Vol 6, No 2 (2018)
- Year: 2018
- Articles: 7
- URL: https://journals.eco-vector.com/2307-9266/issue/view/5630
Articles
ACTUAL PROBLEMS OF RAW MATERIALS CHEMICAL STANDARDIZATION OF MEDICINAL PLANTS OF THE GENUS HAWTHORN ΈCRATAEGUS L.Ή
Abstract
The plants of the genus Hawthorn (Crataegus L.) are shrubs or small trees that have been used in medicine since ancient times. Nowadays, on the basis of raw hawthorn, the preparations are available for treatment and prevention of heart failure. The aim of the work is to analyze and systematize research results in the fi eld of chemical standardization of hawthorn raw materials in pharmacopoeias of various countries. Materials and methods. The study was conducted with the use of the State Pharmacopoeia of the USSR, XI-th edition, the State Pharmacopoeia of the Russian Federation, XIII-th edition, the European Pharmacopoeia, 6-th edition, the United States Pharmacopeia, 32-nd editions, the State Pharmacopoeia of the Republic of Belarus and the Republic of Kazakhstan, as well as the information and search (PubMed) and library databases (eLibrary). Results and discussion. In this review, the results of research in the fi eld of chemical standardization of hawthorn raw materials in pharmacopoeias of various countries are systematized. It is determined that in the methods of analysis of raw materials of the species of the genus Hawthorn (Crataegus L.), included in domestic and foreign Pharmacopoeias, various methodological and methodological approaches to the standardization of fruits, fl owers and leaves are used. Besides, it has been found out that the raw materials of the same name are analyzed using different techniques. In our opinion, the use of various extractants in the methods is not always justifi ed from the point of view of the physical-chemical and spectral characteristics of the substances being analyzed. It is also shown that in the methods of qualitative and quantitative analysis of active substances (fl avonoids, procyanidins), the orientation to diagnostically signifi cant standard substances is not always conducted. Conclusion. The analysis of existing methods of qualitative analysis (the section of authenticity) and quantitative determination of the target substances indicates the necessity to unify the methods of raw materials analysis and preparations of hawthorn species on the basis of scientifi cally based approaches to standardization.
Pharmacy & Pharmacology. 2018;6(2):104-120
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PHENOLIC COMPOUNDS AND PECTIC SUBSTANCES OF EUROPEAN GOOSEBERRY LEAVES ΈGROSSULARIA RECLINATA ΈL.Ή MILL.Ή
Abstract
In the leaves of European gooseberry 23 compounds have been found, and only 13 of them have been identified by the presence of standards. One of the indicators of the bioavailability of drugs is the distribution coefficient of the substances under investigation between the hydrophilic and lipophilic phases, as well as in various biological fluids. Pectic substances have a preventive effect: anti-inflammatory, antibacterial, anti-sclerotic, anti-allergic. The aim of the work is: isolation, identification of phenolic compounds, investigation of the distribution coefficient and the antidislipidemic activity of the pectic substances in European gooseberry leaves (Grossularia reclinata (L.) Mill.). Materials and methods. Degreased raw materials (leaves of European gooseberry) were extracted three times with 40% ethanol by heating for 60 minutes. In the separatory funnel the combined extracts were subsequently treated with chloroform, diethyl ether, ethyl acetate and n-butanol. Isolation of pectin substances from the leaves of European gooseberry was carried out according to N.K. Kochetkov and M. Sinner’s method. When determining the distribution coefficient from organic solvents, diethyl ether and n-octanol, in which the objects under study are readily soluble, have been used. The procedures of the solutions input of the investigated pectic substances and cholesterol solution were separated by a 2-hour interval. After 14 days, venous blood was collected from the animals, followed by the production of serum and determination of the parameters characterizing the state of the lipid-cholesterol blood profile. Results and discussion. As a result of the study of phenolic compounds of European gooseberry leaves, hyperoside, rutin, caffeic acid have been separated for the first time. The data obtained show that for aqueous solutions of pectic substances of European gooseberry, the best distribution from the aqueous layer to the organic layer occurs in n-octanol. When using the pectic substances obtained from European gooseberry leaves, the normalization of the lipid-cholesterol profile in blood was observed in rats in comparison with the animals of the negative control group. Conclusion. By the method of preparative column chromatography, quercetin, hyperoside, rutin, kaempferol, astragaline, and caffeic acid were detected in European gooseberry leaves. It can be assumed that the pectic substances from gooseberry leaves will be better distributed and absorbed in the alkaline environment of intestinal contents. The use of the studied pectic substances from gooseberry leaves promoted the correction of dyslipidemia.
