Ambrosin
Ambrosin is an orally active NF-κβ and BACE1 inhibitor. Ambrosin reduces pro-inflammatory and nitrosative mediators, increases PPARγ levels, inhibits apoptosis (Apoptosis), enhances autophagy (Autophagy), and ameliorates oxidative stress. Ambrosin reduces Amyloid plaque deposition. Ambrosin improves lipopolysaccharide-induced memory impairment and colonic histopathological changes. Ambrosin can be used in research related to Alzheimer's disease and colitis.
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: 509-93-3
- 分子式: C15H18O3
- 分子量:246.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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PPAR-γ |
BACE1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | GI50 |
1.8 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against colon cancer cell line HCT116
The compound was evaluated for cytotoxicity against colon cancer cell line HCT116
|
[PMID: 7650694] |
| KB | ED50 |
0.45 μg/mL
Compound: 12. Ambrosin
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 17336532] |
| KB | ED50 |
1.83 μM
Compound: ambrosin
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 18329753] |
| LOX IMVI | GI50 |
2.2 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against melanoma cell line LOX-IMVI
The compound was evaluated for cytotoxicity against melanoma cell line LOX-IMVI
|
[PMID: 7650694] |
| LOX IMVI | GI50 |
2.2 μM
Compound: 6
|
Antiproliferative activity against human LOXIMVI cells
Antiproliferative activity against human LOXIMVI cells
|
10.1039/C2MD20172K |
| MCF7 | GI50 |
3.9 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against breast cancer cell line MCF-7
The compound was evaluated for cytotoxicity against breast cancer cell line MCF-7
|
[PMID: 7650694] |
| MCF7 | GI50 |
3.9 μM
Compound: 6
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
|
10.1039/C2MD20172K |
| NCI-H522 | GI50 |
1 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against lung cancer cell line NCI-H522
The compound was evaluated for cytotoxicity against lung cancer cell line NCI-H522
|
[PMID: 7650694] |
| NCI-H522 | GI50 |
1 μM
Compound: 6
|
Antiproliferative activity against human NCI-H522 cells
Antiproliferative activity against human NCI-H522 cells
|
10.1039/C2MD20172K |
| OVCAR-5 | GI50 |
4.9 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against ovarian cancer cell line OVCAR-5
The compound was evaluated for cytotoxicity against ovarian cancer cell line OVCAR-5
|
[PMID: 7650694] |
| PC-3 | GI50 |
4.5 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against prostate cancer cell line PC-3
The compound was evaluated for cytotoxicity against prostate cancer cell line PC-3
|
[PMID: 7650694] |
| SF-539 | GI50 |
2.9 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against CNS cancer cell line CNS SF-539
The compound was evaluated for cytotoxicity against CNS cancer cell line CNS SF-539
|
[PMID: 7650694] |
| SN12C | GI50 |
3.4 μM
Compound: 1
|
The compound was evaluated for cytotoxicity against renal cancer cell line SN12C
The compound was evaluated for cytotoxicity against renal cancer cell line SN12C
|
[PMID: 7650694] |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino mice (mature male, 120-130 g, LPS-induced Alzheimer's disease model)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Reduced mean escape latency time on days 3 and 4 to levels similar to the normal group (significantly lower than LPS control).
Increased mean time spent in the target quadrant to 25.59 sec (5 mg/kg) and 25.56 sec (10 mg/kg; LPS control: 12.20 sec; normal group: 23.38 sec).
Increased time spent exploring the novel object vs. the familiar object, and yielded significantly positive discrimination indices (significantly different from LPS control with negative index).
Reduced LPS-induced elevated NF-κβp65 transcript and protein levels in a dose-dependent manner, with 10 mg/kg reducing protein levels to values not significantly different from the normal group.
Significantly reduced LPS-induced elevated TNF-α, IL-1β, COX-2, and iNOS protein levels at 5 mg/kg; reduced these markers to levels similar to the normal group at 10 mg/kg.
Reduced LPS-induced elevated BACE1 protein levels in a dose-dependent manner.
Increased surviving hippocampal CA1 neurons to 35.66 per high power field (5 mg/kg; LPS control: 23.33) and 44.33 per high power field (10 mg/kg).
Reduced amyloid plaques to 2.50 per high power field (5 mg/kg; LPS control: 6.20) and 0.90 per high power field (10 mg/kg).
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Animal Model:BALB/c (male, 16-26 g, DSS-induced colitis)[2]
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Dosage:10 mg/kg
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Administration:p.o.
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Result:Significantly reduced disease activity index (DAI).
Restored colon length compared to DSS-only treated mice.
Increased colonic tissue levels of SIRT1, PPAR-γ, glutathione reductase, glutathione peroxidase, Nrf2, beclin-1, LC3-II, and Bcl-2.
Significantly decreased colonic tissue levels of ROS, iNOS, TLR-4, IL-1β, IL-6, TGF-β1, phospho-p38 MAPK, c-Fos, c-Jun, NLRP3 inflammasome, and caspase-8.
Attenuated DSS-induced histopathological damage, including reduced ulceration, crypt loss, and inflammatory cell infiltration.
Lowered histological disease score.
Reduced NF-κB (p65) nuclear immunostaining.
Improved electron microscopic features of colonic cells (nearly normal apical microvilli, mild cytoplasmic vacuolation, and mild mitochondrial swelling with partially destructed cristae).
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Research Protocol for Inflammation-related Diseases
- Amyloid: Congo Red Amyloid Staining
- Alzheimer’s Disease Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- DSS-Induced Colitis
- TNBS-Induced Colitis
- Autophagy
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
化学情報
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CAS 番号 509-93-3
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分子量 246.31
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分子式 C15H18O3
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SMILES
C[C@]12[C@]3([C@](C(=C)C(=O)O3)(CC[C@H](C)[C@@]1(C=CC2=O)[H])[H])[H]
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Structure Classification
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Initial Source
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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
参考文献
[1]. Khalil MNA, et al. Ambrosin, a potent NF-κβ inhibitor, ameliorates lipopolysaccharide induced memory impairment, comparison to curcumin. PloS one. 2019;14(7):e0219378. [Content Brief]
[2]. Kabel AM, et al. Perindopril/Ambrosin Combination Mitigates Dextran Sulfate Sodium-Induced Colitis in Mice: Crosstalk between Toll-Like Receptor 4, the Pro-Inflammatory Pathways, and SIRT1/PPAR-γ Signaling. Pharmaceuticals (Basel, Switzerland). 2022 May 13;15(5):600. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- Ambrosin
- 509-93-3
- NF-κB
- Beta-secretase
- PPAR
- Apoptosis
- Autophagy
- Amyloid-β
- Nuclear factor-κB
- Nuclear factor-kappaB
- BACE
- β-Secretase
- Peroxisome proliferator-activated receptors
- β-amyloid peptide
- Aβ
- Abeta
- Alzheimer's disease
- sirtuin-1
- PPARγ
- TLR4
- lipopolysaccharide
- colitis
- NF-κβp65
- neurons
- male BALB/c mice
- BACE1
- Inhibitor
- inhibitor
- inhibit