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Nat Prod Res. 2015;29(23):2212-4. doi: 10.1080/14786419.2014.1002404. Epub 2015 Jan 27.

Evaluation of flavonols and derivatives as human cathepsin B inhibitor.

Author information

1
a Department of Chemistry , Federal University of São Carlos , 13565-905 São Carlos , SP , Brazil.
2
b Department de Botany , Federal University of São Carlos , 13565-905 São Carlos , SP , Brazil.

Abstract

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.

KEYWORDS:

cathepsin B; flavonoids; uncompetitive inhibitor

PMID:
25622620
DOI:
10.1080/14786419.2014.1002404
[Indexed for MEDLINE]

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