Thiazoline Peptides and
a Tris-Phenethyl Urea from <i>Didemnum molle</i> with Anti-HIV
Activity
Zhenyu Lu
Mary Kay Harper
Christopher
D. Pond
Louis R. Barrows
Chris M. Ireland
Ryan M. Van Wagoner
10.1021/np300270p.s001
https://acs.figshare.com/articles/journal_contribution/Thiazoline_Peptides_and_a_Tris_Phenethyl_Urea_from_i_Didemnum_molle_i_with_Anti_HIV_Activity/2493328
As part of our screening for anti-HIV agents from marine
invertebrates, the MeOH extract of <i>Didemnum molle</i> was tested and showed moderate <i>in vitro</i> anti-HIV
activity. Bioassay-guided fractionation of a large-scale extract allowed
the identification of two new cyclopeptides, mollamides E and F (<b>1</b> and <b>2</b>), and one new tris-phenethyl urea, molleurea
A (<b>3</b>). 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 <b>2</b> was active
in both assays with IC<sub>50</sub> values of 39 and 78 μM,
respectively. Compound <b>3</b> was active only in the cytoprotective
cell-based assay, with an IC<sub>50</sub> value of 60 μM.
2012-08-24 00:00:00
78 μ M
IC 50 value
Compound
cytoprotective
60 μ M
Didemnum molle
HIV integrase inhibition assay
IC 50 values