Introduction. Medicines of natural origin have advantages over synthetic drugs and occupy a significant share in the assortment of pharmacies. Filipendula ulmaria (L.) Maxim., characterized by a chemical composition rich in phenolic compounds and various types of biological activity has the potential in terms of the development of new herbal medicines. In an in vivo experiment, F. ulmaria extract showed immunomodulatory, anti-inflammatory, osteogenic activity and effectively stimulated myelopoiesis in conditions of microbial damage of bone tissue.Aim. Development of an optimal technology for obtaining dry extract of F. ulmaria by remaceration and investigation of its аcute toxicity.Materials and methods. The technology of extract was developed in a laboratory reactor equipped with a water heater jacket and a stirrer. The content of flavonoids was determined by differential spectrometry. Flowability was determined on a flowability tester for powders and granules, bulk density was determined on a bulk density tester for powders and granules, moisture content was developed on a moisture content analyzer. Acute toxicity was determined on Wistar rats.Results and discussion. The dry extract of F. ulmaria, obtained using 70 % ethanol by remaceration, is effective in conditions of microbial damage of bone tissue and bone marrow, which determined the choice of extragent and the type of extract. The optimal parameters for obtaining the extract were determined (three-fold maceration at a water jacket temperature of 80 °C, the ratio of raw materials to extragent 1 : 14, time 30 min), its main technological characteristics were determined and a wet granulation method for improving them was proposed. In the study of acute toxicity of the extract, according to the results of toxicometry for 14 days after administration and necropsy data, the studied extract was classified as low-toxic substance.Conclusion. The dry extract of F. ulmaria, obtained by remaceration using 70 % ethanol, has specific activity in conditions of microbial damage to bone tissue. Optimal extraction parameters allow to increase the yield of target components, it is advisable to improve the technological parameters of the extract by wet granulation. The assessment of the safety profile of the dry extract from F. ulmaria, along with its high biological activity, provides a perspective for its further study and implementation into medical practice.

Introduction. Lemna minor L. (duckweed) refers to the duckweed subfamily (Lemnaceae S. F. Gray) and widely distributed in ponds of Russia. Literature data confirm the possibility of harvesting significant volumes of this raw material in natural habitat and grown in aquaculture. The process of biosynthetic accumulation in duckweed fronds provides a variety of compounds with a wide spectrum of biological activity. Therefore, the use of raw materials Lemna minor L. is promising for the development of drugs and parapharmaceutical products. Thus, it is an urgent task to quantify active components of duckweed and standardize (determination of criteria for identification, quality and safety) plant material.Aim. Establish macro- and microscopic characteristics of raw materials and develop methods for the quantitative determination of the main groups of biologically active substances (BAS) for standardization of raw duckweed.Materials and methods. Samples of duckweed was collected in natural habitats of Western Siberia. Macro- and microscopic assay, HPLC, UV-spectrometry were used in research process.Results and discussion. Were established the criteria for identification of duckweed fronds by studying external (macroscopic) and microscopic features of raw material Lemna minor L. Was developed and validated the procedure of the quantitative determination of phenolcarboxylic acids in raw material Lemna minor L.Conclusion. The study of external (macroscopic) and microscopic features provided the criteria for identification of the raw material Lemna minor L. The technique for the quantitative analysis of polysaccharides using gravimetry does not need validation, because is a direct method of substance measurement. Was validated quantification method of phenolcarboxylic acids (in terms of chlorogenic acid) by criteria of linearity, repeatability, in-laboratory precision and accuracy. Was established quality criteria for identification and quantitative assay, which can be used in the draft for normative documents for medicinal plant raw material of Lemna minor L. «Duckweed fronds».

In experiments on the golden hamsters-males antiopisthorchiasis activity (with respect to Opisthorchis felineus) of extracts obtained from Centaurea scabiosa L., Centaurea pseudomaculosa Dobrocz., Centaurea jaceae L. and Centaurea phrygia L. Asteraceae family was investigated. Antiopisthorchiasis activity of sesquiterpene lactone guainolide-type cynaropicrin isolated from Centaurea scabiosa L. was confirmed. It’s suggested that sesquiterpene lactones grosshemin and repin has an antihelminthic activity.

The purpose of this research is to study the antiradical activity of various extracts from the Centaurea scabiosa L. aerial part (wild-growing and cultivated) and Centaurea jacea L. as potential sources of antioxidant herbal remedies. In the study of the antiradical activity of extracts from the aerial part of Centaurea jacea L., Centaurea scabiosa L. wild growing and cultivated, in the reaction with a stable diphenylpicrylhydrazyl radical, it was found that the degree of antiradical activity within each species correlates with the quantitative content of flavonoids. Lower values ​​of the antiradical activity of cultivated Centaurea scabiosa L. extracts compared to wild growing Centaurea scabiosa L. extracts are consistent with a lower content of flavonoids in the latter. The dependence of the Centaurea jacea L. and wild growing Centaurea scabiosa L. extracts antiradical activity on flavonoids quantitative and qualitative composition of these species has been established.

We characterized polysaccharide complexes from Centaurea scabiosa L. and Centaurea pseudomaculosа Dobrocz. We proposed the technique of sequential selection of water-soluble polysaccharides and pectin substances from the aerial parts of studied objects. We have discovered that the content of water-soluble polysaccharides in the aerial parts of C. scabiosa was 2.8 times higher (2.7 ± 0.3%, n = 3) than in C. pseudomaculosа (0.97 ± 0.50%, n = 3). The content of pectin substances in the aerial parts of C. scabiosa was 2 times higher (7.6 ± 0.4%, n = 3) than in C. pseudomaculosа (3.9 ± 0.3%, n = 3). The residues of D-galacturonic acid, L-rhamnose, D-xylose, D-mannose, D-glucose, and D-galactose are the monomeric units of polysaccharide complexes from C. scabiosa and C. pseudomaculosa. Using ion-exchange chromatography, three polysaccharide fractions (molecular weights 667, 722, and 1027 kDa), whose monomer units are D-galacturonic acid, L-rhamnose, D-galactose, D-xylose, and D-glucose were isolated from the water-soluble polysaccharides of C. scabiosa.

