Synthesis and characterization of antimicrobial peptide "B1CTcu5" analogs encapsulated in colon-specific microparticles and in vitro an in vivo studies against Mycobacterium tuberculosis

• Grant number: 23/01664-1
• Support Opportunities: Regular Research Grants
• Start date: October 01, 2023
• End date: December 31, 2025
• Field of knowledge: Biological Sciences - Microbiology - Applied Microbiology
• Principal Investigator: Fernando Rogério Pavan
• Grantee: Fernando Rogério Pavan
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
• Associated researchers: Andréia Bagliotti Meneguin ; Marlus Chorilli ; Paul Robert Hansen ; Saulo Santesso Garrido
• Associated scholarship(s): 23/14503-6 - In vitro studies of the antimicrobial peptide "B1CTcu5" against Mycobacterium tuberculosis, BP.TT

Abstract

The development of new molecules is the main approach to work around the serious problem of bacterial resistance to antibiotics. The use of antimicrobial peptides (AMPs) has been an interesting and current area of research because these molecules are not considered drugs and generally do not generate or generate low resistance. Tuberculosis (TB) is a communicable infectious disease caused mainly by the bacillus Mycobacterium tuberculosis. According to the World Health Organization (WHO), this disease is one of the ten main causes of death in the world and the main one caused by a single infectious agent, above HIV/AIDS. The synthetic peptide B1CTcu5 has 21 amino acid residues and was originally isolated from the cutaneous secretion of Clinotarsus curtipes. This peptide showed a promising initial study against M. tuberculosis and low cytotoxicity. However, the oral administration of peptide drugs, the main route of administration of the drug, is hampered due to the instability of these molecules under severe pH conditions and the enzymatic degradability imposed by the upper portions of the gastrointestinal tract. The microencapsulation of active agents with retrograded starch (AR)/pectin (P) mixtures is an important technological tool that allows the targeting of peptides in the colon, an organ of excellence for the absorption of biotherapeutic agents. This peptide encapsulates in specific colon microparticles and studies its potential against M. tuberculosis through its portfolio of in vitro and in vivo studies. (AU)

Scientific publications

(7)

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

ROQUE-BORDA, CESAR AUGUSTO; PRIMO, LAURA MARIA DURAN GLERIANI; FRANZYK, HENRIK; HANSEN, PAUL ROBERT; PAVAN, FERNANDO ROGERIO. Recent advances in the development of antimicrobial peptides against ESKAPE pathogens. HELIYON, v. 10, n. 11, p. 15-pg., 2024-06-15. (23/16711-5, 23/01664-1, 20/16573-3, 23/10440-0, 21/14603-5)

ROQUE-BORDA, CESAR AUGUSTO; CANALES, CHRISTIAN S. CARNERO; PRIMO, LAURA MARIA DURAN GLERIANI; COLTURATO, VITORIA MARIA MEDALHA; POLINARIO, GIULIA; DI FILIPPO, LEONARDO DELELLO; DUARTE, JONATAS L.; CHORILLI, MARLUS; BARUD, HERNANE DA SILVA; PAVAN, FERNANDO R.. Cellulose from bacteria as a delivery system for improved treatment of infectious diseases: A review of updates and prospects. International Journal of Biological Macromolecules, v. 277, p. 18-pg., 2024-08-20. (23/01664-1, 21/14603-5, 20/16573-3)

MENEGUIN, ANDREIA BAGLIOTTI; ROQUE-BORDA, CESAR AUGUSTO; PIPERAS, ANA BEATRIZ GROTTO; POLLINI, MARIA FERNANDA ORTOLANI; CARDOSO, VINICIUS MARTINHO BORGES; PRIMO, LAURA MARIA DURAN GLERIANI; ALEMI, FOROGH; PAVAN, FERNANDO ROGERIO; CHORILLI, MARLUS. Nanofiber-boosted retrograded starch/pectin microparticles for targeted 5-Aminosalicylic acid delivery in inflammatory bowel disease: In vitro and in vivo non-toxicity evaluation. Carbohydrate Polymers, v. 346, p. 10-pg., 2024-08-28. (23/04633-0, 23/01664-1, 23/15205-9, 20/16573-3, 23/10440-0, 22/16773-8, 19/19817-3)

CAMPOS, JULIA VALLADARES; DE PONTES, JANAINA TEIXEIRA COSTA; CANALES, CHRISTIAN SHLEIDER CARNERO; ROQUE-BORDA, CESAR AUGUSTO; PAVAN, FERNANDO ROGERIO. Advancing Nanotechnology: Targeting Biofilm-Forming Bacteria with Antimicrobial Peptides. BME FRONTIERS, v. 6, p. 22-pg., 2025-03-04. (23/15838-1, 20/16573-3, 23/01664-1, 21/14603-5)

ROQUE-BORDA, CESAR AUGUSTO; PRIMO, LAURA MARIA DURAN GLERIANI; MEDINA-ALARCON, KAILA PETRONILA; CAMPOS, ISABELLA C.; NASCIMENTO, CAMILA DE FATIMA; SARAIVA, MAURO M. S.; BERCHIERI, ANGELO; FUSCO-ALMEIDA, ANA MARISA; MENDES-GIANNINI, MARIA JOSE SOARES; PERDIGAO, JOAO; et al. Antimicrobial Peptides: A Promising Alternative to Conventional Antimicrobials for Combating Polymicrobial Biofilms. ADVANCED SCIENCE, v. N/A, p. 29-pg., 2024-11-12. (23/01664-1, 21/14603-5, 20/16573-3)

RIBEIRO, CAMILA MARINGOLO; ROQUE-BORDA, CESAR AUGUSTO; FRANZINI, MARIA CAROLINA; MANIERI, KARYN FERNANDA; DEMARQUI, FERNANDA MANAIA; CAMPOS, DEBORA LEITE; MACHADO, RACHEL TEMPERANI AMARAL; DA SILVA, ISABEL CRISTIANE; LUIZ, MARCELA TAVARES; DI FILIPPO, LEONARDO DELELLO; et al. Liposome-siderophore conjugates loaded with moxifloxacin serve as a model for drug delivery against Mycobacterium tuberculosis. International Journal of Pharmaceutics, v. 655, p. 14-pg., 2024-03-28. (23/01664-1, 20/04793-9, 20/13497-4)

PRATES, JOAO LUCAS BRUNO; SILVA, SAMANTA DE MATOS; MEDINA-ALARCON, KAILA PETROLINA; DOS SANTOS, KELVIN SOUSA; BELIZARIO, JENYFFIE ARAUJO; LOPES, JULIANA ROMANO; MARIN-DETT, FREDDY HUMBERTO; CAMPOS, DEBORA LEITE; GIANNINI, MARIA JOSE SOARES MENDES; FUSCO-ALMEIDA, ANA MARISA; et al. Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities. Molecules, v. 30, n. 5, p. 27-pg., 2025-03-01. (22/15826-0, 19/07574-9, 23/01664-1, 23/03556-1, 23/05739-6)