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  3. Saringosterol

Saringosterol is an orally active steroid found in Sargassum muticum. Saringosterol is a LXR agonist. Saringosterol can lower cholesterol levels and inhibit the mRNA and protein expression of peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT enhancer-binding protein α (C/EBPα). Saringosterol has anti-obesity, anti-atherosclerosis, anti-Mycobacterium tuberculosis and anti-depressant activities.

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Saringosterol

Saringosterol Chemical Structure

CAS No. : 6901-60-6

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Description

Saringosterol is an orally active steroid found in Sargassum muticum. Saringosterol is a LXR agonist. Saringosterol can lower cholesterol levels and inhibit the mRNA and protein expression of peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT enhancer-binding protein α (C/EBPα). Saringosterol has anti-obesity, anti-atherosclerosis, anti-Mycobacterium tuberculosis and anti-depressant activities[1][2][3][4].

IC50 & Target[1]

PPARγ

 

Cellular Effect
Cell Line Type Value Description References
J774 IC50
> 233.3 μM
Compound: 14
Cytotoxicity against mouse J774 cells by alamar blue assay
Cytotoxicity against mouse J774 cells by alamar blue assay
[PMID: 17637068]
Vero IC50
> 128 μg/mL
Compound: Saringosterol
Cytotoxicity against african green monkey Vero cells by celltiter 96 aqueous nonradioactive assay
Cytotoxicity against african green monkey Vero cells by celltiter 96 aqueous nonradioactive assay
[PMID: 11720535]
In Vitro

Saringosterol (12.5-200 μM; 24 h) does not reduce the viability of 3T3-L1 cells[1].
Saringosterol (50-200 μM; 8 days) dose-dependently inhibits lipid and triglyceride accumulation in 3T3-L1 preadipocytes, with 200 μM reducing accumulation to 26.6% of control differentiated cells[1].
Saringosterol (50-200 μM; 24 h) dose-dependently increases glycerol release from 3T3-L1 adipocytes, with 200 μM inducing a statistically significant elevation[1].
Saringosterol (100-200 μM; 8 days) significantly reduces mRNA and protein expression of PPARγ and C/EBPα in 3T3-L1 cells[1].
Saringosterol (100-200 μM; 8 days) significantly reduces mRNA expression of adipogenic marker genes (aP2, adiponectin, resistin, and FAS) in 3T3-L1 cells[1].
Saringosterol (20 μM; 24 h) increases mRNA expression of LXR-regulated cholesterol transport/uptake genes (ABCA1, ABCG1, and IDOL) and reduces cellular cholesterol content in RAW264.7 macrophage-derived foam cells[2].
Saringosterol shows antitubercular activity of MIC of 0.25 μg/mL[3].
Saringosterol exhibits no appreciable toxicity against Vero cells, with an IC50 greater than 128 μg/mL[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: MDI-induced 3T3-L1 cells
Concentration: 100, 200 μM
Incubation Time: 8 days (from initiation of differentiation)
Result: Significantly inhibited mRNA expression of PPARγ and C/EBPα, with both concentrations showing statistically significant inhibition.
Significantly inhibited mRNA expression of aP2, adiponectin, resistin, and FAS, with both concentrations showing statistically significant inhibition.

Western Blot Analysis[1]

Cell Line: MDI-induced 3T3-L1 cells
Concentration: 100, 200 μM
Incubation Time: 8 days (from initiation of differentiation)
Result: Significantly inhibited protein expression of PPARγ and C/EBPα, with both concentrations showing statistically significant inhibition.
In Vivo

Saringosterol (50 mg/kg; p.o.; daily; 2 weeks) reduces atherosclerotic plaque burden, improves serum and hepatic lipid profiles, and modulates LXR-regulated cholesterol metabolism genes in ApoE−/− mice without inducing hepatic lipogenesis[2].
Saringosterol (10-30 mg/kg; i.p., single dose 30 min before testing; 30 mg/kg; p.o., daily for 7 days) produces significant dose-dependent antidepressant-like effects in mouse behavioral despair models[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ApoE−/− mice with a high-fat die with (8-week-old)[2]
Dosage: 50 mg/kg
Administration: p.o.; daily; 2 weeks
Result: Reduced atherosclerotic plaque burden, with en face aortic plaque area (percentage of total aortic area) and aortic root cross-sectional plaque area significantly lower than control mice.
Significantly decreased serum total cholesterol, low-density lipoprotein cholesterol, and triglyceride levels; significantly increased serum high-density lipoprotein cholesterol levels.
No significant change in liver total cholesterol levels; significantly reduced liver triglyceride levels compared to control mice.
Attenuated hepatic steatosis, with reduced liver weight and liver weight-to-body weight ratio compared to control mice; no upregulation of hepatic lipogenic genes (SREBP-1c, ACC, FASN, SCD1, chREBP).
Upregulated mRNA levels of cholesterol efflux transporters ABCA1 and ABCG1, and LDLR-degrading protein IDOL in peritoneal macrophages.
Upregulated hepatic mRNA levels of cholesterol catabolism enzyme CYP7A1, cholesterol efflux transporters ABCG5 and ABCG8, and HDL-cholesterol influx receptor SR-B1.
Downregulated intestinal mRNA levels of cholesterol absorption transporter NPC1L1; upregulated intestinal mRNA levels of cholesterol efflux transporters ABCG5, ABCG8, and ABCA1.
Animal Model: ICR (male, 20-22 g)[4]
Dosage: 10 mg/kg; 20 mg/kg; 30 mg/kg (single dose; behavioral tests); 30 mg/kg (neurotransmitter analysis)
Administration: i.p (10-30 mg/kg); p.o.; daily for 7 days (30 mg/kg)
Result: Reduced immobility time in forced swim test and tail suspension test.
Did not significantly alter locomotor activity in open-field test at all tested doses.
Increased brain serotonin (5-HT) levels, 5-hydroxyindoleacetic acid (5-HIAA) levels and noradrenaline (NE) levels.
Showed no significant effect on brain dopamine (DA) levels.
Molecular Weight

428.69

Formula

C29H48O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(C=C)(O)C(C)C)([H])[C@@]3([H])[C@@](CC1)([H])[C@@]4(C(C[C@H](CC4)O)=CC3)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Saringosterol
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HY-N15574
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