Antileishmanial Constituents of the Panamanian Endophytic Fungus Edenia sp
| Autor: | Gina Della-Togna, Thomas A. Kursar, William H. Gerwick, Sergio Martínez-Luis, Phyllis D. Coley, Luis Cubilla-Rios |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Panama
Stereochemistry Plasmodium falciparum Antiprotozoal Agents Leishmania donovani Pharmaceutical Science Naphthalenes Biology Heterocyclic Compounds 4 or More Rings Article Analytical Chemistry Ascomycota parasitic diseases Drug Discovery Animals Spiro Compounds Amastigote Cytotoxicity Nuclear Magnetic Resonance Biomolecular IC50 Mycelium Pharmacology Molecular Structure Organic Chemistry Leishmania biology.organism_classification Complementary and alternative medicine Molecular Medicine |
| Zdroj: | Journal of Natural Products. 71:2011-2014 |
| ISSN: | 1520-6025 0163-3864 |
| Popis: | Bioassay-directed fractionation of extracts from the fermentation broth and mycelium of the fungus Edenia sp. led tothe isolation of five antileishmanial compounds, preussomerin EG1 (1), palmarumycin CP2 (2), palmarumycin CP17 (3), palmarumycin CP18 (4), and CJ-12,371 (5). Compounds 3 and 4 are new natural products, and this is only the second report of compound 1. The structures of compounds 1-5 were established by spectroscopic analyses (HRMS and NMR). All metabolites caused significant inhibition of the growth of Leishmania donoVani in the amastigote form, with IC50 values of 0.12, 3.93, 1.34, 0.62, and 8.40 microM, respectively. Compounds 1-5 were inactive when tested against Plasmodium falciparum or Trypanasoma cruzi at a concentration of 10 microg/mL, indicating that they have selective activity against Leishmania parasites. Compounds 1-5 showed weak cytotoxicity to Vero cells (IC50 of 9, 162, 174, 152, and 150 microM, respectively); however, the therapeutic window of these compounds is quite significant with 75, 41, 130, 245, and 18 times (respectively) more antileishmanial activity than cytotoxicity. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|