Ukrainian biopharmaceutical journal № 2 (31) 2014

FULL TEXT

Т. Yu. Lykholat, О. A. Lykholat
STATE OF PROTEOLYTIC SYSTEM IN THE RAT ORGANISM BY ALIMENTARY ESTROGENS EXPOSED
Inhibition of the proteolytic processes in the experimental rats’ organism under the influence of the nutritional steroid hormones can lead to apoptosis deceleration due to the violations of signaling path­ways of data transmission and tension in the system of detoxification followed by the development of the proliferative hyperplastic processes and cancer in estrogen-sensitive tissues and in the particular breast. Keywords: proteolytic processes; steroid hormones; apoptosis; proliferation

М. V. Rybalkin, N. I. Filimonova, О. P. Strilets, L. S. Strelnikov
DETERMINING THE ABILITY OF THE INACTIVATED CELLS OF FUNGAL CANDIDA ALBICANS AND CANDIDA TROPICALIS AWAY FORM IMMUNITY AGAINST CANDIDA INFECTION
The immunogenic properties of inactivated fungal cells of Candida albicans and Candida tropicalis have been studied separately. The studies found that immunizing dose that provides the immunity among 3 months after intramuscular administration of 0,2 ml of inactivated Candida albicans fungal cells contain 4 mln/ml and cells inactivated fungi Candida tropicalis contain 5 mln/ml. It has been established that the intramuscular administration of inactivated cells of Candida provides more ef­ficient formation of immunity against Candida infections than the subcutaneous method of admini­stration. Key words: candidiasis; antigen; vaccine; immunity inactivated cells

А. V. Zaychenko, Yu. A. Tatskiy, V. A. Korotkov, А. V. Andriyanenkov, A. A. Ivanova
PHARMACOLOGICAL STUDY OF SUPPOSITORIES WITH OIL EXTRACT OF MACLURA POMIFERA ON THE EXPERIMENTAL MODEL TURPENTINE PROSTATITIS IN RATS
The results of the experimental study of prostate protective action of suppositories with oil extract Madura pomifera on the model of turpentine prostatitis in rats have been suggested. It is found that the use of suppositories with phytoextracts results in reducing the signs of general and systemic in­flammatory responses, inhibition of lipid peroxidation processes, increasing of activity of antioxidant system, normalization of androgenization’s level of male rats, recovering of the functional activity of the prostate. Suppositories with oil extract of Madura pomifera doesn’t concede in protective action to prostaplant forte of dose 35 mg/kg. Key words: prostate; prostatitis turpentine; oil extract of Madura pomifera; male-rats

М. V. Zupanets, S. М. Drogovoz, S. G. Isaev, A. A. Devyatkina
SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF D-(+)-GLUCOSYL AMMONIUM SALTS AND D-(+)-GLUCOSYLAMIDS 3-OXAMOIL SUBSTITUTED OF N-PHENYLANTHRANILIC ACIDS
New substances of the D-(+)-glucosylamonium salts 3-oxsamoilsubstituted of N-phenylanthranilic acids of D-(+)-glucosylamids 3-oxamoilsubstituted of N-phenylanthranilic acids have been synthesized. The structure and purity of substances investigated were confirmed by modern physico-chemical me­thods of elemental, IR-, PMR- spectral chromatographic analysis and qualitative reactions. It was established experimentally that the test substances in equimolecular doses relative to diclofenac sodium have anti-inflammatory activity. The regularities of communication “structure-activity” in newly synthesized compounds have been established. Amongthe last the phenomenon of pharmaco­dynamic synergies has been observed, which was shown as strengthening anti-inflammatory effects of glucosamine and N-phenylanthranilic acid. These researches testify the prospects of further study of these substances as future anti-inflammatory preparation. Key words: arthritis; glucosamine; N-phenylanthranilic acid; non-steroidal anti-inflammatory preparations

