A pH-Dependent rhodamine fluorophore with antiproliferative activity of bladder cancer in Vitro/Vivo and apoptosis mechanism

pH 依赖性罗丹明荧光团具有体外/体内抗膀胱癌增殖活性和凋亡机制

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作者:Dingheng Lu, Tianbao Yang, Niu Tang, Chenghan Li, Yarong Song, Liang Wang, Wai-Yeung Wong, Shuang-Feng Yin, Yifei Xing, Nobuaki Kambe, Renhua Qiu

Abstract

Herein, 26 rhodamine fluorophores were synthesized from readily available Rh-6G and relative amines at room temperature with good selectivity, functional groups compatibility and high yields. We found that one of them 3f showed pH-dependent anticancer bioactivity, with cell viability of 68.4% under pH 6.5 and 83.2% under pH 7.5, LDH fold change of 42.8% under pH 6.5 and 26.4% under pH 7.5 in 22.35 μM in human bladder cancer cell line EJ. Besides, 3f showed anticancer bioactivity in vivo towards human bladder cancer, by triggering apoptosis through mitochondrial pathway.

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