Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling
The aim of the present study is to provide a methodical platform for the development of lead compounds against cholangiocarcinoma. Coptisine was selected as a potential anti-cancer nominee from a pool of phytochemicals using an in silico 3-D docking screening technique and validated the anti-cancer...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2024-01-01
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| Series: | Journal of Functional Foods |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1756464623005492 |
| _version_ | 1797356170094051328 |
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| author | Jungwhoi Lee Jungsul Lee Woogwang Sim Jae-Hoon Kim |
| author_facet | Jungwhoi Lee Jungsul Lee Woogwang Sim Jae-Hoon Kim |
| author_sort | Jungwhoi Lee |
| collection | DOAJ |
| description | The aim of the present study is to provide a methodical platform for the development of lead compounds against cholangiocarcinoma. Coptisine was selected as a potential anti-cancer nominee from a pool of phytochemicals using an in silico 3-D docking screening technique and validated the anti-cancer effects against cholangiocarcinoma through the blockade of EGFR signaling depending on the cellular degradation. We also verified that coptisine had no cytotoxicity in different human normal cells when compared with the clinically approved anti-cancer drug, erlotinib. In vitro and in silico analyses revealed that coptisine can suppress the expression of various oncogenic molecules and administrating coptisine showed an anti-cholangiocarcinoma tumor growth or recurrence using in vivo models. Collectively, we propose that a well-organized methodical 3-D docking screening platform is an innovative technique for the discovery of anti-cancer drugs against malignant tumors, and coptisine might be a safe and effective anti-cancer reagent against cholangiocarcinoma. |
| first_indexed | 2024-03-08T14:22:49Z |
| format | Article |
| id | doaj.art-fe68c57768ef45cc955dd8b50e636c15 |
| institution | Directory Open Access Journal |
| issn | 1756-4646 |
| language | English |
| last_indexed | 2024-03-08T14:22:49Z |
| publishDate | 2024-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Functional Foods |
| spelling | doaj.art-fe68c57768ef45cc955dd8b50e636c152024-01-14T05:37:18ZengElsevierJournal of Functional Foods1756-46462024-01-01112105949Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signallingJungwhoi Lee0Jungsul Lee1Woogwang Sim2Jae-Hoon Kim3Department of Applied Life Science, Jeju National University, Jeju-do 63243, Republic of Korea; Corresponding author at: Department of Biotechnology, College of Applied Life Science, Jeju National University, 102 Jejudaehak-ro, Jeju-si, Jeju-do 63243, Republic of Korea.Department of Bio and Brain Engineering, Korea Advanced Institute of Science and Technology, Daejeon 34141, Republic of KoreaDepartment of Anatomy, University of California San Francisco, CA 94143, United StatesDepartment of Applied Life Science, Jeju National University, Jeju-do 63243, Republic of Korea; Subtropical/tropical Organism Gene Bank, Jeju National University, Jeju-do 690-756, Republic of Korea; Corresponding author at: Department of Biotechnology, College of Applied Life Science, Jeju National University, 102 Jejudaehak-ro, Jeju-si, Jeju-do 63243, Republic of Korea.The aim of the present study is to provide a methodical platform for the development of lead compounds against cholangiocarcinoma. Coptisine was selected as a potential anti-cancer nominee from a pool of phytochemicals using an in silico 3-D docking screening technique and validated the anti-cancer effects against cholangiocarcinoma through the blockade of EGFR signaling depending on the cellular degradation. We also verified that coptisine had no cytotoxicity in different human normal cells when compared with the clinically approved anti-cancer drug, erlotinib. In vitro and in silico analyses revealed that coptisine can suppress the expression of various oncogenic molecules and administrating coptisine showed an anti-cholangiocarcinoma tumor growth or recurrence using in vivo models. Collectively, we propose that a well-organized methodical 3-D docking screening platform is an innovative technique for the discovery of anti-cancer drugs against malignant tumors, and coptisine might be a safe and effective anti-cancer reagent against cholangiocarcinoma.http://www.sciencedirect.com/science/article/pii/S17564646230054923-D docking modelingCoptisineEGFRCholangiocarcinomaDrug-discovery |
| spellingShingle | Jungwhoi Lee Jungsul Lee Woogwang Sim Jae-Hoon Kim Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling Journal of Functional Foods 3-D docking modeling Coptisine EGFR Cholangiocarcinoma Drug-discovery |
| title | Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling |
| title_full | Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling |
| title_fullStr | Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling |
| title_full_unstemmed | Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling |
| title_short | Methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of EGFR signalling |
| title_sort | methodical selected coptisine attenuates the malignancy of cholangiocarcinoma through the blockade of egfr signalling |
| topic | 3-D docking modeling Coptisine EGFR Cholangiocarcinoma Drug-discovery |
| url | http://www.sciencedirect.com/science/article/pii/S1756464623005492 |
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