Coumarins in both the free state and as O-glycosides are known to be widely distributed in nature [1]. The carbohydrate unit occurs at various positions of the benzopyran ring. The sugar component of coumarin O-glycosides can be monosaccharides (D-glucopyranose, L-rhamnopyranose, D-galactopyranose, D-and L-arabinopyranose, D-xylopyranose, etc.) and also certain disaccharides. Compared with the coumarins themselves, their glycosides are very soluble in water. Considering the high biological activity of natural and synthetic coumarins and the broad spectrum of their pharmacological activity, the synthesis and investigation of biologically active glycosides of compounds based on the benzopyran-2-one skeleton is very interesting. Therefore, the present study examined the synthesis of 5-hydroxy-and 7-hydroxy-3,4-cycloannelated coumarin D-glycopyranosides and their anticoagulant activity.Hydroxycoumarins 1-3 that were required for further transformations were prepared by Pechmann condensation of polyphenols (resorcinol and orcinol) with ethyl-2-oxocyclopentanecarboxylate or ethyl-2-oxocyclohexanecarboxylate in the presence of conc. H 2 SO 4 at 0°C [2, 3]; 3-hydroxybenzo[c]chromen-6-one (4), by Hartley condensation in NaOH solution of 2-bromobenzoic acid and resorcinol with a catalyst of copper sulfate solution (10%) [4].3,4-Cyclocondensed coumarin O-glycosides were synthesized using the most convenient method based on condensation of a glycosyl donor and potassium salts of hydroxycoumarins in aqueous acetone with cooling (0°C) (Modified Michael method) and were used successfully to synthesize a similar type of compounds [5][6][7]. Solutions of these salts were prepared using equivalent amounts of the respective hydroxycoumarin and KOH solution (10%) and double (relative to the volume of base) the amount of acetone. The glycosyl donors in this synthesis were acetobromosugars (D-isomers): α-acetobromoglucose (Ac 4 GlupBr), β-acetobromogalactose (Ac 4 GalpBr), α-acetobromoxylose (Ac 3 XylpBr), and β-acetobromoarabinose (Ac 3 ArapBr), which were prepared by known methods [8,9]. The synthesis gave 42-51% yields of the O-peracetates of glucopyranosides 5 and 6, galactopyranoside 7, xylopyranoside 8, and arabinopyranosides 9 and 10, which contain a carbohydrate in the 5-or 7-position of the coumarin ring.The structures of the resulting glycosides and the configurations of their anomeric centers were unambiguously confirmed using PMR spectroscopy. The PMR spectra of 5-10 contain signals for four (for glucosides and galactosides) or three (for arabinosides and xylosides) acetyls at 2.00-2.20 ppm and signals for the carbohydrate and aglycon moieties.

A complex approach based on the use of test organisms belonging to different systematic groups (plants, invertebrates and vertebrates), as well as the nucleolar biomarker and the micronucleus test on their cells, was applied to assess the toxicity, cytotoxicity and genotoxicity of two pharmaceutical substances (metamizole sodium and acetylsalicylic acid) applied at ic(50) concentrations for mammalian cells. The compound acetylsalicylic acid was evaluated at a concentration (1.6 x 10(3) mg l(-1)) that was non-toxic for bioassays based on fish (Carassius auratus gibelio) and hydra (Hydra attenuata) and acutely toxic for bioassays with ceriodaphnia (Ceriodaphnia affinis) and onion (Allium cepa). The metamizole sodium solution (6.25%) demonstrated acute toxicity for the whole set of test organisms. Both drugs, after their 30-360 min influence on the test organisms, first changed the nucleolar size in plant and animal cells (i.e. the transcriptional activity of ribosomal genes was affected most significantly). Moreover, the metamizole sodium solution caused nucleolar structural damage in 90% of hydra cells as early as after 30 min of exposure. The acetylsalicylic acid solution inhibited essentially the rate of cell division in the meristem of onion roots (the mitotic index decreased to 9.6 per thousand, as compared 51.7 per thousand for the control). The carp incubation and the onion germination in the acetylsalicylic acid solution showed a reproducible increase in the frequency of cells with micronuclei (2 and 5.5 times, respectively) and double nuclei (3 and 1.5 times, respectively). The approach described herein may be applied for obtaining rapid, cost-efficient and useful supplementary data on different types of toxicity for marketed drugs as well as for drugs under development.

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The article considers the vaginal suppositories "Melanizol" based on metronidazole, and tea tree oil influence on the museum and clinical microorganisms strains, that may be potential agents of vaginal infections. Established antimicrobial activity of vaginal suppositories "Melanizol" against the following strains of microorganisms Staphylococcus aureus, Basillus subtilis, Klebsiella, and Escherichia coli, and also found their antifungal activity against Candida albicans.

