Thiazoline Peptides and a Tris-Phenethyl Urea from Didemnum molle with Anti-HIV Activity

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• 作者：Zhenyu Lu ; Mary Kay Harper ; Christopher D. Pond ; Louis R. Barrows ; Chris M. Ireland ; Ryan M. Van Wagoner
• 刊名：Journal of Natural Products
• 出版年：2012
• 出版时间：August 24, 2012
• 年：2012
• 卷：75
• 期：8
• 页码：1436-1440
• 全文大小：201K
• 年卷期：v.75,no.8(August 24, 2012)
• ISSN：1520-6025

文摘

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鈥檚 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 IC₅₀ values of 39 and 78 渭M, respectively. Compound 3 was active only in the cytoprotective cell-based assay, with an IC₅₀ value of 60 渭M.