• Pan Jin, Liang Liao, Xiao Lin, Qinggong Guo, Cuiwu Lin, Huayu Wu, Li Zheng, and Jinmin Zhao.
• Department of Orthopedics, The First Hospital Affiliated to Henan University, Kaifeng, Henan, China.; Guangxi Key Laboratory of Regenerative Medicine, Guangxi Medical University, Nanning, Guangxi, China.
• Yonsei Med. J. 2015 May 1; 56 (3): 760-71.

PurposeThis study is intended to investigate the effects of plants or plant-derived antioxidants on prevention of osteoporosis through the maintenance of reactive oxygen species (ROS) at a favorable level.Materials And MethodsIn this study, a novel antioxidant, namely 3,4,5-Trihydroxy-N-[4-(5-hydroxy-6-methoxy-pyrimidin-4-ylsulfamoyl)-phenyl]-benzamide (ZXHA-TC) was synthesized from gallic acid and sulfadimoxine. Its effect on osteoblast metabolism was investigated via the detection of cell proliferation, cell viability, production of ROS, and expression of osteogenic-specific genes including runt-related transcription factor 2 (RUNX2), bone sialoprotein (BSP), osteocalcin (OCN), alpha-1 type I collagen (COL1A1), and osteogenic-related proteins after treatment for 2, 4, and 6 days respectively.ResultsThe results showed that ZXHA-TC has a stimulating effect on the proliferation and osteogenic differentiation of primary osteoblasts by promoting cell proliferation, cell viability, and the expression of genes BSP and OCN. Productions of bone matrix and mineralization were also increased by ZXHA-TC treatment as a result of up-regulation of COL1A1 and alkaline phosphatase (ALP) at the early stage and down-regulation of both genes subsequently. A range of 6.25×10⁻³ microg/mL to 6.25×10⁻¹ microg/mL is the recommended dose for ZXHA-TC, within which 6.25×10⁻² μg/mL showed the best performance.ConclusionThis study may hold promise for the development of a novel agent for the treatment of osteoporosis.

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