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

Dingheng Lu¹, Tianbao Yang², Niu Tang², Chenghan Li², Yarong Song³, Liang Wang⁴, Wai-Yeung Wong⁵, Shuang-Feng Yin², Yifei Xing⁶, Nobuaki Kambe⁷, Renhua Qiu⁸

Affiliations

¹ State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China; Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China.
² State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China.
³ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China. Electronic address: tjmusong@126.com.
⁴ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China.
⁵ Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China.
⁶ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China. Electronic address: yfxing@hust.edu.cn.
⁷ Graduate School of Engineering, Osaka University, Suita, Osaka, 565-0871, Japan.
⁸ State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China. Electronic address: renhuaqiu1@hnu.edu.cn.

PMID: 35385804
DOI: 10.1016/j.ejmech.2022.114293

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

Dingheng Lu et al. Eur J Med Chem. 2022.

. 2022 Jun 5:236:114293.

doi: 10.1016/j.ejmech.2022.114293. Epub 2022 Mar 16.

Authors

Dingheng Lu¹, Tianbao Yang², Niu Tang², Chenghan Li², Yarong Song³, Liang Wang⁴, Wai-Yeung Wong⁵, Shuang-Feng Yin², Yifei Xing⁶, Nobuaki Kambe⁷, Renhua Qiu⁸

Affiliations

¹ State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China; Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China.
² State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China.
³ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China. Electronic address: tjmusong@126.com.
⁴ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China.
⁵ Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China.
⁶ Department of Urology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430074, Hubei, PR China. Electronic address: yfxing@hust.edu.cn.
⁷ Graduate School of Engineering, Osaka University, Suita, Osaka, 565-0871, Japan.
⁸ State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, PR China. Electronic address: renhuaqiu1@hnu.edu.cn.

PMID: 35385804
DOI: 10.1016/j.ejmech.2022.114293

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.

Keywords: Anti-bladder cancer; Cell image; NMIBC; Rhodamine; pH on-off.

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

Affiliations

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

Authors

Affiliations

Abstract

MeSH terms

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LinkOut - more resources

Full Text Sources

Medical