Research Institute of Drug Development, College of Pharmacy, Chonnam National University, Gwangju, Korea.
School of Life Science, Hefei Normal University, Hefei, China.
Chem Biol Drug Des. 2018 Jan;91(1):17-28. doi: 10.1111/cbdd.13050. Epub 2017 Jul 14.
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, H NMR, C 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 antiproliferative 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.
设计、合成并评价了水溶性精氨酸-薯蓣皂素（Arg-DG）缀合物的生物学活性。采用傅里叶变换红外光谱（FT-IR）、氢核磁共振（1H NMR）、碳核磁共振（13C NMR）和高效液相色谱-质谱联用（HPLC-MS）分析对 Arg-DG 缀合物进行了表征，随后对其生物学活性进行了评价。与 DG 相比，Arg-DG 缀合物对 L929 细胞的细胞毒性降低，对肝细胞的增殖抑制活性增加。高灵敏度的 Alamar Blue 检测证实了 Arg-DG 缀合物的安全性，表明其在适宜浓度下可增加细胞代谢活性。Arg-DG 缀合物还可促进内皮管状结构的形成。此外，Arg-DG 缀合物可增强骨形态发生蛋白 2（BMP2）诱导的成骨细胞分化，与碱性磷酸酶（ALP）活性和矿化的协同作用。这些结果表明，本研究中开发的 Arg-DG 缀合物在骨组织工程等生物医学应用中具有巨大潜力。
