Related Experiment Video
Updated: Mar 30, 2026
Reconstruct Human Retinoblastoma In Vitro
Published on: October 11, 2022
Quinoline-Based Compound BPIQ Exerts Anti-Proliferative Effects on Human Retinoblastoma Cells via Modulating
Kai-Chun Cheng1,2,3, Chun-Tzu Hung3,4, Kuo-Jen Chen2
1Graduate Institute of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan.
Abstract:
Retinoblastoma (Rb) is the most common primary intraocular malignant tumor of childhood. It is important to develop the strategy for Rb treatment. We have tested a quinolone derivative 2,9-bis[2-(pyrrolidin-1-yl)ethoxy]-6-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}-11H-indeno[1,2-c]quinolin-11-one (BPIQ) for its anti-cancer effects against Rb via cultured human Rb cell line Y79. Our results showed that BPIQ significantly inhibits cell growth of Y79. Furthermore, the flow cytometer-based assays and Western blotting showed that BPIQ induces the apoptosis of Y79 via increasing the level of reactive oxygen species (ROS). Besides, the activation of γH2AX, a DNA damage sensor in human Y79 cells was also observed, indicating the potential of BPIQ for causing DNA damage of Rb cells. On the contrary, BPIQ-induced apoptosis of Y79 cells was attenuated significantly by N-acetyl-L-cysteine (NAC), an ROS scavenger. The results of Western blot showed that BPIQ down-regulates the levels of anti-apoptotic proteins Bcl-2, survivin and XIAP while up-regulates the pro-apoptotic proteins Bad, Bax and Bid. Our present study demonstrated the anti-proliferative effect of BPIQ in human Y79 cells. The inhibitory effect of BPIQ on the proliferation of Y79 cells is, at least, partly mediated by the regulation of ROS and DNA damage pathway. In conclusion, BPIQ may provide an alternative option in the chemotherapeutics or chemoprevention on the Rb therapy in the future.
Insights
A novel quinolone derivative, BPIQ, effectively inhibits retinoblastoma (Rb) cell growth by inducing apoptosis through reactive oxygen species (ROS) and DNA damage. BPIQ shows promise as a potential therapeutic agent for Rb treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Retinoblastoma (Rb) is the most common intraocular malignancy in children.
- Developing effective treatment strategies for Rb is crucial.
Purpose of the Study:
- To evaluate the anti-cancer effects of a quinolone derivative, BPIQ, against human Rb cell line Y79.
- To investigate the mechanisms underlying BPIQ's anti-cancer activity.
Main Methods:
- Cell viability assays on Y79 cells treated with BPIQ.
- Flow cytometry and Western blotting to assess apoptosis and protein levels.
- Measurement of reactive oxygen species (ROS) and DNA damage marker γH2AX.
- Assessment of BPIQ's effects in the presence of N-acetyl-L-cysteine (NAC).
Main Results:
- BPIQ significantly inhibited Y79 cell growth.
- BPIQ induced apoptosis in Y79 cells, associated with increased ROS and DNA damage (γH2AX activation).
- BPIQ's pro-apoptotic effects were partially reversed by NAC, confirming ROS involvement.
- BPIQ modulated the expression of key apoptosis-related proteins, down-regulating Bcl-2, survivin, and XIAP, while up-regulating Bad, Bax, and Bid.
Conclusions:
- BPIQ exhibits significant anti-proliferative effects on human retinoblastoma Y79 cells.
- The anti-cancer activity of BPIQ is mediated, at least in part, by ROS generation and DNA damage induction.
- BPIQ represents a potential therapeutic or chemopreventive agent for retinoblastoma.
