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2011 Vol IX #2

Development of 11β-HSD1 inhibitors for the treatment
of metabolic syndrome

V.V. Lipson1,2, L.L. Zamigajlo3, O.N. Petrova3

1 Antidiabetic Drug Laboratory, State Institution «V.Ya. Danilevsky Institute for Endocrine Pathology Problems» of the Academy of Medical Sciences of Ukraine
Artema St., 10, 61002, Kharkov, Ukraine

1,2 V.N. Karazin Kharkov National University, Organic Chemistry Department
Svobody Sq., 4, 61077, Kharkov, Ukraine

3 State Scientific Institution «Institute for Single Crystals» of the National Academy of Sciences of Ukraine Lenina Prosp. 60, 61001, Kharkov, Ukraine

Summury. 11β-Hydroxysteroid dehydrogenase type I (11β-HSD1) is the enzyme that converts inactive 11-ketoglucocorticoids into active 11β-hydroxy-forms in metabolically relevant tissues such as the liver, adipose tissue and skeletal muscles. Chronically elevated local glucocorticoid action as a result of increased 11β-HSD1 activity is associated with metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus and cardiovascular complications. Inhibition of 11β-HSD1 has been proposed as a strategy to suppress glucocorticoid action in tissue-specific manner. A large variety of 11β-HSD1 inhibitors from different series of nitrogen containing heterocycles are now under investigation to treat type 2 diabetes and obesity.

Keywords: 11β-hydroxysteroid dehydrogenase, cortisol, metabolic syndrome, obesity, drug development.

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The influence of aluminum ions on actomyosin superprecipitation and myosin ATPase activity in cardiac muscle

Ê.². Bogutska1, Yu.². Prylutskyy1, Yu.P. Sklyarov2

1 Taras Shevchenko National University of Kyiv
64 Volodymyrska Str., Kyiv, 01601, Ukraine

2 National O. Bogomolets Medical University
13 T. Shevchenko Avenue, Kyiv, 01601, Ukraine

Summary. The inhibition of actomyosin superprecipitation reaction and myosin ATPase activity by aluminum ions in cardiac muscle have been found to depend on the concentration of aluminum ions, which causes the development of pathological processes in organism.

Êeywords: cardiac muscle, actomyosin, myosin, ATPase, superpreñipitation.

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Results of algae viruses search in human clinical material

O.A. Stepanova1, Ye.V. Solovyova2, A.V. Solovyov3

1 A.Î. Kovalevsky Institute of Biology of Southern Seas, NAS of Ukraine
2, Nakhimov Ave., Sevastopol, 99011, Ukraine

2 V.K. Gusak Institute of Urgent and Reconstructive Surgery, AMN of Ukraine
47, Lenin Ave., Donetsk, 83045, Ukraine

3 M. Gorky Donetsk National Medical University
16, Ilyich Ave., Donetsk, 83003, Ukraine

Summary. For the first time from a clinical material were isolated algae viruses. This fact testifies about probable role of algae viruses in a human pathology and establishes a new unknown ways in ecology of marine viruses and demands the further extended researches.

Keywords: viral ecology, algae viruses, clinical material.

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Âiological activity of some ½-geterilsubstitutes of L-cysteine and their analogs

Y.Y. Petrusha, L.A. Omelyanchik, A.A. Brazhko, M.P. Zavgorodny

Zaporizhzhya National University
66, Zhukovskogo Str., Zaporizhzhya, Ukraine, 69600

Summary. It was investigated biological activity (antibacterial, cytotoxic, psychotropic) new synthesized ½-geterilsubstitutes of L-cysteine and their structural analogs.

Keywords: ½-geterilsubstitutes of L-cysteine, cytotoxicity, antibacterial activity, «open field», the test of Porsolt.

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Study in vitro for antimicrobic activity of new oxazole derivatives and products of its transformations

I.M. Kopernik1, V.M. Blagodatnyj2, O.V. Petrenko2, L.E. Kalashnikova1, V.V. Prokopenko1, K.M. Kondratyuk1, O.I. Lukashuk1, O.V. Golovchenko1, S.A. Chumachenko1, O.V. Shablykin1, L.O. Metelitsa1, V.S. Brovarets1

1 Institute of Bioorganic and Petroleum Chemistry, NAS of Ukraine
1, Murmanska Str., Kyiv, Ukraine, 02660

2 P.L. Shupik National Medical Academy of Post-Graduate Education
9, Dorogozhytska Str., Kyiv, Ukraine, 04112

Summary. New water soluble derivatives of 4-cyano- and 4-phosphorylsubstituted 1,3-oxazoles and products if its transformations fungistatic and bacteriostatic activity was studied.

Keywords: 5-amino-1,3-oxazoles, 5-mercapto-1,3-oxazoles, 1,3,4-thiadiazole, phosphonic acids, fungistatic, bacteriostatic activity.

