Cerulenin (Synonyms: Helicocerin, NSC 116069) |
| Catalog No.GC14025 |
지방산 합성 효소(FASN)의 강력한 천연 억제제인 세룰레닌은 곰팡이 세팔로스포리움 카에룰레우스(Cephalosporium caeruleus)에 의해 생성되는 에폭사이드입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 17397-89-6
Sample solution is provided at 25 µL, 10mM.
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Cerulenin covalently binds to the catalytic site of FAS and disrupts the condensation reaction of acetyl-COA and malonyl-COA, inhibiting the biosynthesis of fatty acids and sterols in yeast. The Flavonoids quercetin and trans-Chalcone are effective against T. rubrum, with MICs of 125 and 7.5 μg/mL for the wild-type strain (MYA3108) and of 63 and 1.9 μg/mL for the ABC transporter mutant strain (ΔTruMDR2), respectively. The MICs of the Fluconazole and Cerulenin controls are 63 and 125 μg/mL for the wild-type strain and 30 and 15 μg/mL for the mutant strain, respectively[1]. To explore the underlying mechanism of Steroidogenic acute regulatory protein (StAR)’s protective effect on endothelial dysfunction model, the inhibitor of fatty acid synthase and HMG-CoA reductase, Cerulenin ( 5 μg/mL) and Lovastatin, are used before palmitic acid (PA) added. The mRNA expression of IL-1β, TNFα, VCAM-1 and IL-6 are reduced while NO production is recovered with inhibitor treatment[2].
Cerulenin treatment of ob/ob mice has obvious effects on body weight. With 2 days of treatment, body weight in treated mice is decreased compared to a 5.7% weight gain in the controls. With prolonged (7 days) treatment, no body weight loss is observed, but body weight gain is slowed. In all groups, 60 mg/kg of Cerulenin is more effective than 30 mg/kg in inhibiting weight gain. If given daily or every other day, ATP content are increased 58.1% and 61.5% respectively by 7-day treatment of 60 mg/kg Cerulenin. Significant ATP elevation is also observed with only 2 days of treatment with 60 mg/kg Cerulenin. In contrast, 30 mg/kg Cerulenin, given either 2 or 7 days, does not show any significant effect on cellular ATP content[3].
Reference:
[1]. Bitencourt TA, et al. Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complement Altern Med. 2013 Sep 17;13:229.
[2]. Tian D, et al. Overexpression of steroidogenic acute regulatory protein in rat aortic endothelial cells attenuates palmitic acid-induced inflammation and reduction in nitric oxide bioavailability. Cardiovasc Diabetol. 2012 Nov 21;11:144.
[3]. Cheng G, et al. Cerulenin blockade of fatty acid synthase reverses hepatic steatosis in ob/ob mice. PLoS One. 2013 Sep 27;8(9):e75980.
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Cell experiment: |
Rat aortic endothelial cells (RAECs) are isolated and cultured with minor modifications. Briefly, segments of thoracic aorta are excised from male Wistar rats (150-180 g) and immediately placed in cold PBS containing 100 U/mL Penicillin and 100 mg/mL Streptomycin. The aorta is cut into 1 millimeter wide rings after the periadventitial fat is removed. Following transferred to a T-25 cm2 flasks, the rings are cultured in Medium 199 containing 20% fetal bovine serum, 2.5 ng/mL basic fibroblast growth factors, 100U/mL Penicillin and 100 mg/mL Streptomycin. The aorta rings are placed at 37°C in a humidified atmosphere with 5% CO2 for 72-80 h without movement. All pieces of aorta rings are removed when cells migrated. Its microvascular cytological characteristics are demonstrated by CD31 and vWF staining. In experiments involving PA treatment, M199 medium supplemented with 1% bovine serum albumin is used. All experiments are performed with RAECs up to passage 4. In the experiments with inhibitor, 5 μg/mL Cerulenin (in ethonal), or 5 μM Lovastatin (in DMSO), or 3.3 μg/mL Cerulenin plus 3.3 μM Lovastatin is added in culture media 24 hours prior to PA treatment. The same volume of solvents is added at the same time as control[2]. |
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Animal experiment: |
mice[3]Cerulenin is given to 6-8 week old male ob/ob mice in RPMI medium containing 20% DMSO intraperitoneally (i.p.). Controls are injected similarly with vehicle alone. The experimental groups (4 mice each) are as follows: A: 60 mg/kg/day Cerulenin, injected daily for 7 days; B: 60 mg/kg every other day for 7 days; C: 30 mg/kg/day for 7 days; D: 30 mg/kg every other day for 7 days; E: vehicle, daily for 7 days; F: 60 mg/kg/day Cerulenin for 2 days; G: 30 mg/kg/day Cerulenin for 2 days; H: vehicle, daily for 2 days; I: control. All animals are sacrificed on the same day under anesthesia. Blood is collected by portal vein puncture. Liver samples are snap-frozen in liquid N2 and stored at -80°C until analysis, or paraformaldehyde-fixed for histological analysis. |
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References: [1]. Bitencourt TA, et al. Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complement Altern Med. 2013 Sep 17;13:229. |
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| Cas No. | 17397-89-6 | SDF | |
| Synonyms | Helicocerin, NSC 116069 | ||
| Chemical Name | 2R,3S-epoxy-4-oxo-7,10-dodecadienamide | ||
| Canonical SMILES | C/C=C/C/C=C/CCC([C@@H]1[C@H](C(N)=O)O1)=O | ||
| Formula | C12H17NO3 | M.Wt | 223.3 |
| Solubility | ≤20mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4783 mL | 22.3914 mL | 44.7828 mL |
| 5 mM | 0.8957 mL | 4.4783 mL | 8.9566 mL |
| 10 mM | 0.4478 mL | 2.2391 mL | 4.4783 mL |
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Quality Control & SDS
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- Purity: >97.60%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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