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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Evaluation of flavonols and derivatives as human cathepsin B inhibitor

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Author(s):
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]
Total Authors: 7
Affiliation:
[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
Total Affiliations: 2
Document type: Journal article
Source: NATURAL PRODUCT RESEARCH; v. 29, n. 23, p. 2212-2214, 2015.
Web of Science Citations: 2
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 8.2mM, respectively, and mode of inhibition as uncompetitive on catB. The results demonstrated polyhydroxylated flavonols as promising inhibitors of catB. (AU)