Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling
Chemotherapy is commonly used clinically to treat colorectal cancer, but it is usually prone to drug resistance, so novel drugs need to be developed continuously to treat colorectal cancer. Neocryptolepine derivatives have attracted a lot of attention because of their good cytotoxic activity; howeve...
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| Veröffentlicht in: | International journal of molecular sciences 2023-10, Vol.24 (20), p.15142 |
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| creator | Ma, Yunhao Zhu, Hongmei Jiang, Xinrong Zhou, Zhongkun Zhou, Yong Tian, Yanan Zhang, Hao Sun, Mengze Tu, Lixue Lu, Juan Niu, Yuqing Liu, Huanxiang Liu, Yingqian Chen, Peng |
| description | Chemotherapy is commonly used clinically to treat colorectal cancer, but it is usually prone to drug resistance, so novel drugs need to be developed continuously to treat colorectal cancer. Neocryptolepine derivatives have attracted a lot of attention because of their good cytotoxic activity; however, cytotoxicity studies on colorectal cancer cells are scarce. In this study, the cytotoxicity of 8-methoxy-2,5-dimethyl-5H-indolo[2,3-b] quinoline (MMNC) in colorectal cells was evaluated. The results showed that MMNC inhibits the proliferation of HCT116 and Caco-2 cells, blocks the cell cycle in the G2/M phase, decreases the cell mitochondrial membrane potential and induces apoptosis. In addition, the results of western blot experiments suggest that MMNC exerts cytotoxicity by inhibiting the expression of PI3K/AKT/mTOR signaling pathway-related proteins. Based on these results, MMNC is a promising lead compound for anticancer activity in the treatment of human colorectal cancer. |
| doi_str_mv | 10.3390/ijms242015142 |
| format | Article |
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Neocryptolepine derivatives have attracted a lot of attention because of their good cytotoxic activity; however, cytotoxicity studies on colorectal cancer cells are scarce. In this study, the cytotoxicity of 8-methoxy-2,5-dimethyl-5H-indolo[2,3-b] quinoline (MMNC) in colorectal cells was evaluated. The results showed that MMNC inhibits the proliferation of HCT116 and Caco-2 cells, blocks the cell cycle in the G2/M phase, decreases the cell mitochondrial membrane potential and induces apoptosis. In addition, the results of western blot experiments suggest that MMNC exerts cytotoxicity by inhibiting the expression of PI3K/AKT/mTOR signaling pathway-related proteins. Based on these results, MMNC is a promising lead compound for anticancer activity in the treatment of human colorectal cancer.</description><identifier>ISSN: 1422-0067</identifier><identifier>ISSN: 1661-6596</identifier><identifier>EISSN: 1422-0067</identifier><identifier>DOI: 10.3390/ijms242015142</identifier><identifier>PMID: 37894822</identifier><language>eng</language><publisher>Basel: MDPI AG</publisher><subject>Antimitotic agents ; Antineoplastic agents ; Apoptosis ; Breast cancer ; Cancer ; Cancer therapies ; Cell cycle ; Cell growth ; Chemotherapy ; Colorectal cancer ; Cytotoxicity ; Drug resistance ; Ethylenediaminetetraacetic acid ; Flow cytometry ; Kinases ; Leukemia ; Liver cancer ; Lung cancer ; Natural products ; Oncology, Experimental ; Pharmaceutical industry ; Proteins ; Quinoline</subject><ispartof>International journal of molecular sciences, 2023-10, Vol.24 (20), p.15142</ispartof><rights>COPYRIGHT 2023 MDPI AG</rights><rights>2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). 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Neocryptolepine derivatives have attracted a lot of attention because of their good cytotoxic activity; however, cytotoxicity studies on colorectal cancer cells are scarce. In this study, the cytotoxicity of 8-methoxy-2,5-dimethyl-5H-indolo[2,3-b] quinoline (MMNC) in colorectal cells was evaluated. The results showed that MMNC inhibits the proliferation of HCT116 and Caco-2 cells, blocks the cell cycle in the G2/M phase, decreases the cell mitochondrial membrane potential and induces apoptosis. In addition, the results of western blot experiments suggest that MMNC exerts cytotoxicity by inhibiting the expression of PI3K/AKT/mTOR signaling pathway-related proteins. 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| subjects | Antimitotic agents Antineoplastic agents Apoptosis Breast cancer Cancer Cancer therapies Cell cycle Cell growth Chemotherapy Colorectal cancer Cytotoxicity Drug resistance Ethylenediaminetetraacetic acid Flow cytometry Kinases Leukemia Liver cancer Lung cancer Natural products Oncology, Experimental Pharmaceutical industry Proteins Quinoline |
| title | Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
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