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Phenethyl caffeate

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Chemical Structure| 104594-70-9 同义名 : 咖啡酸苯乙酯 ;Caffeic acid phenethyl ester;CAPE;BAF-IN-C09;β-Phenylethyl Caffeate;2-Phenylethyl Caffeate;Caffeic Acid phenylethyl ester;Phenylethyl Caffeate
CAS号 : 104594-70-9
货号 : A158279
分子式 : C17H16O4
纯度 : 98%
分子量 : 284.31
MDL号 : MFCD00866470
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(369.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • NF-κB
描述 NF-κB is a transcription factor with heterodimer or homodimer form of rel family proteins including RelA (p65), RelB, cRel, p50 and p52. Caffeic Acid Phenethyl Ester (CAPE) is an NF-κB inhibitor isolated from propolis. Treatment with CAPE at concentration ranging in 20-40μM for 2h could dose-dependently inhibit phosphorylation of IκBα and subsequently nuclear translocation of NF-κB (present as p65) induced by LPS in hepatic stellate cells. The increased nitrite production and the transcription and protein synthesis of MCP-1, IL-6 and iNOS induced by LPS could be significantly reduced by CAPE at concentration ranging in 5-40μM in a concentration-dependent manner in the same cells. Similarly, TNF-activated binding of NF-κB to DNA, phosphorylation of IκBα (within 30min) and p65 nuclear translocation could be observed in U937 cells pre-treated with 25μg/ml CAPE. Oral administration of 30mg/kg of CAPE daily for 4 weeks could improve the glucose sensitivity associated with the improvement in insulin-stimulated phosphorylation of the insulin receptor substrate-2 and an increase in Akt phosphorylation, promote amelioration in hepaticsteatosis, as well as reduced the induction of the inflammatory pathway, including JNK, NF-κB and COX-2 pathway, in high-fat-diet mice.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=26.8 μM 20673727
human BCG823 cells Cytotoxic assay Cytotoxicity against human BCG823 cells by MTT assay, IC50=44.6 μM 18952420
human Bel7402 cells Cytotoxic assay Cytotoxicity against human Bel7402 cells by MTT assay, IC50=5.5 μM 18952420
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02744703 Matrix Metalloproteinase Inhib... 展开 >>itors Composite Resins 收起 << Not Applicable Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.17mL

7.03mL

3.52mL
参考文献

[1]Banskota AH, Nagaoka T, et al. Antiproliferative activity of the Netherlands propolis and its active principles in cancer cell lines. J Ethnopharmacol. 2002 Apr;80(1):67-73.

[2]Natarajan K, Singh S, et al. 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.

[3]Kumar M, Kaur D, et al. Caffeic Acid Phenethyl Ester (CAPE) Prevents Development of STZ-ICV Induced dementia in Rats. Pharmacogn Mag. 2017 Jan;13(Suppl 1):S10-S15.

[4]Iraz M, Fadillioglu E, et al. Role of vagal activity on bradicardic and hypotensive effects of caffeic acid phenethyl ester (CAPE). Cardiovasc Toxicol. 2005 Fall;5(4):391-6.

[5]Bozkurt Y, Bozkurt M, et al. Caffeic acid phenethyl ester protects kidneys against acetylsalicylic acid toxicity in rats. Ren Fail. 2012;34(9):1150-5.

[6]Wei X, Zhao L, et al. Caffeic acid phenethyl ester prevents neonatal hypoxic-ischaemic brain injury. Brain. 2004 Dec;127(Pt 12):2629-35. Epub 2004 Oct 6.

[7]Wang X, Pang J, et al. Pharmacokinetics of caffeic acid phenethyl ester and its catechol-ring fluorinated derivative following intravenous administration to rats. Biopharm Drug Dispos. 2009 Jul;30(5):221-8.