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J Nat Prod ; 79(11): 2767-2773, 2016 11 23.
Article in English | MEDLINE | ID: mdl-27809507

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.


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Rubiaceae/chemistry , Amino Acid Sequence , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Breast Neoplasms/drug therapy , Caco-2 Cells , Colorectal Neoplasms/drug therapy , Cyclotides/chemistry , Drug Screening Assays, Antitumor , Female , Humans , Inhibitory Concentration 50 , Molecular Sequence Data , Molecular Structure , Plant Leaves/chemistry , Plant Proteins/chemistry , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
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