β-Sitosterol (beta-sitosterol, BS), a plant derived nutrient with anticancer properties against breast cancer, prostate cancer, colon cancer, lung cancer, stomach cancer, ovarian cancer, and leukemia[3]. β-sitosterol significantly ameliorated HFWD(high-fat western-style diet)-induced fatty liver and metabolic abnormalities, including elevated levels of hepatic total lipids, triacylglycerols, cholesterol and liver histopathology. It decreased the levels of intestinal bile acids, accompanied by markedly increased fecal lipid levels.β-Sitosterol was less effective in affecting most of these parameters[4]. β-sitosterol protected against in vitro H/R(hypoxia/reoxygenation)-induced cardiomyocyte injury and in vivo myocardial I/R (ischemia/reperfusion) injury[5]. The combination of β-sitosterol and naringenin exerted a synergistic effect on wound closure without decreasing the viability of fibroblasts, increased antioxidant defense mechanism and decreased IL-β[6].
β-Sitosterol/β-谷甾醇 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone marrow-derived macrophages (BMDMs)
5, 25, 50 µM
1 day
To investigate the effect of BS on macrophage polarization. Results showed that BS significantly repressed M1 polarization and augmented M2 polarization. In 25 μM BS-treated M1-polarized BMDMs, the expression of iNOS, IL-1β, CD86, and MHCII was reduced by 50.2%, 47.1%, 87.1%, and 31.3%, respectively, while in 25 μM BS-treated M2-polarized BMDMs, the expression of arginase-1, IL-10, CD163, and CD206 was increased by 65.6%, 107.4%, 23.5%, and 51.3%, respectively.
Pharm Biol. 2019 Dec;57(1):161-168
CHO-CCK1R-W166A cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK1R W166A mutant, results showed that 100 μM β-sitosterol had no effect on CCK signaling.
Clin Nutr. 2016 Dec;35(6):1374-1379
CHO-CCK1R-Y237A cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK1R Y237A mutant, results showed that 100 μM β-sitosterol had no effect on CCK signaling.
Clin Nutr. 2016 Dec;35(6):1374-1379
CHO-CCK1R-Y140A cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK1R Y140A mutant, results showed that 100 μM β-sitosterol had no effect on CCK signaling.
Clin Nutr. 2016 Dec;35(6):1374-1379
CHO-CCK2R cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK2R function, results showed that 100 μM β-sitosterol had no significant impact on CCK2R function.
Clin Nutr. 2016 Dec;35(6):1374-1379
SRD15-CCK1R cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK1R signaling in a high cholesterol environment, results showed that 100 μM and 10 μM β-sitosterol significantly improved the defective signaling of CCK1R.
Clin Nutr. 2016 Dec;35(6):1374-1379
CHO-CCK1R cells
100 µM
15 minutes
To study the effect of β-sitosterol on CCK1R signaling in a high cholesterol environment, results showed that 100 μM and 10 μM β-sitosterol significantly improved the defective signaling of CCK1R.
Clin Nutr. 2016 Dec;35(6):1374-1379
CuFi-1 cells
100 nM
16 hours
Β-Sitosterol significantly inhibited P. aeruginosa-induced expression of IL-8, GRO-α, and GRO-β
Front Pharmacol. 2017 May 12;8:236
IB3-1 cells
100 nM
16 hours
Β-Sitosterol significantly inhibited P. aeruginosa-induced expression of IL-8, GRO-α, and GRO-β
Front Pharmacol. 2017 May 12;8:236
HEK293 cells
150–450 μg/mL
24 hours
Inhibited TNF-α or IAV-induced NF-κB activation
Acta Pharmacol Sin. 2020 Sep;41(9):1178-1196
A549 cells
150–450 μg/mL
24 hours
Suppressed inflammatory response in IAV-infected cells via NF-κB and p38 MAPK signaling, reducing pro-inflammatory cytokines and chemokines
Acta Pharmacol Sin. 2020 Sep;41(9):1178-1196
Bovine mammary epithelial cells (MAC-T)
1 µM
24 hours
Β-Sitosterol significantly reduced LPS-induced oxidative stress and inflammation, while increasing the expression of anti-apoptotic proteins and activating the HIF-1α/mTOR signaling pathway to inhibit apoptosis and improve lipid synthesis-related gene expression
Int J Mol Sci. 2023 Sep 27;24(19):14644
293 T cells
5 μg/mL, 10 μg/mL, 20 μg/mL
24, 48, 72 hours
No significant effect on cell viability
Hum Cell. 2024 Jul;37(4):1156-1169.
