A potent inhibitor of NF-κB activation
Caffeic acid phenethyl ester (CAPE) is an inhibitor of NF-κB activation [1].
CAPE derives from honeybee propolis and has several biological activities. It is found to be an inhibitor of NF-κB activation. In U937 cells, CAPE inhibits the TNF-dependent activation of NF-κB dose-dependently. The maximum effect occurs at dose of 25μg/ml. CAPE also inhibits NF-κB activation induced by phorbol ester, ceramide, okadaic acid and hydrogen peroxide. It is reported that CAPE prevents NF-κB from binding to DNA without affecting other transcription factors. CAPE also has angiogenesis efficacy. It shows inhibition effect on the formation of capillary-like tubes. Besides, it reduces the production of VEGF both in CT26 cell culture and in animal model. In addition, CAPE effectively prevents CT26 cells from secreting MMP-2 and MMP-9 [1, 2].
参考文献:
[1] Natarajan K, Singh S, Burke TR Jr, Grunberger D, Aggarwal BB. Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B. Proc Natl Acad Sci U S A. 1996 Aug 20;93(17):9090-5.
[2] Liao HF, Chen YY, Liu JJ, Hsu ML, Shieh HJ, Liao HJ, Shieh CJ, Shiao MS, Chen YJ. Inhibitory effect of caffeic acid phenethyl ester on angiogenesis, tumor invasion, and metastasis. J Agric Food Chem. 2003 Dec 31;51(27):7907-12.
| Cell experiment [1]: | |
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Cell lines |
The human histiocytic cell line U937 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0, 5, 10, 15, 25 and 30 μg/ml; 2 h |
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Applications |
In U937 cells, Caffeic Acid Phenethyl Ester (CAPE) inhibited the TNF-dependent activation of NF-KB in a dose-dependent manner, with maximum effect occurring at 25 ug/ml. CAPE (25 ug/ml) also blocked NF-KB activation induced by Phorbol Ester, Ceramide, Okadaic Acid, and Hydrogen Peroxide. |
| Animal experiment [2]: | |
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Animal models |
CT26-bearing BALB/c male mice with pulmonary metastases |
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Dosage form |
10 mg/kg/day, intraperitoneal injection |
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Application |
In CT26-bearing BALB/c male mice with pulmonary metastases, CAPE decreased tumor colonization in the lung. Mice treated with CAPE survived longer than untreated controls. CAPE reduced plasma VEGF levels by 53.2%. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1] Natarajan K, Singh S, Burke TR Jr, Grunberger D, Aggarwal BB. Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B. Proc Natl Acad Sci U S A. 1996 Aug 2;93(17):9090-5. [2] Liao HF, Chen YY, Liu JJ, Hsu ML, Shieh HJ, Liao HJ, Shieh CJ, Shiao MS, Chen YJ. Inhibitory effect of caffeic acid phenethyl ester on angiogenesis, tumor invasion, and metastasis. J Agric Food Chem. 2003 Dec 31;51(27):7907-12. | |
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