Synthesis and biological evaluation of arginyl-diosgenin conjugate as a potential bone tissue engineering agent

Abstract

Water-soluble arginyl-diosgenin (Arg-DG) conjugate was designed, synthesized, and evaluated for a biological activity. The Arg-DG conjugate was characterized using FT-IR, ¹H NMR, ¹³C NMR, and HPLC-MS analyses, followed by a biological activity evaluation. Compared with DG, the Arg-DG conjugate showed a decreased cytotoxicity against L929 cells and an increased anti-proliferative activity against hepatocellular cells. The safety of the Arg-DG conjugate was confirmed using the highly sensitive Alamar Blue assay, which indicated that it increased the cellular metabolic activity at suitable concentrations. The Arg-DG conjugate promoted an endothelial tube formation as well. Furthermore, the Arg-DG conjugate improved the bone morphogenetic protein 2 (BMP2)-induced osteoblastic differentiation with synergistic effects on alkaline phosphatase (ALP) activity and mineralization. These results suggest that the Arg-DG conjugate developed in this study has great potentials for biomedical applications such as bone tissue engineering.

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Arginyl-diosgenin (Arg-DG) conjugate was successfully synthesized and characterized to increase solubility of poorly water-soluble diosgenin (DG). Arg-DG conjugate was manifested to reduce the cytotoxicity of DG against normal cells and increase the cellular metabolic activity of normal cells in vitro, while enhancing the anti-proliferative activity against HepG2 cell. Arg-DG conjugate was demonstrated to promote endothelial tube formation and BMP2- induced osteogenesis potentially resulting in synergistically stimulating alkaline phosphatase activity and mineralization.

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