Pharmacy & Pharmacology. 2018;6(2):121-134
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STUDY OF THE COMPONENT COMPOSITION OF POLYPHENOLES OF THE KURIL TEA PLANT ΈPENTAPHYLLOIDES FRUTICOSA L.Ή
Abstract
Kuril tea is a popular plant of traditional medicine of China and Mongolia. The available scientifi c evidence indicates the presence of the plant expressed antioxidant properties, conjugated with the presence of polyphenols. The plant has also a number of other pharmacological effects, in particular antibacterial, fungicidal, hypoglycemic, anti-infl ammatory and antiulcer. However, the content of polyphenols in the plant varies greatly depending on the geological growing region, which affects its therapeutic activity. Therefore, the aim of this research was to study the qualitative composition of polyphenols in P. fruticosa L. for further standardization of its raw materials. Materials and methods. As a research object, a sample of P. fruticosa L. herb collected in the Altai Territory was taken. The analysis was carried out using high-performance liquid chromatography in the reversed-phase version. Results and discussion. The chemical composition of the plant is has been established. It includes 18 compounds of polyphenolic nature, represented by glycosides and aglyconsflavonols, proanthocyanidins, oxycinnamic acids, ellagatannins. By the method of internal normalization, the relative content of each component in the sum is has been calculated. As a result, glycosides of quercetin have been found to prevail. After acid hydrolysis the composition of aglyconflavonols was determined. It included quercetin, kaempferol and ramnetin, with predominance of quercetin. One of the components of acid hydrolysis was cyanidine, which is a strong proof of the presence of proanthocyanidins in the plant. A fairly high content of proanthocyanidins amounting to about 24% of the total amount of polyphenols is typical of it. Conclusion. The obtained results make it possible to assert that standardization of the investigated object can be carried out in terms of quercetin as the dominant component of the sum of polyphenols after preliminary hydrolysis.
Pharmacy & Pharmacology. 2018;6(2):135-150
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DEVELOPMENT AND OPTIMIZATION OF ULTRASOUND EXTRACTION OF CHAMOMILE FLOWERS CHAMOMILLAE RECUTITA FLORES
Abstract
The article deals with the development of ultrasound extraction technology of chamomile flowers. The aim of this work is working out and optimization of ultrasound extraction technology of the sum of flavonoids from chamomile flowers with further determination of the essential oil content in the extraction obtained. Materials and methods. The object of the research is the medicinal plant raw material (MRPM) of chamomile flowers (Chamomillae recutita ores) bought in a pharmacy. The extraction method is a two-level maceration with ultrasound procession of (MRPM). The extraction was performed in the ultrasound bath “Sapphire” of Technical and Commercial Center (TCC) (RMD) of 9.5 l. For the technological process optimal parameters determination of the sum of flavonoid extraction, the orthogonal factorial plan of Type 32 was built. Results and discussion. The following factors’ influence on the extraction process of the sum of chamomile flowers flavonoids have been studied: the size of particles of (MRPM), the quantity of extraction steps, ethanol content in alcohol-water mixture, ratio (MRPM) /extragent, extraction time, media temperature. The regression equations describing the process of ultrasound extraction of chamomile flowers flavonoids at the first and second steps of maceration have been obtained. The following parameters of the technological process of chamomile flowers sum of flavonoids ultrasound extraction have been worked out: for the first step the extraction time was 22 min., the content of ethanol in alcoholwater mixture was 52% at the ratio MRPM/extragent 1:7 and the room temperature; for the second step: the extraction time was 27 min., the media temperature was 61°C at the ratio MRPM/extragent 1:5 (52% ethanol was used as an extragent). The general yield of the flavonoids sum was 97% and that of the essential oil was 81%. Thus, the ultrasound extraction technology of the sum of chamomile flowers flavonoids has been developed and optimized, allowing to obtain extracts with a high yield of the essential oil.
