Vol 7, No 5 (2019)


Phenolic compounds of laurus nobilis (review)

Konovalov D.A., Alieva N.M.


One of the most famous plants of the laurel family (Lauraceae) is Laurus nobilis L.The aim of the study was to review scientific information on the study of phenolic compounds of wild-growing and cultivated Laurus nobilis L.Materials and methods. The study was performed using information retrieval (PubMed, ScholarGoogle) and library databases (eLibrary, Cyberleninca), as well as ResearchGate application for semantic search. The research methods are analysis and synthesis of the scientific literature data for the period from 2000 up to the present.Results. The data presented in the review show that leaves, fruits, and shoots of Laurus nobilis L. are valuable sources of phenolic compounds, such as phenolic acids, flavonoids, and proanthocyanidins. The quantitative content of these groups of substances varies depending on the collecting ground, the source of raw materials (cultivated or wild plants), the time (phase) of their harvesting, the method of drying, extraction from raw materials, etc. Phenolic compounds exhibit a pronounced antioxidant and antiradical activity, have an inhibitory effect on NO production, sodium-potassium adenosine triphosphatase, on tumour cell lines (HeLa, MCF7, NCI-H460 and HCT15), and are characterised by an antibacterial action against gram-positive and gram-negative bacteria.Conclusion. The analysis of the available scientific information showed that the phenolic compounds of Laurus nobilis L. are one of the main groups of the active compounds of this plant. The use of this information is essential for the development of new effective medicines based on the raw materials of Laurus nobilis L..
Pharmacy & Pharmacology. 2019;7(5):244-259
pages 244-259 views

Collagenases in medical practice: modern collagenase-based preparations and prospects for their improvement

Mayorova A.V., Sysuev B.B., Ivankova J.O., Hanalieva I.A.


The aim of this study was to assess the coverage of studies of collagenolytic enzymes (collagenases) in the sphere of their use in wounds and scars treatment, the resource of their production and the range of collagenase products to identify the areas for their improvement.Materials and methods. The information from retrieval and library databases (eLIBRARY, PubMed, Scopus, ScholarGoogle, ResearchGate), patent information databases (freepatent.ru, ntpo.com, fips.ru), the State register of medicines (GRLS) and the State register of medical devices, as well as technical information provided by manufacturers of medicines and medical devices, was used in the article.Results. The analysis of the information database has shown that collagenolytic enzymes are effective proteolytic complexes because of their ability to provide the breakdown of collagen, the main component of wounds and scars.Hepatopancreas crustaceans is currently one of the available raw resources of collagenases in Russia. It is noted that proteolytic enzymes from the Paralithodes camtschatica hepatopancreas are characterized by a broad specificity: they are able to hydrolyze both native collagen and other protein substrates. There are data confirming the capability of collagenases to accelerate the process of reparation in addition to wound cleansing from a necrosis. The results of clinical studies of collagenases anti-scar properties, indicate the effectiveness of their use for the skin scar correction. The content analysis has shown that there is a small amount of collagenase-based products in the Russian pharmaceutical market: lyophilized powder for preparation of the injection solution "Collalysin", recommended for scars treatment; a medical dressing "Digestol" with collagenase, recommended for wounds and necrotic lesions treatment; "Fermencol" (gel and powder), the "Karipain plus" gel for scars treatment. Drugs are represented by only powder lyophilisate "Collalysin".Conclusion. The development of gel compositions (Aerosil-based oleogels) and atraumatic dressings with collagenase from Paralithodes camtschatica hepatopancreas as the most affordable raw materials can be considered problem number one of practical pharmacy at present. This provides for the creation of the dosage forms, improved in terms of stability and efficiency, as well as ease of use.
Pharmacy & Pharmacology. 2019;7(5):260-270
pages 260-270 views

Study of distribution of biologically active substances from flowers of helichrysum arenarium between phases of the extraction system

Boyko N.N., Zhilyakova E.T., Malyutina A.Y., Naplekov D.K., Shestopalova N.N., Martceva D.S., Novikov O.O., Pisarev D.I., Mizina P.G.