HCCLM3 cells
5 μg/mL, 10 μg/mL, 20 μg/mL
24, 48, 72 hours
Inhibited cell viability and proliferation
Hum Cell. 2024 Jul;37(4):1156-1169.
Huh-7 cells
5 μg/mL, 10 μg/mL, 20 μg/mL
24, 48, 72 hours
Inhibited cell viability and proliferation
Hum Cell. 2024 Jul;37(4):1156-1169.
U87 cells
0, 10, 20, 30, 40, 50 µM
24, 48, 72 hours
Β-Sitosterol significantly inhibited the proliferation and viability of U87 cells, with IC50 values of 35.82 μM at 24 h, 31.75 μM at 48 h, and 9.43 μM at 72 h.
Acta Biochim Biophys Sin (Shanghai). 2024 Feb 25;56(2):223-238
MDCK cells
0.975 µg/mL
3 days
Evaluate the in vitro antiviral activity of β-Sitosterol against A/H1N1 virus, showing significant antiviral effects
Vaccines (Basel). 2023 Jan 19;11(2):228
Vascular Smooth Muscle Cells (VSMCs)
5, 10, 20 µM
30 minutes
Inhibited oxLDL-induced lipid deposition and phenotypic transformation in VSMCs
Heliyon. 2024 Aug 2;10(15):e35639
C2C12 myotubes
0.5 mM
48 hours
To evaluate the protective effect of β-sitosterol on dexamethasone-induced muscle atrophy. Results showed that β-sitosterol increased myotube width, restored the fusion index, and reduced the expression of MAFbx and MuRF1.
Nutrients. 2022 Jul 14;14(14):2894
Huh7 cells
8.71±0.21 µg/mL (IC50)
48 hours
Β-Sitosterol significantly reduced Huh7 cell viability and induced apoptosis via caspase pathway activation
Molecules. 2020 Jul 2;25(13):3021
HepG2 cells
6.85±0.61 µg/mL (IC50)
48 hours
Β-Sitosterol inhibited HepG2 cell proliferation in a dose-dependent manner, induced apoptosis and activated caspase-3 and -9
Molecules. 2020 Jul 2;25(13):3021
β-Sitosterol/β-谷甾醇 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
Depression model (TST and FST)
Intraperitoneal injection
0.1–100 mg/kg
Single administration, tested after 60 minutes
To evaluate the antidepressant effects of β-sitosterol and its derivatives. Results showed that Sit-S (4 mg/kg) exhibited the strongest antidepressant-like activity in the TST, mediated by the 5-HT, DA, and GABAergic systems.
RSC Adv. 2018 Jan 2;8(2):671-680
Mice
High-fat western-style diet-induced NAFLD model
Dietary intake
0.4% diet
17 weeks
To investigate the effects of β-sitosterol on alleviating HFWD-induced NAFLD. Results showed that β-sitosterol significantly ameliorated HFWD-induced fatty liver and metabolic abnormalities, including decreased levels of hepatic total lipids, triacylglycerols, cholesterol and improved liver histopathology.
After 1 week of feeding, treated with 1.5% DSS in drinking water for 5 days
Β-Sitosterol significantly inhibited colon shortening, lowered fecal hemoglobin contents, and reduced the severity of colitis in the middle and distal colon.
Food Funct. 2017 Nov 15;8(11):4179-4186
Adult male Wistar rats
Nitroglycerin-induced migraine model
Intraperitoneal injection
10 mg/kg
Daily for 10 days
Β-Sitosterol significantly improved anxiety behaviors in migraine-induced rats by alleviating oxidative/nitrosative stress and enhancing mitochondrial function.
CNS Neurosci Ther. 2024 Sep;30(9):e14892
Mice
Anxiety model
Intraperitoneal injection and oral gavage
100 mg/kg
1 hour before testing
Β-Sitosterol shows anxiolytic effects when administered alone and in combination with the SSRI fluoxetine
Cell Rep Med. 2021 May 18;2(5):100281
Wistar rats
Trypanosoma congolense infection model
Oral
15 and 30 mg/kg
Daily administration for 14 days
Β-Sitosterol significantly reduced parasitemia, ameliorated parasite-induced anemia, and significantly down-regulated the expression of TconTS1 gene.
