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

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

Research output: Journal article publicationJournal articleAcademic researchpeer-review

1 Citation (Scopus)

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.

Original languageEnglish
Article number114293
JournalEuropean Journal of Medicinal Chemistry
Volume236
DOIs
Publication statusPublished - 5 Jun 2022

Keywords

  • Anti-bladder cancer
  • Cell image
  • NMIBC
  • pH on-off
  • Rhodamine

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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