Pharmacy & Pharmacology. 2018;6(2):151-166
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CEREBROPROTECTIVE ACTIVITY OF NEW DERIVATIVES OF PIRIMIDINE4 1H ONE PIR9 AND PIR10 IN IRREVERSIBLE OCCLUSION OF THE COMMON CAROTID ARTERY
Abstract
The frequency of cerebral hemodynamics disorders remains one of the most relevant problems in the modern world. Disorders of brain blood supply lead to high disability of the population, director disability, as well as fatal outcomes. There is an extensive group of drugs that contribute to the treatment and prevention of cerebrovascular disorders, however, they do not fully meet the requirements of practitioners. In this regard, the task of purposeful search and study of new substances with anti-ischemic activity becomes a task of experimental pharmacology. The aim of this work is to study the cerebroprotective activity of the new derivatives of Pirimidine-4-(1H)-OHA PIR-9 and PIR-10 in irreversible occlusion of the common carotid artery. Materials and methods. The study was carried out on 120 male rats of the Wistar line, weighing 200-220 g, divided into 6 equal groups. The investigated substances - PIR-9 and PIR-10 (50 mg / kg), vinpocetine (3.2 mg / kg), cinnarizine (5.6 mg / kg), a suspension of puri ed water with Tween-80 – were injected intraperitoneally for 10 days , as well as an hour before the operation. Global cerebral ischemia was modeled under chloral hydrate anesthesia (350 mg / kg) by dressing the common carotid arteries. 24 hours after the ischemia model, the survival, behavioral activity, cognitive and mnestic functions as well as certain metabolic disorders were evaluated. Results and discussion. In the experimental study of cerebroprotective action of the compounds PIR-9 and PIR-10 (derivatives of pyrimidine-4-(1H)-OHA) a decrease in neurological, locomotor, tentative research, cognitive, mental disorders in the background of ligation of common carotid artery was established. In addition, after preventive administration of the studied substances PIR-9 and PIR-10, there was an improvement in the processes of energy metabolism in the postischemic period. Conclusion. As for the cerebroprotective activity, the experimental substances (PIR-and PIR 9-10) were superior to the reference preparation of Vinpocetine and were comparable with Cinnarizine. That proves the feasibility of further study of derivatives of pyrimidine-4(1H)-ONA as potential anti-ischemic agents.
