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

Abstract

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 (IC 50 value 15 mM) in comparison to cisplatin, a positive cytotoxic drug (IC 50 value ¼8.9 ± 1.9 mM). ATX 11, bearing iodine at meta position, showed robust cytotoxicity against HK-1 cells with an IC 50 value of 4.7 ± 0.7 mM. Molecular docking interactions between ATX 11 and cyclooxygenase-2 demonstrated a robust binding affinity value of À8.1 kcal/mol as compared to aspirin's binding affinity value of À6.4 kcal/mol. The findings represent a promising lead molecule from natural product with excellent cytotoxic activity against NPC cell lines.

A network pharmacology approach to evaluate the synergistic effect of dihydromyricetin and myricitrin in vine tea on the proliferation of B16F10 cells

“…This inhibitory effect has two main aspects: inhibiting cancer cell proliferation and promoting cancer cell apoptosis (45)(46)(47). Recent studies have shown inhibitory effects on the expansion of human acute promyelocytic leukemia cells and K562 cells (48), Bel-7402 cells (49), human breast cancer cells (50,51), and nasopharyngeal carcinoma HK -1 cells (27). We expected that both DMY and MYT would have inhibitory effects on B16F10 cells.…”

“…After treatment for 72 h, 10 µL of 5 mg/mL MTT was added to each well. The media containing MTT was removed after 4 h, and 100 µL DMSO was added to each well to dissolve the formazan crystals (27). The plate was shaken for 1 min, the absorbance at 490 nm was measured, the inhibition rate of the drug on cell growth was calculated, and the general equation for the dose-effect relationship was obtained according to the following formula.…”

Synthesis of Silver (I) Coordination of Aspirinate Azo Ligands as Potential Antibacterial Agents

“…Hybridization of azo dyes with natural product-based compounds with multifunctional groups can increase the efficiency and probability of additional interactions with biological targets/receptors [3]. Our preliminary studies on azo dyes bearing natural product-based compounds such as aspirin and kojic acid showed antibacterial activities [3,8,9,10] and anticancer activity [11,12].…”

Effect of Microwave and Ultrasound-Assisted Extraction on the Phytochemical and In Vitro Biological Properties of Willow (Salix alba) Bark Aqueous and Ethanolic Extracts

“…Among medicinal plants with interesting bioactive content, the genus Salix (willow) presents great potential, comprising about 500 species that grow well in marginal wet land distributed worldwide. This large number of species makes this plant one of the most abundant sources of renewable raw materials for multiple end-uses [3][4][5][6]. Willow extracts and herbal tea derived from the plant bark are currently available from the species S. purpurea, S. daphnoides, and S. fragilis [7].…”