Synthesis of Quinoline-2-Carboxylic Acid Aryl Ester and Its Apoptotic Action on PC3 Prostate Cancer Cell Line.

Abstract

The aim of the present study is to synthesise an aryl ester compound from quinoline-2-carboxylic acid to evaluate its apoptotic, cell cycle blockade, and antiproliferative activity on the prostate cancer cell lines (PC3). Chromatographic and spectroscopic analysis was used to identify the synthesised carboxylic acid compound. The synthesised compound was treated with a PC3 cell line for 24h with control. The cells were treated at various concentration ranges of 0, 3.91, 7.81, 15.63, 31.25, 62.5, 125, 250, 500, and 1000µg/mL each. The cytotoxicity effect was studied by MTT assay, and their anticancer activity was further evaluated using cell cycle analysis, DNA fragmentation assay, acridine orange-ethidium bromide staining, and Western blot analysis. The end antiproliferative result showed that PC3 cell viability decreases in a concentration-dependent manner and the synthesised compound exhibited potent cytotoxicity against PC3 cells with an IC50 value of 26µg/mL at the concentration of 125µg. The increase in the number of apoptotic cells was observed after treating PC3 cells with the sample in double-staining methods. S phase of the cell cycle was significantly blocked by the test sample, and a typical ladder pattern of internucleosomal fragmentation was observed. A decrease in the live cells was observed with the sample in AO/ET-BR. A significant increase in the Bax expression and a decrease in Bcl-2 expression observed enhance the activity of caspases-7 and -9. The synthesised compound had shown to possess excellent cytotoxic effect through inducing apoptosis, especially causing cell cycle arrest at the S phase.