Pharmacy & Pharmacology. 2018;6(2):167-181
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EFFECT OF ROSUVASTATIN ON CAROTID INTIMAMEDIA THICKNESS IN PATIENTS WITH CORONARY ARTERY DISEASE OF DIFFERENT GENDER AND CARDIOVASCULAR RISK PROFILE
Abstract
Secondary prevention in patients with coronary artery disease (CAD) is provided by the use of statins, as well as by the impact on modiable risk factors. Rosuvastatin causes the regression of intima-media thickness (IMT) of common carotid artery (CCA), which is signicantly associated with CAD. The aim of the study was to evaluate the change in carotid intima-media thickness (CIMT) in patients with CAD of different gender, and having different number of cardiovascular risk factors, provided that patients attain target levels of total cholesterol (TC<4.0 mmol/l) and low density lipoprotein-cholesterol (LDL-C><1.8 mmol/l). Materials and methods. 72 patients with CAD: Stable angina of functional Classes II–III were recruited. They were treated with rosuvastatin, with gradual increase of its dose from 5 to 40 mg daily to attain target levels of TC and LDL-C. Maximum CIMT was assessed at the time of inclusion into the study and after 12 months of therapy. Results and discussion. In conditions of attaining target TC and LDL-C levels, maximum CIMT signi cantly decreased both in men (p=0,006) and in women (p=0,002), the latter had lower CIMT (p=0,03) than men after 1 year of therapy, taking into account no difference in baseline values. The patients who had 2 or fewer risk factors (RF) (hypertension, a family history of cardiovascular disease, smoking, obesity, diabetes mellitus were taken into consideration) showed decrease in CIMT (p=0.0001), and those who were characterized by 3 or more RF, showed only lack of its growth (p=0.07). Attained lipid levels in the compared groups of different gender and number of RF did not differ. Conclusion. The study revealed the differences in the change of CIMT in patients with CAD of different sex, and of different number of cardiovascular risk factors. Keywords: coronary artery disease, rosuvastatin, carotid intima-media thickness, gender, cardiovascular risk factor ><4.0 mmol/l) and low density lipoprotein-cholesterol (LDL-C<1.8 mmol/l). Materials and methods. 72 patients with CAD: Stable angina of functional Classes II–III were recruited. They were treated with rosuvastatin, with gradual increase of its dose from 5 to 40 mg daily to attain target levels of TC and LDL-C. Maximum CIMT was assessed at the time of inclusion into the study and after 12 months of therapy. Results and discussion. In conditions of attaining target TC and LDL-C levels, maximum CIMT signicantly decreased both in men (p=0,006) and in women (p=0,002), the latter had lower CIMT (p=0,03) than men after 1 year of therapy, taking into account no difference in baseline values. The patients who had 2 or fewer risk factors (RF) (hypertension, a family history of cardiovascular disease, smoking, obesity, diabetes mellitus were taken into consideration) showed decrease in CIMT (p=0.0001), and those who were characterized by 3 or more RF, showed only lack of its growth (p=0.07). Attained lipid levels in the compared groups of different gender and number of RF did not differ. Conclusion. The study revealed the differences in the change of CIMT in patients with CAD of different sex, and of different number of cardiovascular risk factors.
Pharmacy & Pharmacology. 2018;6(2):182-196
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SELECTION OF FILMPROOFERS IN MICROCAPSULATION OF VINPOCETIN
Abstract
Introduction. The scientific and practical interest in the problem of microencapsulation remains high, as evidenced by the extensive literature on this subject. The choice of a film former as a carrier of the active substance in microencapsulation is determined by its required release rate of the latter, which depends largely on the physical properties of the latter. Biodegradable polymers, sodium alginate and gelatin, are often used as a coating. The aim of the research is a comparative analysis of the thermodynamic characteristics of the release of vinpocetine from microcapsules containing gelatin, sodium alginate as a shell, into water and ethanol. Materials and methods. For calculating the thermodynamic characteristics of the release of vinpocetine from polymers, the conformation of the “polymer-vinpocetine” system after thermodynamic equilibration by the molecular dynamics method in the Bioevrica program was the initial state. Results and discussion. The release of vinpocetine from sodium alginate to water with pH = 2 is an energetically beneficial process, and is accompanied by an increase in entropy, which indicates a higher thermodynamic probability of the final state (vinpocetine in solution). The release of vinpocetine from gelatin into water at pH = 2 is an energetically favorable process, as well as accompanied by an increase in entropy, which indicates a higher thermodynamic probability of the final state (vinpocetine in solution). The release of vinpocetine from sodium alginate to ethanol is energetically less favorable than its release to water. The release of vinpocetine from gelatin to ethanol is energetically less favorable than its release into water. Conclusion. A comparative analysis of the results of the quantum-chemical calculation of the thermodynamic characteristics of the release of vinpocetine from sodium alginate and gelatin makes it possible to conclude that vinpocetine has more affinity for sodium alginate in various environments. As a consequence, there may be a higher degree of vinpocetine release into a solution of HCl 0.01 M and an ethanol from gelatin compared to sodium alginate.
Pharmacy & Pharmacology. 2018;6(2):197-210
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