Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/51816
Type: Artigo de Periódico
Title: Calix[n]arene-based immunogens: a new non-proteic strategy for anti-cocaine vaccine
Authors: Leonardo da Silva Neto
Angélica Faleiros da Silva Maia
Adriana Martins Godin
Paulo Sérgio de Almeida Augusto
Raissa Lima Gonçalves Pereira
Sordaini Maria Caligiorne
Rosemeire Brondi Alves
Simone Odília Antunes Fernandes
Valbert Nascimento Cardoso
Gisele Assis Castro Goulart
Felipe Terra Martins
Maila de Castro Lourenço das Neves
Frederico Duarte Garcia
Ângelo de Fátima
Abstract: Introduction Cocaine use disorder is a significant public health issue without a current specific approved treatment. Among different approaches to this disorder, it is possible to highlight a promising immunologic strategy in which an immunogenic agent may reduce the reinforcing effects of the drug if they are able to yield sufficient specific antibodies capable to bind cocaine and/or its psychoactive metabolites before entering into the brain. Several carriers have been investigated in the anti-cocaine vaccine development; however, they generally present a very complex chemical structure, which potentially hampers the proper assessment of the coupling efficiency between the hapten units and the protein structure. Objectives The present study reports the design, synthesis and preclinical evaluation of two novel calix[n]arene-based anti-cocaine immunogens (herein named as V4N2 and V8N2) by the tethering of the hydrolysis-tolerant hapten GNE (15) on calix[4]arene and calix[8]arene moieties. Methods The preclinical assessment corresponded to the immunogenicity and dose–response evaluation of V4N2 and V8N2. The potential of the produced antibodies to reduce the passage of cocaine analogue through the blood–brain-barrier (BBB), modifying its biodistribution was also investigated. Results Both calix[n]arene-based immunogens elicited high titers of cocaine antibodies that modified the biodistribution of a cocaine radiolabeled analogue (99mTc-TRODAT-1) and decreased cocaine-induced behavior, according to an animal model. Conclusion The present results demonstrate the potential of V4N2 and V8N2 as immunogens for the treatment of cocaine use disorder.
Subject: Cocaína
Dependência química
Imunoterapia
language: eng
metadata.dc.publisher.country: Brasil
Publisher: Universidade Federal de Minas Gerais
Publisher Initials: UFMG
metadata.dc.publisher.department: FAR - DEPARTAMENTO DE ALIMENTOS
FAR - DEPARTAMENTO DE ANÁLISES CLÍNICAS E TOXICOLÓGICAS
FAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
MED - DEPARTAMENTO DE SAÚDE MENTAL
Rights: Acesso Aberto
metadata.dc.identifier.doi: https://doi.org/10.1016/j.jare.2021.09.003
URI: http://hdl.handle.net/1843/51816
Issue Date: May-2022
metadata.dc.url.externa: https://www.sciencedirect.com/science/article/pii/S2090123221001715
metadata.dc.relation.ispartof: Journal of Advanced Research
Appears in Collections:Artigo de Periódico

Files in This Item:
File Description SizeFormat 
Calix[n]arene-based immunogens A new non-proteic strategy for anti-cocaine vaccine.pdf2.27 MBAdobe PDFView/Open


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.