title: Stimulating effect of a novel synthesized sulfonamido-based gallate ZXHA-TC on primary osteoblasts.
abstract: OBJECTIVE
  This 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.
  
  
  METHODS
  In 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.
  
  
  RESULTS
  The 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.
  
  
  CONCLUSIONS
  This study may hold promise for the development of a novel agent for the treatment of osteoporosis.
authors.affiliation: 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.
authors.forename: Pan
authors.initials: P
authors.lastname: Jin
authors.affiliation: Guangxi Key Laboratory of Regenerative Medicine, Guangxi Medical University, Nanning, Guangxi, China.; Department of Orthopedic Trauma and Hand Surgery, The First Affiliated Hospital of Guangxi Medical University, Nanning, Guangxi, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Liao
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi, China.; Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Traditional Medical and Pharmaceutical Sciences, Nanning, Guangxi, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lin
authors.affiliation: Department of Orthopedics, The First Hospital Affiliated to Henan University, Kaifeng, Henan, China.
authors.forename: Qinggong
authors.initials: Q
authors.lastname: Guo
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi, China.
authors.forename: Cuiwu
authors.initials: C
authors.lastname: Lin
authors.affiliation: Department of Cell Biology & Genetics, School of Premedical Sciences, Guangxi Medical University, Nanning, Guangxi, China.
authors.forename: Huayu
authors.initials: H
authors.lastname: Wu
authors.affiliation: Guangxi Key Laboratory of Regenerative Medicine, Guangxi Medical University, Nanning, Guangxi, China.; The Medical and Scientific Research Center, Guangxi Medical University, Nanning, Guangxi, China. zhengli224@163.com.
authors.forename: Li
authors.initials: L
authors.lastname: Zheng
authors.affiliation: Guangxi Key Laboratory of Regenerative Medicine, Guangxi Medical University, Nanning, Guangxi, China.; Department of Orthopedic Trauma and Hand Surgery, The First Affiliated Hospital of Guangxi Medical University, Nanning, Guangxi, China. zhaojinmin@126.com.
authors.forename: Jinmin
authors.initials: J
authors.lastname: Zhao
mesh_terms: D000469:Alkaline Phosphatase / Q000378:metabolism; D019485:Bone Morphogenetic Proteins / Q000494:pharmacology; D002454:Cell Differentiation / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D024042:Collagen Type I / Q000235:genetics; D000090602:Collagen Type I, alpha 1 Chain; D050659:Core Binding Factor Alpha 1 Subunit; D015536:Down-Regulation; D005707:Gallic Acid; D010006:Osteoblasts / Q000187:drug effects*; D015675:Osteocalcin / Q000378:metabolism; D010012:Osteogenesis / Q000187:drug effects; D010024:Osteoporosis / Q000517:prevention & control*; D017382:Reactive Oxygen Species; D015854:Up-Regulation
chemical_list: D019485:Bone Morphogenetic Proteins; D024042:Collagen Type I; D000090602:Collagen Type I, alpha 1 Chain; D050659:Core Binding Factor Alpha 1 Subunit; D017382:Reactive Oxygen Species; D015675:Osteocalcin; D005707:Gallic Acid; D000469:Alkaline Phosphatase
keywords: Gallic acid; osteoblast; osteogenesis; osteoporosis; sulfonamido
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