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KMID : 0043320190420090790
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Archives of Pharmacal Research
2019 Volume.42 No. 9 p.790 ~ p.814
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Effect of thiazolidinedione phenylacetate derivatives on wound-healing activity
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Park So-Hee
Choi Du-Bok
Cho Hoon
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Abstract
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The aim of this work was to evaluate the synthesis and structure?activity relationship of 4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenyl 2-phenylacetate derivatives as potential wound-healing agents. The IC50 values of the lead compounds ranged from 0.01 to 0.05 μM. These compounds also increased the levels of extracellular prostaglandin E2 (PGE2) in A549 cells. Among the synthesized compounds, compounds 66, 67, 69, and 86 increased PGE2 levels 3- to 4-fold of those achieved with the negative control. Introduction of a halogen at the intermediate phenyl ring, compounds 66, 67, 69, and 86 resulted in higher IC50 values, which indicated lower cytotoxicity than that observed upon the introduction of other substituents at the same position. In particular, cells exposed to compound 69 showed significantly improved wound healing, and the wound closure rate achieved was approximately 3.2-fold higher than that of the control. Therefore, compound 69 can be used for tissue regeneration and treatment of diverse diseases caused by PGE2 deficiency. Overall, our findings suggested that compound 69 might be a novel candidate for skin wound therapy.
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KEYWORD
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Thiazolidinedione phenylacetate, 15-PGDH inhibitors, PGE2, Wound healing
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