ReferenceID 5112
Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways
Biochem Pharmacol
Dictamnine (Dic), a naturally occurring small-molecule furoquinoline alkaloid isolated from the root bark of Dictamnus dasycarpus Turcz., is reported to display anticancer properties. However, little is known about the d
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Record Fields
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- Reference Id
- 5112
- Evidence Id
- 21702
- Core Evidence Id
- 21702
- Source Reference Id
- 3511
- Herb2 Reference Id
- HBREF004308
- Subject Paper Key
- HBIN023700_34861243
- Pubmed Id
- 34861243
- Doi
- 10.1016/j.bcp.2021.114864
- Paper Title
- Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways
- Paper Abstract
- Dictamnine (Dic), a naturally occurring small-molecule furoquinoline alkaloid isolated from the root bark of Dictamnus dasycarpus Turcz., is reported to display anticancer properties. However, little is known about the direct target proteins and anticancer mechanisms of Dic. In the current study, Dic was found to suppress the growth of lung cancer cells in vitro and in vivo, and to attenuate the activation of PI3K/AKT/mTOR and mitogen-activated protein kinase (MAPK) signaling pathways by inhibiting the phosphorylation and activation of receptor tyrosine kinase c-Met. Moreover, the binding of Dic to c-Met was confirmed by using cellular thermal shift assay (CETSA) and drug affinity responsive target stability (DARTS) assay. Among all cancer cell lines tested, Dic inhibited the proliferation of c-Met-dependent EBC-1 cells with the greatest potency (IC50 = 2.811 muM). Notably, Dic was shown to synergistically improve the chemo-sensitivity of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI)-resistant lung cancer cells to gefitinib and osimertinib. These results suggest that Dic is a c-Met inhibitor that can serve as a potential therapeutic agent in the treatment of lung cancer, especially against EGFR TKI-resistant and c-Met-dependent lung cancer.
- Journal
- Biochem Pharmacol
- Publish Year
- 2022
- Experiment Subject
- c-met-dependent ebc-1 cells; cancer cell lines; epidermal growth factor receptor-tyrosine kinase inhibitor (egfr-tki)-resistant lung cancer cells
- Experiment Type
- Cell Experiment
- Phenotype Related
- C-met-dependent Lung Cancer; Lung Cancer; Cancer
- Paper Title Cn
- Paper Title En
- Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways
- Bilingual Status
- semi_complete