Aim. To study the hypoglycemic effect of the Medicago Sativa leaves extract in intact rats and in rats with a glucose load. Methods. At the first stage, hypoglycemic effect of Medicago Sativa leaves extract was determined in intact rats. 50 mg/kg of metformin and 18 mg/kg of herbal anti-diabetic «Arfazetin» tea were used as comparator drugs. At the second stage, hypoglycemic effect of Medicago Sativa leaves extract was determined in rats with glucose load. Blood samples for glucose analysis were taken before and in 15, 30, 60 and 120 minutes after loading. Blood glucose level was determined by glucose oxidase method. Results. Medicago Sativa leaves extract showed hypoglycemic effect both in intact animals and in animals with glucose load. 25 mg/kg of Medicago Sativa leaves extract decreased blood glucose level in intact animals at 4, 6 and 8 hours by 1.04, 1.14 and 1.11 times compared to the baseline level; the effect was comparable with herbal anti-diabetic «Arfazetin» tea and was inferior to metformin. A single 25 mg/kg dose of Medicago Sativa leaves extract showed hypoglycemic effect in animals with glucose load and significantly reduced blood glucose level in 15, 30, 60 and 120 minutes compared to control. Conclusion. The findings suggest that 25 mg/kg of Medicago Sativa leaves extract can be used as a herbal medication in the complex treatment of type II diabetes mellitus for its hypoglycemic properties.

Vaginitis is one of the most common reasons of women during calls to the gynecologist. The best method of their treatment is vaginal suppositories that contain antibacterial and anti-inflammatory components. We have studied vaginal suppositories "Klimedeks" in female-rats with experimental vaginitis caused by irritants mixture of a gum turpentine and dimethylsulfoxide. Treatment of vaginitis was 8 days. At 5th and 8th days animals were taken out of the experiment by method of euthanasia and researched vaginal mucosa by histologically. Vaginal suppositories "Klimedeks" at the fifth day of the experiment positively impact on the mucosa of the vagina in 87.5 % female rats of the animals had no signs of damage and inflammation of the lining of the vagina and superior comparator vaginal tablets "Mikozhynaks" for therapeutic effect. On the eighth day of the experiment, 100 % structural and functional state of animals mucous membrane of the vagina fully recovered. Placebo did no positive impact on the vagina of rats.

Вплив мазі, що містить сухий екстракт кореня солодки, на морфологічний стан шкіри мурчаків з алергічним контактним дерматитом Актуальність. У лікуванні зовнішніх запальних захворювань шкіри перспективними є лікарські засоби рослинного походження, які чинять комплексну фармакологічну дію, можуть тривало застосовуватися без іс-тотних побічних ефектів, характеризуються відносно низькою вартістю і простотою виробництва.Метою роботи було вивчення впливу мазі «Алерголік», яка містить сухий екстракт кореня солодки, на морфологічний стан шкіри мурчаків з алергічним контактним дерматитом (АКД).Матеріали та методи. АКД моделювали за методом Залкан П. М., Ієвлєвої Е. А., в якості алергену викорис-товували 2,4-динітрохлоробензол. Мазь «Алерголік» розроблена на кафедрі технології ліків НФаУ, в якості пре-парату порівняння використовували мазь «Фладекс».Результати та їх обговорення. Отримані морфологічні дані показали, що нашкірне нанесення 2,4-динітрохло-робензолу призводить до розвитку морфологічної картини АКД. Лікування маззю «Алерголік» запобігало розвитку АКД -зміни у шкірі тварин носили помірний залишковий характер. Мазь «Фладекс» проявляла невиразний позитив-ний вплив на морфологічний стан шкіри мурчаків із модельною патологією.Висновки. На основі проведеного морфологічного дослідження стану шкіри в мурчаків з АКД показано, що мазь «Алерголік» має виражений протиалергічний та протизапальний ефект і за ефективністю перевищує дію препарату порівняння -мазі «Фладекс». Отже, перспективним є подальше вивчення мазі «Алерголік» з метою її використання в терапії алергодерматозів. Influence of the ointment "Allergolik", which containes the dry extract of licorice rhizome, to the morphological state of guinea pigs' skin with allergic contact dermatitis Topicality. Herbal medicinal products are perspective for external application of the inflammatory skin diseases, which have complex pharmacological effect, can be used continuously without significant side effects, characterized low cost and ease manufacture.Aim. To investigate the influence of ointment "Allergolik", which contains the dry extract of licorice rhizome, to the morphological state of guinea pigs' skin with allergic contact dermatitis (ACD).Materials and methods. Modeling of ACD was performed by the method Zalkan P. M., Iyevleva E. A., as allergen 2,4-dinitrochlorobenzene was used. The ointment "Allergolik" was developed at the Department of Drug Technology the National University of Pharmacy. Ointment "Fladeks" was used as a reference drug.Results and discussion. Obtained morphological data showed that cutaneous application of 2,4-dinitrochlorobenzene leads to the development of the morphological picture of the ACD. The treatment with ointment "Allergolik" has prevented the ACD development -changes in the skin of animals were moderate and residual. Ointment "Fladeks" showed light positive effect on the skin morphology of guinea pigs with model pathology.Conclusions. Based on our study of the morphological state of guinea pigs' skin with ACD it was shown that the oi...

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