Gomisin A from the fruit of Schisandra chinensis has many pharmacological properties, including hepato-protective, anti-diabetic, and anti-oxidative stress. Gomisin A inhibited reactive oxygen species production even in the SIPS-HDF (stress-induced premature senescence-human diploid fibroblast) cells. Gomisin A was also able to attenuate the activity of senescence-associated β-galactosidase and the production of pro-inflammatory molecules in the SIPS as well as aged HDF cells. In addition, gomisin A promoted the autophagy and mitochondrial biogenesis factors through the translocation of nuclear factor erythroid 2-related factor-2, and inhibited aging progression in the SIPS-HDF cells[3]. Using human liver microsomes, a reversible inhibition assay revealed that Gom A ( Gomisin A) was a competitive inhibitor with a KI value of 1.10 µM, and the time- and NADPH-dependent CYP3A inhibition of Gom A was observed in a time-dependent inhibition assay (KI = 0.35 µM, kinact = 1.96 min-1)[4]. Both oral and intraperitoneal administration of G.A (50 mg/kg) inhibited lung metastasis of CT26 cells. G.A (Gomisin A) significantly decreased the viability of various CRC (colorectal cancer) cell lines, whereas it did not change the proliferation of normal colon cells. Moreover, the migration and invasion of CRC cells were reduced by G.A treatment. Especially, G.A decreased matrix metalloproteinase (MMP)-2 and MMP-9 expressions and activities[5].
Schisandrol B/五味子醇乙 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse liver microsomes
2.5, 5, 10, 20, 40, 80 µM
10 minutes
To evaluate the inhibitory effect of SolB on APAP metabolic activation, results showed that SolB significantly inhibited the formation of NAPQI-GSH in a dose-dependent manner.
Toxicol Sci. 2015 Jan;143(1):107-15
MCF-7 cells
25 µM, 50 µM, 100 µM
144 hours
To evaluate the effect of Schisandrol B on the proliferation of MCF-7 cells. Results showed that Schisandrol B significantly promoted the proliferation of MCF-7 cells.
Pharmaceutics. 2021 Jul 15;13(7):1082
LO-2 cells
5, 10, 20, 40 µM
24 hours
To evaluate the protective effect of Schisandrol B on APAP-induced hepatocyte injury. Results showed that Schisandrol B dose-dependently improved cell viability and inhibited LDH release.
Front Pharmacol. 2021 Jun 3;12:655531.
INS-1 cells
1 µM, 2.5 µM, 5 µM
24 hours
To evaluate the effect of Schisandrol B on glucose-stimulated insulin secretion in INS-1 cells, results showed that Schisandrol B had no significant effect on GSIS.
Molecules. 2021 Oct 28;26(21):6509
HK-2 cells
10 µM
24 hours
To evaluate the protective effect of Schisandrol B on UA-injured HK-2 cells, results showed that Schisandrol B significantly improved cell viability and inhibited cell apoptosis.
Front Pharmacol. 2025 Apr 29;16:1563676
Huh7 cells
2.5, 10, and 40 µM
24 hours
To evaluate the effect of SolB on PXR-regulated gene expression. Results showed that SolB exhibited similar inducible effects on target genes in Huh7 cells as in HepG2 cells.
Br J Pharmacol. 2017 Apr;174(8):672-688
HepG2 cells
2.5, 10, and 40 µM
24 hours
To evaluate the effect of SolB on PXR-regulated gene expression. Results showed that SolB significantly and dose-dependently increased CYP3A4, UGT1A1, and OATP2 mRNA levels.
Br J Pharmacol. 2017 Apr;174(8):672-688
HEK293T cells
2.5, 10, and 40 µM
24 hours
To evaluate the effect of SolB on hPXR reporter gene activity. Results showed that SolB concentration-dependently enhanced hPXR reporter gene activity by 3.6-fold at 40μM.