The aim of this study is to confirm the adequacy of the proposed hypothesis, which explains and quantitatively describes the distribution of biologically active substances (BAS) within the extraction system consisting of Helichrysum arenarium flowers and the solvent using a regressive analysis for the theoretically predicted coordinates.Materials and methods. For this research, milled officinal flowers of Helichrysum arenarium (Helichrysum arenarium L. flores) were used. The analysis of the extractions was carried out by RP HPLC method. Isosalipurposide, salipurposide, and chlorogenic acid of >98.0% purity were used as reference substances. The analytical wavelengths were 370, 290, and 325 nm. Results. The obtained experimental data are well-approximated by regressive linear equations in the theoretically predicted coordinates 1/C=f(V) and ln(b/a)=f(1/T). Wherein, the coefficient of determination of regressive equations was R2>0.998, which indicates functional dependence between the studied parameters and confirms the adequacy of the developed mathematical model. The experimental work identified the necessity of implementation of additional constant values into the mathematical model.Conclusion. A new hypothesis was proposed to explain and quantitatively describe the distribution of BAS in the extraction system of Helichrysum arenarium flowers and 80% ethanol. With this working hypothesis, mathematical models were developed and their adequacy was proved using a regressive analysis in the theoretically predicted coordinates. The results obtained could not deny that a mechanism of BAS distribution between the phases is explained and described by the classic Boltzmann distribution for discrete values of molecular energy (or quantum distribution according to Fermi and Dirac).
Pharmacy & Pharmacology. 2019;7(5):271-278
pages 271-278 views

Morphological, technological and biopharmaceutical studies of alginate-chitosan microcapsules with vinpocetine

Polkovnikova Y.A., Severinova N.A., Koryanova K.N., Tulskaya U.A., Grechkina M.V.


The aim of the investigation is to study morphological, technological and biopharmaceutical properties of alginate-chitosan microcapsules with Vinpocetine.Materials and Methods: Alginate-chitosan microcapsules with different concentrations of sodium alginate (0.5%, 1%, 1.5%, 2%, 2.5% and 3%) and a medium viscosity chitosan solution (0.25-0,5%), as well as microcapsules not treated with a solution of chitosan, were obtained. The surface morphology was studied by methods of atomic-powered microscopy with the use of an NT-MDT Corporation probe scanning microscope (model Solver P47 Pro). To study biopharmaceutical properties of the obtained microcapsules, the "Rotating Basket" apparatus was used.Results: It has been found out that the microcapsules not treated with a chitosan solution, have a smooth, transversely striated surface with large heights and deep cavities. With an increase in the concentration of sodium alginate, the surface becomes smoother, the peaks become larger, higher and wider, the cavities get deeper and more sinuous. The microcapsules treated with a chitosan solution, on the contrary, have a rough surface, low heights and shallow cavities, and with an increase in the concentration of sodium alginate, the surface becomes rougher, the heights are evenly distributed along the microcapsule. The spectrophotometry method was used to determine the efficiency of microencapsulation and the release rate of Vinpocetine from the microcapsules per unit time. When the concentration of a sodium alginate solution is 2.5%, the efficiency of microencapsulation is maximum (86.8%). At this concentration, saturation occurs and with its further increase, the efficiency decreases. The maximum release rate of Vinpocetine from microcapsule samples is observed when the concentration of a sodium alginate solution is 1%: it amounts to 41.17%.Conclusion. The amplitude parameters of the microcapsules surface are different at different concentrations. There is a pattern of alternating signs of asymmetry and excess in the samples with chitosan. With a change in the scale of scanning, the surface characteristics of the microcapsules change. The most distinctive details of the structure are visible at the scale of 2 x 2 pm2. At the concentration of sodium alginate of 2.5%, the efficiency of microencapsulation is maximum (86.8%). Studying the effect of the concentration of a sodium alginate solution on the release rate of Vinpocetine from the microcapsule samples has shown that at the concentration of 1%, the release rate is 41.17%, and at the concentration of 2.5% it is 4.5%. These microcapsules can be used in order to produce capsules with modified release.
Pharmacy & Pharmacology. 2019;7(5):279-290
pages 279-290 views

Correction of psychological and neurological signs of alcohol hangover in rats with acetylcysteine

Kurkin D.V., Morkovin E.I., Osadchenko N.A., Knyshova L.P., Bakulin D.A., Abrosimova E.E., Gorbunova Y.V., Tyurenkov I.N.


