Inhibited LPS-induced iNOS, TNF-α, and COX-2 expression by suppressing I-κBα phosphorylation, p65 nuclear translocation, and C/EBP and/or AP-1 activation
Br J Pharmacol. 2003 May;139(1):11-20
Raw264.7 cells
1–30 µM
1–18 hours
Sauchinone inhibited LPS-inducible iNOS, TNF-α, and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation and of C/EBP and/or AP-1 activation.
Br J Pharmacol. 2003 May;139(1):11-20
Human dermal fibroblasts
1 µM
12 days
Restored mitochondrial function and reduced ROS levels
Antioxidants (Basel). 2025 Feb 24;14(3):259
Human dermal fibroblasts
1 µM
12 days
To evaluate the effect of Sauchinone on cell proliferation, results showed 1 µM Sauchinone significantly increased cell proliferation
Antioxidants (Basel). 2025 Feb 24;14(3):259
Human dermal fibroblasts
4 µM
12 days
To evaluate the effect of Sauchinone on mitochondrial ROS levels, results showed Sauchinone significantly reduced mitochondrial ROS levels
Antioxidants (Basel). 2025 Feb 24;14(3):259
HepG2 cells
30 µM
12-24 hours
Sauchinone significantly increased the mRNA and protein levels of GCL and NQO1, indicating its ability to induce antioxidant and cytoprotective enzymes.
Br J Pharmacol. 2011 Aug;163(8):1653-65
HepG2 cells
30 µM
12-24 hours
Sauchinone significantly increased the mRNA and protein levels of GCL and NQO1, indicating its induction of antioxidant enzymes via activation of the Nrf2 pathway.
Br J Pharmacol. 2011 Aug;163(8):1653-65
Human liver microsomes (HLMs)
0-200 µM
15 or 60 minutes
Evaluated the inhibitory effect of Sauchinone on UGT1A1, 1A3, 1A6, and 2B7 activities, with IC50 values of 8.83, 43.9, 0.758, and 0.279 μM, respectively
Molecules. 2018 Feb 9;23(2):366
Human liver microsomes (HLMs)
0-200 µM
15 or 60 minutes
Evaluate the inhibitory effect of Sauchinone on UGT1A1, 1A3, 1A6, and 2B7 activities, with IC50 values of 8.83, 43.9, 0.758, and 0.279 μM respectively
Molecules. 2018 Feb 9;23(2):366
Microglial BV-2 cells
1, 5, and 10 µM
24 hours
Inhibited LPS-induced inflammatory responses, reduced ROS and NO generation, and decreased iNOS and COX-2 expression
J Neuroinflammation. 2014 Jul 2;11:118
Astrocytes
1, 5, and 10 µM
24 hours
Inhibited LPS-induced inflammatory responses, reduced ROS and NO generation, and decreased iNOS and COX-2 expression
J Neuroinflammation. 2014 Jul 2;11:118
Microglial BV-2 cells
1, 5, and 10 µM
24 hours
To investigate the inhibitory effect of ent-Sauchinone on LPS-induced inflammatory responses, results showed that ent-Sauchinone significantly reduced ROS and NO generation and iNOS and COX-2 expression.
J Neuroinflammation. 2014 Jul 2;11:118
Astrocytes
1, 5, and 10 µM
24 hours
To investigate the inhibitory effect of ent-Sauchinone on LPS-induced inflammatory responses, results showed that ent-Sauchinone significantly reduced ROS and NO generation and iNOS and COX-2 expression.
J Neuroinflammation. 2014 Jul 2;11:118
Mouse primary hepatocytes
10, 100 µM
24 hours
Sauchinone inhibits PCSK9 expression in mouse primary hepatocytes.
Sci Rep. 2018 Apr 30;8(1):6737
HepG2 cells
10, 20, 100 µM
24 hours
Sauchinone regulates cholesterol metabolism by downregulating PCSK9 expression and upregulating LDLR expression, thereby increasing LDL-C uptake.
Evaluation of reversible inhibition of Sauchinone on CYP2B6, 2C19, 2E1, and 3A4, showing non-competitive inhibition with Ki values of 14.3, 16.8, 41.7, and 6.84 μM, respectively
Molecules. 2018 Mar 2;23(3):555
Human liver microsomes (HLMs)
0-300 µM
30 minutes
Sauchinone reversibly inhibited CYP2B6, 2C19, 2E1, and 3A4 activities with Ki values of 14.3, 16.8, 41.7, and 6.84 μM, respectively.
Molecules. 2018 Mar 2;23(3):555
Human liver microsomes
0-300 µM
30 minutes pre-incubation, 10 minutes incubation
Evaluation of time-dependent inhibition of Sauchinone on CYP2B6, 2E1, and 3A4, with IC50 shifts of 9.28, 20.9, and 21.4-fold, respectively
Molecules. 2018 Mar 2;23(3):555
Human liver microsomes (HLMs)
0-300 µM
30-min pre-incubation
Sauchinone time-dependently inhibited CYP2B6, 2E1, and 3A4 activities with IC50 shifts of 9.28, 20.9, and 21.4-fold, respectively.
Molecules. 2018 Mar 2;23(3):555
Human renal mesangial cells
0.1–1 µM
48 hours
To investigate the effect of Sauchinone on AngII-induced proliferation of renal mesangial cells. Results showed that Sauchinone inhibited AngII-induced cell proliferation in a dose-dependent manner.