Br J Pharmacol. 2017 Apr;174(8):672-688
HepG2 cells
2.5-20 µM
24 hours
To evaluate the effect of SolB on NRF2 activation, results showed that SolB dose-dependently increased the luciferase activity of the NRF2 reporter gene.
Acta Pharmacol Sin. 2016 Mar;37(3):382-9
CYP3A5*3/*3 genotyped HLMs
0-8 µM
30 minutes
Evaluate TDI of SZB on CYP3A4, showing kinact=0.37 min-1, KI=0.69 μM
Int J Mol Sci. 2022 Apr 19;23(9):4485
CYP3A5*1/*3 genotyped HLMs
0-16 µM
30 minutes
Evaluate TDI of SZB on CYP3A5, showing kinact=0.009 min-1, KI=0.5 μM
Int J Mol Sci. 2022 Apr 19;23(9):4485
Human liver microsomes (HLMs)
0-20 µM
30 minutes
Determine IC50 of SZB on CYP3A, showing time-dependent inhibition (IC50 shift=21.39)
Int J Mol Sci. 2022 Apr 19;23(9):4485
Human liver microsomes (HLM)
0.5-25 µM
60 minutes
To evaluate the reversible inhibition of Schisandrol B on CYP2C8-mediated metabolism of imatinib. Results showed that Schisandrol B strongly reversibly inhibited CYP2C8 enzyme.
Br J Clin Pharmacol. 2020 Oct;86(10):2080-2094
Recombinant CYP3A4 enzyme
0.5-25 µM
60 minutes
To evaluate the reversible inhibition of Schisandrol B on CYP3A4-mediated metabolism of imatinib and bosutinib. Results showed that Schisandrol B reversibly inhibited CYP3A4-mediated metabolism of imatinib and bosutinib.
Br J Clin Pharmacol. 2020 Oct;86(10):2080-2094
Schisandrol B/五味子醇乙 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
APAP-induced hepatotoxicity model
Oral
12.5, 50, 200 mg/kg/d
7 administrations with 12-hour intervals
To evaluate the protective effect of SolB against APAP-induced hepatotoxicity, results showed that SolB significantly reduced ALT and AST activities and decreased liver necrosis and hemorrhage in a dose-dependent manner.
Toxicol Sci. 2015 Jan;143(1):107-15
C57BL/6 mice
Acetaminophen (APAP)-induced acute hepatotoxicity model
Gavage
200 mg/kg/d
Every 12 hours, 7 times, for 3 days
To evaluate the protective effect of SolB against APAP-induced hepatotoxicity, results showed that SolB pretreatment significantly alleviated liver injury, increased nuclear accumulation of NRF2 and its downstream protein expression.
Acta Pharmacol Sin. 2016 Mar;37(3):382-9
SD rats
Allergic asthma model
Gavage
3.09 g/kg, 1.54 g/kg, and 0.77 g/kg
Once daily for 28 days
To evaluate the therapeutic effect of Schisandrol B on allergic asthma, the results showed that WSC was more effective than RSC at the same dose.
Chin Med. 2023 Jan 30;18(1):10
C57BL/6 mice
BDL and CCl4-induced hepatic fibrosis models
Gavage
40 mg/kg
Once daily for 14 days
To evaluate the inhibitory effect of Schisandrol B on BDL and CCl4-induced hepatic fibrosis. Results showed that Schisandrol B significantly alleviated hepatic injury and fibrosis and inhibited the expression of α-SMA.
Front Pharmacol. 2021 Jun 3;12:655531.
C57BL/6J mice
LCA-induced intrahepatic cholestasis model
Oral
6.25, 25, and 100 mg/kg
Twice daily for 7 days
To evaluate the protective effect of SolB against LCA-induced cholestatic liver injury. Results showed that SolB dose-dependently reversed LCA-induced increases in ALT, AST, and ALP, and significantly reduced serum TBA and Tbili levels. Additionally, SolB treatment significantly decreased mortality in cholestatic mice.
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