In vitro cytotoxicity evaluation of thioureaderivatives bearing Salix sp. constituent againstHK-1 cell lines

Norsyafikah Asyilla, Nordin and Vannessa, Lawai and Zainab, Ngaini and Ainaa Nadiah, Abd Halim and Siaw, San Hwang and Reagan, Entigu Linton and Boon, Kiat Lee and Paul Matthew, Neilsen (2020) In vitro cytotoxicity evaluation of thioureaderivatives bearing Salix sp. constituent againstHK-1 cell lines. Natural Product Research, 34 (11). pp. 1505-1514. ISSN 1478-6427

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Abstract

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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