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Vol 22, No 9 (2019)

Articles

Studies relating to the development of a galenical drug with antimicrobial activity from clove buds

Boyko N.N., Pisarev D.I., Zhilyakova E.T., Maljutina A.Y., Novikov O.O., Osolodchenko T.P., Ghazaryan M.S.

Abstract

The article presents the results of studies on the development of a galenical drug with antimicrobial activity from clove buds. For studies, we used grinded clove buds with particles fraction less than 0.5 mm. As an extractant, we used ethanol with different concentration 26, 43, 56, 72, 82, 97±1% v/v. Methods of extraction: simple maceration and filtration extraction. Methods of analyses: RP HPLC and gravimetry. Standard substances were eugenol and gallic acid. Analytical wave lengths were 370, 282, and 270 nm. For the antibacterial study of extracts, we used the agar well diffusion method. In our research, we used six test-strain microorganisms: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 885/653, and Bacillus subtilis ATCC 6633. Ethanol concentration, which extracts most of the substances was found; minimal eugenol concentration in the extract and tincture for their standardizations was suggested; the level of antimicrobial activity of ethanol-water extracts equivalent to a reference drug was determined. It was found that the major yield among the substances determined is observed with an ethanol concentration of 80±5% v/v. It was found that using filtration extraction method for one hour of the extraction process, we could obtain the liquid extract 1:1 m/v with eugenol concentration of 13.8% m/v and its yield 93%. In two and a half hours of the extraction process, we could obtain the tincture 1:5 m/v with eugenol concentration of 3.0% m/v and its yield 100%. RP HPLC method of analysis determined the presence of the following nine main substances: eugenol, acetyl eugenol, gallic acid, three flavonoids, and three non-identified substances in ethanol-water extracts from clove buds. It was suggested to carry out standardization of the resulting galenical drugs by eugenol. For the extract (1:1 m/v), low limit of eugenol concentration 13.0% m/v was suggested, and for the tincture (1:10 m/v), low limit of eugenol concentration 1.3% m/v was suggested. Antimicrobial activity of ethanol-water solutions of the extract (1:1 m/v) was studied; the lowest eugenol concentration of 0.44% m/v in ethanol-water solutions equivalent in terms of its antimicrobial activity to the reference drug 0.05% chlorhexidine digluconate water solution.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):3-11
pages 3-11 views

Analysis of the mechanism of action of the Galega officinalis L

Martinchik I.A., Trumpe T.E., Ferubko E.V.

Abstract

Galega medicinal (Galega officinalis L.) is a perspective medicinal plant of antidiabetic action. Positive influence of a galega on various links of pathological process at a diabetes mellitus is explained by the maintenance of a complex of biologically active agents, one of which is guanidinovy alkaloid galegine (izoamilen-guadin). Galegine can work like guanyl guanidines - group of synthetic glucose-lowering drugs, for example as Metforminum, the patients with a diabetes mellitus who are applied to treatment. The similarity of pharmacological activity of galegine and metformin is caused by proximity of chemical composition and respectively proximity of mechanisms of effect of the specified substances. According to literary data an important target of Metforminum is adenosinemono-phosphate - the activated protein kinase (AMFK) - the key regulator of power metabolism of a cell. Activation of AMFK leads to reduction of endothelial dysfunction, easing of an oxidative stress, improvement of utilization of glucose and increase in biological activity of insulin. Such metabolic activity does this enzyme by one of major factors of protection of a cardiovascular system in the conditions of a diabetes mellitus and can explain various effects of guanyl guanidines. Also the LKB1/AMFK mechanism provides molecular interrelation between a diabetes mellitus and cancer. Metforminum reduces metabolic defect and restored generation of T-memory cells. The mechanism of effect of metformin and a galega medicinal opens a wide range of their pharmacological action.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):12-15
pages 12-15 views

Computational modelling of interaction between isovaltrate and adenosine A1 eceptor

Kurakin G.F., Lopina N.P., Bordina G.E.

Abstract

Isovaltrate, a valepotriate contained in valerian roots, is an inverse agonist of adenosine Ai receptor with micromolar affinity. Here, we present results of molecular modelling of its binding to this receptor by flexible docking with Galaxy7TM web server. We modelled isovaltrate binding to human and rat adenosine A1 receptor. The modelling has shown that isovaltrate mimics xanthine antagonists upon binding to adenosine A1 receptor. It occupies similar position and forms analogous interactions: hydrogen bond with Asn254 and hydrophobic contacts with Phe171, Leu250, Ile274. Despite lacking aromatic structure, bicyclic core formed vast hydrophobic interactions with Phe171 positioning itself similar to xanthine and flavonoid core. Other studied valepotriates, valtrate and deacetylisovaltrate, were unabe to fully mimic there interactions. We proposed that xanthine, flavonoid and isovaltrate binding is provided by common structural features: flat or almost flat bicyclic core, hydrogen bond acceptor attached to it and side chains. Obtained modelling data can be used for designing new adenosine receptor blockers and sedative drugs.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):16-23
pages 16-23 views

The current state and prospects of using proteomics methods in chemical-toxicological analysis (review)

Kutyakov V.A., Kharitonova E.V., Olovyannikova R.Y., Salmina A.B.

