Abstract
The present study reports the identification of two new staurosporine derivatives, 2-hydroxy-7-oxostaurosporine (1) and 3-hydroxy-7-oxostaurosporine (2), obtained from mid-polar fractions of an aqueous methanol extract of the tunicate Eudistoma vannamei, endemic to the northeast coast of Brazil. The mixture of 1 and 2 displayed IC50 values in the nM range and was up to 14 times more cytotoxic than staurosporine across a panel of tumor cell lines, as evaluated using the MTT assay.
Highlights
Tunicates are a group of marine invertebrates abundant along coastal regions, often found as the dominant organisms in sessile benthic communities [1]
The present study reports the bioactivity-guided isolation of two new members of the staurosporine group of alkaloids from the extract of E. vannamei
The aqueous methanol extract from E. vannamei was submitted to cytotoxicity-guided fractionation, resulting in the isolation of 5 mg of an active fraction, which appeared as a single spot by thin layer chromatography (TLC) and a single peak via LC-MS analysis
Summary
Tunicates are a group of marine invertebrates abundant along coastal regions, often found as the dominant organisms in sessile benthic communities [1]. The faunal list for the state of Ceará, on the northeastern coast of Brazil, indicated that 22 species of ascidians were registered [5,6], including novel species and many cases of regional endemism. This coastline has been scarcely explored as a source of natural products. In 2003, a pioneering study investigated the cytotoxicity of aqueous methanol extracts of the ten most abundant ascidians of Ceará The results of these assays suggested that Eudistoma vannamei Millar, 1977 (Figure 1a) might be of interest due to its marked bioactivity, especially the inhibition of growth in tumor cell lines [7]. The present study reports the bioactivity-guided isolation of two new members of the staurosporine group of alkaloids from the extract of E. vannamei
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