Yonsei Med J.  2015 May;56(3):760-771. 10.3349/ymj.2015.56.3.760.

Stimulating Effect of a Novel Synthesized Sulfonamido-Based Gallate ZXHA-TC on Primary Osteoblasts

  • 1Department of Orthopedics, The First Hospital Affiliated to Henan University, Kaifeng, Henan, China.
  • 2Guangxi Key Laboratory of Regenerative Medicine, Guangxi Medical University, Nanning, Guangxi, China. zhengli224@163.com, zhaojinmin@126.com
  • 3Department of Orthopedic Trauma and Hand Surgery, The First Affiliated Hospital of Guangxi Medical University, Nanning, Guangxi, China.
  • 4School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi, China.
  • 5Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Traditional Medical and Pharmaceutical Sciences, Nanning, Guangxi, China.
  • 6Department of Cell Biology & Genetics, School of Premedical Sciences, Guangxi Medical University, Nanning, Guangxi, China.
  • 7The Medical and Scientific Research Center, Guangxi Medical University, Nanning, Guangxi, China.


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.
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.
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 6.25x10(-3) microg/mL to 6.25x10(-1) microg/mL is the recommended dose for ZXHA-TC, within which 6.25x10(-2) microg/mL showed the best performance.
This study may hold promise for the development of a novel agent for the treatment of osteoporosis.


Gallic acid; sulfonamido; osteoporosis; osteogenesis; osteoblast

MeSH Terms

Alkaline Phosphatase/metabolism
Bone Morphogenetic Proteins/pharmacology
Cell Differentiation/*drug effects
Cell Proliferation/*drug effects
Collagen Type I/genetics
Core Binding Factor Alpha 1 Subunit
Gallic Acid
Osteoblasts/*drug effects
Osteogenesis/drug effects
Osteoporosis/*prevention & control
Reactive Oxygen Species
Alkaline Phosphatase
Bone Morphogenetic Proteins
Collagen Type I
Core Binding Factor Alpha 1 Subunit
Gallic Acid
Reactive Oxygen Species
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