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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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.
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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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