Esculeogenin A
Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.
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- No. CAS: 854381-37-6
- Fòrmula: C27H45NO4
- Peso molecular:447.65
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Almacenamiento:
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Actividad biológica
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ACAT-1 |
ACAT-2 |
PPARα |
NF-κB |
Esculeogenin A (24 h) dose-dependently inhibits acetyl-LDL-induced cholesterol ester accumulation (but not triglyceride accumulation) in human monocyte-derived macrophages without inducing cytotoxicity[2].
Esculeogenin A (5 h) does not inhibit the association or degradation of acetyl-LDL in human monocyte-derived macrophages[2].
Esculeogenin A (24 h) dose-dependently inhibits cholesterol ester accumulation in Chinese hamster ovary cells overexpressing human ACAT-1 or human ACAT-2 without inducing cytotoxicity[2].
Esculeogenin A (15 min) dose-dependently inhibits ACAT activity in microsomes from human monocyte-derived macrophages, Chinese hamster ovary cells overexpressing human ACAT-1, and Chinese hamster ovary cells overexpressing human ACAT-2, with 50 μmol/L inhibiting HMDM ACAT activity by 40%[2].
Esculeogenin A (24 h) dose-dependently reduces ACAT-1 protein expression in human monocyte-derived macrophages without altering the expression of SR-A or SR-BI[2].
Esculeogenin A (10-100 μM; 24 h) potently inhibits cholesterol ester accumulation in human monocyte-derived macrophages (HMDMs) in a dose-dependent manner without affecting acetyl-LDL uptake or degradation, with 50 μM reducing accumulation by 40%[3].
Esculeogenin A (10-100 μM; 24 h) dose-dependently inhibits cholesterol ester accumulation in both hACAT-1 CHO cells and hACAT-2 CHO cells[3].
Esculeogenin A (10-100 μM) dose-dependently inhibits ACAT activity in human monocyte-derived macrophages (HMDMs), hACAT-1 CHO cells, and hACAT-2 CHO cells[3].
Esculeogenin A (10-50 μM; 24 h) dose-dependently reduces ACAT-1 protein expression in human monocyte-derived macrophages (HMDMs) without altering SR-A or SR-BI expression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human monocyte-derived macrophages (HMDMs)
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Concentration:10, 30, 50 μM
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Incubation Time:24 h
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Result:Reduced ACAT-1 protein expression in HMDMs in a dose-dependent manner.
Left SR-A and SR-BI protein expression unchanged relative to controls.
Esculeogenin A (100 mg/kg/day; p.o.; daily; 90 days), produced in vivo from orally administered Esculeoside A (HY-N18067), is detectable in the aortas of apoE-deficient mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 10-11 weeks old, ~165 g initial weight, HFD-induced)[1]
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Dosage:50 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:p.o.; daily; 12 weeks
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Result:Dose-dependently reduced serum ALT, AST, GGT, serum/hepatic TGs, CHOL, LDL-c, liver weight/liver-to-body weight ratio, NF-κB nuclear activity, IKKβ activity, hepatic MDA, IL-6, TNF-α, and hepatic SREBP1, ACC mRNA.
Dose-dependently increased hepatic Nrf2 (mRNA, cytoplasmic, nuclear), GSH, SOD, CAT, HO-1, and hepatic PPARα, CPT I mRNA.
Dose-dependently reduced hepatocellular fat vacuoles and improved liver structure.
200 mg/kg reduced serum/hepatic TGs, CHOL, serum LDL-c in normal diet-fed rats, with no adverse effects on body weight, fat pad weight, or glucose/insulin parameters.
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Animal Model:C57BL/6.KOR-Apoeshl (apoE-deficient)[2]
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Dosage:50 mg/kg/day; 100 mg/kg/day (as esculeoside A, converted in vivo to esculeogenin A)
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Administration:p.o.; daily; 90 days
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Result:Reduced serum total cholesterol by approximately 25%, serum LDL cholesterol by approximately 25%, and serum triglycerides by approximately 45%.
Reduced total aortic surface atherosclerotic lesions to 8.2%.
Reduced aortic sinus cross-sectional lesion area by 52%.
Was detected in the aortas of treated mice, confirming in vivo conversion from Esculeoside A.
Chemical Information
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No. CAS 854381-37-6
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Peso molecular 447.65
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Fòrmula C27H45NO4
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SMILES
C[C@@H]1[C@@]2([C@@H](C[C@@H](CN2)CO)O)O[C@]3([H])[C@@]1([H])[C@@]4([C@@]([C@@]5([H])[C@]([C@@]6([C@@](C[C@H](CC6)O)([H])CC5)C)([H])CC4)([H])C3)C
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Al Jadani JM, et al. Esculeogenin A, a Glycan from Tomato, Alleviates Nonalcoholic Fatty Liver Disease in Rats through Hypolipidemic, Antioxidant, and Anti-Inflammatory Effects. Nutrients. 2023;15(22):4755. Published 2023 Nov 11. [Content Brief]
[2]. Zhang Y, et al. Effects of Treatment on Glucose Metabolism, Inflammation, Lipid Profile, and Atherosclerotic Lesions in db/db Mice. J Pharmacol Exp Ther. 2024; 380(2): 156-163. [Content Brief]
[3]. Nohara T, et al. The tomato saponin, esculeoside A. J Nat Prod. 2010;73(10):1734-1741. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Esculeogenin A Related Classifications
HY-N18066 Related Classifications
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- Esculeogenin A
- 854381-37-6
- Drug Derivative
- Acyltransferase
- NF-κB
- PPAR
- Fatty Acid Synthase (FASN)
- Keap1-Nrf2
- nuclear factor kappa B kinase subunit beta
- human monocyte-derived macrophages
- apoE-deficient mice
- carnitine palmitoyltransferase I
- acetyl-CoA carboxylase
- nuclear factor erythroid 2-related factor 2
- nuclear factor-kappa beta
- Chinese hamster ovary cells
- peroxisome proliferator-activated receptor α
- sterol regulatory element-binding protein 1
- Inhibitor
- inhibitor
- inhibit