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Publikācija: Glyoxalase 1 and 2 Enzyme Inhibitory Activity of 6-Sulfamoylsaccharin and Sulfocoumarin Derivates

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā Glyoxalase 1 and 2 Enzyme Inhibitory Activity of 6-Sulfamoylsaccharin and Sulfocoumarin Derivates
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Marina Makrecka
Raivis Žalubovskis
Edijs Vavers
Jekaterīna Ivanova
Aiga Grandane
Maija Dambrova
Atslēgas vārdi 1, 2-benzoxathiine 2, 2-dioxide, Glyoxalase 1, Glyoxalase 2, 6-sulfamoylsaccharin, Sulfocoumarin, Trans-cinnamic acid - See more at: http://www.eurekaselect.com/109010/article#sthash.a6GKTwHi.dpuf
Anotācija The glyoxalase enzymes represent a cellular defence system against the accumulation of cytotoxic α- oxoaldehydes leading to apoptosis. The potential of glyoxalase inhibitors to act as novel anti-cancer agents for drugresistant tumours that over-express glyoxalase is currently under investigation. In the present study, a series of 6- sulfamoylsaccharin and 1,2-benzoxathiine 2,2-dioxide (sulfocoumarin - coumarin bioisostere) derivates, as well as, transcinnamic acid (the mimic of coumarin hydrolysis product) have been tested for the inhibition of glyoxalase 1 and 2. For the first time, it has been demonstrated, that 6-sulfamoylsaccharin possesses glyoxalase 1 inhibitory activity (IC50=90±15 μM). Two compounds, 5b and 9c, slightly inhibited the activity of glyoxalase 2. In addition, it has been demonstrated that trans-cinnamic acid inhibits glyoxalase 1 activity (IC50=84±4 μM). These data indicate that the modification of 6- sulfamoylsaccharin structure and coumarin hydrolysis products can be used to develop potential glyoxalase 1 inhibitors. - See more at: http://www.eurekaselect.com/109010/article#sthash.a6GKTwHi.dpuf
DOI: 10.2174/1570180811310050007
Hipersaite: http://www.eurekaselect.com/109010/article 
Atsauce Makrecka, M., Žalubovskis, R., Vavers, E., Ivanova, J., Grandane, A., Dambrova, M. Glyoxalase 1 and 2 Enzyme Inhibitory Activity of 6-Sulfamoylsaccharin and Sulfocoumarin Derivates. Letters in Drug Design & Discovery, 2013, Vol.10, Iss.5, 410.-415.lpp. ISSN 1570-1808. e-ISSN 1875-628X. Pieejams: doi:10.2174/1570180811310050007
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