In vitro and in vivo studies of antimicrobial peptide B1CTcu5 analogs encapsulated in colon-specific microparticles against Mycobacterium tuberculosis

• Grant number: 20/16573-3
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: June 01, 2021
• End date: March 31, 2026
• Field of knowledge: Biological Sciences - Microbiology - Applied Microbiology
• Principal Investigator: Fernando Rogério Pavan
• Grantee: Cesar Augusto Roque Borda
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
• Associated scholarship(s): 21/14603-5 - Drug discovery and design: antimicrobial peptide B1CTcu5 analogs promising against Mycobacterium tuberculosis, BE.EP.DR

Abstract

The development of new molecules is the basis of Pharmaceutical Microbiology, mainly because bacteria rapidly develop resistance to various drugs, including first-line drugs. 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

(18)

(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; SOUZA SARAIVA, MAURO DE MESQUITA; MONTE, DANIEL F. M.; RODRIGUES ALVES, LUCAS BOCCHINI; DE ALMEIDA, ADRIANA MARIA; FERREIRA, TAISA SANTIAGO; DE LIMA, TULIO SPINA; PEREIRA BENEVIDES, VALDINETE; CABRERA, JULIA MEMRAVA; CLAIRE, SUNIL; et al. HPMCAS-Coated Alginate Microparticles Loaded with Ctx(Ile(21))-Ha as a Promising Antimicrobial Agent against Salmonella Enteritidis in a Chicken Infection Model. ACS INFECTIOUS DISEASES, v. 8, n. 3, p. 10-pg., 2022-03-11. (20/13497-4, 18/25707-3, 20/16573-3, 16/00446-7)

DI FILIPPO, LEONARDO DELELLO; DUARTE, JONATAS LOBATO; ROQUE-BORDA, CESAR AUGUSTO; PAVAN, FERNANDO ROGERIO; MENEGUIN, ANDREIA BAGLIOTTI; CHORILLI, MARLUS; MELERO, ANA; GUILLOT, ANTONIO JOSE; SPAGNOL, CAROLINE MAGNANI; CORREA, MARCOS ANTONIO. In Vitro Skin Co-Delivery and Antibacterial Properties of Chitosan-Based Microparticles Containing Ascorbic Acid and Nicotinamide. LIFE-BASEL, v. 12, n. 7, p. 14-pg., 2022-07-01. (19/25125-7, 15/19097-0, 16/20957-6, 15/02619-3, 20/16573-3)

ROQUE-BORDA, CESAR AUGUSTO; DA SILVA, PATRICIA BENTO; RODRIGUES, MOSAR CORREA; FILIPPO, LEONARDO DELELLO DI; DUARTE, JONATAS L.; CHORILLI, MARLUS; VICENTE, EDUARDO FESTOZO; GARRIDO, SAULO SANTESSO; PAVAN, FERNANDO ROGENIO. Pharmaceutical nanotechnology: Antimicrobial peptides as potential new drugs against WHO list of critical, high, and medium priority bacteria. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 241, p. 18-pg., 2022-08-12. (21/14603-5, 20/13497-4, 20/16573-3, 18/25707-3)

DE SOUZA, GUILHERME DA COSTA; ROQUE-BORDA, CESAR AUGUSTO; PAVAN, FERNANDO R.. Beta-lactam resistance and the effectiveness of antimicrobial peptides against KPC-producing bacteria. Drug Development Research, v. 83, n. 7, p. 21-pg., 2022-08-30. (21/14603-5, 20/13497-4, 20/16573-3)

DI FILIPPO, LEONARDO DELELLO; DUARTE, JONATAS; FONSECA-SANTOS, BRUNO; TAVARES JUNIOR, ALBERTO GOMES; ARAUJO, VICTOR; ROQUE BORDA, CESAR AUGUSTO; VICENTE, EDUARDO FESTOZO; CHORILLI, MARLUS. Mucoadhesive Nanosystems for Nose-to-Brain Drug Delivery in the Treatment of Central Nervous System Diseases. Current Medicinal Chemistry, v. 29, n. 17, p. 32-pg., 2022-01-01. (20/12622-0, 19/25125-7, 20/16573-3, 18/23416-1)

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; SARAIVA, MAURO DE MESQUITA SOUZA; JUNIOR, WAGNER DIAS MACEDO; MONTESINOS, JOSE CARLOS ESTANISLAO MARQUEZ; MENEGUIN, ANDREIA BAGLIOTTI; BORGES, ANNA BEATRIZ TOLEDO; JUNIOR, EDSON CRUSCA; GARRIDO, SAULO SANTESSO; ALMEIDA, ADRIANA MARIA DE; MARCHETTO, REINALDO; et al. Chitosan and HPMCAS double-coating as protective systems for alginate microparticles loaded with Ctx(Ile21)-Ha antimicrobial peptide to prevent intestinal infections. Biomaterials, v. 293, p. 15-pg., 2022-12-27. (18/25707-3, 20/16573-3, 16/00446-7)

