See our screening results in In_Vivo database and NCI-60 screening results in NCI_tested database in Database Center
Our screening data see in database fields:
CLEAV_ALT_EC (mM) - effective concentration of compound resulted in alteration
of quick successive cell divisions in the early embryo, mmol
CLEAV_ARR_EC (mM) - effective concentration of compound resulted in total
block of quick successive cell divisions in the early embryo, mmol
EMB_SPIN_EC(mM) - effective concentration of compound resulted in quick
embryo rotation on the bottom of the vessel instead of normal forward swimming, mmol
1. Semenova, M.; Kiselyov, A.S.; Semenov, V.V. Sea urchin embryo as a model organism for the rapid functional screening of tubulin modulators. BioTechniques 2006, 40, 765-774;
2. Semenova M.N.; Kiselyov A.S.; Titov, I.Y.; Raihstat, M.M.; Molodtsov, M.; Grishchuk, E.; Spiridonov, I.; Semenov, V.V. In Vivo evaluation of indolyl glyoxamides in the sea urchin embryo model: correlation with in vitro tubulin dynamics effects. Chem. Biol. Drug Design 2007, 70, 485-490.
3. Semenova M.A., at all; A Synthetic Derivative of Plant Allylpolyalkoxybenzenes Induces Selective Loss of Motile Cilia in Sea Urchin Embryos; ACS Chemical Biology, 2008, 3(2), 95-100
4. Kiselyov A.S.; Semenova M.N.; at all; Novel derivatives of 1,3,4-oxadiazoles are potent mitostatic agents featuring strong microtubule depolymerizing activity in the sea urchin embryo and cell culture assays. European Journal of Medicinal Chemistry 45 (2010) 1683-1697
5. Semenov V.V., Kiselyov A.S; at all; Synthesis of Antimitotic Polyalkoxyphenyl Derivatives of Combretastatin Using Plant Allylpolyalkoxybenzenes. J. Nat. Prod. 2010, 73, 1796-1802
6. Sheremetev A.B., Dmitriev D.E., at all; New functionaized aminofurazans as potential antimitotic agents in the sea urchin embryo assay. Mendeleev Commun., 2010, 20, 132-134
7. Semenova M.A., at all; Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues; Bioorganic & Medicinal Chemistry Letters (in press)
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.
||tubulin destabilizing drugs
Download video (DivX, 2.5Mb)
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.