Evaluation of Mongolian compound library for potential antimalarial and anti-Toxoplasma agents |
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| Institution: | 1. Laboratório de Bioquímica Celular, Instituto de Bioquímica Médica Leopoldo de Meis, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil;2. Instituto de Química, Departamento de Bioquímica, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, Brazil;3. Instituto Nacional de Ciência e Tecnologia em Biologia Estrutural e Bioimagem, Rio de Janeiro, RJ, Brazil;4. Laboratório de Bioquímica de Tripanosomatideos, Instituto Oswaldo Cruz (IOC), Fundação Oswaldo Cruz-FIOCRUZ, Pavilhão Leônidas Deane, 4° andar, sala 405A, Manguinhos, 21045-900 Rio de Janeiro, RJ, Brazil;1. Laboratorio de Epidemiologia y Economía Veterinaria, Facultad de Medicina Veterinaria, Universidad Nacional Mayor de San Marcos, Av. Circunvalacion 2800, Lima 41, Peru;2. Center for Global Health, Universidad Peruana Cayetano Heredia, Av. Honorio Delgado 430, Lima 31, Peru;3. Departament de Sanitat i Antomia Animals, Facultad de Veterinaria, Universitat Autònoma de Barcelona, Bellaterra, E-08193 Barcelona, Spain |
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| Abstract: | 179 compounds in a Mongolian compound library were investigated for their inhibitory effect on the in vitro growth of Plasmodium falciparum and Toxoplasma gondii. Among these compounds, brachangobinan A at a half-maximal inhibition concentration (IC50) of 2.62 μM and a selectivity index (SI) of 27.91; 2-(2′-hydroxy-5′-O-methylphenyl)-5-(2″,5″-dihydroxyphenyl)oxazole (IC50 3.58 μM and SI 24.66); chrysosplenetin (IC50 3.78 μM and SI 15.26); 4,11-di-O-galloylbergenin (IC50 3.87 μM and SI 13.38); and 2-(2′,5′-dihydroxyphenyl)-5-(2″-hydroxyphenyl)oxazole (IC50 6.94 μM and SI 11.48) were identified as potential inhibitors of P. falciparum multiplication. Additionally, tricin (IC50 12.94 μM and SI > 23.40) was identified as a potential inhibitor of T. gondii multiplication. Our findings represent a good starting point for developing novel antimalarial and anti-Toxoplasma therapeutics from Mongolian compounds. |
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