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)

ROQUE-BORDA, CESAR AUGUSTO; DE LIMA GUALQUE, MARCOS WILLIAM; DA FONSECA, FAULLER HENRIQUE; PAVAN, FERNANDO ROGERIO; SANTOS-FILHO, NORIVAL ALVES. Nanobiotechnology with Therapeutically Relevant Macromolecules from Animal Venoms: Venoms, Toxins, and Antimicrobial Peptides. PHARMACEUTICS, v. 14, n. 5, p. 21-pg., 2022-05-01. (20/13497-4, 20/16573-3)

ROQUE-BORDA, CESAR AUGUSTO; PAVAN, FERNANDO ROGERIO; MENEGUIN, ANDREIA BAGLIOTTI. Pharmaceutical Biotechnology. LIFE-BASEL, v. 12, n. 8, p. 3-pg., 2022-08-01. (20/16573-3, 20/13497-4, 16/00446-7, 18/25707-3)

ROQUE-BORDA, CESAR AUGUSTO; DA SILVA, PATRICIA BENTO; RODRIGUES, MOSAR CORREA; AZEVEDO, RICARDO BENTES; DI FILIPPO, LEONARDO; DUARTE, JONATAS L.; CHORILLI, MARLUS; VICENTE, EDUARDO FESTOZO; PAVAN, FERNANDO ROGERIO. Challenge in the Discovery of New Drugs: Antimicrobial Peptides against WHO-List of Critical and High-Priority Bacteria. PHARMACEUTICS, v. 13, n. 6, JUN 2021. (20/16573-3, 18/25707-3, 20/13497-4)

ROQUE-BORDA, CESAR AUGUSTO; ANTUNES, BRUNA FERNANDES; BORGUES, ANNA BEATRIZ TOLEDO; PONTES, JANAINA TEIXEIRA COSTA DE; MENEGUIN, ANDREIA BAGLIOTTI; CHORILLI, MARLUS; TROVATTI, ELIANE; TEIXEIRA, SILVIO RAINHO; PAVAN, FERNANDO ROGERIO; VICENTE, EDUARDO FESTOZO. Conjugation of Ctx(Ile(21))-Ha Antimicrobial Peptides to Chitosan Ultrathin Films by N-Acetylcysteine Improves Peptide Physicochemical Properties and Enhances Biological Activity. ACS OMEGA, v. 7, n. 32, p. 10-pg., 2022-08-16. (20/16573-3, 20/13497-4, 18/25707-3)

COSTA DE PONTES, JANAINA TEIXEIRA; TOLEDO BORGES, ANNA BEATRIZ; AUGUSTO ROQUE-BORDA, CESAR; PAVAN, FERNANDO ROGERIO. Antimicrobial Peptides as an Alternative for the Eradication of Bacterial Biofilms of Multi-Drug Resistant Bacteria. PHARMACEUTICS, v. 14, n. 3, p. 20-pg., 2022-03-01. (20/16573-3, 20/13497-4)

POLINARIO, GIULIA; PRIMO, LAURA MARIA DURAN GLERIANI; ROSA, MAIARA ALANE BARALDI CERQUETANI; DETT, FREDDY HUMBERTO MARIN; BARBUGLI, PAULA ABOUD; ROQUE-BORDA, CESAR AUGUSTO; PAVAN, FERNANDO ROGERIO. Antimicrobial peptides as drugs with double response against Mycobacterium tuberculosis coinfections in lung cancer. FRONTIERS IN MICROBIOLOGY, v. 14, p. 17-pg., 2023-06-02. (22/09728-6, 20/16573-3, 20/13497-4, 21/14603-5)

CANALES, CHRISTIAN S. CARNERO; CAZORLA, JESSICA INGRID MARQUEZ; CAZORLA, RENZO MARIANITO MARQUEZ; ROQUE-BORDA, CESAR AUGUSTO; POLINARIO, GIULIA; BANDA, RUFO A. FIGUEROA; SABIO, RAFAEL MIGUEL; CHORILLI, MARLUS; SANTOS, HELDER A.; PAVAN, FERNANDO ROGERIO. Breaking barriers: The potential of nanosystems in antituberculosis therapy. BIOACTIVE MATERIALS, v. 39, p. 29-pg., 2024-09-01. (20/16573-3, 22/02661-3, 14/50928-2)

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)

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)

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)