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Abstract
We investigated the ability of polyphenol fatty acid esters to inhibit the activity of serine proteases trypsin, thrombin, elastase and urokinase. Potent protease inhibition in micromolar range was displayed by rutin and rutin derivatives esterified with medium and long chain, mono- and polyunsaturated fatty acids (1e–m), followed by phloridzin and esculin esters with medium and long fatty acid chain length (2a–d, 3a–d), while unmodified compounds showed only little or no effect. QSAR study of the compounds tested provided the most significant parameters for individual inhibition activities, i.e. number of hydrogen bond donors for urokinase, molecular volume for thrombin, and solvation energy for elastase. According to the statistical analysis, the action of elastase inhibitors is opposed to those of urokinase and thrombin. Cluster analysis showed two groups of compounds: original polyphenols together with rutin esters with short fatty acid chain length and rutin esters with long fatty acid chain length.
Acknowledgments
We are thankful to Ing. Ladislav Soltes, Dr.Sc. for scientific advice and critical comments.
Declaration of interest
The work was supported by The Agency of the Ministry of Education, Science, Research and Sport of the Slovak Republic for the Structural Funds of EU, OP R&D of ERDF in the frame of the Project, Evaluation of natural substances and their selection for prevention and treatment of lifestyle diseases (ITMS 26240220040), by the Slovak Research and Development Agency LPP-0251-07 and by Grants VEGA 2/0030/11 and VEGA 2/0038/11. The authors report no declarations of interest.