In vitro cytotoxicity evaluation of thioureaderivatives bearing Salix sp. constituent againstHK-1 cell lines
In searching for drugs from natural product scaffolds has gained inter-est among researchers. In this study, a series of twelve halogenatedthiourea (ATX 1-12)viachemical modification of aspirin (a naturalproduct derivative) and evaluated for cytotoxic activity against naso-pharyngeal carcinoma (NPC)...
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| Main Authors: | , , , , , , , |
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| Format: | E-Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2020
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| Subjects: | |
| Online Access: | http://ir.unimas.my/id/eprint/30123/1/In%20vitro%20cytotoxicity%20evaluation%20of%20thioureaderivatives%20bearing%20Salix%20sp.%20constituent%20againstHK-1%20cell%20lines_Abstract.pdf http://ir.unimas.my/id/eprint/30123/ https://www.tandfonline.com/loi/gnpl20 |
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| Institution: | Universiti Malaysia Sarawak |
| Language: | English |
| Summary: | In searching for drugs from natural product scaffolds has gained inter-est among researchers. In this study, a series of twelve halogenatedthiourea (ATX 1-12)viachemical modification of aspirin (a naturalproduct derivative) and evaluated for cytotoxic activity against naso-pharyngeal carcinoma (NPC) cell lines, HK-1 via MTS-based colorimetricassay. The cytotoxicity studies demonstrated that halogens atmetapos-ition ofATXshowed promising activity against HK-1 cells (IC50value�15mM) in comparison to cisplatin, a positive cytotoxic drug (IC50value¼8.9 ± 1.9mM).ATX 11, bearing iodine atmetaposition, showed robustcytotoxicity against HK-1 cells with an IC50value of 4.7 ± 0.7mM.Molecular docking interactions betweenATX 11and cyclooxygenase-2demonstrated a robust binding affinity value of�8.1 kcal/mol as com-pared to aspirin’sbindingaffinityvalueof�6.4 kcal/mol. The findingsrepresent a promising lead molecule from natural product with excel-lent cytotoxic activity against NPC cell lines. |
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