DI Giacomo Silvia, DI Sotto Antonella, El-Readi Mahmoud Zaki, Mazzanti Gabriela, Wink Michael
Department of Physiology and Pharmacology V. Erspamer, Sapienza University of Rome, Rome, Italy.
Department of Physiology and Pharmacology V. Erspamer, Sapienza University of Rome, Rome, Italy
Anticancer Res. 2016 Jul;36(7):3347-51.
α-Hexylcinnamaldehyde (HCA), a compound derived from cinnamaldehyde, was evaluated for its potential chemosensitizing properties.
The cytotoxicity of HCA was tested against Caco-2, CCRF/CEM and CEM/ADR5000 human cancer cells. Furthermore, its ability to increase doxorubicin cytotoxicity was evaluated in combination assays. Rhodamine123 efflux assay was carried out in order to highlight the possible interference of HCA with functionality of ATP-binding cassette (ABC)-transporters.
In spite of a low cytotoxicity, HCA increased the antiproliferative effect of doxorubicin in all the cell lines tested, being particularly effective in CCRF/CEM. The compound also reduced the rhodamine123 efflux in Caco-2 and CEM/ADR5000 cells, suggesting a possible interference with ABC transporter functionality.
Considering that the greatest synergism between HCA and DOX was found against CCRF/CEM cells (lacking ABC pumps), it seems likely that non-specific mechanisms, including the alteration of membrane permeability, could be involved in the chemosensitizing effect of HCA.
评估源自肉桂醛的化合物α-己基肉桂醛（HCA）的潜在化学增敏特性。
测试了HCA对人癌细胞Caco-2、CCRF/CEM和CEM/ADR5000的细胞毒性。此外，在联合试验中评估了其增强阿霉素细胞毒性的能力。进行罗丹明123外排试验以突出HCA对ATP结合盒（ABC）转运蛋白功能的可能干扰。
尽管细胞毒性较低，但HCA在所有测试细胞系中均增强了阿霉素的抗增殖作用，在CCRF/CEM中尤为有效。该化合物还减少了Caco-2和CEM/ADR5000细胞中的罗丹明123外排，表明可能对ABC转运蛋白功能有干扰。
鉴于在CCRF/CEM细胞（缺乏ABC泵）中发现HCA与阿霉素之间具有最大的协同作用，非特异性机制（包括膜通透性改变）似乎可能参与了HCA的化学增敏作用。
