Rosolic acid
Rosolic acid is a Michael acceptor molecule isolated from the rhizomes of Plantago asiatica L. Rosolic acid inhibits Keap1, promotes Nrf2 nuclear translocation, and upregulates HO-1 and NQO-1. Rosolic acid reduces ER stress markers PERK, ATF-6, GRP78, and CHOP, as well as oxidative stress, ROS production, inflammation, and apoptosis. Rosolic acid upregulates SOD, CAT, and GPx activities, induces angiogenesis and insulin secretion, and restores endothelial function and pancreatic beta cell protection under ER stress. Rosolic acid can be used in research on diabetes and endothelial dysfunction.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 603-45-2
- 分子式: C19H14O3
- 分子量:290.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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KI696KEAP1/NRF2 Protein-protein Interaction Inhibitor
生物活性
製品説明
体外実験
Rosolic acid (2.5-25 μM; 24 h) does not exhibit cytotoxicity in EA.hy926 cells at concentrations up to 25 μM[1].
Rosolic acid (15 μM; 24-48 h) is well tolerated by bovine aortic endothelial cells with no cytotoxicity up to 48 h[3].
Rosolic acid (2.5-25 μM; 24 h) protects EA.hy926 cells against Thapsigargin (HY-13433)-induced ER stress cytotoxicity at 5 and 10 μM[1].
Rosolic acid pretreatment (10 μM; 24 h) reduces Thapsigargin-induced ER stress markers GRP78 and CHOP in EA.hy926 cells in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) decreases GRP-78 and CHOP protein levels in EA.hy926 cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells restores BCL2 expression in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells rescues PDX1 expression in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells normalizes GRP78 and CHOP expression in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells restores intracellular insulin levels in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid treatment (10 μM; 24 h) upregulates Nrf2, HO-1, and NQO-1 expression in EA.hy926 cells under ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells upregulates Nrf2 and NQO-1 expression in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells suppresses increased MDA levels in MIN6 pancreatic beta cells under Thapsigargin-induced ER stress in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) reduces Thapsigargin-induced inflammatory cytokines and chemokines in EA.hy926 cells in the co-culture setup[1].
Rosolic acid pretreatment (10 μM; 24 h) of EA.hy926 cells protects MIN6 pancreatic beta cells against Thapsigargin-induced reduction in viability in the co-culture setup[1].
Rosolic acid (15 μM; 6-18 h) induces sustained HO-1 protein expression in bovine aortic endothelial cells, with continued up-regulation at 18 h[3].
Rosolic acid (15 μM; 6 h) protects bovine aortic endothelial cells against hydrogen peroxide-induced oxidative stress[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EA.hy926 endothelial cells
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Concentration:2.5 μM; 5 μM; 10 μM; 25 μM
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Incubation Time:24 h
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Result:Observed cytotoxicity at doses higher than 25 μM.\n
Protected cells against aThapsigargin-induced cytotoxicity at 5 and 10 μM in a dose-dependent manner.
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Cell Line:EA.hy926 endothelial cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly repressed Thapsigargin-induced GRP78 and CHOP expression to levels comparable to control.\nUpregulated Nrf2, HO-1, and NQO-1 expression.
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Cell Line:EA.hy926 endothelial cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Decreased GRP-78 and CHOP protein levels compared to Thapsigargin-exposed cells.
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Cell Line:MIN6 pancreatic beta cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Restored BCL2 expression to control level.\nRescued PDX1 expression.\nUpregulated Nrf2 and NQO-1 gene expression.\nNormalized GRP78 and CHOP expression.
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Cell Line:MIN6 pancreatic beta cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Showed an intracellular insulin level comparable to control.
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Cell Line:MIN6 pancreatic beta cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Protected MIN6 pancreatic beta cells from Thapsigargin-induced loss of viability in a co-culture system.
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Cell Line:Bovine aortic endothelial cells
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Concentration:15 μM
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Incubation Time:6 h
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Result:Increased heme oxygenase activity to 2676 pmol bilirubin/mg protein/h compared to 453 pmol bilirubin/mg protein/h in control cells.
Achieved cell viability of 94% of control.
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Cell Line:Bovine aortic endothelial cells
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Concentration:15 μM
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Incubation Time:6 h; 18 h
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Result:Was the most potent inducer of HO-1 at 6 h among the compounds tested.
Further enhanced HO-1 expression at 18 h, whereas it was gradually decreasing with curcumin, CAPE, or 2'-hydroxychalcone.
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Cell Line:Bovine aortic endothelial cells
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Concentration:15 μM
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Incubation Time:24 h; 48 h
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Result:Did not produce any evident cytotoxicity at 24 or 48 h, unlike curcumin or CAPE, which caused a time-dependent decrease in cell viability.
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Cell Line:Bovine aortic endothelial cells
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Concentration:15 μM
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Incubation Time:6 h pretreatment; 2 h
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Result:Significantly attenuated hydrogen peroxide-mediated cytotoxicity in endothelial cells.
体内実験
Rosolic acid (1-30 mg/kg b.w.; i.p.; daily; 21 days) is safe at doses up to 10 mg/kg b.w., but doses of 30 mg/kg b.w. cause mild hepatic and renal toxicity in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar Albino rats (male, 100-150 g, 5-7 weeks old, high-fat diet-fed and streptozotocin-induced type-2 diabetic model)[2]
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Dosage:5 mg/kg b.w.; 10 mg/kg b.w.
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Administration:i.p.; once daily; 21 days
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Result:Reduced cholesterol to 255.36 ± 6.83 mg/dL, triglycerides to 56.82 ± 5.63 mg/dL, VLDL to 11.38 ± 2.27 mg/dL, and LDL to 181.35 ± 11.25 mg/dL, and increased HDL to 61.28 ± 5.19 mg/dL at 10 mg/kg.
Decreased blood glucose levels starting from Day 7 at 10 mg/kg.
Improved glucose tolerance in OGTT starting from 60 minutes with peak reduction at 180 minutes.
Restored aortic tissue architecture at 5 and 10 mg/kg.
Increased NRF2 and downstream targets NQO1 and HO-1 gene expression, with a 1.8-fold increase in NRF2 protein levels at 10 mg/kg.
Dose-dependently reduced ER stress markers GRP78 and CHOP, inflammatory markers ICAM-1 and VCAM-1, and endothelin-1 expression with 5- and 2-fold reductions at 5 and 10 mg/kg, respectively.
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Animal Model:Wistar rats (female)[2]
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Dosage:1 mg/kg b.w.; 3 mg/kg b.w.; 10 mg/kg b.w.; 30 mg/kg b.w.
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Administration:i.p.; daily; 21 days
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Result:Induced hepatic toxicity characterized by cellular damage and structural alterations in liver tissues and significant impairment of serum liver function parameters at 30 mg/kg b.w.
Induced pronounced renal cell damage including structural alterations in renal tubules and glomeruli and a significant increase in blood urea nitrogen (BUN) levels at 30 mg/kg b.w.
No toxicity or functional impairments were observed at 1, 3, and 10 mg/kg.
化学情報
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CAS 番号 603-45-2
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性状 Solid
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分子量 290.31
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分子式 C19H14O3
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Color White to off-white
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SMILES
C1=C(C=CC(=C1)O)C(=C2C=CC(=O)C=C2)C3=CC=C(C=C3)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Rosolic acid 関連分類
HY-W104821 関連分類
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