A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo
Abstract
:1. Introduction
2. Results
2.1. High-Throughput Screening
2.2. Flow Cytometry Assay
2.3. Cytotoxic Assay
2.4. ATPase Assay
2.5. Reverse Transcription-Quantitative Polymerase Chain Reaction
2.6. Antitumor Activity In Vivo
3. Discussion
4. Materials and Methods
4.1. Screening of Chemical Compounds
4.2. Chemicals
4.3. Cell Lines
4.4. High-Throughput Screening
4.5. Flow Cytometry
4.6. Cytotoxic Assay
4.7. Preparation of the Phenylfurocoumarin Derivative
4.8. ATPase Assay
4.9. Reverse Transcription-Quantitative Polymerase Chain Reaction (RT-qPCR)
4.10. In Vivo Antitumor Activity
4.11. Statistical Analysis
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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IC50 ± SE (µM) a | Fold Reversal b | IC50 ± SE (µM) a | Fold Reversal b | |
---|---|---|---|---|
HCT-116 | HCT-116/BCRP | |||
Medium | 0.11 ± 0.0037 | 1.0 | 2.59 ± 0.24 | 1.0 |
Ko143 1 µM | 0.11 ± 0.0036 | 1.0 | 0.26 ± 0.027 | 10.1 |
PFC 5 µM | 0.077 ± 0.022 | 1.4 | 0.36 ± 0.11 | 7.3 |
PFC 10 µM | 0.057 ± 0.013 | 1.9 | 0.19 ± 0.018 | 13.8 |
IC50 ± SE (µM) a | ||
---|---|---|
HCT-116 | HCT-116/BCRP | |
Ko143 1 µM | 77.97 ± 2.33 | 115.79 ± 4.85 |
PFC 10 µM | 42.70 ± 2.42 | 43.07 ± 3.18 |
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Kokubo, S.; Ohnuma, S.; Murakami, M.; Kikuchi, H.; Funayama, S.; Suzuki, H.; Kajiwara, T.; Yamamura, A.; Karasawa, H.; Sugisawa, N.; et al. A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo. Int. J. Mol. Sci. 2021, 22, 12502. https://doi.org/10.3390/ijms222212502
Kokubo S, Ohnuma S, Murakami M, Kikuchi H, Funayama S, Suzuki H, Kajiwara T, Yamamura A, Karasawa H, Sugisawa N, et al. A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo. International Journal of Molecular Sciences. 2021; 22(22):12502. https://doi.org/10.3390/ijms222212502
Chicago/Turabian StyleKokubo, Shoji, Shinobu Ohnuma, Megumi Murakami, Haruhisa Kikuchi, Shota Funayama, Hideyuki Suzuki, Taiki Kajiwara, Akihiro Yamamura, Hideaki Karasawa, Norihiko Sugisawa, and et al. 2021. "A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo" International Journal of Molecular Sciences 22, no. 22: 12502. https://doi.org/10.3390/ijms222212502