Curcumenol is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities[2]. Curcumenol also remarkably enhanced myogenic differentiation and mitochondrial function[3]. Curcumenol diminishes the proinflammatory mediators and the expression of the regulatory genes in LPS-stimulated BV-2 by inhibiting Akt-dependent NF-κB activation and downregulation of Akt and p38 MAPKs signaling[4]. Curcumenol mitigated inflammation in ATDC5 chondrocytes and primary mice chondrocytes, and also ameliorated OA (osteoarthritis) in a DMM(destabilization of medial meniscus)‑induced mouse model[5].
Curcumenol/莪术烯醇 细胞实验
Cell Line
Concentration
Treated Time
Description
References
JIMT-1 cells
25, 50, 100 μg/mL
24 and 48 hours
Evaluate the effect of XLLXF on the proliferation of HER2-positive breast cancer cells, results showed that XLLXF dose-dependently inhibited the proliferation of JIMT-1 cells
Acta Biochim Biophys Sin (Shanghai). 2024 Mar 25;56(3):462-473.
SK-BR-3 cells
25, 50, 100 μg/mL
24 and 48 hours
Evaluate the effect of XLLXF on the proliferation of HER2-positive breast cancer cells, results showed that XLLXF dose-dependently inhibited the proliferation of SK-BR-3 cells
Acta Biochim Biophys Sin (Shanghai). 2024 Mar 25;56(3):462-473.
H460 cells
300 μg/ml
24 hours
To evaluate the antitumor potential of Curcumenol in lung cancer cells, results showed that Curcumenol significantly inhibited cell survival and proliferation, and induced ferroptosis.
Bioact Mater. 2021 Nov 19;13:23-36.
H1299 cells
300 μg/ml
24 hours
To evaluate the antitumor potential of Curcumenol in lung cancer cells, results showed that Curcumenol significantly inhibited cell survival and proliferation, and induced ferroptosis.
Bioact Mater. 2021 Nov 19;13:23-36.
Primary chondrocytes
50 µM
24 hours
To evaluate the inhibitory effect of curcumenol on TNF-α and IL-1β-induced inflammatory response, results showed that curcumenol inhibited the NF-κB and MAPK signaling pathways and decreased MMP3 expression levels.
Int J Mol Med. 2021 Oct;48(4):192.
ATDC5 chondrocytes
50 µM
24 hours
To evaluate the inhibitory effect of curcumenol on TNF-α and IL-1β-induced inflammatory response, results showed that curcumenol inhibited the NF-κB and MAPK signaling pathways and decreased MMP3 expression levels.
Int J Mol Med. 2021 Oct;48(4):192.
Rat primary NP cells
50 µM
24 hours
Evaluate the inhibitory effect of Curcumenol on TNFα-induced inflammatory response, results showed that Curcumenol could effectively inhibit TNFα-induced up-regulation of MMP family genes and down-regulation of Col2a1
Front Pharmacol. 2022 Jun 20;13:905966.
BV2 microglial cells
20 µM
24 hours
Evaluate the effect of Curcumenol on LPS-induced NO release, results showed no significant inhibitory effect of Curcumenol on NO release
Molecules. 2022 Jan 25;27(3):784.
BV2 microglial cells
20 µM
24 hours
To evaluate the effect of Curcumenol on NO release in LPS-stimulated BV2 cells, results showed no significant inhibitory effect of Curcumenol on NO release.
Molecules. 2022 Jan 25;27(3):784.
NP cell line
0, 12.5, 25, 50 µM
24, 48, 72 hours
Evaluate the cytotoxicity of Curcumenol on NP cell line, results showed that Curcumenol had little cytotoxicity in NP cell line and did not affect the proliferation rate of these cells
0.63 g/kg/d (low-dose group) and 0.95 g/kg/d (high-dose group)
Once daily for 17 weeks
Improve myocardial infarction, blood stasis, and blood lipid levels, and regulate the PI3K/AKT/mTOR signaling pathway
rhizome against coronary heart disease based on integrated network pharmacology, pharmacological evaluation and lipidomics. Front Pharmacol
BALB/c nude mice
Lung cancer subcutaneous xenograft model
Intravenous injection
200 mg/kg/day
Once daily, continuous treatment
To evaluate the antitumor efficacy of Curcumenol in vivo, results showed that Curcumenol significantly inhibited tumor growth, and its antitumor effect could be abolished by ferroptosis inhibitor DFO.
Bioact Mater. 2021 Nov 19;13:23-36.
C57/BL mice
DMM-induced osteoarthritis model
Intraperitoneal injection
4 mg/kg/time
Twice a week for 2 months
To evaluate the therapeutic effect of curcumenol on DMM-induced osteoarthritis, results showed that curcumenol alleviated cartilage degeneration by inhibiting TNF-α and IL-1β expression.
Int J Mol Med. 2021 Oct;48(4):192.
C57/BL mice
Lumbar spine instability mouse model
Intraperitoneal injection
4 mg/kg/time
Twice a week for one month
Evaluate the therapeutic effect of Curcumenol on lumbar spine instability-induced intervertebral disc degeneration, results showed that Curcumenol could effectively restore disc height and prevent disc degeneration
Front Pharmacol. 2022 Jun 20;13:905966.
BALB/c nude mice
HER2-positive breast cancer xenograft model
Oral gavage
5.26 mg/kg
Once daily for 4 weeks
Evaluate the inhibitory effect of XLLXF combined with trastuzumab on tumor growth in HER2-positive breast cancer xenograft model, results showed that the combination significantly inhibited tumor growth
Acta Biochim Biophys Sin (Shanghai). 2024 Mar 25;56(3):462-473.
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