Ubiquitin-dependent proteasomal proteolysis is the perspective target for the therapy of the high amount of different diseases. the special attention is paid to the therapy of inflammatory processes of both origins: infection and aseptic. Besides proteolytic processing of the inhibitor of NFkappaB proteasome is important for activation of polymorphonuclear neutrophils (PMN) and neutrophil extrcellular traps (NETs) formation. Basing on the mentioned above information we have evaluated some plant extracts included in the medical compound «Healthy Tonsils» that is used for the treatment of the chronic tonsillitis for their ability to inhibit activity of 20S proteasome.
For in vitro experiments the purified 20S proteasome was used. 20S proteasome was incubated for 30 minutes at 36 C degrees in a mixture with phytobalm components. After the next 30 minutes of incubation with 6 microM solution of corresponded fluorogenic substrates the measurement of fluorescence products was performed (exciting/emission wave length was 360/440) on the spectrofluorimeter Hitachi-4000 with the use of free 7-amido-4-methylcoumarine for a standard curve.
In the same concentrations the compounds investigated has demonstrated different ability to inhibit activity of purified 20S proteasome. The most effective compound was the extract of Nigella sativa that inhibits chemotrypsin-like and caspase-like activities of purified 20S proteasome on 69 % and 85 % correspondingly.
Thus, our results allow to explaine the anti-inflammatory activity of phytobalm particularly by ability of some of its compounds to inhibit proteasomal proteolysis.