Inhibitory effects on HIV-1 protease of tri-p-coumaroylspermidine from Artemisia caruifolia and related amides.
From a methanol extract of Artemisia caruifolia, which showed a moderate inhibitory activity on HIV-1 protease in a preliminary screening, N1,N5,N10-tri-p-coumaroylspermidine and three dicaffeoylquinic acids were isolated. The former compound was found to appreciably inhibit HIV-1 protease. Of related amides which were chemically synthesized, N1,N5,N10,N14-tetra-p-coumaroylspermine and N1,N4,N7,N10,N13-penta-p-coumaroylte-traethylenepentamine inhibited HIV-1 protease more potently than N1,N5,N10-tri-p-coumaroylspermidine.
Ma
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Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Sugitani, Japan.
Nakamura
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N
Hattori
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D000577:Amides / Q000302:isolation & purification / Q000494:pharmacology; D019306:Artemisia / Q000737:chemistry*; D003373:Coumaric Acids / Q000737:chemistry* / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000494:pharmacology; D021241:Spectrometry, Mass, Electrospray Ionization; D013095:Spermidine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*
D000577:Amides; D003373:Coumaric Acids; D017320:HIV Protease Inhibitors; C440200:N1,N5,N10-tris(4-coumaroyl)spermidine; D010936:Plant Extracts; D013095:Spermidine