Abstract

Purpose. The authors analyzed the current state and the possibility of using proteomic methods during chemical-toxicological studies. The factors that impede the detection, identification and determination of toxicants in complex biological matrices are indicated. At the same time, the peculiarities of modern expert practice, which determine the introduction of high-tech techniques that differ from those currently used, are noted. The possibility of using dysregulation of gene expression as an alternative method of identifying substances that are harmful to health is considered. As a diagnostic method for diseases of chemical etiology (including substance abuse), it is possible to apply the methods of proteomics. The article provides a comparative description of sample preparation methods, analysis, their advantages and possible disadvantages. The conclusion is made about the need to create biobanks of objects that can serve as benchmarks for comparison in subsequent studies. Emphasis is placed on the need to improve computational analysis tools for processing toxicoproteome data, the creation of mathematical models of poisoning, along with the development of analytical methods. Taking into account the peculiarities of the chemical-toxicological analysis, the authors proposed a scheme (methodology) of a proteomic study of a limited list of objects (blood, urine). Conclusion. Based on the analysis of literature data, the authors of the article propose a new promising tool for carrying out chemical-toxicological studies, which has undoubted advantages - personalized analytical toxicology.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):24-29
pages 24-29 views

Evaluation of the effectiveness of virus removal during the purification of immunoglobulin G by chromatography

Zubkova N.V., Kuznetsova M.M., Ivanov A.V., Filatova E.V., Orlova E.V., Nikolaeva A.M., Staroverov S.M., Karasev V.S.

Abstract

Introduction. An innovative manufacturing process was developed to produce the highly purified preparation BioGam® "Human Immunoglobulin Normal, solution for infusion, 50 mg / ml, 100 mg / ml" using a combination of ethanol fractionation and chromatography on ion exchange and hydrophobic resin and an additional virus inactivation steps to achieve a reliable level of preparation safety. Aim. This study aimed to investigate the nucleic acids (NA) clearance efficacy of the hepatitis B (HBV), hepatitis C viruses (HCV) and parvovirus B19 (B19 V) during chromatography process for the isolation and purification of immunoglobulin G from precipitate A (Cohn fraction II + III). Materials and methods. Investigations were performed in model experiments with 3 series of precipitate A (II+III) samples knowingly contaminated with a virus containing material in which NA concentration of HBV virus was (1.77 ± 0.42) · 104 IU / ml, HCV virus was (1.42 ± 0.14) · 103 IU / ml, B19V virus (1.82 ± 0.14) · 105 IU / ml and which were exposed to chromatographic separation on the scale-down model of the manufacturing process. The virus reduction factor was determined by the change in viral load in product fractions before and after the chromatography process. Results. It has been established that the chromatography process demonstrated a reliable and reproducible level of virus nucleic acids reduction including to an undetectable by PCA level providing a reduction factor for HBV (3.61 ± 0.11) lg, for HCV (2.23 + 0.03) lg and for B19V (3.77 ± 0.02) lg. Conclusion. A chromatographic stage in the manufacturing process of preparation BioGam® makes a significant contribution to ensuring its viral safety wherein the removal efficiency of blood-transmissible agents has been confirmed experimentally.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):30-36
pages 30-36 views

The use of medicinal plant raw material waste for the iotechnological obtaining of hydrolytic enzymes

Nikitina Z.K., Gordonova I.K.

Abstract

Currently, the drugs based on medicinal plant materials are widely used for the treatment of many chronic diseases. Modern plant-based drugs, as a rule, combine high efficiency, relative safety and wide therapeutic action. When you receive many galenic and neogalenic herbal drugs in most cases, plant raw materials wastes are generate. They usually contain different biopolymers, including cellulose, which can induce under certain conditions the hydrolase synthesis. The study is devoted to the solution of the actual problem connected with the use of plant raw materials wastes for hydrolytic enzymes biotechnological production. As an example of plant material waste were used two samples of Tanacetum vulgare flowers waste. Previously the authors have shown that micromycetes from the collection of GNU VILAR have the ability to hydrolyze some unsoluble proteins and various types of cellulose. In this regard, the attempt to use these biological objects not only for waste conversion, but also to cellulases obtaining was held. It was shown that all the investigated filamentous fungi grew well on media with replacement of sucrose to the Tanacetum vulgare flowers waste. Micromycetes formed lysis zones in surface cultivation and synthesized cellulases in deep cultivation. Thus, approaches to the use of medicinal plant materials waste for the cellulases production have been developed.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):37-42
pages 37-42 views

Activity of muscle enzymes in the blood bobsleigh athletes

Radzhabkadiev R.M.

