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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...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10606936/ https://www.ncbi.nlm.nih.gov/pubmed/37894822 http://dx.doi.org/10.3390/ijms242015142 |
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author | 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 |
author_facet | 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 |
author_sort | Ma, Yunhao |
collection | PubMed |
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. |
format | Online Article Text |
id | pubmed-10606936 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-106069362023-10-28 Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling 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 Int J Mol Sci Article 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. MDPI 2023-10-13 /pmc/articles/PMC10606936/ /pubmed/37894822 http://dx.doi.org/10.3390/ijms242015142 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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/). |
spellingShingle | Article 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 Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
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 |
title_full | Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
title_fullStr | Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
title_full_unstemmed | Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
title_short | Biological Evaluation of 8-Methoxy-2,5-dimethyl-5H-indolo[2,3-b] Quinoline as a Potential Antitumor Agent via PI3K/AKT/mTOR Signaling |
title_sort | biological evaluation of 8-methoxy-2,5-dimethyl-5h-indolo[2,3-b] quinoline as a potential antitumor agent via pi3k/akt/mtor signaling |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10606936/ https://www.ncbi.nlm.nih.gov/pubmed/37894822 http://dx.doi.org/10.3390/ijms242015142 |
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