4.4 Article

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

Journal

NATURAL PRODUCT RESEARCH
Volume 34, Issue 11, Pages 1505-1514

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2018.1517120

Keywords

Aspirin; thiourea; cytotoxicity; molecular docking; cyclooxygenase-2

Funding

  1. Universiti Malaysia Sarawak
  2. Malaysia Ministry of Science, Technology and Innovation [FRGS/ST02(01)/1115/2014(01), FRGS/ST01(01)/1298/2015(15)]
  3. Universiti Sultan Zainal Abidin [UniSZA/2017/DPU/02]

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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 mu M) in comparison to cisplatin, a positive cytotoxic drug (IC50 value =8.9 +/- 1.9 mu M). ATX 11, bearing iodine at meta position, showed robust cytotoxicity against HK-1 cells with an IC50 value of 4.7 +/- 0.7 mu M. 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.

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