New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities
Copyright policy )New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities
Biscoumarin derivatives 1-27 were tested for their inhibition of snake venom and human nucleotide pyrophosphatase phosphodiesterase-1 enzymes. Lineweaver-Burk and Dixon plots and their secondary replots showed that these compounds are pure non-competitive inhibitors of both the enzymes. Ki and IC50 values of biscoumarins were found to be in the range of 50 to 1000 and 164 to > 1000 microM, respectively, against human recombinant phosphodiesterase 1 enzyme and 8.0 to 1150 and 9.44 to > 1000 microM, respectively, against snake venom phosphodiesterase. Compounds 1, 3, 4, 6, 7, 17, 26, and 30 were found to be non-competitive and non-cytotoxic upto a concentration of 200 microg/mL as evident by less than 10% cell death after 3 h of incubation.
Cell Death, Phosphoric Diester Hydrolases, Drug Evaluation, Preclinical, Inhibitory Concentration 50, Kinetics, Coumarins, Phosphodiesterase I, Humans, Enzyme Inhibitors, Pyrophosphatases, Snake Venoms
Cell Death, Phosphoric Diester Hydrolases, Drug Evaluation, Preclinical, Inhibitory Concentration 50, Kinetics, Coumarins, Phosphodiesterase I, Humans, Enzyme Inhibitors, Pyrophosphatases, Snake Venoms
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