Characterization of a Bioactive Acyclotide from Palicourea rigida.

Basic Information

ID: ALA4002558

Journal: J Nat Prod

Title: Characterization of a Bioactive Acyclotide from Palicourea rigida.

Authors: Pinto MF, Silva ON, Viana JC, Porto WF, Migliolo L, B da Cunha N, Gomes N, Fensterseifer IC, Colgrave ML, Craik DJ, Dias SC, Franco OL.

Abstract: The extraction and purification of parigidin-br3, a cyclotide analogue belonging to the "bracelet" subfamily, from Palicourea rigida leaves is discussed. Unlike conventional cyclotides, parigidin-br3 has free N- and C-termini, as identified by MALDI-TOF/TOF analysis and confirmed by gene structure elucidation, and is one of a small number of acyclotides discovered during recent years. Parigidin-br3 showed cytotoxic activity against MCF-7 (breast cancer) and CACO2 (colorectal adenocarcinoma) cells, with IC50 values of ∼2.5 μM and less than 10% hemolytic activity. Overall, parigidin-br3 is a promising new molecule with cytotoxic properties against tumor cell lines and, unlike many synthetic acyclic analogues, demonstrates that cytotoxic activity is not limited to conventional (i.e., cyclic) cyclotides.

CiteXplore: 27809507

DOI: 10.1021/acs.jnatprod.6b00270

Patent ID: