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Evaluation of anti-denaturation activity of C-5' - substituted uridine derivatives.

Katarzyna Kral Jadwiga Paszkowska Natalia Jaśkowiak Ilona Wandzik 1

1. Silesian University of Technology, Department of Organic Chem., Bioorganic Chem. and Biotechnol., Krzywoustego 4, Gliwice 44-100, Poland

Abstract

Denaturation of tissue proteins is one of the well-documented causes of inflammation. Agents that can prevent protein denaturation would be worthwhile for anti - inflammatory drug development. Currently used anti - inflammatory drugs (salicylic acid, diclofenac, etc.) have shown dose dependent ability to inhibit heat induce protein denaturation. Inflammation which is a pattern of response to injury, involves the accumulation of cells and exudates in irritated tissues, that allows protection from further damage. This process has been studied in an attempt to combat its effects on the body [1].

In our research anti - denaturation study was performed by using several albumin (e.g. BSA, HSA, OVA) as it is practiced in research [2]. It is known that nonsteroidal anti - inflammatory drugs such as dicolfenac sodium and salicylic acid prevent denaturation of these albumins. We have observed that some new C-5’- substituted uridine derivatives prevent heat-induced albumin denaturation at the level similar to known anti – inflammatory drugs. Studies on anti-denaturation effect were carried out at 50 -70°C in various buffer systems (e.g. HEPES, Tris, phosphate).

The highest effect was observed at pH below 5 in HEPES buffer. Comparison of effects of different compounds and IC50  values will be presented.

Acknowledgement

Research studies part-financed by the European Union within the European Regional Development Fund (POIG.01.01.02-14-102/09).

References:

[1] L. Saso, G. Valentini, M. Casini, E. Grippa, M. T., Gatto, M. G. Leone, B. Silvestrini, Arch. Pharm. Res., 2001, 24, 150–158.

[2] E. L. Gelamo, C. H. T. P. Silva, H. Imasato, M. Tabak, Biochim. Biophys. Acta, 2002, 1594, 84-99.

 

 

 

 

 

 

 

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Submitted: 2014-03-06 18:23
Revised:   2014-05-02 12:22