Advanced search
Start date
Betweenand

Obtaining structural analogues of pimaradienoic acid through the process of fungal biotransformation and study of the effect of these metabolites on the activity of the TcDHODH enzyme and on the contraction of the vascular smooth muscle of the aorta artery of mice

Abstract

The present work has the general objective of obtaining structural analogues of pimaradienoic acid, a diterpene present in large quantity in the roots of Viguiera arenaria Baker, which has proven a significant capacity to inhibit the contractile response of the vascular smooth muscle of mice, due to its capacity to reduce the influx of Ca+2 through the blocking of the channels operated by voltage and receiver. In addition to this well-established activity, preliminary studies showed the arterial pressure of mice normotense in vivo, as well as inhibiting the dihydroorotate dehydrogenase enzyme of Trypanossoma cruzi (TcDHODH), an excellent pharmacological target for the discovery of new potentially promising substances to combat parasites that cause Chagas disease. The structural modifications proposed in this Project will be achieved through the technique of fungal biotransformation, using four different genuses of fungus, so as to guarantee the variability of the analogues produced. The diterpenes isolated and identified will then be evaluated on the inhibitory capacity of the TcDHODH enzyme and the contraction of the vascular smooth muscle in the aorta of mice, with the aim of selecting new compounds more active than pimaradienoic acid, so that in a stage beyond the development of this Project they can be tested with regard to their antihypertensive and trypanocide potential. (AU)

Articles published in Agência FAPESP Newsletter about the research grant:
Articles published in other media outlets (0 total):
More itemsLess items
VEICULO: TITULO (DATA)
VEICULO: TITULO (DATA)

