Zhang Yuan, Liao Zhi, Zhang Li-juan, Xiao Hong-tao
Department of Pharmacy, Hospital of the University of Electronic Science and Technology of China and Sichuan Provincial People's Hospital , Chengdu , China.
Curr Med Res Opin. 2015 May;31(5):1009-13. doi: 10.1185/03007995.2015.1025731. Epub 2015 Mar 17.
The anti-malarial drug chloroquine has recently been discovered as a novel anti-tumor agent. This article is to review the recent development of chloroquine being used in cancer therapy.
PubMed, ScienceDirect and ClinicalKey served as the major databases. Key words included 'chloroquine', 'cancer', and 'autophagy'. The publication date was up to June 2015.
Chloroquine mainly executes its anti-tumor function through inhibition of autophagy. It can accumulate inside the lysosome resulting in lysosomal membrane permeabilization (LMP) which will eventually lead to apoptosis. Chloroquine has been shown to stabilize p53 and induce p53-dependent apoptosis or cell cycle arrest. It can also inhibit ABC (ATP-binding cassette) family protein. The anti-cancer effect of chloroquine has been observed both in vitro and in vivo. However, it is considered more as a potential chemotherapy and radiotherapy sensitizer rather than an antineoplastic.
Although the utility of chloroquine is promising in cancer therapy, some safety issues have been brought to attention, and further studies on safety profile and the signs of clinical activity of chloroquine including its derivatives should be conducted.
抗疟药物氯喹最近被发现是一种新型抗肿瘤药物。本文旨在综述氯喹在癌症治疗中的最新进展。
以PubMed、ScienceDirect和ClinicalKey作为主要数据库。关键词包括“氯喹”、“癌症”和“自噬”。发表日期截至2015年6月。
氯喹主要通过抑制自噬发挥其抗肿瘤功能。它可在溶酶体内蓄积，导致溶酶体膜通透性增加（LMP），最终引发凋亡。氯喹已被证明可稳定p53并诱导p53依赖性凋亡或细胞周期阻滞。它还能抑制ABC（ATP结合盒）家族蛋白。氯喹的抗癌作用已在体外和体内得到观察。然而，它更多地被视为一种潜在的化疗和放疗增敏剂，而非抗肿瘤药。
尽管氯喹在癌症治疗中的应用前景广阔，但一些安全问题已引起关注，应对氯喹及其衍生物的安全性和临床活性迹象开展进一步研究。
