Abstract
Bioassay-guided fractionation and purification of the aerial parts of Piper submultinerve led to the isolation of a new conjugated amide-dimer, submultinamide A (1), along with 11 known compounds. The structures were determined on the basis of spectroscopic methods. Among the tested compounds, pellitorine (2), guineensine (4), N-benzylcinnamide (6) and aristolactam BII (8) showed significant activities in the anti-syncytium assay using (ΔTat/Rev)MC99 virus and 1A2 cell line system, whereas 2 was most active (EC₅₀ 35.1 µM and selectivity index 4.7). In the HIV-1 reverse transcriptase assay, only 4 was active with IC₅₀ 50.8 µM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkenes / chemistry
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Alkenes / pharmacology
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Amides / chemistry
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Amides / isolation & purification
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Amides / pharmacology
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / isolation & purification
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Anti-HIV Agents / pharmacology*
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Cell Line / virology
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Dimerization
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Drug Evaluation, Preclinical / methods
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Fatty Acids, Unsaturated / chemistry
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Fatty Acids, Unsaturated / pharmacology
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HIV Reverse Transcriptase / metabolism
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Heterocyclic Compounds, 2-Ring / chemistry
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Heterocyclic Compounds, 2-Ring / pharmacology
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Humans
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Inhibitory Concentration 50
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Lactams / chemistry
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Lactams / pharmacology
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Molecular Structure
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Piper / chemistry*
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Plant Components, Aerial / chemistry
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Plant Extracts / chemistry
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Plant Extracts / pharmacology
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Polyunsaturated Alkamides / chemistry
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Polyunsaturated Alkamides / pharmacology
Substances
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Alkenes
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Amides
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Anti-HIV Agents
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Fatty Acids, Unsaturated
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Heterocyclic Compounds, 2-Ring
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Lactams
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Plant Extracts
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Polyunsaturated Alkamides
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aristolactam BII
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guineensine
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submultinamide A
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pellitorine
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reverse transcriptase, Human immunodeficiency virus 1
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HIV Reverse Transcriptase