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Campo DC | Valor | Idioma |
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dc.contributor.author | Silva, Luiz Francisco Rocha e | - |
dc.contributor.author | Montoia, Andréia | - |
dc.contributor.author | Amorim, Rodrigo C.N. | - |
dc.contributor.author | Melo, Márcia R.S. | - |
dc.contributor.author | Henrique, Marycleuma Campos | - |
dc.contributor.author | Nunomura, Sergio Massayoshi | - |
dc.contributor.author | Costa, Mônica Regina Farias | - |
dc.contributor.author | Andrade Neto, Valter Ferreira de | - |
dc.contributor.author | Costa, David Siqueira | - |
dc.contributor.author | Dantas, Glucia L.S. | - |
dc.contributor.author | Lavrado, João | - |
dc.contributor.author | Moreira, Rui R.N. | - |
dc.contributor.author | Paulo, Alexandra | - |
dc.contributor.author | Pinto, A. C. | - |
dc.contributor.author | Tadei, Wanderli Pedro | - |
dc.contributor.author | Zacardi, R. S. | - |
dc.contributor.author | Eberlin, M. N. | - |
dc.contributor.author | Pohlit, Adrian Martin | - |
dc.date.accessioned | 2020-05-24T21:19:36Z | - |
dc.date.available | 2020-05-24T21:19:36Z | - |
dc.date.issued | 2012 | - |
dc.identifier.uri | https://repositorio.inpa.gov.br/handle/1/16094 | - |
dc.description.abstract | Indole alkaloids ellipticine (1), cryptolepine triflate (2a), rationally designed 11-(4-piperidinamino)cryptolepine hydrogen dichloride (2b) and olivacine (3) (an isomer of 1) were evaluated in vitro against Plasmodium falciparum and in vivo in Plasmodium berghei-infected mice. 1-3 inhibited P. falciparum (IC50 ≤ 1.4 μM, order of activity: 2b > 1 > 2a > 3). In vitro toxicity to murine macrophages was evaluated and revealed selectivity indices (SI) of 10-12 for 2a and SI > 2.8 × 102 for 1, 2b and 3. 1 administered orally at 50 mg/kg/day was highly active against P. berghei (in vivo inhibition compared to untreated control (IVI) = 100%, mean survival time (MST) > 40 days, comparable activity to chloroquine control). 1 administered orally and subcutaneously was active at 10 mg/kg/day (IVI = 70-77%; MST = 27-29 days). 3 exhibited high oral activity at ≥50 mg/kg/day (IVI = 90-97%, MST = 23-27 days). Cryptolepine (2a) administered orally and subcutaneously exhibited moderate activity at 50 mg/kg/day (IVI = 43-63%, MST = 24-25 days). At 50 mg/kg/day, 2b administered subcutaneously was lethal to infected mice (MST = 3 days) and moderately active when administered orally (IVI = 45-55%, MST = 25 days). 1 and 3 are promising compounds for development of antimalarials. © 2012 Elsevier GmbH. | en |
dc.language.iso | en | pt_BR |
dc.relation.ispartof | Volume 20, Número 1, Pags. 71-76 | pt_BR |
dc.rights | Attribution-NonCommercial-NoDerivs 3.0 Brazil | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/br/ | * |
dc.subject | Cryptolepine Derivative | en |
dc.subject | Cryptolepine Triflate | en |
dc.subject | Ellipticine | en |
dc.subject | Olivacine | en |
dc.subject | Unclassified Drug | en |
dc.subject | Animals Experiment | en |
dc.subject | Antimalarial Activity | en |
dc.subject | Controlled Study | en |
dc.subject | Drug Cytotoxicity | en |
dc.subject | Ic 50 | en |
dc.subject | In Vitro Study | en |
dc.subject | In Vivo Study | en |
dc.subject | Lethal Dose | en |
dc.subject | Mouse | en |
dc.subject | Nonhuman | en |
dc.subject | Plasmodium | en |
dc.subject | Plasmodium Berghei | en |
dc.subject | Priority Journal | en |
dc.subject | Survival Time | en |
dc.subject | Animal | en |
dc.subject | Antimalarials | en |
dc.subject | Aspidosperma | en |
dc.subject | Ellipticines | en |
dc.subject | Female | en |
dc.subject | Indole Alkaloids | en |
dc.subject | Macrophages | en |
dc.subject | Malaria | en |
dc.subject | Mice | en |
dc.subject | Mice, Inbred Strains | en |
dc.subject | Phytotherapy | en |
dc.subject | Plant Extracts | en |
dc.subject | Plasmodium Berghei | en |
dc.subject | Plasmodium Falciparum | en |
dc.subject | Quinolines | en |
dc.subject | Murinae | en |
dc.subject | Mus | en |
dc.subject | Plasmodium Berghei | en |
dc.subject | Plasmodium Falciparum | en |
dc.title | Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog | en |
dc.type | Artigo | pt_BR |
dc.identifier.doi | 10.1016/j.phymed.2012.09.008 | - |
dc.publisher.journal | Phytomedicine | pt_BR |
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