dependent manner
Molecules. 2022 Jul 6;27(14):4345.
K7M2 WT cells
100 nM
48 h
Curcumol combined with CDDP significantly increased apoptosis in K7M2 WT cells
Molecules. 2022 Jul 6;27(14):4345.
U2OS cells
37.67 nM
72 h
Curcumol combined with CDDP significantly inhibited U2OS cell proliferation
Molecules. 2022 Jul 6;27(14):4345.
MG63 cells
41.41 nM
72 h
Curcumol combined with CDDP significantly inhibited MG63 cell proliferation
Molecules. 2022 Jul 6;27(14):4345.
KHOS cells
28.3 nM
72 h
Curcumol combined with CDDP significantly inhibited KHOS cell proliferation
Molecules. 2022 Jul 6;27(14):4345.
HSC-LX2 cells
30 μM
24 h
Curcumol upregulates the phosphorylation levels of RIPK1 and RIPK3, promotes their aggregation to form necrosome in HSCs, and eventually induces HSC necroptosis.
Redox Biol. 2018 Oct;19:375-387.
LO2 cells
15, 30, 60 μM
24 h
Curcumol was capable of ameliorating ethanol-induced cell damage and effectively suppressed ethanol-induced lipid accumulation and cellular senescence in LO2 cells.
Front Pharmacol. 2022 Jun 28;13:912825.
Curcumol/莪术醇 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
LVG Golden Syrian hamsters
High-fat diet-induced NAFLD model
Oral gavage
15, 30, 60 mg/kg
Once daily for 4 weeks
Curcumol significantly improved liver injury and steatosis induced by a high-fat diet and inhibited hepatocyte senescence.
Cell Prolif. 2021 Sep;54(9):e13107.
Rats
Sprague Dawley (SD) rats
Oral and intravenous
10, 40, 80 mg/kg (oral), 2.0 mg/kg (intravenous)
Single dose
To investigate the pharmacokinetics, tissue distribution, and plasma protein binding rate of curcumol in rats. Results indicated that curcumol was rapidly absorbed and eliminated in rats, with oral bioavailability ranging from 9.2% to 13.1%. The maximum concentration of curcumol was observed in most organs within 0.5-1.0 hours, with high accumulation in the small intestine, colon, liver, and kidney. The plasma protein binding rate ranged from 85.6% to 93.4%.
Front Pharmacol. 2022 Nov 30;13:1036732
C57BL/6 mice
Middle cerebral artery occlusion (MCAO) model
Intraperitoneal injection
0.1 g/kg or 0.3 g/kg
Once daily for 7 days
Curcumol treatment reduced infarct volume, attenuated neuronal damage and inflammation, and improved motor function recovery in MCAO mice. Curcumol also promoted anti-inflammatory M2 microglial polarization in vivo and reduced local T cell infiltration, impairing the Treg/Th17 balance.
Cell Death Discov. 2024 Jun 24;10(1):300.
BALB/c nude mice
Nasopharyngeal carcinoma xenograft model
Gavage
80 mg/kg
Once daily for 2 weeks
To investigate the inhibitory effect of Curcumol on nasopharyngeal carcinoma xenografts in vivo, the results showed that Curcumol significantly inhibited tumor growth and reduced the expression of UBE2C.
Biomolecules. 2024 Sep 9;14(9):1142.
C57BL/6 mice
Middle cerebral artery occlusion (MCAO) model
Intraperitoneal injection
0.1 g/kg or 0.3 g/kg
Once daily for 7 days
Curcumol reduced infarct volume, attenuated neuronal damage and neuroinflammation, and improved motor function recovery in MCAO mice. Additionally, Curcumol promoted anti-inflammatory M2 microglial polarization and modulated Treg/Th17 balance.
Cell Death Discov. 2024 Jun 24;10(1):300.
BALB/c mice
K7M2 WT orthotopic transplantation model
Curcumol: oral, CDDP: intraperitoneal
30 mg/kg
Curcumol: daily, CDDP: once per week, for 31 days
Curcumol combined with CDDP significantly inhibited tumor growth and reduced M2-type macrophage recruitment
Molecules. 2022 Jul 6;27(14):4345.
ICR mice
CCl4-induced liver fibrosis model
Intraperitoneal injection
15, 30, 60 mg/kg
Every other day for 5-8 weeks
Curcumol ameliorates CCl4-induced liver fibrosis in mice by inducing RIPK1/RIPK3 complex-dependent necroptosis.
Redox Biol. 2018 Oct;19:375-387.
C57BL/6J mice
Alcoholic fatty liver disease model
Oral
30, 45, 60 mg/kg
Once daily for 30 days
Curcumol alleviated ethanol-induced liver injury and lipid deposition, and effectively inhibited hepatocyte senescence.
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