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Simferopol’, Ukraine

Fleishaker D.L.,Pfizer | Garcia Meijide J.A.,Hospital Ntra. Sra. de la Esperanza | Petrov A.,Crimean State Medical University | Kohen M.D.,Avivoclin Clinical Services | And 7 more authors.
Arthritis Research and Therapy

Introduction: The purpose of this study was to determine whether maraviroc, a human CC chemokine receptor 5 (CCR5) antagonist, is safe and effective in the treatment of active rheumatoid arthritis (RA) in patients on background methotrexate (MTX).Methods: This phase IIa study comprised two distinct components: an open-label safety study of the pharmacokinetics (PK) of MTX in the presence of maraviroc, and a randomized, double-blind, placebo-controlled, proof-of-concept (POC) component. In the PK component, patients were randomized 1:1 to receive maraviroc 150 or 300 mg twice daily (BID) for four weeks. In the POC component, patients were randomized 2:1 to receive maraviroc 300 mg BID or placebo for 12 weeks. Patients were not eligible for inclusion in both components.Results: Sixteen patients were treated in the safety/PK component. Maraviroc was well tolerated and there was no evidence of drug-drug interaction with MTX. One hundred ten patients were treated in the POC component. The study was terminated after the planned interim futility analysis due to lack of efficacy, at which time 59 patients (38 maraviroc; 21 placebo) had completed their week 12 visit. There was no significant difference in the number of ACR20 responders between the maraviroc (23.7%) and placebo (23.8%) groups (treatment difference -0.13%; 90% CI -20.45, 17.70; P = 0.504). The most common all-causality treatment-emergent adverse events in the maraviroc group were constipation (7.8%), nausea (5.2%), and fatigue (3.9%).Conclusions: Maraviroc was generally well tolerated over 12 weeks; however, selective antagonism of CCR5 with maraviroc 300 mg BID failed to improve signs and symptoms in patients with active RA on background MTX.Trial Registration: ClinicalTrials.gov: NCT00427934. © 2011 Fleishaker et al.; licensee BioMed Central Ltd. Source

Kovalenko S.I.,Zaporozhye State Medical University | Nosulenko I.S.,Zaporozhye State Medical University | Voskoboynik A.Yu.,Zaporozhye State Medical University | Berest G.G.,Zaporozhye State Medical University | And 3 more authors.
Medicinal Chemistry Research

The series of novel N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c] quinazoline-6-yl)thio]acetamides were obtained by aminolysis of activated acids 1a-1d and by alkylation of potassium salts 2a-2d by N -aryl-2-chloroacetamies. The structures of compounds were determined by IR, 1H, 13C NMR, LC- and EI-MS analyses. The results of cytotoxicity evaluation by bioluminescence inhibition of bacterium Photobacterium leiognathi Sh1 showed that compounds reveal moderate cytotoxicity. Screening of anticancer activity in vitro yielded the most active compounds 3t, 4b, 4f, 4l and 4n in micromolar concentrations with the GI50 level (logGI50 is from -7.57 to -4.05 for different cell lines, and logGI50 mean graph midpoint varied from -5.30 to -4.50). Moreover, compound 4b had a distinctive selectivity against renal cancer, 4f - colon cancer and melanoma and 4l - renal cancer. The highest sensitivity to compound 4b showed renal cancer cell lines A498 (logGI50 = -7.57). SAR-analysis was discussed, COMPARE analysis and docking was studied. Graphical Abstract: The novel synthesis methods of the N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio] acetamides are proposed. Anticancer activity and Photobacterium leiognathi Sh1 bioluminescence inhibition of synthesized compounds are discussed. SAR-analysis was discussed, and COMPARE analysis and docking was studied. © 2012 Springer Science+Business Media New York. Source

Knyazev S.A.,KV Inc | Efetov K.A.,Crimean State Medical University | Ponomaryov K.B.,KV Inc
Entomological Review

The fauna of the family Zygaenidae of Omsk Province is reviewed. 12 species are listed, among which 7 are recorded from this territory for the first time. © 2015, Pleiades Publishing, Inc. Source

Taran M.V.,National University of Life and Environmental Sciences of Ukraine | Starodub N.F.,National University of Life and Environmental Sciences of Ukraine | Katsev A.M.,Crimean State Medical University | Guidotti M.,National Research Council Italy | And 3 more authors.
Progress in Biomedical Optics and Imaging - Proceedings of SPIE

The effect of silver and zinc oxide nanoparticles in combination with alginate on bioluminescent Photobacterium leiognathi Sh1 bacteria was investigated. Silver nanoparticles were found to be more toxic than zinc oxide nanoparticles on bioluminescent bacteria. The nanoparticles and their ions released results in the same effect, however, it was absent in combination with alginate. The effective inhibiting concentration (EC50) for silver nanoparticles was found about 0.3 - 0.4 μg mL-1, which was up to two times larger then for zinc oxide nanoparticles. The absence of sodium chloride in the tested media prevented the formation of colloidal particles of larger size and the effective inhibition concentrations of metal derivatives were lower than in the presence of sodium chloride. © 2013 SPIE. Source

Efetov K.A.,Crimean State Medical University | Parshkova E.V.,Crimean State Medical University | Baevsky M.Y.,Taurida National University | Poddubov A.I.,Taurida National University
Ukrain'skyi Biokhimichnyi Zhurnal

2-butyl 2-dodecenoate has been synthesized from lauric acid and sec-butanol. The study of the biological activity of this substance has demonstrated its property as a sex attractant for males of Jordanita graeca, Jordanita globulariae and Theresimima ampellophaga (Lepidoptera: Zygaenidae, Procridinae). The latter species is the grape pest in southern Europe. The attractant obtained can be used for the detection of species, for monitoring their numbers in nature and for the elaboration of ecological methods of pest control. Source

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