Portal de Programas de Pós-Graduação (UFSJ)

SIGAA - Sistema Integrado de Gestão de Atividades Acadêmicas

PPGCS PROGRAMA DE PÓS-GRADUAÇÃO EM CIÊNCIAS DA SAÚDE PRÓ-REITORIA DE PESQUISA E PÓS-GRADUAÇÃO Phone: Not available E-mail: melinapinheiro@ufsj.edu.br http://www.ufsj.edu.br//ppgcs

Banca de QUALIFICAÇÃO: ANA CLAUDIA DE SOUZA PINTO

Uma banca de QUALIFICAÇÃO de MESTRADO foi cadastrada pelo programa.
DISCENTE : ANA CLAUDIA DE SOUZA PINTO
DATA : 21/08/2020
HORA: 10:00
LOCAL: Campus Centro-Oeste
TÍTULO:

EVALUATION OF TWO STRATEGIES USED IN ANTIMALARIAL CHEMOTHERAPY: DETERMINATION OF ANTIPLASMODIAL ACTIVITY OF NEW SYNTHETIC ISOCUMARINES AND POLYMERIC NANOCAPPSULES WITH QUININE OR CURCUMINA

PALAVRAS-CHAVES:

Malaria, Isocoumarins, Chemotherapy

PÁGINAS: 77
GRANDE ÁREA: Ciências Biológicas
ÁREA: Bioquímica
RESUMO:

The resistance of malaria parasites to existing drugs continues to grow and

progressively narrowing the therapeutic arsenal available for its treatment. In this

sense, it is necessary to search for new antimalarial candidates. In this work an

evalution of the antiplasmodial and cytotoxic activity in vitro of 28 synthetic

compounds belonging to the class of Isocoumarins (01 to 28), was performed. The

antiplasmodial activity of the compounds was evaluated using the traditional method

in chloroquine resistant Plasmodium falciparum strains (W2). The cytotoxicity of the

compounds was evaluated with human fibroblast cells lines (ATCC: WI-26 VA4)

using the MTT colorimetric method. The concentration that inhibits 50 % of cell

viability (IC50) was determined.The IC50 values were calculated using OriginPro 8.0

software. Among the compounds tested, the compounds 07 and 16 were the most

active against P. falciparum, with IC50 values equal to 0.68 and 0.82 µM,

respectively.

Both showed low cytotoxicity against the human lineage (IC50> 100 µM). According to

the physical-chemical parameters analyzed by the software DataWarrior V5.0.0,

these compounds obey the Linpinski rule of 5, presenting a good profile for oral

bioavailability. In order to determine a potential molecular target, the compounds

were submitted to an inverse virtual screening process, using the Brazilian Malaria

Molecular Targets (BraMMT) database. As a result, it was possible to observe that

the compounds 07 and 16 presented better interaction values (∆G kcal.mol-1)

with the Plasmodium falciparum Protein Kinase 7 (PfPK7) (PDB: 2PML) target, with

values of -8.90 and -9.40 kcal/mol, respectively, being -6.90 kcal/mol the value

for the crystallographic binder. In this way, the data indicate the compounds 07 and

16 as potential candidates for development as antimalarials.

MEMBROS DA BANCA:
Interno - 1422156 - FERNANDO DE PILLA VAROTTI
Interno - 1084423 - RAFAEL GONCALVES TEIXEIRA NETO
Externo ao Programa - 1300132 - WHOCELY VICTOR DE CASTRO

Notícia cadastrada em: 07/07/2020 16:23