Abstract
As part of our screening for anti-HIV agents from marine invertebrates, the MeOH extract of Didemnum molle was tested and showed moderate in vitro anti-HIV activity. Bioassay-guided fractionation of a large-scale extract allowed the identification of two new cyclopeptides, mollamides E and F (1 and 2), and one new tris-phenethyl urea, molleurea A (3). The absolute configurations were established using the advanced Marfey's method. The three compounds were evaluated for anti-HIV activity in both an HIV integrase inhibition assay and a cytoprotective cell-based assay. Compound 2 was active in both assays with IC(50) values of 39 and 78 μM, respectively. Compound 3 was active only in the cytoprotective cell-based assay, with an IC(50) value of 60 μM.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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HIV Integrase Inhibitors / chemistry
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HIV Integrase Inhibitors / isolation & purification*
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HIV Integrase Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Papua New Guinea
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Peptides, Cyclic / chemistry
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Peptides, Cyclic / isolation & purification*
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Peptides, Cyclic / pharmacology*
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Phenylurea Compounds / chemistry
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Phenylurea Compounds / isolation & purification*
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Phenylurea Compounds / pharmacology*
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Thiazolidines / chemistry
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Thiazolidines / isolation & purification*
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Thiazolidines / pharmacology*
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Urochordata / chemistry*
Substances
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HIV Integrase Inhibitors
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Peptides, Cyclic
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Phenylurea Compounds
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Thiazolidines
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mollamide E
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mollamide F
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molleurea A