Mitochondria-localizing curcumin-cryptolepine Zn(II) complexes and their antitumor activity
作者:Li-Qin Qin、Chun-Jie Liang、Zhen Zhou、Qi-Pin Qin、Zu-Zhuang Wei、Ming-Xiong Tan、Hong Liang
DOI:10.1016/j.bmc.2020.115948
日期:2021.1
mitochondria after treatment, indicating increases in Ca2+ and reactive oxygen species levels, loss of the mitochondrial membrane potential, and consequent induction of mitochondrial dysfunction at low concentrations. In addition, the probe Zn2 effectively (50.7%) inhibited the growth of T-24 bladder tumor cells in vivo. The probe Zn2 shows potential for use in cancer therapy while retaining the H-Curc as an
许多金属配合物是作为线粒体靶向剂的有效候选物。在本研究中,四种新型 Zn(II) 配合物,[Zn(BPQA)Cl 2 ] ( Zn1 ), [Zn(BPQA)(Curc)]Cl ( Zn2 ), [Zn(PQA)Cl 2 ] ( Zn3 ),和 [Zn(PQA)(Curc)]Cl ( Zn4 ),含有N , N-双(吡啶-2-基甲基)苯并呋喃 [3,2- b ] 喹啉-11-胺 (BPQA), N-(吡啶-合成了2-基甲基)苯并呋喃[3,2 - b ]喹啉-11-胺(PQA)和姜黄素(H-Curc)。MTT 分析表明Zn1 – Zn4对 SK-OV-3/DDP 和 T-24 肿瘤细胞具有很强的抗癌活性,IC 500.03–6.19 μM 的值。重要的是,Zn1和Zn2对正常 HL-7702 细胞显示出低毒性。机理实验表明,探针Zn2在光谱的红色区域显示出明显的荧光,处理后在线粒体中发生了大量的Zn2积累,表明