Author(s): Marques,Emerson F. ; Vieira,Paulo C. ; Severino,Richele P.
Date: 2016
Origin: Oasisbr
Subject(s): cathepsin L; inhibitors; natural products; acridone alkaloids
Document details
ALCALOIDES ACRIDÔNICOS INIBEM CATEPSINA L E V
Description
Cathepsins represent a class of enzymes that has the primary function of randomly degrading proteins in the lysosomes, although are also involved in different pathologies. The aim of this paper was to evaluate the capacity of acridone alkaloids isolated from Swinglea glutinosa (Rutaceae) to inhibit cathepsin L in vitro . The IC50 values found were in the 0.8-57 µM range and the most promising compounds were alkaloids 1 and 2, with IC50 of 0.9 and 0.8 µM, respectively. Enzyme kinetics revealed that they are reversible competitive inhibitors with respect to the substrate Z-FR-MCA. This small series of acridone alkaloids showed low selectivity for both cathepsins, but represent promising lead candidates for the further development of competitive cathepsin L and V inhibitors.
Document Type
Journal article
Language Portuguese
Language Portuguese
