Antiprotease and Antimetastatic Activity of Ursolic Acid Isolated from Salvia officinalis

Author:

Jedinák Andrej1,Mučková Marta2,Košt’álová Daniela3,Maliar Tibor4,Mašterová Irena3

Affiliation:

1. Institute of Molecular Physiology and Genetics, Vlárska 5, Bratislava 83334, Slovakia. Fax: +421254773666.

2. VULM a.s., Horná 36, Modra 90001, Slovakia

3. Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University, Odbojárov 10, Bratislava 83232, Slovakia

4. VULM a.s., Horná 36, Modra 90001, Slovakia / Department of Biotechnology, University of Saint Cyril and Method in Trnava, Nám. J. Hedru 2, Trnava 91701, Slovakia

Abstract

Abstract Proteases play a regulatory role in a variety of pathologies including cancer, pancreatitis, thromboembolic disorders, viral infections and many others. One of the possible strategies how to combat with these pathologies seems to be the use of low molecular inhibitors. Natu­ral products were evaluated in the in vitro antiprotease assay on serine proteases (trypsin, thrombin and urokinase) and on the cysteine protease cathepsin B. We found interesting results for β-ursolic acid isolated from Salvia officinalis, which significantly inhibited all tested proteases in vitro in the micromolar range. β-Ursolic acid showed the strongest inhibition activity to urokinase (IC50 = 12 μᴍ) and cathepsin B (IC50 = 10 /μᴍ) as proteases included in tumour invasion and metastasis indicated possible anticancer effectivity. Therefore, we tested the ability of β-ursolic acid at doses of 50, 75 and 100 mg/kg given i.p. to inhibit lung coloniza­tion of B16 mouse melanoma cells in vivo. We found, that β-ursolic acid significantly de­creased the number of B16 colonies in the lungs of mice at the dose 50 mg/kg (p < 0.05).

Publisher

Walter de Gruyter GmbH

Subject

General Biochemistry, Genetics and Molecular Biology

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