Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA
Mitochondria have a crucial role in regulating energy metabolism and their dysfunction has been linked to tumorigenesis. Cancer diagnosis and intervention have a great interest in the development of new agents that target biomolecules within mitochondria. However, monitoring and modulating mitochond...
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-03-01
|
| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/28/6/2690 |
| _version_ | 1827748362088087552 |
|---|---|
| author | Bo-Zheng Wang Ying-Chen Zhou Yu-Wei Lin Xiu-Cai Chen Ze-Yi Yu Yao-Hao Xu Jia-Heng Tan Zhi-Shu Huang Shuo-Bin Chen |
| author_facet | Bo-Zheng Wang Ying-Chen Zhou Yu-Wei Lin Xiu-Cai Chen Ze-Yi Yu Yao-Hao Xu Jia-Heng Tan Zhi-Shu Huang Shuo-Bin Chen |
| author_sort | Bo-Zheng Wang |
| collection | DOAJ |
| description | Mitochondria have a crucial role in regulating energy metabolism and their dysfunction has been linked to tumorigenesis. Cancer diagnosis and intervention have a great interest in the development of new agents that target biomolecules within mitochondria. However, monitoring and modulating mitochondria RNA (mtRNA), an essential component in mitochondria, in cells is challenging due to limited functional research and the absence of targeting agents. In this study, we designed and synthesized a fluorescent quinolinium derivative, <b>QUCO-1</b>, which actively lit up with mtRNA in both normal and cancer cells in vitro. Additionally, we evaluated the function of <b>QUCO-1</b> as an mtRNA ligand and found that it effectively induced severe mitochondrial dysfunction and OXPHOS inhibition in RKO colorectal cancer cells. Treatment with <b>QUCO-1</b> resulted in apoptosis, cell cycle blockage at the G2/M phase, and the effective inhibition of cell proliferation. Our findings suggest that <b>QUCO-1</b> has great potential as a promising probe and therapeutic agent for mtRNA, with the potential for treating colorectal cancer. |
| first_indexed | 2024-03-11T06:07:28Z |
| format | Article |
| id | doaj.art-8878e8f93cc4401a8ba71e24843c8a4c |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-11T06:07:28Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-8878e8f93cc4401a8ba71e24843c8a4c2023-11-17T12:53:49ZengMDPI AGMolecules1420-30492023-03-01286269010.3390/molecules28062690Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNABo-Zheng Wang0Ying-Chen Zhou1Yu-Wei Lin2Xiu-Cai Chen3Ze-Yi Yu4Yao-Hao Xu5Jia-Heng Tan6Zhi-Shu Huang7Shuo-Bin Chen8Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaGuangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaMitochondria have a crucial role in regulating energy metabolism and their dysfunction has been linked to tumorigenesis. Cancer diagnosis and intervention have a great interest in the development of new agents that target biomolecules within mitochondria. However, monitoring and modulating mitochondria RNA (mtRNA), an essential component in mitochondria, in cells is challenging due to limited functional research and the absence of targeting agents. In this study, we designed and synthesized a fluorescent quinolinium derivative, <b>QUCO-1</b>, which actively lit up with mtRNA in both normal and cancer cells in vitro. Additionally, we evaluated the function of <b>QUCO-1</b> as an mtRNA ligand and found that it effectively induced severe mitochondrial dysfunction and OXPHOS inhibition in RKO colorectal cancer cells. Treatment with <b>QUCO-1</b> resulted in apoptosis, cell cycle blockage at the G2/M phase, and the effective inhibition of cell proliferation. Our findings suggest that <b>QUCO-1</b> has great potential as a promising probe and therapeutic agent for mtRNA, with the potential for treating colorectal cancer.https://www.mdpi.com/1420-3049/28/6/2690RNA fluorescent probeOXPHOS inhibitormitochondrial RNAanticancer |
| spellingShingle | Bo-Zheng Wang Ying-Chen Zhou Yu-Wei Lin Xiu-Cai Chen Ze-Yi Yu Yao-Hao Xu Jia-Heng Tan Zhi-Shu Huang Shuo-Bin Chen Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA Molecules RNA fluorescent probe OXPHOS inhibitor mitochondrial RNA anticancer |
| title | Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA |
| title_full | Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA |
| title_fullStr | Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA |
| title_full_unstemmed | Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA |
| title_short | Fluorescent Quinolinium Derivative as Novel Mitochondria Probe and Function Modulator by Targeting Mitochondrial RNA |
| title_sort | fluorescent quinolinium derivative as novel mitochondria probe and function modulator by targeting mitochondrial rna |
| topic | RNA fluorescent probe OXPHOS inhibitor mitochondrial RNA anticancer |
| url | https://www.mdpi.com/1420-3049/28/6/2690 |
| work_keys_str_mv | AT bozhengwang fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT yingchenzhou fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT yuweilin fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT xiucaichen fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT zeyiyu fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT yaohaoxu fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT jiahengtan fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT zhishuhuang fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna AT shuobinchen fluorescentquinoliniumderivativeasnovelmitochondriaprobeandfunctionmodulatorbytargetingmitochondrialrna |