Scientific publications (10)
(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)
DE SOUZA, JONATHAN MESSIAS; CONCEICAO SANTOS, MARIO FERREIRA; NASCIMENTO PEDROSO, RITA CASSIA; PIMENTA, LETICIA PEREIRA; SIQUEIRA, KATIA APARECIDA; SOARES, MARCOS ANTONIO; DIAS, GUSTAVO MUNIZ; LINHARI RODRIGUE PIETRO, ROSEMEIRE CRISTINA; RAMOS, HENRIQUE PEREIRA; ANDRADE SILVA, MARCIO LUIS; et al. Optimization of (-)-cubebin biotransformation to (-)-hinokinin by the marine fungus Absidia coerulea 3A9. Archives of Microbiology, v. 203, n. 7, p. 4313-4318, . (14/19184-7, 17/14261-1, 07/54762-8)
SEVERIANO, MARCELA E.; SIMAO, MARILIA R.; RAMOS, HENRIQUE P.; PARREIRA, RENATO L. T.; ARAKAWA, NILTON S.; SAID, SURAIA; FURTADO, NIEGE A. J. C.; DE OLIVEIRA, DIONEIA C. R.; GREGORIO, LUIS E.; TIRAPELLI, CARLOS R.; et al. Biotransformation of ent-pimaradienoic acid by cell cultures of Aspergillus niger. Bioorganic & Medicinal Chemistry, v. 21, n. 18, p. 5870-5875, . (09/12458-6, 07/54762-8)
PORTO, THIAGO S.; SIMAO, MARILIA R.; CARLOS, LUCAS Z.; MARTINS, CARLOS H. G.; FURTADO, NIEGE A. J. C.; SAID, SURAIA; ARAKAWA, NILTON S.; DOS SANTOS, RAQUEL A.; VENEZIANI, RODRIGO C. S.; AMBROSIO, SERGIO R.. Pimarane-type Diterpenes Obtained by Biotransformation: Antimicrobial Properties Against Clinically Isolated Gram-positive Multidrug-resistant Bacteria. Phytotherapy Research, v. 27, n. 10, p. 1502-1507, . (07/54762-8, 08/07696-2)
PORTO, THIAGO S.; DA SILVA FILHO, ADEMAR A.; MAGALHAES, LIZANDRA G.; DOS SANTOS, RAQUEL A.; FURTADO, NIEGE A. J. C.; ARAKAWA, NILTON S.; SAID, SURAIA; DE OLIVEIRA, DIONEIA C. R.; GREGORIO, LUIZ E.; RODRIGUES, VANDERLEI; et al. Fungal Transformation and Schistosomicidal Effects of Pimaradienoic Acid. CHEMISTRY & BIODIVERSITY, v. 9, n. 8, p. 1465-1474, . (07/54762-8, 08/07696-2)
PORTO, THIAGO S.; RANGEL, RANDER; FURTADO, NIEGE A. J. C.; DE CARVALHO, TATIANE C.; MARTINS, CARLOS H. G.; VENEZIANI, RODRIGO C. S.; DA COSTA, FERNANDO B.; VINHOLIS, ADRIANA H. C.; CUNHA, WILSON R.; HELENO, VLADIMIR C. G.; et al. Pimarane-type Diterpenes: Antimicrobial Activity against Oral Pathogens. Molecules, v. 14, n. 1, p. 191-199, . (07/54762-8)
SEVERIANO, MARCELA E.; SIMAO, MARILIA R.; PORTO, THIAGO S.; MARTINS, CARLOS H. G.; VENEZIANI, RODRIGO C. S.; FURTADO, NIEGE A. J. C.; ARAKAWA, NILTON S.; SAID, SURAIA; DE OLIVEIRA, DIONEIA C. R.; CUNHA, WILSON R.; et al. Anticariogenic Properties of ent-Pimarane Diterpenes Obtained by Microbial Transformation. Molecules, v. 15, n. 12, p. 8553-8566, . (07/54762-8)
DE SOUZA, JONATHAN MESSIAS; CONCEICAO SANTOS, MARIO FERREIRA; NASCIMENTO PEDROSO, RITA CASSIA; PIMENTA, LETICIA PEREIRA; SIQUEIRA, KATIA APARECIDA; SOARES, MARCOS ANTONIO; DIAS, GUSTAVO MUNIZ; LINHARI RODRIGUE PIETRO, ROSEMEIRE CRISTINA; RAMOS, HENRIQUE PEREIRA; ANDRADE SILVA, MARCIO LUIS; et al. Optimization of (-)-cubebin biotransformation to (-)-hinokinin by the marine fungus Absidia coerulea 3A9. Archives of Microbiology, . (17/14261-1, 14/19184-7, 07/54762-8)
DA COSTA, RICARDO M.; BASTOS, JAIRO K.; COSTA, MARIA C. A.; FERREIRA, MARCIA M. C.; MIZUNO, CASSIA S.; CARAMORI, GIOVANNI F.; NAGURNIAK, GLAUCIO R.; SIMAO, MARILIA R.; DOS SANTOS, RAQUEL A.; VENEZIANI, RODRIGO C. S.; et al. In vitro cytotoxicity and structure-activity relationship approaches of ent-kaurenoic acid derivatives against human breast carcinoma cell line. Phytochemistry, v. 156, p. 214-223, . (11/13630-7, 11/23028-2, 07/54762-8, 11/07623-8)
SOUZA, ARIANA B.; MARTINS, CARLOS H. G.; SOUZA, MARIA G. M.; FURTADO, NIEGE A. J. C.; HELENO, VLADIMIR C. G.; DE SOUSA, JOAO P. B.; ROCHA, ERILDA M. P.; BASTOS, JAIRO K.; CUNHA, WILSON R.; VENEZIANI, RODRIGO C. S.; et al. Antimicrobial Activity of Terpenoids from Copaifera langsdorffii Desf. Against Cariogenic Bacteria. Phytotherapy Research, v. 25, n. 2, p. 215-220, . (07/54762-8, 08/09656-8, 09/09438-3)
PORTO, THIAGO SOUZA; FURTADO, NIEGE A. J. C.; HELENO, VLADIMIR C. G.; MARTINS, CARLOS H. G.; DA COSTA, FERNANDO B.; SEVERIANO, MARCELA E.; SILVA, ALINE N.; VENEZIANI, RODRIGO C. S.; AMBROSIO, SERGIO R.. Antimicrobial ent-pimarane diterpenes from Viguiera arenaria against Gram-positive bacteria. Fitoterapia, v. 80, n. 7, p. 432-436, . (07/54762-8)

Please report errors in scientific publications list using this form.