Abstract
Investigation of the bioactive crude extract from the sponge Plakortis angulospiculatus from Brazil led to the isolation of plakortenone ( 1) as a new polyketide, along with five known polyketides ( 2- 6) previously isolated from other Plakortis sponges. The known polyketides were tested in antileishmanial, antitrypanosomal, antineuroinflammatory, and cytotoxicity assays. The results show that plakortide P ( 3) is a potent antiparasitic compound, against both Leishmania chagasi and Trypanosona cruzi, and exhibited antineuroinflammatory activity. The known polyketides 2- 6 were tested for cytotoxicity against four human cancer cell lines, but displayed only moderate cytotoxic activity.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / pharmacology*
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / isolation & purification*
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Antiprotozoal Agents / pharmacology*
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Brazil
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Cricetinae
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Drug Screening Assays, Antitumor
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Erythrocytes / drug effects
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Humans
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Leishmania infantum / drug effects
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Leishmania infantum / ultrastructure
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Macrolides / chemistry
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Macrolides / isolation & purification*
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Macrolides / pharmacology*
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Macrophages / drug effects
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Marine Biology
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Mesocricetus
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Mice
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Mice, Inbred BALB C
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Molecular Structure
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Neurogenic Inflammation / drug therapy
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Nitric Oxide / biosynthesis
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Plakortis / chemistry*
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Trypanosoma cruzi / drug effects
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antineoplastic Agents
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Antiprotozoal Agents
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Macrolides
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plakortenone
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Nitric Oxide