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

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
, 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 publication › Journal article › Academic research › peer-review

10 Citations (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 language	English
Article number	114293
Journal	European Journal of Medicinal Chemistry
Volume	236
DOIs	https://doi.org/10.1016/j.ejmech.2022.114293
Publication status	Published - 5 Jun 2022

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

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

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

More information

10.1016/j.ejmech.2022.114293

Cite this

@article{8c3fc42dfc24428896ced61aa4aa9e62,

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

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, pH on-off, Rhodamine",

author = "Dingheng Lu and Tianbao Yang and Niu Tang and Chenghan Li and Yarong Song and Liang Wang and Wong, \{Wai Yeung\} and Yin, \{Shuang Feng\} and Yifei Xing and Nobuaki Kambe and Renhua Qiu",

note = "Funding Information: The authors thank the Natural Science Foundation of China (Nos. 21676076 , 21878071 , 21971060 ), Hu-Xiang High Talent of Hunan Province ( 2018RS3042 ), and Recruitment Program for Foreign Experts of China ( WQ20164300353 ) for financial support. W.-Y.W. is grateful to the financial support from Hong Kong Research Grants Council ( PolyU153058/19P ), the Hong Kong Polytechnic University (1-ZE1C) and Ms Clarea Au for the Endowed Professorship in Energy (847S). Publisher Copyright: {\textcopyright} 2022",

year = "2022",

month = jun,

day = "5",

doi = "10.1016/j.ejmech.2022.114293",

language = "English",

volume = "236",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

TY - JOUR

T1 - A pH-Dependent rhodamine fluorophore with antiproliferative activity of bladder cancer in Vitro/Vivo and apoptosis mechanism

AU - Lu, Dingheng

AU - Yang, Tianbao

AU - Tang, Niu

AU - Li, Chenghan

AU - Song, Yarong

AU - Wang, Liang

AU - Wong, Wai Yeung

AU - Yin, Shuang Feng

AU - Xing, Yifei

AU - Kambe, Nobuaki

AU - Qiu, Renhua

N1 - Funding Information: The authors thank the Natural Science Foundation of China (Nos. 21676076 , 21878071 , 21971060 ), Hu-Xiang High Talent of Hunan Province ( 2018RS3042 ), and Recruitment Program for Foreign Experts of China ( WQ20164300353 ) for financial support. W.-Y.W. is grateful to the financial support from Hong Kong Research Grants Council ( PolyU153058/19P ), the Hong Kong Polytechnic University (1-ZE1C) and Ms Clarea Au for the Endowed Professorship in Energy (847S). Publisher Copyright: © 2022

PY - 2022/6/5

Y1 - 2022/6/5

N2 - 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.

AB - 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.

KW - Anti-bladder cancer

KW - Cell image

KW - NMIBC

KW - pH on-off

KW - Rhodamine

UR - https://www.scopus.com/pages/publications/85127315238

U2 - 10.1016/j.ejmech.2022.114293

DO - 10.1016/j.ejmech.2022.114293

M3 - Journal article

C2 - 35385804

AN - SCOPUS:85127315238

SN - 0223-5234

VL - 236

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

M1 - 114293

ER -

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

Abstract

UN SDGs

Keywords

ASJC Scopus subject areas

More information

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