Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies
Sulfated galactans (SG) isolated from red alga <i>Gracilaria fisheri</i> have been reported to inhibit the growth of cholangiocarcinoma (CCA) cells, which was similar to the epidermal growth factor receptor (EGFR)-targeted drug, cetuximab. Herein, we studied the anti-cancer potency of SG...
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MDPI AG
2021-04-01
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| author | Boonyakorn Boonsri Kiattawee Choowongkomon Buabarn Kuaprasert Thanvarin Thitiphatphuvanon Kittiya Supradit Apinya Sayinta Jinchutha Duangdara Tawut Rudtanatip Kanokpan Wongprasert |
| author_facet | Boonyakorn Boonsri Kiattawee Choowongkomon Buabarn Kuaprasert Thanvarin Thitiphatphuvanon Kittiya Supradit Apinya Sayinta Jinchutha Duangdara Tawut Rudtanatip Kanokpan Wongprasert |
| author_sort | Boonyakorn Boonsri |
| collection | DOAJ |
| description | Sulfated galactans (SG) isolated from red alga <i>Gracilaria fisheri</i> have been reported to inhibit the growth of cholangiocarcinoma (CCA) cells, which was similar to the epidermal growth factor receptor (EGFR)-targeted drug, cetuximab. Herein, we studied the anti-cancer potency of SG compared to cetuximab. Biological studies demonstrated SG and cetuximab had similar inhibition mechanisms in CCA cells by down-regulating EGFR/ERK pathway, and the combined treatment induced a greater inhibition effect. The molecular docking study revealed that SG binds to the dimerization domain of EGFR, and this was confirmed by dimerization assay, which showed that SG inhibited ligand-induced EGFR dimer formation. Synchrotron FTIR microspectroscopy was employed to examine alterations in cellular macromolecules after drug treatment. The SR-FTIR-MS elicited similar spectral signatures of SG and cetuximab, pointing towards the bands of RNA/DNA, lipids, and amide I vibrations, which were inconsistent with the changes of signaling proteins in CCA cells after drug treatment. Thus, this study demonstrates the underlined anti-cancer mechanism of SG by interfering with EGFR dimerization. In addition, we reveal that FTIR signature spectra offer a useful tool for screening anti-cancer drugs’ effect. |
| first_indexed | 2024-03-10T11:49:28Z |
| format | Article |
| id | doaj.art-b21866fb7087493089f472053a99e853 |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-03-10T11:49:28Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-b21866fb7087493089f472053a99e8532023-11-21T17:52:46ZengMDPI AGMarine Drugs1660-33972021-04-0119525810.3390/md19050258Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro StudiesBoonyakorn Boonsri0Kiattawee Choowongkomon1Buabarn Kuaprasert2Thanvarin Thitiphatphuvanon3Kittiya Supradit4Apinya Sayinta5Jinchutha Duangdara6Tawut Rudtanatip7Kanokpan Wongprasert8Department of Anatomy, Faculty of Science, Mahidol University, Bangkok 10400, ThailandDepartment of Biochemistry, Faculty of Science, Kasetsart University, Bangkok 10900, ThailandResearch and Facility Division, Synchrotron Light Research Institute (Public Organization), Nakhorn Ratchasima 30000, ThailandDepartment of Anatomy, Faculty of Medicine, Siam University, Bangkok 10160, ThailandDepartment of Anatomy, Faculty of Science, Mahidol University, Bangkok 10400, ThailandDepartment of Anatomy, Faculty of Science, Mahidol University, Bangkok 10400, ThailandDepartment of Anatomy, Faculty of Science, Mahidol University, Bangkok 10400, ThailandDepartment of Anatomy, Faculty of Medicine, Khon Kean University, Khon Kean 40002, ThailandDepartment of Anatomy, Faculty of Science, Mahidol University, Bangkok 10400, ThailandSulfated galactans (SG) isolated from red alga <i>Gracilaria fisheri</i> have been reported to inhibit the growth of cholangiocarcinoma (CCA) cells, which was similar to the epidermal growth factor receptor (EGFR)-targeted drug, cetuximab. Herein, we studied the anti-cancer potency of SG compared to cetuximab. Biological studies demonstrated SG and cetuximab had similar inhibition mechanisms in CCA cells by down-regulating EGFR/ERK pathway, and the combined treatment induced a greater inhibition effect. The molecular docking study revealed that SG binds to the dimerization domain of EGFR, and this was confirmed by dimerization assay, which showed that SG inhibited ligand-induced EGFR dimer formation. Synchrotron FTIR microspectroscopy was employed to examine alterations in cellular macromolecules after drug treatment. The SR-FTIR-MS elicited similar spectral signatures of SG and cetuximab, pointing towards the bands of RNA/DNA, lipids, and amide I vibrations, which were inconsistent with the changes of signaling proteins in CCA cells after drug treatment. Thus, this study demonstrates the underlined anti-cancer mechanism of SG by interfering with EGFR dimerization. In addition, we reveal that FTIR signature spectra offer a useful tool for screening anti-cancer drugs’ effect.https://www.mdpi.com/1660-3397/19/5/258red alga <i>Gracilaria fisheri</i>sulfated galactanssynchrotron-FTIR-MSmolecular dockingepidermal growth factor receptoranti-cancer |
| spellingShingle | Boonyakorn Boonsri Kiattawee Choowongkomon Buabarn Kuaprasert Thanvarin Thitiphatphuvanon Kittiya Supradit Apinya Sayinta Jinchutha Duangdara Tawut Rudtanatip Kanokpan Wongprasert Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies Marine Drugs red alga <i>Gracilaria fisheri</i> sulfated galactans synchrotron-FTIR-MS molecular docking epidermal growth factor receptor anti-cancer |
| title | Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies |
| title_full | Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies |
| title_fullStr | Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies |
| title_full_unstemmed | Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies |
| title_short | Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies |
| title_sort | probing the anti cancer potency of sulfated galactans on cholangiocarcinoma cells using synchrotron ftir microspectroscopy molecular docking and in vitro studies |
| topic | red alga <i>Gracilaria fisheri</i> sulfated galactans synchrotron-FTIR-MS molecular docking epidermal growth factor receptor anti-cancer |
| url | https://www.mdpi.com/1660-3397/19/5/258 |
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