Разработана методика количественного определения содержания цинаропикрина в сухом экстракте василька шероховатого на 40 % этаноле и проведена оценка ее валидности. Методика является специфичной для анализа, обладает корректной точностью и воспроизводимостью результатов, а также линейной зависимостью в аналитической области ± 30 %, и может использоваться для достоверной оценки качества сухого экстракта василька шероховатого.

An HPLC method for quantitative determination of cynaropicrin in Centaurea scabiosa L. dry extract obtained using 40% aqueous ethanol has been developed and its performance has been validated. The proposed method is specific; ensures high accuracy, reproducibility, and linearity in an analytical range of ±30%; and can be used for reliable quality control of C. scabiosa L. dry extract and related preparations.

The quantitative determination of flavonoids in the above-ground part of greater knapweed (Centaurea scabiosa L.) has been carried out by differential spectrophotometry in combination with a modified method of forming flavonoid complexes with aluminium chloride in hydrochloric acid. Depending on the site of plant collection, the quantitative content of flavonoids in the aboveground part of greater knapweed varied within 1.3 - 2.0% (as recalculated for rutin). The random error of measurement did not exceed 3% at а confidence probability of 0.95. The systematical error of the proposed method did not exceed the error of determination. The dynamics of accumulation of flavonoids in above-ground part of greater knapweed during vegetative period in 2006 has been traced for the plants growing in the Tomsk and Kemerovo regions. The maximum content of flavonoids (1.70 ± 0.04% recalculated for rutin) was observed in the stage of full blossom, which is therefore the optimum period for collecting the above-ground part of plants for the maximum yield of flavonoids. The maximum amount of flavonoids was accumulated in leaves (1.96 ± 0.04 %), which is somewhat greater than the content of flavonoids in the entire above-ground part of greater knapweed (1.70 ± 0.04%).

Quantitative determination of flavonoids from the aerial part of greater knapweed ( Centaurea scabiosa L.) has been carried out by differential spectrophotometry in combination with a modified method of forming flavonoid complexes with aluminum chloride in HCl. Depending on the plant collection site, the quantitative content of flavonoids in the aerial part of greater knapweed varied within 1.3 – 2.0% (calculated as rutin). The random error of measurement did not exceed 3% at a confidence probability of 0.95. The systematic error of the proposed metohd did not exceed the error of determination. The accumulation dynamics of flavonoids in the aerial part of greater knapweed during the 2006 vegetative peroid have been tracked for plants growing in Tomsk and Kemerovo regions. The maximum content of flavonoids (1.70 ± 0.04% calculated as rutin) was observed in the stage of full flowering, which is therefore the optimum period for collecting the aerial part of the plants for the maximum yield of flavonoids. The maximum amount of flavonoids was accumulated in leaves (1.96 ± 0.04%), which is somewhat greater than the content of flavonoids in the entire aerial part of greater knapweed (1.70 ± 0.04%).

Previously [1] we described the preparation of crowberry (Empetrum nigrum) extract used in the anticonvulsant phytopreparation empetrin. The crowberry extract was obtained by treating the plant sprouts with boiling chloroform followed by purification of the concentrated infusion with acetone. The results of elemental analyses showed the presence of oxygen-containing compounds and the absence of nitrogen-containing components in empetrin. An analysis of the IR, 1 H and 13 C NMR, and mass spectra of the phytopreparation showed that the extract components include aliphatic higher esters, acids, alcohols, ketones, macrocyclic alkanes, triterpene compounds, and a considerable amount of paraffins [2 – 5]. In order to remove the paraffin fraction and other low-polarity components from the phytopreparation, we used extraction with pentane in a Sohxlet apparatus. Subsequent pharmacological tests using two commonly accepted methods (maximum electroshock and corazole “titration”) showed that the anticonvulsant activity is present in the pentane-insoluble residue. Separation of this residue into components presented a difficult experimental problem. As is known, titanium tetrachloride (TiCl 4 ) is capable of forming complexes with hydrophobic oxygen-containing compounds dissolved in alcohol, water, and water – alcohol mixtures [6, 7]. However, in using complexation for the isolation of high-molecular-weight heteroatomic compounds, it is necessary to take into account the retarding effect of the growing hydrocarbon fragment, which increases the hydrophobic properties and weakens the characteristic properties of a heteroatom in the functional group. In order to overcome the hydrophobicity barrier, we used complexation with titanium tetrachloride in hydrocarbon solvents [8] because molecules of titanium tetrachloride (possessing a zero dipole moment) exhibit unlimited solubility in such solvents. It is especially important that the molecular polarizability of TiCl 4 is comparable with that of hydrocarbons. Titanium tetrachloride exhibits a high donor – acceptor capacity with respect to oxygen-containing ligands, which can be readily recovered from the titanium chloride complexes. Taking into account the hydrophobic character of empetrin components (insoluble in pentane), we studied the possibility of separating the oxygen-containing substances in crowberry extract by the method of fractional complexation with titanium tetrachloride in a hydrocarbon medium.

Four phenolic components are isolated from the CHCl3extract ofEmpetrum nigrumL. Three of them are known from this plant. The fourth (6,8-dimethylpinocembrine) is isolated from crowberry for the first time. The previously proposed structure for 2'-methoxy-4'-hydroxy- α,β-dihydrochalcone is confirmed by x-ray structure analysis