Int J Mol Sci. 2020 Sep 23;21(19):7003
MTV/TM-011 cells
12.5, 25, 50 µM
48 hours
To evaluate the effect of sauchinone on cell viability, results showed that sauchinone significantly inhibited the viability of breast cancer cells in a dose-dependent manner.
Biosci Rep. 2021 Oct 29;41(10):BSR20211067
MDA-MB-231 cells
12.5, 25, 50 µM
48 hours
To evaluate the effect of sauchinone on cell viability, results showed that sauchinone significantly inhibited the viability of breast cancer cells in a dose-dependent manner.
Biosci Rep. 2021 Oct 29;41(10):BSR20211067
Human renal mesangial cells
0.1–1 µM
48 hours
To investigate the effect of Sauchinone on AngII-induced proliferation of renal mesangial cells. Results showed that Sauchinone inhibited AngII-induced cell proliferation in a dose-dependent manner.
Int J Mol Sci. 2020 Sep 23;21(19):7003
MTV/TM-011 cells
12.5, 25, 50 µM
48 hours
To evaluate the effect of sauchinone on breast cancer cell viability. Results showed that sauchinone significantly inhibited the viability of breast cancer cells in a dose-dependent manner.
Biosci Rep. 2021 Oct 29;41(10):BSR20211067
MDA-MB-231 cells
12.5, 25, 50 µM
48 hours
To evaluate the effect of sauchinone on breast cancer cell viability. Results showed that sauchinone significantly inhibited the viability of breast cancer cells in a dose-dependent manner.
Biosci Rep. 2021 Oct 29;41(10):BSR20211067
MCF-10A cells
25, 50 µM
72 hours
To evaluate the effect of sauchinone on normal breast cell viability. Results showed that sauchinone at 25 and 50 μM concentrations did not significantly affect the viability of MCF-10A cells.
Biosci Rep. 2021 Oct 29;41(10):BSR20211067
Sauchinone/三白草酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Myocardial ischemia/reperfusion injury model
Intraperitoneal injection
10 mg/kg
Single dose, lasted until the end of the experiment
To investigate the protective effect of Sauchinone against myocardial ischemia/reperfusion injury and its mechanism. Results showed that Sauchinone significantly reduced the infarct size and inhibited the phosphorylation of p38 and JNK, but had no effect on the phosphorylation of ERK1/2, Akt, and GSK-3β.
J Korean Med Sci. 2012 May;27(5):572-5
Rats
Myocardial ischemia/reperfusion injury model
Intraperitoneal injection
10 mg/kg
Single dose, lasting until 2 hours after reperfusion
To investigate the protective effect of Sauchinone against myocardial ischemia/reperfusion injury and its mechanism. Results showed that Sauchinone significantly reduced the infarct size and inhibited the phosphorylation of p38 and JNK, but had no effect on the phosphorylation of ERK1/2, Akt, and GSK-3β.
J Korean Med Sci. 2012 May;27(5):572-5
Mice
ICR mice
Oral
100 mg/kg
Single dose
Co-administration with sauchinone increased systemic exposure of sibutramine, clopidogrel, and chlorzoxazone by 23.6%, 31.0%, and 61.1%, respectively.
Evaluate the inhibitory effect of Sauchinone on UGT2B7-mediated zidovudine metabolism, results showed Sauchinone increased systemic exposure of zidovudine
Molecules. 2018 Feb 9;23(2):366
ICR mice
High-fat diet-induced obese mouse model
Oral
100 mg/kg/day
Once daily for 15 days
Sauchinone increases hepatic LDLR expression through PCSK9 inhibition, reduces serum LDL-C levels, and improves hepatic steatosis and lipid metabolism in high-fat diet-induced obese mice.
Pretreatment with sauchinone significantly inhibited the increase in plasma ALT, AST, and LDH activities caused by APAP and reduced hemorrhage and necrosis in the central area of the liver, indicating its protective effect against APAP-induced liver injury. This effect was abolished in Nrf2 knockout mice, demonstrating its dependence on Nrf2 activation.
Br J Pharmacol. 2011 Aug;163(8):1653-65
Mice
APAP-induced liver injury model
Oral
30 mg/kg
Once daily for 3 days
Sauchinone pretreatment significantly reduced the increase in plasma ALT, AST, and LDH activities induced by APAP and alleviated histopathological liver damage. These protective effects were absent in Nrf2 knockout mice, indicating that sauchinone exerts hepatoprotective effects via the Nrf2 pathway.
Br J Pharmacol. 2011 Aug;163(8):1653-65
C57BL/6 mice
DSS-induced ulcerative colitis model
Intragastric administration
Low-dose (5 μg/g), middle-dose (10 μg/g), and high-dose (20 μg/g)
Once every 2 days until the end of the experiment
Sauchinone alleviated pathological symptoms, inhibited inflammation, and prevented mucosal barrier damage in DSS-induced UC mice. It also inhibited the NF-κB pathway by upregulating NQO1. Additionally, sauchinone regulated the diversity and composition of the gut microbiota in mice.
Evaluate the therapeutic effect of sauchinone on DSS-induced ulcerative colitis, results showed that sauchinone alleviated pathological symptoms, inhibited inflammation, and prevented mucosal barrier damage.
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