title: A novel synthesized sulfonamido-based gallic acid--LDQN-C: effects on chondrocytes growth and phenotype maintenance.
abstract: Chondrocyte based therapy is promising to treat symptomatic chondral and osteochondral lesions. Growth factors to accelerate the proliferation and retain the phenotype of chondrocytes in vitro are imperative. However, the high cost and rapid degradation of growth factors limited their further application. Therefore, it is significant to find substitutes that can preserve chondrocytes phenotype and ensure sufficient cells for cytotherapy. Antioxidant and anti-inflammatory agents or their derivatives that have effect on arthritis may be an alternative. In this study, we synthesized sulfonamido-based gallate - LDQN-C and investigated its effect on rat articular chondrocytes through examination of the cell proliferation, morphology, viability, glycosaminoglycans (GAGs) synthesis and cartilage specific gene expression. Results showed that LDQN-C could enhance secretion and synthesis of cartilage extracellular matrix (ECM) by up-regulating expression levels of aggrecan, collagen II and Sox9 genes compared to the GA treated group and control group. Expression of collagen type II was effectively up-regulated while collagen I was down-regulated, which demonstrated that the inhibition of chondrocytes dedifferentiation by LDQN-C. Range of 1.36×10(-9)M to 1.36×10(-7)M is recommended dose of LDQN-C, among which the most profound response was observed with 1.36×10(-8)M. GA at concentration of 0.125μg/mL was compared. This study might provide a basis for the development of a novel agent for the treatment of articular cartilage defect.
authors.affiliation: The Medical and Scientific Research Center, Guangxi Medical University, Nanning 530021, China; Research Center for Regenerative Medicine, Guangxi Medical University, Nanning 530021, China.
authors.forename: Zhenhui
authors.initials: Z
authors.lastname: Lu
authors.affiliation: The Medical and Scientific Research Center, Guangxi Medical University, Nanning 530021, China.
authors.forename: Shixiu
authors.initials: S
authors.lastname: Wei
authors.affiliation: Department of Cell Biology & Genetics, School of Premedical Sciences, Guangxi Medical University, Nanning, Guangxi 530021, China.
authors.forename: Huayu
authors.initials: H
authors.lastname: Wu
authors.affiliation: Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Traditional Medical and Pharmaceutical Sciences, Nanning 530022, China; School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lin
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China.
authors.forename: Cuiwu
authors.initials: C
authors.lastname: Lin
authors.affiliation: Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Traditional Medical and Pharmaceutical Sciences, Nanning 530022, China.
authors.forename: Buming
authors.initials: B
authors.lastname: Liu
authors.affiliation: The Medical and Scientific Research Center, Guangxi Medical University, Nanning 530021, China; Research Center for Regenerative Medicine, Guangxi Medical University, Nanning 530021, China. Electronic address: zhengli224@163.com.
authors.forename: Li
authors.initials: L
authors.lastname: Zheng
authors.affiliation: Research Center for Regenerative Medicine, Guangxi Medical University, Nanning 530021, China.
authors.forename: Jinmin
authors.initials: J
authors.lastname: Zhao
mesh_terms: D000818:Animals; D002358:Cartilage, Articular / Q000166:cytology / Q000187:drug effects / Q000502:physiology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D019902:Chondrocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D020219:Chondrogenesis / Q000187:drug effects*; D005707:Gallic Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D013449:Sulfonamides; D005707:Gallic Acid
keywords: Chondrocyte based therapy; Gallic acid; Phenotype maintenance; Pro-chondrogenesis; Sulfachloropyrazine sodium