Abstract

Objective: Boron-based molecules have attracted the attention of researchers in recent years, as they have become one of the largest and fastest-growing research areas. Presented in this study, various effects of tetrahedral boronate ester (BE) on, VCAM-1, E-selectin, and MCP-1 gene, and protein expression in ox-LDL induced in vitro atherosclerotic model were determined. Methods: IC₅₀ concentrations and effects of tetrahedral BE on cell survival were detected using XTT assay. Real-Time PCR (RT-PCR) was used to evaluate the mRNA expression levels of VCAM-1, E-selectin, MCP-1 genes and, western blotting determined the protein expression. Results: Tetrahedral BE compound did not show cytotoxicity against HUVECs at 50 µM concentration. ox-LDL treatment caused an increase in E-selectin, VCAM-1, and MCP-1 gene and protein expression levels in cell culture samples. Tetrahedral BE suppressed adhesion molecule expression such as VCAM-1 and E-selectin. Discussion: Tetrahedral BE treatment reversed all increases in E-selectin gene and protein expression levels in any of the treatment groups. ox-LDL increased VCAM-1 gene and protein expression, which was reversed by BE treatment in a dose-dependent manner. Moreover, ox-LDL triggered MCP-1 protein and gene expression levels and these increases were reversed significantly only by a mid and low-dose of BE treatment. The results showed that tetrahedral BE stabilized with N→B dative bond plays a protective role in the early stages of atherosclerosis. Conclusions: We reported a new tetrahedral boronate ester molecule based on trigonal-planar boronate ester and 4-hydroxy pyridine were designed and synthesized via B←N coordinate covalent bond. We have shown that boron-compound has decreased gene and protein expression of MCP-1, VCAM-1, and E-selectin increased by ox-LDL in the atherosclerosis model. These findings emerged that boron-based compounds could be an option for atherosclerosis treatment.