Dione-thiophene conjugate inhibits proliferation and metastasis of nasopharyngeal carcinoma cells through calcium binding protein-P down-regulation.

ABSTRACT

In the present study a series of dione-thiophenol conjugates was prepared and evaluated against nasopharyngeal carcinoma (NPC) cells. MTT assay showed that compound 4a reduced proliferation of C666-1 and CNE-1 cells to 26 and 24%, respectively at 10 µmol/l concentration. Flow cytometry revealed that increasing the concentration of compound 4a from 2 to 10 µmol/l increased the proportion of early apoptotic C666-1 cells from 2.76 to 69.43%. A significant (P < 0.001) decrease in the expression of S100P was caused by compound 4a. In compound 4a treated C666-1 cells the expression of RAGE, EGFR, CD44, MMP2 and MMP9 was markedly decreased. In summary, compound 4a inhibits nasopharyngeal cancer cell proliferation and induces apoptosis through down-regulation of S100P. Moreover, compound 4a also decreases MMP-2, MMP-9, EGFR, CD44 and RAGE expression in nasopharyngeal cancer cells. Thus, compound 4a can be investigated further as a drug candidate for the treatment of nasopharyngeal cancer.