English version Ukrainian version
Last issue Archive Editorial board Instructions to authors Contact us




This site supported by
 
2012 Vol Õ # 2


Peculiarities of protein metabolism at administration to prenatal alcoholized rats of aza-15-crown-5 ether derivative with nootropic activity

T.L. Karaseva, J.M. Tsapenko, S.S. Basok

A.V. Bogatsky Physico-Chemical Institute National Academy of Sciences of Ukraine
86, Lyustdorfska doroga, Odesa, 65080, Ukraine

Summary. It was studied the influence of crow ether (CE), possessing nootropic activity on peculiarities of protein metabolism in various structures of brain in prenatal alcoholized rats. It was found, that CE (25 mg/kg) removed the disturbances in protein synthesis in postnatal period. It is manifested in the increasing of protein content and its fractions, in activation of protein synthesis in the most regions of rats brain. CE is able to activate protein metabolism in CNS after 2 months of its administration.

Keywords: crown ether, prenatal alcoholization, brain proteins content, protein synthesis.

Full-text in PDF Contact authors


Synthesis and antioxidant activity of 3-aryl-4,7-dihydroxycoumarins

S.P. Bondarenko

National University of Food Technologies
68, Volodymirska Str., Kyiv, Ukraine, 01601

Summary. A number of substituted of 3-aryl-4,7-dihydroxy coumarins were synthesized and tested their antioxidant activity in vitro. The carried research has shown promising of the further search for compounds possessed antioxidant activity among 3-aryl-4,7-dihydroxycoumarins with expansion of investigating compounds database.

Keywords: 3-aryl-4,7-dihydroxycoumarin, antioxidative activity, tween 80, malonaldehyde, 2-thiobarbituric acid.

Full-text in PDF Contact authors


Search of new low-molecular protein kinase CK2 inhibitors among 3,4,5,6-tetrahydrotiopirano[2,3-d]thiazole derivatives

O.V. Ostrynska, V.G. Bdzhola, A.P. Kukharenko, S.M. Yarmoluk

Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

Summary. This article is about search of new protein kinase CK2 inhibitors among 3,4,5,6-tetrahydrotiopirano[2,3-d]thiazole derivatives by receptor-based virtual screening method. Compounds inhibitory activity was confirmed by biochemical tests in vitro. All inhibitors has IC50 values in the range of 0,2 to 24,5 µÌ. The structure-activity relationship of 3,4,5,6-tetrahydrotiopirano[2,3-d]thiazole derivatives was investigated and the binding modes of their interaction with protein kinase CK2 ATP-acceptor site were proposed.

Keywords: protein kinase CK2, 3,4,5,6-tetrahidrotiopirano[2,3-d]thiazole derivetives, inhibitor, docking, tumor.

Full-text in PDF Contact authors


Mutagenic properties of 5-halogen derivatives of uracil: quantum-chemical investigation

O.O. Brovarets’

Department of Molecular and Quantum Biophysics, Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

Research and Educational Center «State Key Laboratory of Molecular and Cell Biology»
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

Department of Molecular Biology, Biotechnology and Biophysics, Institute of High Technologies, Taras Shevchenko National University of Kyiv
2g, Hlushkova Ave, Kyiv, 03022, Ukraine

Summary. The mechanisms of the intra- and intermolecular tautomerisation of 5XUra bases (X = H, CH3, Br, Cl, F) and mispairs involving them and guanine (Gua) or adenine (Ade) have been studied to analyse their implications for the origin of the induced point mutations using quantum-chemical calculations at the MP2/6-311++G(3df,2pd)//B3LYP/6-311++G(d,p) level of theory in the free state. For the first time it has been established that the substitution of the hydrogen atom at the C5 position of Ura for the halogen (Hal = Br, Cl, F) has practically no effect on the main physico-chemical characteristics of intramolecular tautomerisation. The lifetime of the mutagenic tautomers of the 5-halogenuracils exceeds typical time of the DNA replication in the cell (~103 s) by 4-13 orders. The absence of intramolecular H-bonds in the canonical and mutagenic tautomeric forms of bases determines their high stability. These results confirm the adequacy of classical «rare tautomeric hypothesis» for substitution mutagenesis originally proposed by Watson and Crick. For the first time the influence of the halogen derivatives of Ura on replication and incorporation errors in DNA has been studied. It was shown that Ura halogenization does not induce replication errors, however causes incorporation errors due to the lowering of the barrier of the Gua·5XUra (X = Hal) wobble base pairs tautomerisation into the Gua*·5XUra base pairs with Watson-Crick geometry in comparison with Gua·Thy base pair.

Keywords: 5-halogen derivatives of Ura, mutagenic properties, induced point mutations, quantum-chemical calculations.

Full-text in PDF Contact authors


Structural-dynamical properties of pyrimidine-pyrimidine DNA base pairs with cis-oriented glycosidic bonds: a quantum-chemical study

O.Î. Brovarets’

Department of Molecular and Quantum Biophysics,
Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

Research and Educational Center «State Key Laboratory of Molecular and Cell Biology»
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

Department of Molecular Biology, Biotechnology and Biophysics,
Institute of High Technologies, Taras Shevchenko National University of Kyiv
2g, Hlushkova Ave, Kyiv, 03022, Ukraine

Summary. It was found for the first time that Cyt·Cyt*, Thy·Thy* and Cyt·Thy pyrimidine-pyrimidine DNA base pairs with cis-orientation of glycosidic bonds are propeller-like structures that are stabilized by two antiparallel H-bonds and O2...O2 van der Waals contact. The dipole-active interconversion of their enantiomers occurs via the planar transition state with a characteristic frequency ~5·1011 Hz. Based on the obtained results the author concluded that the fitting of the mismatched pyrimidine-pyrimidine DNA base pairs in the active site of the high fidelity DNA-polymerase in order to acquire the Watson-Crick sizes, ensuring their incorporation into the structure of the DNA double helix, occurs due to the periodic interconversion of their enantiomers. It is suggested that an additional fitting of the mismatches into the competent dimensions is also provided by the deformation of the sugar residue relative to the base.

Keywords: spontaneous point mutations in DNA; transversions; pyrimidine-pyrimidine DNA base pairs; interconversion of the enantiomers; quantum-chemical methods.

Full-text in PDF Contact authors




Full-text in PDF Contact authors

 

Home