Front Microbiol. 2023 Sep 27;14:1282257
C57BL/6 mice
70% hepatectomy model
Dietary supplementation
20 mg/kg/day
Once daily until 72 hours post-surgery
To verify the promoting effect of β-sitosterol diet on liver regeneration, results showed that β-sitosterol significantly enhanced liver regeneration rate and accelerated TRAS resolution.
Int J Nanomedicine. 2024 Aug 8;19:8117-8137
C57BL/6 mice
Collagen-induced arthritis (CIA) model
Intraperitoneal injection
20 or 50 mg/kg
Every 2 days until the end of the experiment
To evaluate the therapeutic effect of BS on CIA. Results showed that BS treatment significantly alleviated ankle swelling (vehicle group: 3.13 ± 0.102 mm; 20 mg/kg BS group: 2.64 ± 0.043 mm; 50 mg/kg BS group: 2.36 ± 0.084 mm), reduced the levels of collagen-specific antibodies (IgG and IgG1, but not IgG2c, p<0.05) and pro-inflammatory cytokines (p<0.05), and increased the level of anti-inflammatory cytokine IL-10.
Pharm Biol. 2019 Dec;57(1):161-168
C57BL/6 mice
Dexamethasone-induced muscle atrophy model
Oral
200 mg/kg
Once daily for 3 weeks
To evaluate the protective effect of β-sitosterol on dexamethasone-induced muscle atrophy. Results showed that β-sitosterol protected mice from muscle mass loss, increased the thickness of gastrocnemius muscle fibers, restored grip strength and creatine kinase activity, and reduced the expression of MAFbx and MuRF1.
Nutrients. 2022 Jul 14;14(14):2894
ApoE−/− mice
High-fat diet-induced atherosclerosis model
Oral
25, 50, 100 mg/kg
Once daily for 1 month
Β-Sitosterol alleviates atherosclerosis by regulating CAT and inhibiting the PI3K/Akt/mTOR signaling pathway
Heliyon. 2024 Aug 2;10(15):e35639
Red swamp crayfish (Procambarus clarkii)
White spot syndrome virus (WSSV) infection model
Intraperitoneal injection
50 mg/kg
Single injection, observed up to 72 hours
Β-Sitosterol significantly inhibited WSSV replication, reduced viral gene transcription levels, and increased the survival rate of infected crayfish (57.14%).
Int J Mol Sci. 2022 Sep 9;23(18):10448
BALB/c mice
Influenza A virus-induced acute lung injury model
Intragastric
50, 200 mg/kg/day
Once daily for 2 days
Ameliorated IAV-mediated recruitment of pathogenic cytotoxic T cells and immune dysregulation, protected mice from lethal IAV infection
Acta Pharmacol Sin. 2020 Sep;41(9):1178-1196
Zebrafish (Danio rerio)
CuSO4-induced inflammation model
Immersion
70 or 100 μg/mL
Pretreatment for 1 h followed by exposure to CuSO4 for 20 min or 1 h
Β-Sitosterol significantly reduced CuSO4-induced oxidative stress, upregulated the expressions of sod and gpx4b, and inhibited neutrophil migration and the expressions of inflammatory genes il-8 and myd88.
Antioxidants (Basel). 2023 Feb 6;12(2):391
C57BL/6 mice
U87 xenograft nude mouse model
Intraperitoneal injection
80 mg/kg
Once daily for 28 days
Β-Sitosterol significantly inhibited tumor growth, reducing the average tumor size from 1282.164±221.869 mm3 in the control group to 113.126±81.405 mm3 in the β-sitosterol group, and the mean tumor weight from 0.899±0.180 g to 0.054±0.033 g.
Acta Biochim Biophys Sin (Shanghai). 2024 Feb 25;56(2):223-238
C57BL/6 mice
S. pneumoniae infection model
Subcutaneous injection
80 mg/kg
Treatment started 1 hour after infection, every 4 hours for 48 hours
To evaluate the protective effect of β-sitosterol against S. pneumoniae infection, results showed that β-sitosterol significantly reduced mortality and alleviated pulmonary inflammation in mice.
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