The development of medications to treat alcohol hangover is important for a large number of people, especially those, who perform responsible and dangerous types of work. The severity of the hangover syndrome is determined by the toxic effect of acetaldehyde and its metabolic rate, which decreases with the depletion of glutathione, worsening and prolonging the hangover.The aim of the article is to provide an experimental basis for use of acetylcysteine as a precursor of glutathione in treatment of psychological, neurological and cognitive symptoms of ethanol hangover.Materials and methods. The study was performed in male Wistar rats. The ethanol hangover was modeled via an acute ethanol injection (i.p., 3 g/kg). After awakening, the animals were divided into 2 groups, receiving acetylcysteine (p.o., 1 mg/ kg) or saline. The intact group of the animals received saline only. Before and after acetylcysteine or saline administration, the animals were assessed according to Combs and D'Alecy scale. The adhesive test, the open field test, the passive avoidance test and Morris water maze test were also performed twice. The liver glutathione level was assessed in sacrificed animals. Results. The control group animals showed signs of neurological deficits and cognitive impairment, including a decreased locomotion, motor deficits and a memory decline. The rats administered with acetylcysteine after the ethanol intoxication, had a less severe impairment associated with an improved performance in the adhesive test, Morris water maze test and the passive avoidance test, and demonstrated an increased locomotion in the open field test. The liver glutathione content in the animals treated with acetylcysteine, was comparable to the glutathione content in the liver of the animals not exposed to the ethanol intoxication.Conclusion. Against the background of an acute ethanol intoxication, an oral administration of acetylcysteine in the rats, promoted an increase in liver glutathione levels and led to a decrease in severity of neurological and cognitive deficits in the animals.
Pharmacy & Pharmacology. 2019;7(5):291-299
pages 291-299 views

Pharmacology complex compound of pro-gly-pro-leu with heparin: hypoglycemic, fibrinolitic and anticoagulant effects in rats with hyperglycemia

Obergan T.Y., Myasoedov N.F., Grigorjeva M.E., Lyapina L.A., Shubina T.A., Andreeva L.A.


Previously it was shown that the use of regulatory peptides of the glyprolin family helps to normalize the hemostasis system and blood glucose levels in experimental resistant hyperglycemia in rats, similar to type 2 diabetes mellitus in humans. It is also known that the anticoagulant heparin inhibits blood coagulation and exhibits a hypoglycemic effect in the body.The aim of the study is to obtain a complex of the Pro-Gly-Pro-Leu (PGPL) peptide and the unfractionated heparin, to study its effect on glucose and anticoagulant fibrinolytic properties and show its ability to restore the impaired functions of the insular and coagulating blood systems in experimental hyperglycemia in rats.Materials and Methods. Laboratory Wistar male rats, intact and with experimentally induced hyperglycemia, were used in the experiment. A complex compound of PGPL and heparin was created with a component ratio of 1:1 (mol/mol), which was administered intranasally to hyperglycemic rats once a day for 5 days at the dose of 1 mg/kg. Similarly, the constituent parts of the complex were administrated in equivalent amounts. The anticoagulant activity was determined by the test of activated partial thromboplastin time, fibrinolysis parameters - by tests of total, enzymatic and non-enzymatic fibrinolytic activities, as well as the activity of a tissue plasminogen activator. In addition, blood glucose was measured using special test strips. Results. The use of the PGPL-heparin complex in the animals with hyperglycemia led to normalization of blood glucose levels, an increase in the anticoagulant and fibrinolytic background of blood plasma. These effects persisted for 6 days after the cancellation of the peptide-heparin complex administration to rat.Conclusion. In the development of experimental hyperglycemia, the PGPL complex with heparin exhibits a combined hypo-glycemic, anticoagulant and fibrinolytic enzymatic and non-enzymatic nature of the effect. In the future, the studied peptide-heparin complex can be used for the prevention and treatment of type 2 diabetes mellitus, complicated by increased blood coagulation.
Pharmacy & Pharmacology. 2019;7(5):300-307
pages 300-307 views

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