In vitro and in vivo antimalarial activity of puberulic acid and its new analogs, viticolins A-C, produced by Penicillium sp. FKI-4410
| Autor: | Miyuki Namatame, Masato Iwatsuki, Satoshi Omacr, Kenichi Nonaka, Aki Nishihara-Tsukashima, Kazuro Shiomi, Rokuro Masuma, Shohei Takada, mura, Kazuhiko Otoguro, Mihoko Mori, Aki Ishiyama |
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| Rok vydání: | 2010 |
| Předmět: |
Antiparasitic
medicine.drug_class Cell Survival Plasmodium berghei Plasmodium falciparum Pharmacology Cell Line chemistry.chemical_compound Antimalarials Inhibitory Concentration 50 Mice Parasitic Sensitivity Tests In vivo Drug Discovery medicine Animals Humans Antimalarial Agent Cytotoxicity biology Penicillium biology.organism_classification Tropolone In vitro Malaria Treatment Outcome chemistry Biochemistry |
| Zdroj: | The Journal of antibiotics. 64(2) |
| ISSN: | 1881-1469 |
| Popis: | In the course of screening for antimalarial agents, five tropolone compounds were isolated from the culture broth of Penicillium sp. FKI-4410. Two were known compounds, puberulic acid and stipitatic acid. Three were new analogs of puberulic acid, designated viticolins A-C. Among them, puberulic acid exhibited potent antimalarial inhibition, with IC(50) values of 0.01 μg ml(-1) against chloroquine-sensitive and -resistant Plasmodium falciparum strains in vitro. Furthermore, puberulic acid showed weak cytotoxicity against human MRC-5 cells, with an IC(50) value of 57.2 μg ml(-1). The compound also demonstrated a therapeutic effect in vivo, which compared well against the currently used antimalarial drugs, and thus shows promise as a leading candidate for development into a new antimalarial compound. |
| Databáze: | OpenAIRE |
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