Semenova M.A., at all;
Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues; Bioorganic & Medicinal Chemistry Letters
Identification of anti-mitotic molecules that affect tubulin dynamics is a multi-step procedure. It includes in vitro tubulin polymerization assay, studies of a cell-cycle effect and general cytotoxicity assessment. To simplify this lengthy screening protocol, we have introduced and validated an assay system based on the sea urchin embryos. The proposed two-step procedure involves
i) fertilized egg test for mitotic arrest
ii) behavioral assessment of a free-swimming blastulae
In order to validate the assay, we have analyzed the effect of a panel of known anti-proliferative agents on the sea urchin embryo. For all tubulin destabilizing drugs, we observed rapid spinning and lack of forward movement of an embryo.
Both effects are likely to result from the in vivo microtubule disassembly caused by test molecules. Notably, the described assay yields rapid information on antiproliferative, antimitotic, cytotoxic, and tubulin destabilizing activities of the molecules along with their solubility and permeability potential. Moreover, measured potencies of the test articles correlated well with the reported values in both in vitro and cell-based assays.