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1.
Ann Parasitol ; 68(2): 323-330, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35810364

RESUMO

Schistosomosis is a worldwide tropical disease primarily caused by Schistosoma mansoni. Praziquantel is the only available drug for controlling schistosomosis, with many challenges. This study aims to evaluate the in vitro anti-Schistosoma effect of Ganoderma lucidum (G. lucidum) against adult and larval stages of Schistosoma based on the prediction of the binding activity of G. lucidum protein with proteins of various stages of S. mansoni by molecular docking to confirm its inhibitory potential through an insilico study. Results showed that Leu143, Ser165, Met214, and Asn213 were the primary crucial amino acids involved in the binding, with a promising large area of interactions between the two studied proteins. The in vitro study evaluated the motility and survival of adult and larval stages, compared to praziquantel and niclosamide, respectively. There was a significant reduction in the motility of adults after the two-hour incubation, with all concentrations and 100% death of all parasites with the minimal concentration (10 µg/ml) within 4 and 6 h of incubation (P<0.01). Regarding the cercariae, at a concentration of 10 µg/ml, all the cercariae (100%) died (P<0.01) after 15 min, and the miracidial complete mortality rate (100%) (P<0.01) occurred at a concentration of 10 µg/ml after 8 min. This study first predicted the binding activity of G. lucidum protein with proteins of S. mansoni at various stages and proved the anti-Schistosoma effect of G. lucidum in vitro, considered a promising treatment for schistosomosis.


Assuntos
Reishi , Esquistossomose , Animais , Larva , Simulação de Acoplamento Molecular , Praziquantel/farmacologia , Schistosoma mansoni
2.
J Nat Prod ; 77(9): 1987-91, 2014 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-25084548

RESUMO

Antileishmanial bioassay guided fractionation of Geosmithia langdonii has resulted in the isolation and identification of two new compounds (1 and 2) together with 10 known compounds (3-12). The structures of the isolated metabolites were elucidated based on comprehensive 1D and 2D NMR spectroscopic data as well as mass spectrometry. The absolute configuration at C4, C5, and C6 of 2 was determined as R using a modified Mosher esterification method and NOESY correlations. The extracts and the isolated metabolites were evaluated for their antileishmanial activities. Compounds 3, 9, 11, and 12 were found to be active against Leishmania donovani with IC50 values of 6.9, 3.3, 8.5, and 9.2 µM, respectively, while compounds 1, 5, and 10 showed lower activities against L. donovani with IC50 values of 13.0, 47.3, and 34.0 µM, respectively.


Assuntos
Compostos Benzidrílicos/isolamento & purificação , Compostos Benzidrílicos/farmacologia , Cicloexanonas/isolamento & purificação , Cicloexanonas/farmacologia , Hypocreales/química , Leishmania donovani/efeitos dos fármacos , Salicilatos/isolamento & purificação , Salicilatos/farmacologia , Antineoplásicos Fitogênicos/química , Aspergillus fumigatus/efeitos dos fármacos , Compostos Benzidrílicos/química , Candida/efeitos dos fármacos , Cicloexanonas/química , Escherichia coli/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Complexo Mycobacterium avium/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Salicilatos/química
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