Abstract

Purpose of the study: to evaluate some biochemical blood parameters of athletes, mainly training strength endurance. Materials and methods. We examined 40 elite bobsleigh athletes of both sexes (28 men and 12 women) in the pre-competitive period of sports training. The average age of men was 22.1±2.53 years, women - 23.7±3.63 years. In the serum studied biochemical parameters activity of alanine amino - (ALT) and aspartate aminotransferase (AST), creatine phosphokinase (CK), creatine phosphokinase MB (CK-MB). Results. In both gender groups revealed a significant excess of CK activity relative to reference values (on average, 2.9 and 1.9 times, respectively). Creatine kinase activity in men was 44.1% higher than in women (p < 0,05). Also in men, in 47.6% and 23.8% of cases, elevated AST and ALT values were observed, respectively, relative to reference intervals. The muscle damage index (CPK/AST) in 95.2% of cases in men and 75% of cases in women was more than 10, which indicates the presence of damage to muscle cells. Conclusions. The data obtained indicate that high values of metabolic biomarkers are characteristic of bobsleighs. This is probably due to mechanical damage to myocytes during intense physical exertion and the development of the creatine-phosphokinase mechanism of energy supply in athletes of this group.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):43-46
pages 43-46 views

Anti-allergic effect of the new combined nasal spray in experimental allergic rhinitis mode

Pozdnyakova A.E., Khadzieva Z.D., Zagorskaya N.S., Pozdnyakov D.I.

Abstract

The aim of the study: to evaluate the anti-allergic properties of the new combined nasal spray in experiment. Materials and methods: the study was performed on 70 male mice of the BALB/c line, which reproduced ovalbumin-induced allergic rhinitis. The animals were immunized for 14 days, after that they provoked acute rhinitis by intranasal administration of ovalbumin. Further, blood sampling was performed in mice with subsequent serum and determination of the concentration of proallergic markers: histamine, IFN-γ, IL-6, IgE and TNF-α by ELISA. The test-spray in doses of 2.5; 5 and 7.5 p/nostril and the reference drugs levocabastine at a dose of 5 p /nostril and beclomethasone in the dose of 3.5 p /nostril was administred intranasally 30 min before provocation of acute allergic rhinitis. Results: when administered to the animals of the test-spray in doses of 2.5, 5 and 7.5 pg/nostril, a decrease in the severity of the allergic reaction in mice with experimental allergic rhinitis was noted, which may be evidenced by a decrease in serum concentrations of histamine, IFN-γ, IL-6, IgE, and TNF-α. At the same time, against the background of intranasal administration of the test-spray at a dose of 5 pg/nostril, the content of histamine, IFN-γ, IL-6, IgE, and TNF-α in serum decreased by 69.1% ((p<0,05); 38.1% ((p<0,05); 130.8% ((p<0,05); 248.2% ((p<0,05); 53.8% ((p<0,05), respectively, which was comparable to the effect of beclomethasone, and exceeded the therapeutic effect of levocabastine. Conclusions: based on the obtained data, assume the equivalent therapeutic efficacy of the test-spray with intranasal glucocorticoids (beclomethasone), which determines the relevance of further study of this composition.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):47-51
pages 47-51 views

Evaluation of anti-inflammatory and gastroprotective properties of extracts of moldavian dragonhead

Kurmanova E.N., Ferubko E.V., Sheichenko O.P.

Abstract

In VILAR developed Moldavian dragonhead herb extract dry Lyukatil. The study of the effect of the extract Lyukatil on the course of exudative phase of inflammation in mice and the condition of the gastric mucosa of rats in acute experimental ulcers using the ethanol model. It was found that the extract at a dose of 200 mg/kg with a three-day administration has a significant antiinflammatory effect, suppressing the development of the exudative phase of inflammation caused by formalin by 33.7%, compared with the control group of animals. In terms of ethanol, the experimental models of gastric ulcers when administered extract at a dose of 100 mg/kg, significant gastroprotective effect - the reduction in area of ulcers by 23.5%. With an increase in the dose of the extract to 200 mg/kg, the area of ulcerative defects was reduced by 86.16%. The results of these studies, the authors found that Lyukatil is a promising target for further pharmacological examination.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(9):52-55
pages 52-55 views

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