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Vol 25, No 10 (2022)

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Restricted Access Access granted
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Articles

Comparative study of Vitexagnus-castus fruits and vitex negundo fruits

Adamov G.V., Saybel O.L., Konyaeva E.A., Lupanova I.A., Tsitsilin A.N.

Abstract

The purpose of the work is to identify differences in the morphological and anatomical structure, chemical composition and biological activity of the fruits of VA and VN to justify the rationing of impurities and harmonize the quality requirements for VA fruits with foreign pharmacopoeias. Material and methods. The objects of the study were the fruits of the VA harvested in the Republic of Crimea and the fruits of the VN, collected in the Krasnodar Territory in 2019. To develop a method for identifying the admixture of the fruits of the VN in the fruits of the VA, their microscopic analysis, phytochemical study and assessment of biological activity were carried out. To identify differences in the anatomical structure, the outer epidermis of the calyx of the fetus and crushed micropreparations of the fetus were studied, microphotographs were taken. As diagnostic features, the presence of drusen and calcium oxalate crystals in the parenchyma of the fruits of the VN, a different structure of simple and glandular hairs are indicated. Phytochemical study was carried out using the method of high performance liquid chromatography with ultraviolet detection. Results. Under these conditions, in addition to the casticin used in the European Pharmacopoeia 8.0, two more marker compounds were identified. To substantiate the inadmissibility of the fruits of the VN in the fruits of the VA, a screening study of biological activity in vitro in relation to the activation of dopamine receptors was carried out. Conclusions. VN does not show targeted pharmacological properties and cannot be used as a medicinal plant material along with VA.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):3-11
pages 3-11 views

Component analysis of the essential oil of the above ground part of Dracocephalum botryoides Steven

Vagabova F.A., Aliev A.M.

Abstract

The purpose of the study was to study the component composition of the essential oil of the aerial part of Dracocephalum botryoides Steven by chromatography-mass spectrometry to evaluate its use as a promising medicinal raw material. Material and methods. The raw materials for the study were collected in August 2013 during the flowering phase in the Dagestan natural population at an altitude of 2615 m above sea level (Dagestan, Russia). The yellow essential oil (0.31% of the air-dry flow) is obtained by hydrodistillation on a Clevenger apparatus for 4 hours. Results. In the course of the analyzes carried out on the method of chromato-mass spectrometry, 41 components were identified, of which 16 components (α-thuyene, thuya-2,4(10)-diene, sabinene, α-terpinene, p-cymene, γ-terpinene, β -thujone, linalool, α-muurolol, β-elemen, caryophyllene oxide, terpinen-4-ol, γ-elemen, trans-caryophyllene, β-elemenone, γ-muurolen) are the main compounds of D. botryoides essential oil. Three monoterpenes (α-thuyene, sabinene and p-cymene) occur in the maximum amount, which is 48.1% of the total amount of all identified components. Conclusions. For the first time, data are presented on the study of the composition of the essential oil of the aerial part of D. botryoides. Comparison of the results of the component composition of the essential oil of the studied sample with other species of the genus Dracocephalum revealed both similarity and difference in the composition of essential oils. The results obtained make it possible to characterize the essential oil of D. botryoides as a source of valuable components known for their biological activity, which is of great interest for further research

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):12-19
pages 12-19 views

Study of poloxamer 188 and polyethylene glycols influence on in situ systems thermoreversible properties

Bakhrushina E.O., Pomyutkina M.V., Popova A.A., Khodenok A.I., Demina N.B.

Abstract

Relevance. Poloxamers are the most promising polymers in modern pharmaceutical development due to their ability to make a sol-gel phase transition under physiological conditions and provide a sustained release, so these polymers are ideal for creating thermoreversible in situ drug delivery systems. Complexes with other polymers are created to give optimal characteristics to such systems. Aim. Study of poloxamer 188 and polyethylene glycols influence on in situ systems thermoreversible properties (gelation temperature, viscosity). Material and methods. Commercial samples of poloxamer 407, poloxamer 188 and polyethylene glycols from BASF company were used. Experimental compositions were obtained by dispersing the components in purified water on IKA C-mag HS 7 digital magnetic stirrer (IKA, Germany) and subsequent gel structuring in a refrigerator. The gelation temperature was measured once a week for 12 months, from the moment the sample in a polymer container removed from the storage place, settled and then was immersed in the ODA-LQ40 ultrasonic bath (ODA, Russia) in the heating mode. As an indicator of the gelation temperature, the values determined with an increase of sample dynamic viscosity in the process of mixing using a measuring thermal probe were taken. The stability of the indicator was described using statistical analysis. For the most stable compositions with optimal temperatures rheological properties were studied on a coaxial rotational viscometer Lamy Rheology RM 220 (Lamy, France). Results. In long-term tests, a direct dependence of the average gelation temperature on the concentration of poloxamer 188 was revealed. It was shown the addition of polyethylene glycol 1500 not only increase the gelation temperature, but also positively affects its stability. Also, rheological characteristics were studied. Conclusions. The effect of poloxamer 188 and polyethylene glycol 1500 on the gelation temperature and its stability during long-term storage, as well as the promise of these polymers for the pharmaceutical development of in situ thermoreversible systems, was shown in our study.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):20-25
pages 20-25 views

Identification of 4F-MDMB-BINACA metabolites in human blood and urine with LC-QTOF

Gofenberg M.A., Shevyrin V.A., Dvorskaya O.N., Kataev S.S., Grigoryev A.M.

