In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines

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building INTELEK Repository
caption Natural Product Research, 2018. doi: 10.1080/14786419.2018.1517120
collection Online Access
collectionurl https://intelek.unisza.edu.my/intelek/pages/search.php?search=!collection407072
copyright © 2018 Informa UK Limited, trading as Taylor & Francis Group
date 2018-11-29 15:02:55
format Restricted Document
id 11841
institution UniSZA
originalfilename 6141-01-FH02-FF-18-19751.pdf
person Nordin Norsyafikah Asyilla
Lawai Vannessa
Ngaini Zainab
Abd Halim Ainaa Nadiah
Hwang Siaw San
Linton Reagan Entigu
Lee Boon Kiat
Neilsen Paul Matthew
recordtype oai_dc
resourceurl https://intelek.unisza.edu.my/intelek/pages/view.php?ref=11841
spelling 11841 https://intelek.unisza.edu.my/intelek/pages/view.php?ref=11841 https://intelek.unisza.edu.my/intelek/pages/search.php?search=!collection407072 Restricted Document Article Journal application/pdf 11 1.6 Adobe Acrobat Pro DC 20 Paper Capture Plug-in Nordin Norsyafikah Asyilla Lawai Vannessa Ngaini Zainab Abd Halim Ainaa Nadiah Hwang Siaw San Linton Reagan Entigu Lee Boon Kiat Neilsen Paul Matthew © 2018 Informa UK Limited, trading as Taylor & Francis Group 2018-11-29 15:02:55 Natural Product Research, 2018. doi: 10.1080/14786419.2018.1517120 Aspirin thiourea cytotoxicity molecular docking cyclooxygenase-2 In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines 6141-01-FH02-FF-18-19751.pdf In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines UniSZA Private Access In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines Natural Product Research In searching for drugs from natural product scaffolds has gained interest among researchers. In this study, a series of twelve halogenated thiourea (ATX 1-12) via chemical modification of aspirin (a natural product derivative) and evaluated for cytotoxic activity against nasopharyngeal carcinoma (NPC) cell lines, HK-1 via MTS-based colorimetric assay. The cytotoxicity studies demonstrated that halogens at meta position of ATX showed promising activity against HK-1 cells (IC50 value �15 mM) in comparison to cisplatin, a positive cytotoxic drug (IC50 value ¼8.9±1.9 mM). ATX 11, bearing iodine at meta position, showed robust cytotoxicity against HK-1 cells with an IC50 value of 4.7±0.7mM. Molecular docking interactions between ATX 11 and cyclooxygenase-2 demonstrated a robust binding affinity value of �8.1 kcal/mol as compared to aspirin’s binding affinity value of �6.4 kcal/mol. The findings represent a promising lead molecule from natural product with excellent cytotoxic activity against NPC cell lines. 1 1 1-10
spellingShingle In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
subject Aspirin
thiourea
cytotoxicity
molecular docking
cyclooxygenase-2
summary In searching for drugs from natural product scaffolds has gained interest among researchers. In this study, a series of twelve halogenated thiourea (ATX 1-12) via chemical modification of aspirin (a natural product derivative) and evaluated for cytotoxic activity against nasopharyngeal carcinoma (NPC) cell lines, HK-1 via MTS-based colorimetric assay. The cytotoxicity studies demonstrated that halogens at meta position of ATX showed promising activity against HK-1 cells (IC50 value �15 mM) in comparison to cisplatin, a positive cytotoxic drug (IC50 value ¼8.9±1.9 mM). ATX 11, bearing iodine at meta position, showed robust cytotoxicity against HK-1 cells with an IC50 value of 4.7±0.7mM. Molecular docking interactions between ATX 11 and cyclooxygenase-2 demonstrated a robust binding affinity value of �8.1 kcal/mol as compared to aspirin’s binding affinity value of �6.4 kcal/mol. The findings represent a promising lead molecule from natural product with excellent cytotoxic activity against NPC cell lines.
title In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
title_full In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
title_fullStr In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
title_full_unstemmed In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
title_short In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
title_sort in vitro cytotoxicity evaluation of thiourea derivatives bearing salix sp. constituent against hk-1 cell lines