The Antileishmanial Potential of C-3 Functionalized Isobenzofuranones against Leishmania (Leishmania) Infantum Chagasi
| Autor: | Márcia Rogéria de Almeida, Raphael de Souza Vasconcellos, Juliana Lopes Rangel Fietto, Wagner Luiz Pereira, Adalberto Manoel da Silva, Rodrigo Saar Gomes, Gustavo Costa Bressan, Abelardo Silva Júnior, Rafaela de Cássia Firmino, Christiane Mariotini-Moura, Róbson Ricardo Teixeira, Luís Carlos Crocco Afonso |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Cell Survival
Antiprotozoal Agents Drug Evaluation Preclinical Pharmaceutical Science phthalides Genus: Leishmania Article Analytical Chemistry Microbiology lcsh:QD241-441 Mice in vitro leishmanicidal activity lcsh:Organic chemistry Drug Discovery parasitic diseases ANTILEISHMANIAL DRUGS medicine Parasite hosting Animals visceral leishmaniasis Physical and Theoretical Chemistry Leishmania infantum Leishmaniasis isobenzofuranones Benzofurans Visceral leishmaniasis Leishmania (L.) infantum chagasi biology Macrophages Organic Chemistry In vitro leishmanicidal activity biology.organism_classification medicine.disease Leishmania Isobenzofuranones RAW 264.7 Cells Chemistry (miscellaneous) Immunology Molecular Medicine Phthalides Leishmania infantum chagasi |
| Zdroj: | Molecules Volume 20 Issue 12 Pages 22435-22444 Molecules, Vol 20, Iss 12, Pp 22435-22444 (2015) LOCUS Repositório Institucional da UFV Universidade Federal de Viçosa (UFV) instacron:UFV Molecules; Volume 20; Issue 12; Pages: 22435-22444 |
| ISSN: | 1420-3049 |
| Popis: | Leishmaniases are diseases caused by protozoan parasites of the genus Leishmania. Clinically, leishmaniases range from cutaneous to visceral forms, with estimated global incidences of 1.2 and 0.4 million cases per year, respectively. The treatment of these diseases relies on multiple parenteral injections with pentavalent antimonials or amphotericin B. However, these pharmaceuticals are either too toxic or expensive for routine use in developing countries. These facts call for safer, cheaper, and more effective new antileishmanial drugs. In this investigation, we describe the results of the assessment of the activities of a series of isobenzofuran-1(3H)-ones (phtalides) against Leishmania (Leishmania) infantum chagasi, which is the main causative agent of visceral leishmaniasis in the New World. The compounds were tested at concentrations of 100, 75, 50, 25 and 6.25 µM over 24, 48, and 72 h. After 48 h of treatment at the 100 µM concentration, compounds 7 and 8 decreased parasite viability to 4% and 6%, respectively. The concentration that gives half-maximal responses (LC50) for the antileishmanial activities of compounds 7 and 8 against promastigotes after 24 h were 60.48 and 65.93 µM, respectively. Additionally, compounds 7 and 8 significantly reduced parasite infection in macrophages. |
| Databáze: | OpenAIRE |
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