Evaluation of flavonols and derivatives as human cathepsin B inhibitor
| Autor: | Maria Inês Salgueiro Lima, Suelem D. Ramalho, M. Fátima das G. F. da Silva, João B. Fernandes, Paulo C. Vieira, Lorena R.F. de Sousa, Marcela Carmen de Melo Burger |
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| Rok vydání: | 2015 |
| Předmět: |
Flavonols
Plant Science Biochemistry Cathepsin B Analytical Chemistry chemistry.chemical_compound Inhibitory Concentration 50 Myrcia Humans IC50 chemistry.chemical_classification Flavonoids biology Plant Extracts Organic Chemistry biology.organism_classification Cysteine protease Myrica chemistry Myricetin Quercetin Uncompetitive inhibitor |
| DOI: | 10.6084/m9.figshare.1295385 |
| Popis: | Cathepsin B (catB) is a cysteine protease involved in tumour progression and represents a potential therapeutic target in cancer. Among the 15 evaluated extracts from cerrado biome, Myrcia lingua Berg. (Myrtaceae) extract demonstrated to be a source of compounds with potential to inhibit catB. Using bioactivity-guided fractionation, we have found flavonols as inhibitors and also some other derivatives were obtained. From the evaluated compounds, myricetin (5) and quercetin (6) showed the most promising results with IC50 of 4.9 and 8.2 μM, respectively, and mode of inhibition as uncompetitive on catB. The results demonstrated polyhydroxylated flavonols as promising inhibitors of catB. |
| Databáze: | OpenAIRE |
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