Department of Pathology, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, Ostrogórska 30, Sosnowiec 41-200, Poland.
Department of Pharmaceutical Chemistry, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, Jagiellońska 4, Sosnowiec 41-200, Poland.
Molecules. 2017 Sep 15;22(9):1554. doi: 10.3390/molecules22091554.
Studies show that caffeic acid (CA) and caffeic acid phenethyl ester (CAPE) are compounds with potent chemopreventive effects. Breast cancer is a common form of aggressive cancer among women worldwide. This study shows a comparison of CA and CAPE activity on triple-negative human caucasian breast adenocarcinoma line cells (MDA-MB-231). MDA-MB-231 cells were treated by CA and CAPE with doses of from 10 to 100 µM, for periods of 24 h and 48 h. Cytotoxicity MTT tests, apoptosis by Annexin V, and cell cycle with Dead Cell Assays were performed. Cytotoxic activity was greater for CAPE compared to CA (both incubation times, same dosage). IC values for CAPE were 27.84 µM (24 h) and 15.83 µM (48 h) and for CA > 10,000 µM (24 h) and > 1000 µM (48 h). Polyphenols induced apoptosis, while CAPE (dose dependently), induced a higher apoptotic effect. CAPE also induced cell cycle arrest in S phase (time and dose dependently), CA did it only for 50 and 100 µM. A dose dependent decline was seen for the G0/G1 phase (CAPE, 48 h), as well as elimination of phase G2/M by 100 µM of CAPE (only mild effect for CA). Comparing CA and CAPE activity on MDA-MB-231, CAPE clearly showed better activity for the same dosages and experiment times.
研究表明,咖啡酸(CA)和咖啡酸苯乙酯(CAPE)是具有强大化学预防作用的化合物。乳腺癌是全球女性中常见的侵袭性癌症。本研究比较了 CA 和 CAPE 对三阴性人白种人乳腺癌腺癌细胞(MDA-MB-231)的活性。MDA-MB-231 细胞用 CA 和 CAPE 处理,剂量为 10 至 100 µM,孵育 24 小时和 48 小时。进行了细胞毒性 MTT 试验、Annexin V 诱导的细胞凋亡和细胞周期与死细胞检测。与 CA 相比,CAPE 的细胞毒性活性更高(两种孵育时间,相同剂量)。CAPE 的 IC 值为 27.84 µM(24 h)和 15.83 µM(48 h),而 CA 为> 10,000 µM(24 h)和> 1000 µM(48 h)。多酚诱导细胞凋亡,而 CAPE(剂量依赖性)诱导更高的凋亡作用。CAPE 还诱导 S 期细胞周期停滞(时间和剂量依赖性),而 CA 仅在 50 和 100 µM 时才会发生。G0/G1 期(CAPE,48 h)呈剂量依赖性下降,G2/M 期也被 100 µM CAPE 消除(CA 仅产生轻微影响)。比较 CA 和 CAPE 对 MDA-MB-231 的活性,CAPE 在相同剂量和实验时间下表现出更好的活性。