S. Chekman, G. A. Pogotova, Т. Yu. Nebesna, N. A. Gorchakova
QUANTUM-PHARMACOLOGICAL STUDY OF ANTIOXIDANT PROPERTIES OF SILYMARIN
In the article quantum-chemical parameters of the electronic and spatial structure of silybin molecule have been analyzed: topological characteristics, the charges of atoms, localization of HOMO and LUMO, electrostatic potential distribution in molecules, energies parameters. Keywords: silymarin; silybin; hepatoprotector; quantum pharmacology



N. V. Ruda, G. I. Stepanyuk, О. P. Drachuk
CHARACTERISTICS OF ACTOPROTECTIVE ACTION OF AMINOACIDS DERIVATIVES OF 1,4-NAPHTHOQUINONE UNDER CONDITIONS OF HYPO- AND HYPERTHERMY
It was shown in experiments on the rats that after unitary intraperitoneale introduction of amino-acids derivatives 1,4-naphtoguinone (substances III – 10,2 mg/kg and VI – 7,4 mg/kg) as a bemithylum (34 mg/kg) into organism physical endurance of animals (swimming test) rises under hyperthermic conditions (38-40 °С) on 61,7; 83,6 and 48,7 % and under hypothermic conditions (10-12 °С) rises on 39,2; 46,0 and 51,6 % (p < 0,05) accordingly. Such action of these compounds indicates that they have actoprotective effect. Compound VI, contains in its structure a glycine residue, is interested for in-depth study of its actoprotective properties and mechanisms of action. Key words: actoprotective action; derivatives of 1,4-naphtoguinone; hypo- and hyperthermy

D. V. Semeniv
STUDY OF PHARMACOLOGICAL ACTION OF OINTMENT WITH ARONIA MELANOCARPA OIL
According to medical statistics the prevalence of pathologies accompanied by wound process is ex­tremely high. Considering orientation of pharmacologically active substances ointment with Aronia melanocarpa oil is perspective to create a soft medicinal form with Aronia melanocarpa oil. The aim of this study was conducting research of anti-alterative activities of ointment with Aronia melano­carpa oil in comparison with sea buckthorn oil on the model of aseptic chronic inflammation of the skin and subcutaneous tissue in rats. During these studies it was found that according to anti-altera­tive activity (area of wounds, speed healing, temperature of skin) ointment with Aronia melanocarpa oil showed more pronounced pharmacological activity then sea buckthorn oil. Key words: ointment with Aronia melanocarpa oil; wound process; anti-alterative activities; sea buckthorn oil.

A. L. Zagayko, L. V. Galuzinskaya
THE SEARCH OF NEW SUBSTANCES OF PLANT ORIGIN FOR TREATMENT OF PSORIASIS
The medicines with anti-inflammatory and reparative activities have the important role in the com­plex treatment of psoriasis. In connection with this fact the search of new effective means for the local use, what influence on the facilitation of the psoriasis clinical course, remains actual. These data prove that the cream “Enopsor” has shown a pronounced anti-inflammatory and reparative proper­ties on the model of skin inflammation with dominated alteration – ultraviolet erythema. This allows us to suppose that the leading role has the stabilization of cell membranes, mediated inhibition of LPO (lipid peroxidation) and restoring the antioxidant defense of organism. Key words: psoriasis; anti-inflammatory activity; alteration; polyphenols.

Yu. N. Avidzba, О. М. Koshovyi, О. S. Kukhtenko, А. М. Komissarenko
STUDY OF INTEGRATED PROCESSING PRODUCTS FROM EUCALYPTUS LEAVES AFTER PRODUCTION ESSENTIAL OIL
The qualitative and quantitative composition of phenolic compounds content of eucalyptus leaves hydrophilic extracts derived from the waste and the distillation liquid after essential oil production were studied. It has been established that the extracts contain aminoacids, polysaccharides, hydroxy-cinnamic acids, flavonoids, a significant amount of the hydrolyzable tannins. Qualitative and quanti­tative composition of basic biological active substances were studied. Antimicrobial, anti-inflamma­tory and anabolic activity of total dry extract from Eucalyptus leaves, obtained by complex processing were investigated.

