Discovery, Synthetic Methodology, and Biological Evaluation for Antiphotoaging Activity of Bicyclic[1,2,3]triazoles: In Vitro and in Vivo Studies
Copyright policy )Discovery, Synthetic Methodology, and Biological Evaluation for Antiphotoaging Activity of Bicyclic[1,2,3]triazoles: In Vitro and in Vivo Studies
Novel bicyclic[1,2,3]triazoles (4, 7, 11, 15) have been synthesized using a one-pot metal free strategy with high structural diversity as photoprotective agents, and their effect on UVA-induced senescence in human dermal fibroblast cells (FB) and the associated mechanism are delineated. 11d plus UVA can induce a decrease in reactive oxygen species (ROS) production and senescence-associated β-galactosidase (SA-β-gal) activity but an increase in adenosine triphosphate (ATP) synthesis and mitochondrial membrane potential (ΔΨmt). The mRNA levels of six senescence-associated genes, matrix metalloproteinase-1 (MMP-1), was decreased, while elastin, procollagen I type I, fibronectin, COL1α1, and tissue inhibitor of metalloproteinase-1 (TIMP-1) were increased. 11d plus UVA also decreased MMP-1 and increased TIMP-1 protein levels. Additionally, the thickness of the murine dorsal skin and epidermis, by UVA, was decreased by topical 11d treatment. Our results indicate that bicyclic[1,2,3]triazoles protect UVA-induced senescence-like characteristics in FB cells, which may provide potential prevention against photoaging.
- Kaohsiung Medical University Taiwan
Membrane Potential, Mitochondrial, Mice, Inbred ICR, Molecular Structure, Reverse Transcriptase Polymerase Chain Reaction, Immunoblotting, Gene Expression, Fibroblasts, Collagen Type I, Elastin, Fibronectins, Collagen Type I, alpha 1 Chain, Mice, Models, Chemical, Drug Design, Animals, Humans, Female, Matrix Metalloproteinase 1, Reactive Oxygen Species, Cells, Cultured
Membrane Potential, Mitochondrial, Mice, Inbred ICR, Molecular Structure, Reverse Transcriptase Polymerase Chain Reaction, Immunoblotting, Gene Expression, Fibroblasts, Collagen Type I, Elastin, Fibronectins, Collagen Type I, alpha 1 Chain, Mice, Models, Chemical, Drug Design, Animals, Humans, Female, Matrix Metalloproteinase 1, Reactive Oxygen Species, Cells, Cultured
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