Evaluation of flavonols and derivatives as human cathepsin B inhibitor

Autor(es)

Ramalho, Suelem D. ^[1] ; de Sousa, Lorena R. F. ^[1] ; Burger, Marcela C. M. ^[1] ; Lima, Maria Ines S. ^[2] ; da Silva, M. Fatima das G. F. ^[1] ; Fernandes, Joao B. ^[1] ; Vieira, Paulo C. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Carlos, Dept Chem, BR-13565905 Sao Carlos, SP - Brazil

^[2] Univ Fed Sao Carlos, Dept Bot, BR-13565905 Sao Carlos, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: NATURAL PRODUCT RESEARCH; v. 29, n. 23, p. 2212-2214, 2015.
• Citações Web of Science: 2

Resumo

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 8.2mM, respectively, and mode of inhibition as uncompetitive on catB. The results demonstrated polyhydroxylated flavonols as promising inhibitors of catB. (AU)

• Processo FAPESP: 10/52326-9 - Estudo de produtos naturais oriundos de plantas do cerrado e mata atlântica: conhecimento químico-biológico aliado à preservação
• Beneficiário: Paulo Cézar Vieira
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Regular