Abstract

Relevance. Synthetic cannabinoid receptor agonists are ones of leading psychoactive substances, newly identified both in Russia and in the world. Their use is common cause of acute poisoning, sometimes fatal. As is known, synthetic cannabimimetics are intensively metabolized in human body and almost not excreted in the urine unchanged, that creates difficulties in detecting cannabinoid receptor agonists in biological material and hinders correct clinical diagnosis making. It is necessary for establishing the causes of psychoactive substances poisoning in a timely manner to explore metabolic pathways of new synthetic cannabimimetics. Aim of the work. The aim of the work is to detect of 4F-MDMB-BINACA I and II metabolite phases analysing a large number of human urine samples of the use of liquid chromatography in combination with time of flight mass spectrometry. Material and methods. We used 25 urine samples, 2 heparinized blood samples of living persons and 2 post-mortem urine samples to search for metabolites and their glucuronides 4F-MDMB-BINACA. Also we used 1290 Infinity II LC System with Zorbax Eclipse Plus C18 column for liquid chromatography and quadrupole time of flight LC/MS Agilent 6545 (Agilent Technologies, USA). Results. There were 49 4F-MDMB-BINACA metabolites found in human urine samples. These substances were presumably identified as hydrolyzates and hydroxylates of different fragments, defluorination with hydroxylation or carboxylation products, dihydrodiol formation derivates, N-dealkylation products and results of these reactions combination. Also were detected products of tert-leucine residue dehydrogenation, characteristics of which involve intramolecular cyclization with lactone formation. Main metabolic pathways were hydrolysis and defluorination, accompanied by carboxylation. Most metabolites were present in urine in free form as well as glucuronated. We have made recommendations on how metabolites and markers of new cannabimimetic could be detected using urine hydrolysis with or without sample preparation. Conclusion. Findnings of this research can be used for 4F-MDMB-BINACA acute poisoning diagnosis and to predict metabolic pathways of new synthetic cannabimimetics having similar structural elements.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):26-37
pages 26-37 views

Gamma-lactones effects on growth and chemical communication in Chromobacterium subtsugae

Inchagova K.S., Duskaev G.K., Deryabin D.G.

Abstract

Relevance. Currently, the search for natural compounds that inhibit density-dependent chemical communication in pathogenic bacteria is the most promising strategy for alternative antimicrobial chemotherapy. Goal of the study. Screening of chemically synthesized plant-derived gamma-lactone analogs for effects on growth and N-hexanoyl-L-homoserine lactone (C6-AHL) mediated chemical communication in a Chromobacterium subtsugae model. Material and methods. Five gamma-lactones containing a common five-membered oxolane ring and a linear alkyl radical of 2, 3, 4, 5, or 8 carbon atoms were included in the study. Genetically related strains of wild-type C. subtsugae ATCC 31532 and C6-AHL-deficient mutant C. subtsugae NCTC 13274 were model objects. The criteria for the gamma-lactones bioactivity were 50% suppression of bacterial growth and 50% inhibition of C6-AHL-dependent pigment violacein biosynthesis, respectively. Results. The inhibitory effect of gamma-lactones on chemical communication in bacteria was shown in the range from 1.04 mg/ml to 0.02 mg/ml against C. subtsugae ATCC 31532 and from 0.35 mg/ml to 0.02 mg /ml against C. subtsugae NCTC 13274, while the growth suppression required significantly higher concentrations. The intensity of these effects were directly proportional to the alkyl radical length in the screened molecules, increasing from short chain gamma-caprolactone to long chain gamma-dodecalactone. Conclusions. The nature of the anti-infective activity of medicinal plants containing gamma-lactones compounds is hypothesized. This point of view provides a perspective for an in-depth analysis of the gamma-lactone bioactivity mechanism, suggesting their interference with structurally similar AHLs in density-dependent chemical communication systems of bacteria.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):38-43
pages 38-43 views

The use of regulatory peptides in neurological and dental patients

Boldyreva Y.V., Lebedev I.A., Bragin A.V., Gadjiumarova E.A.

Abstract

Currently, new molecules of short peptides are being actively studied and created. These substances are able to influence the processes of protein biosynthesis in the body, which normalizes the work of an organ whose function is impaired. Oligopeptides are widely used in medicine as both preventive and therapeutic agents, complementing traditional treatment regimens for various diseases. Objective - to study the literature data on the use of regulatory peptides in neurological and dental patients. Short peptide molecules have great clinical applications. One of the relevant sections of medicine where the widespread use of this class of substances is possible is gerontology. As the body undergoes age-related changes, there is a decrease in the formation of protein molecules, namely, regulatory peptides. This is due to the fact that the function of the main organs and systems that ensure the vital activity of the body is fading. As a result of improving the processes of protein synthesis, there is an improvement in the processes of regulation and exchange of information molecules. This, in turn, contributes to the improvement of the immune, endocrine and many other systems that increase the adaptation of the body to changing factors of the external and internal environment.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):44-49
pages 44-49 views

Biochemical and spectral analysis of the impact of office teeth whitening on the organic composition of oral fluid

Ryskina E.A., Magsumova O.A., Postnikov M.A., Chigarina S.E., Simanovskaya O.E., Korchagina M.S., Polkanova V.A.