Keywords: Eucalyptus viminalis Labill.; leaves; hydrophilic extract; chemical composition; antimi­crobial, anabolic, anti-inflammatory activity

А. V. Glushchenko
QUANTITATIVE DETERMINATION OF FLAVONOIDS IN THE EXTRACTS OF SALSOLA COLLINA L.
In the review the method of quantitative determination of flavonoids in the extracts from above-ground of the Salsola collina has been presented. The determination of flavonoids has been carried out in aqua and ethanol (30 %, 50 %, 70 %) extracts by spectrophotometric method at wavelength set 411 nm by method of standards. Above 0,52 % of flavonoids in the above-ground of the Salsola collina have been founded. The highest content of flavonoids has been determined in 70 % ethanol extract. Results of this research will be used for the development of quality control methods for the analyzed herbal materials. Key words: Salsola collina; flavonoids; above-ground; spectrophotometric determination

G. Kaplaushenko
ACYLATION OF 4-MONO- AND 4,5-DISUBSTITUTED OF l,2,4-TRIAZOL-3-THIONE AND DATA OF ACUTE TOXICITY OF REACTION PRODUCTS
Acylation reaction of 4-R1-l,2,4-triazolil-3-thiones and 5-R-4-Rr 1,2,4- triazolil-3-thiones derivatives has been studied. Thus preparative production methods of relevant 3-acylthio derivatives that in­volve short-term heating of initial substances on bain-marie have been developed. It was established that a prolonged heating of initial thiones with anhydride acetic acid results to formation of diacyl derivatives confirmed with chromatography-mass spectrometry. The structure of the synthesized compounds has been confirmed with combined using of physical chemical analysis methods such as elemental analysis , IR-spectroscopy and NMR-spectrometry Investigation of acute toxicity for S-acetyltio-R- and 5-R-4-R1-l,2,4-triazoles showed that LD50 values of these compounds are within 947-1248 mg/kg and these substances belong to the fourth toxicity class and they are low-toxic sub­stances according to Sidorov’s classification. Key words: 1,2,4-triazoles; acylation; acute toxicity

Yu. Klimenko, S. M. Trut, G. P. Petyunin, T. A. Kostina
National University of Pharmacy
Kharkiv Medical Academy of Postgraduate Education
DETERMINING ACCURACY IN VALIDATION OF UV-SPECTROPHOTOMETRIC METHODS OF QUANTITATIVE MEASUREMENT IN FORENSIC TOXICOLOGICAL ANALYSIS

М. О. Shcherbak, A. G. Kaplaushenko

THE EFFECT OF ADSORPTION PROPERTIES OF 3-ALKYLTHIO-5-(2-, 3-, 4-NITROPHENYL)-4-AMINO-l,2,4-TRIAZOLES ON THEIR TOXICITY AND ACTOPROTECTIVE ACTIVITY
One of the major social and economic goals of the pharmaceutical industry nowadays is the crea­tion of new domestic medicines, which are competitive with expensive imported drugs. A key step in the creation of original drugs is the targeted synthesis of biologically active compounds with high pharmacological effect and low toxicity. It is known that increasing of the carbon chain length of the surfactants leads to increase of adsorption, to enhancement of pharmacological activity and higher data of toxicity. That’s why we made the definition of the surface activity effect and the relative ad­sorption of 3-alkylthio-5-(2-, 3-, 4-nitrophenyl)-4-amino-l,2,4-triazoles, which are representatives of one type of homologous series and made the correlation of the results with indicators of toxicity and actoprotective activity of the compounds synthesized. Key words: 1,2,4-triazole; surface tension; surface activity; adsorption; toxicity; actoprotective activity