It is structurally related to other marine cyanobacterial
metabolites such as
somocystinamide A[2] and
curacin A, which have inspired extensive investigations into their use as a lead for
anticancer therapies.[3][4][5][6] Its biological activity profile has not been fully evaluated due to decomposition of the natural sample. However, it has shown moderate
cytotoxicity against
H460 human lung cancer cells.[1]
In order to examine the possibility that LcA's true bioactivity was diminished by
solubility issues, Taylor et al. chemically
synthesized LcA.[7] This synthetic sample was incorporated into an emulsifier
PEG400 and tested for its cytotoxicity against H460 cells. This sample did not show any more activity than the natural sample, implying that LcA only has moderate cytotoxicity. In addition, simple
enamide analogs showed no activity.[7] This work implies that the exceptional antiproliferative activity of
somocystinamide A arises from the
dimeric nature of its structure and not from the enamide moiety.