Abstract

Relevance. When studying the process of absorption of inorganic and organic substances by enamel and increasing their concentration, the question inevitably arises of the role of oral fluid - the environment in which the tooth is constantly located, since substances can enter the enamel only in an ionized form, i.e. after dissolution in a liquid medium. Studies of the composition of the oral fluid make it possible to detect changes occurring in the enamel and directly in the oral cavity, because it is a medium for the accumulation of organic components and mineralization of hard dental tissues. The aim of the work is to evaluate changes in the organic composition of oral fluid after office teeth whitening. Material and methods. The study involved 81 patients aged 22 to 35 years and used 2 systems for the office teeth whitening procedure: chemical teeth whitening and modified office teeth whitening. To analyze the effect of the office bleaching procedure on the organic composition of the oral fluid, Raman spectroscopy and biochemical analysis of changes in the concentration of total protein and urea were used. All oral fluid samples were divided into 4 groups: group 1 - oral fluid before the teeth whitening procedure, group 2 -after the teeth whitening procedure, group 3 - 2 weeks after the teeth whitening procedure, group 4 - 1 month after the teeth whitening procedure. Results. The main changes in the spectrum after bleaching are observed on the lines 1745 cm-1 (phospholipids), 1426 cm-1 (CH2scissoringvibration (lipidband)), 1570 cm-1 (Amid II), 876 cm-1 (n(C-C), hydroxyproline (protein assignment)). After the office teeth whitening procedure, there is a tendency to a decrease in the lipid composition of the oral fluid, which is probably associated with an increase in the activity of the antioxidant system of the oral cavity, and, as a result, the activation of lipid peroxidation processes and the development of oxidative stress, as well as an increase in the concentration of total protein and urea.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):50-55
pages 50-55 views

A retrospective analysis of the experimental and clinical study of pasenin, a drug for the treatment of dyslipidemia in patients with diabetes mellitus

Karabayeva V.V., Krepkova L.V., Lupanova I.A., Babenko A.N., Mizina P.G.

Abstract

Relevance. The currently used hypolipidemic drugs to reduce the risk of cardiovascular complications in patients with diabetes mellitus are quite effective, but when prescribed for a long time can cause undesirable side effects. The use of herbal medicines for dyslipidaemia also has a positive experience with safe and effective use. One of the perspective plants showing hypolipidemic and hypoglycemic activity is Trigonella foenum-graecum from which seeds the medicine «Pasenin» was created. Purpose. To carry out the retrospective analysis of experimental and clinical researches of pasenin as dyslipidemic medicine for diabetes mellitus. Material and methods. Preclinical studies were carried out in rats using models of hyperlipidemia induced by administration of 10% fructose solution and by feeding an atherogenic diet as well as in the cholesterol atherosclerosis model in rabbits by Anichkov. Blood levels of glucose, total cholesterol (TC), low and high density lipoprotein cholesterol (LDL and HDL), triglycerides (TG) and phospholipids were determined to assess hyperlipidemia. Clinical studies were conducted at the Department of Internal Medicine, Sechenov University, involving 106 patients with type I and type II diabetes mellitus. «Pasenin» was given to patients against the background of basic hypoglycemic therapy Patients in the control group received placebo according to a similar treatment. The research included an interview, anthropometric, objective and laboratory examination data, blood coagulation and fibrinolysis parameters. All patients underwent light capillaroscopy of the nail bed. The hypocoagulatory effect was calculated from the graph obtained with the help of an electrocoagulograph. Results. Experimental and clinical studies have confirmed hypolipidemic and hypoglycemic action of passenin. Administration of pasenin in patients with diabetes mellitus led to a decrease in atherogenic fractions: TG, total lipids, LDL with moderate lipid metabolism abnormalities. The drug showed the greatest therapeutic effect in patients with diabetes mellitus type I and II in the compensation stage of the disease. Long-term (16 weeks) administration of «Pasenin» increased a blood clotting time, activated fibrinolysis and improved a microcirculatory blood flow. Conclusions. «Pasenin» can be the drug of choice in therapy of dyslipidemia in patients with diabetes mellitus, including with signs of diabetic angiopathy.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):56-63
pages 56-63 views

Ivan Vasil'evich Savchenko (k 80-letiyu so dnya rozhdeniya)

Editorial B.
Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):64-64
pages 64-64 views

Praskov'ya Georgievna Mizina (k 70-letiyu so dnya rozhdeniya)

Editorial B.
Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(10):65-66
pages 65-66 views

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