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Thiazoline peptides and a tris-phenethyl urea from Didemnum molle with anti-HIV activity.

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 ?M, respectively. Compound 3 was active only in the cytoprotective cell-based assay, with an IC(50) value of 60 ?M.

SUBMITTER: Lu Z

PROVIDER: S-EPMC4176947 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature

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Thiazoline peptides and a tris-phenethyl urea from Didemnum molle with anti-HIV activity.

Lu Zhenyu Z Harper Mary Kay MK Pond Christopher D CD Barrows Louis R LR Ireland Chris M CM Van Wagoner Ryan M RM

Journal of natural products 20120730 8

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 ...[more]

PMID: 22845329

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