Evaluation of flavonols and derivatives as human cathepsin B inhibitor.

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.

journal_name

Nat Prod Res

journal_title

Natural product research

authors

Ramalho SD,de Sousa LR,Burger MC,Lima MI,da Silva MF,Fernandes JB,Vieira PC

doi

10.1080/14786419.2014.1002404

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

2212-4

issue

23

eissn

1478-6419

issn

1478-6427

journal_volume

29

pub_type

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