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 Resjournal_title
Natural product researchauthors
Ramalho SD,de Sousa LR,Burger MC,Lima MI,da Silva MF,Fernandes JB,Vieira PCdoi
10.1080/14786419.2014.1002404subject
Has Abstractpub_date
2015-01-01 00:00:00pages
2212-4issue
23eissn
1478-6419issn
1478-6427journal_volume
29pub_type
杂志文章abstract::Stichopus hermanni and Stichopus vastus are sea cucumber species from the Stichopodidae family within the coastal waters of Malaysia. The integument of these invertebrates is hypothesised to contain abundant glycosaminoglycans (GAGs). GAGs are divided into non-sulphated and sulphated GAGs. Sulphated GAGs have various ...
journal_title:Natural product research
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