Novel compounds that increase expression of Hsp70 and its biological activity

Autor: Sergey G. Polonik, Irina V. Guzhova, Boris A. Margulis, O. I. Antimonova, O. G. Shekalova, E. M. Eremenko
Rok vydání: 2010
Předmět:
Zdroj: Cell and Tissue Biology. 4:251-257
ISSN: 1990-5203
1990-519X
DOI: 10.1134/s1990519x10030065
Popis: The Hsp70 protein has chaperone activity, which is associated with the protective function that demonstrated in experiments using several cell lines and animals. Therefore, the search for the substances able to harmlessly elevate the chaperone concentration in the organism cells and tissues is particularly important. In our work, we screened more than 60 compounds and revealed two chemicals, i.e., derivatives of shikonin and echinochrome, that, at micromolar concentrations, were able to increase the chaperone level in various human cells. Under the effects of both of these substances, in human erythroleukemia K-562 cells, a significant increase in the absolute Hsp70 chaperone activity was also observed, which can indicate the mobilization of the entire cellular chaperone mechanism. The estimation of the biological activity of these two substances has shown that their action upon the treatment of cells with severe heat stress, hydrogen peroxide, and staurosporine leads to a decrease in cell mortality by 20–50% depending on the cytotoxic factor. These results show that, by effecting noncomplicated chemical modifications of the chosen substances, it is possible to obtain pharmacogenic agents of the wide profile of action.
Databáze: OpenAIRE
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