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Conformational space of 2’,3’-didehydro-2’,3’-dideoxyuridine and 2’,3’-didehydro-2’,3’-dideoxycytidine, nucleosides HIV-1 reverse transcriptase inhibitors: a comprehensive quantum chemical study

A.G. Ponomareva1, Ye.P. Yurenko1-3, R.O. Zhurakivsky1,2, D.M. Hovorun1-3

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

2 Research and Education Center State Key Laboratory of Molecular and Cellular Biology
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

3 Institute of High Technologies of Taras Shevchenko Kyiv National University
2, Hlushkova Ave., Kyiv, 03127, Ukraine

Summary. The work reports a comprehensive quantum chemical conformational analysis of two nucleoside analogues: 2’,3’-didehydro-2’,3’-dideoxyuridine (d4U) and 2’,3’-didehydro-2’,3’-dideoxycytidine (d4C). The electronic structure calculations were performed at the MP2/6-311++G(d,p)//DFT B3LYP/6-31++G(d,p) level of theory. It was found that d4U adopts 20 conformers (the corresponding number for d4C is 19), which are relative to local minima on the energy landscapes. Conformers of d4U and d4C are stabilized by a complicated network of specific intramolecular interactions, which includes conventional (OH×××O) and non-conventional (CH×××O, CH×××HC) H-bonds as well as closed-shell van der Waals contacts (C×××O). It has been shown that there is no conformational obstacles for d4U and d4C incorporation into the double helical DNA in A and B forms. Less pronounced biological activity of d4U as compared to 2’,3’-didehydro-2’,3’-dideoxythymidine (d4T) is due to the presence of the bulky methyl group in position 5 of d4T, which can be recognized by the target enzymes.

Keywords: 2’,3’-didehydro-2’,3’-dideoxyuridine, 2’,3’-didehydro-2’,3’-dideoxycytidine, conformational analysis, hydrogen bonds, biological activity, topological analysis of the electron density, NBO analysis.

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Investigation of structure and biological activity of aqueous solutions of metal nanoparticles

V.V. Olishevsky1, K.G. Lopatko2, Yu.O. Dashkovsky1, Y.G. Aftandilyants2, A.I. Marinin1, S.N. Zakharchenko3, N.N. Bilera2, S.V. Tkachenko1, O.M. Gonchar2,  I.V. Zhitnetsky1

1 National University of Food Technologies
68, Volodymirs’ka Str., Kyiv, 01601, Ukraine

2 National University of bioresources and nature management of Ukraine
12, Geroiv Oborony Str., Kyiv, 03041, Ukraine

3 Institute of Electrodynamics National Academy of Sciences of Ukraine
56, Peremohy Ave., Kyiv, 03057, Ukraine

Summary. The described method of dispersing electro conductive materials for specific formulations of nanomaterials and possible long-term storage of chemical and biological activity. The results of the study of structure and properties of nanoparticles in aqueous solution (colloidal). A study on the toxicity of copper in solution nanocomposites compared with solutions of salts on wheat. Investigated fungicidal and bactericidal activity of silver on microorganisms nanosolutions genus Trichoderma virens. Established that the investigated nanomaterials in their formulations, morphological characteristics, structural-phase composition, potentially biologically available material for use in biotechnology.

Keywords: aqueous solutions of metal nanoparticles, spark discharges, z-potential, ultrasonic vibrations, fungicidal activity.

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Two new pentacyclic triterpenoids from the roots of Achellia Fragrantissima F. and their biological activity

Y.A. Selim

Faculty of Specific Education, Zagazig University, Egypt

Summary. Two new pentacyclic triterpenoids, 2α-hydroxy-3-oxours-12-en-28-oic acid (1) and 2α-hydroxy-3-oxours-12,18-dien-28-oic acid (2) were isolated from the roots of Achellia Fragrantissima F., along with two known terpenes namely, α-amyrine (3) and ursolic acid (4). The structures of the new compounds (1) & (2) were elucidated by spectroscopic data interpretation. The antimicrobial activity of new two terpenoids (1) & (2) was studied on Escherichia coli, Staphylococcus aureus, Enterococcus faecalis and Pseudomonas aeruginosa.

Keywords: triterpenoids, plant extraction, spectroscopic analyses.

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The synthesis of inhibitors of human protein kinase CK2 among the derivatives of 2-phenylisothiazolidine-3-one-1,1-dioxide

M.O. Chekanov, A.R. Synyugin, S.M. Yarmoluk

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

Summary. We have synthesized nine novel derivatives of 2-phenylisothiazolidine-3-one-1,1-dioxide and tested their inhibitory activity toward human protein kinase CK2.

Keywords: 2-phenylisothiazolidine-3-one-1,1-dioxides, CK2 inhibitors, molecular docking.

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