Caffeic Acid Phenethyl Ester is a naturally occurring phenylpropanoid compound found in propolis, possessing a variety of biological activities[1]. Caffeic Acid Phenethyl Ester potently and specifically inhibits the activation of the nuclear transcription factor NF-κB by preventing the nuclear translocation of its p65 subunit[2]. Caffeic Acid Phenethyl Ester exhibits significant antioxidant and anticancer activities[3-4].
In vitro, co-treatment of OV7, HTB76, and CRL1572 ovarian cancer cells with Caffeic Acid Phenethyl Ester (50–100μM) and 10nM paclitaxel (PTX) for 6–24 hours significantly enhanced the cytotoxicity of PTX and induced apoptosis[5]. Treatment of LPS (1μg/ml)-stimulated MDA-MB-231 cells with Caffeic Acid Phenethyl Ester (25–100μM) for 12–48 hours significantly inhibited cell proliferation, migration, and invasion, and reduced mitochondrial membrane potential[6].
In vivo, daily intraperitoneal injection of Caffeic Acid Phenethyl Ester (20–40mg/kg) for 24 days in a mouse model of experimental autoimmune encephalomyelitis (EAE) significantly reduced disease incidence and severity[7]. Daily intraperitoneal administration of Caffeic Acid Phenethyl Ester (20mg/kg) for 7 days to female C57BL/6 mice infected with enterotoxigenic Bacteroides fragilis(ETBF) significantly alleviated ETBF-induced colitis symptoms, including suppressing body weight loss, reducing spleen weight, and decreasing the colon weight-to-length ratio[8].
References:
[1] Murtaza G, Karim S, Akram MR, et al. Caffeic acid phenethyl ester and therapeutic potentials. Biomed Res Int. 2014;2014:145342.
[2] Pandey P, Khan F, Upadhyay TK, Therapeutic efficacy of caffeic acid phenethyl ester in cancer therapy: An updated review. Chem Biol Drug Des. 2023 Jul;102(1):201-216.
[3] Olgierd B, Kamila Ż, Anna B, et al. The Pluripotent Activities of Caffeic Acid Phenethyl Ester. Molecules. 2021 Mar 2;26(5):1335.
[4] Lv L, Cui H, Ma Z, et al. Recent progresses in the pharmacological activities of caffeic acid phenethyl ester. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jul;394(7):1327-1339.
[5] Kleczka A, Dzik R, Kabała-Dzik A. Caffeic Acid Phenethyl Ester (CAPE) Synergistically Enhances Paclitaxel Activity in Ovarian Cancer Cells. Molecules. 2023 Aug 1;28(15):5813.
[6] Zhou Y, Wang J, Chang Y, et al. Caffeic Acid Phenethyl Ester Protects against Experimental Autoimmune Encephalomyelitis by Regulating T Cell Activities. Oxid Med Cell Longev. 2020 Oct 9;2020:7274342.
[7] Lan Z, Qu LJ, Liang Y, et al. AZD1390, an ataxia telangiectasia mutated inhibitor, attenuates microglia-mediated neuroinflammation and ischemic brain injury. CNS Neurosci Ther. 2024 Apr;30(4):e14696.
[8] Hwang S, Jo M, Hong JE, et al. Caffeic Acid Phenethyl Ester Administration Reduces Enterotoxigenic Bacteroides fragilis-Induced Colitis and Tumorigenesis. Toxins (Basel). 2024 Sep 18;16(9):403.
Caffeic Acid Phenethyl Ester是一种天然存在蜂胶中的苯丙素类化合物，具有多种生物学活性[1]。Caffeic Acid Phenethyl Ester能够强效且特异地抑制核转录因子NF-κB的活化，通过阻止NF-κB的p65亚单位进入细胞核来发挥作用[2]。Acid Phenethyl Ester有显著的抗氧化活性和抗癌活性[3-4]。
在体外，Caffeic Acid Phenethyl Ester（50–100μM）与10nM紫杉醇（PTX）联合处理OV7、HTB76和CRL1572卵巢癌细胞6–24小时，Caffeic Acid Phenethyl Ester显著增强紫杉醇的细胞毒性并诱导细胞凋亡[5]。Caffeic Acid Phenethyl Ester（25–100μM）处理经LPS（1μg/ml）刺激的MDA-MB-231细胞12–48小时，Caffeic Acid Phenethyl Ester显著抑制细胞增殖、迁移和侵袭，并降低线粒体膜电位[6]。
在体内，Caffeic Acid Phenethyl Ester（20–40mg/kg）每日腹腔注射实验性自身免疫性脑脊髓炎（EAE）小鼠模型24天，显著降低了疾病发生率和严重程度[7]。Caffeic Acid Phenethyl Ester（20mg/kg）每日腹腔注射处理经Bacteroides fragilis（ETBF）感染的C57BL/6雌鼠7天，显著减轻了ETBF诱导的结肠炎症状，包括抑制体重下降、减少脾脏重量及结肠重量/长度比值[8]。