Popova Y. V., Mazulin O. V., Burak V. P., Mazulin G. V., Оstapenko А. О.
Zaporozhye State Medical University
The herb of Cirsium arvense (L.) Scop. is perspective source of modern herbal drugs
The aim of the work was studied the herb of Cirsium arvense (L.) Scop. of Ukrainian flora as perspective source of modern herbal drugs. The flores and leafs of C. arvense (L.) Scop. were standardizated by content of biologically active substances in flowering period. The component composition and quantitative content of flavonoids and hydroxycinnamic acids in genus herbal raw materials of C. arvense (L.) Scop. were studied. A detection оf flavonoids and hydroxycinnamic acids were conducted by chemical reactions and thin layer chromatography on «Aluminium oxide 150 F 254» (0.20 mm) (MERCK, Germany) plates. The quantitative contents of the component composition of flavonoids and hydroxycinnamic acids were conducted by HLPC chromatograph «Shimadzu LC-20 Prominence» (Japan). The chromatographic column «Phenomenex Luna C18(2)» (250 mm × 4.6 mm × 5 μm). The 16 flavonoids and 5 hydroxycinnamic acids by HPTLC were identified. Quantitative content of flavonoids in the flores (up to (3.10 ± 0.29) %), hydroxycinnamic acids (up to (0.21 ± 0.02) %); flavonoids in the leafs (up to (2.59 ± 0.25) %), hydroxycinnamic acids (up to (0.13 ± 0.01) %). Quercetin-3-O-β-D-glucopyranoside, lutelin-5-O-β-D-glucopiranoside, gispidulin-7-O-β-D-glucopyranoside, kampherol-3-O-β-D-glucopyranoside, caftaric, protocatechuic and neochlorogenic acids firstly were identified. Prevailing of contens there were flavonoids derivates of luteolin. The method of C. arvense (L.) Scop. herbal raw materials standardization by content of the main flavonoid luteolin derivatives was proposed. The lyophilized extract of C. arvense (L.) Scop. herbal raw material is non-toxic substance. The herb of C. arvense (L.) Scop. is perspective to obtain a lyophilized extracts with hepatoprotective, antioxidant and anti-inflammatory activities.
Keywords: Cirsium arvense (L.) Scop., flavonoids, hydroxycinnamic acids, HPLC, hepatoprotective activities, antioxidant activities, anti-inflammatory activities.
Odyntsova V. M., Panasenko O. I., Knysh E. G.
Zaporozhye State Medical University
Synthesis, physical-chemical properties, antibacterial and antifungal activity of 2-[(5- (adamantane-1-yl) -4-R-4H-1,2,4-triazoles-3-yl) thio] -N'-R1-atsetohydrazides
The pharmaceutical industry is one of the most, which is dynamically developing despite the difficult conditions today, what greatly contributes to the development of pharmaceutical science. Creation of a native quality drug consists of many stages, one of them is the synthesis of perspective substances. The active pharmacophore is 1,2,4-triazoles system, which became the basis for the synthesis of compounds with different types of activity. The combination of 1,2,4-triazole and adamantane in one molecule creates favorable conditions for the synthesis of new compounds with low toxicity and pronounced pharmacological activity. Perspective in this direction of research is 2-[(5-(adamantane-1-yl)-4-R-4H-1,2,4-triazoles-3-yl)thio]-N’-R1-atsetohydrazides. The aim of this work is the synthesis of 2-[(5-(adamantane-1-yl)-4-R-4H-1,2,4-triazol-3-yl)thio]-N’-R1-acetylhydrazide, studying of their physic-chemical properties, antimicrobial and antifungal activity. The melting temperature indicated by open capillary method on the Opti Melt MPA 100 apparatus. The elementary composition established on the universal analyzer Elementar Vario L cube (CHNS) (sulfanilamide as a standard). The 1H NMR spectra were recorded on a Varian Mercury VX-200 spectrometer (1H, 200 MHz) in a dimethylsulfoxide-d6 (tetramethylsilane as internal standard) and decoded by means of ADVASP(tm) program and Analyzer program (Umatek International Inc.). Chromatography mass spectral researches were performed on the gas-liquid chromatograph Agilent 1260 Infinity HPLC with equipped mass spectrometer Agilent 6120 (ionization in the electro-spray ESI). The identification of antimicrobial and antifungal activity performed by the method of double serial dilutions in liquid nutrient mediums. Synthesized new 2-[(5-(adamantane-1-yl)-4-R-4H-1,2,4-triazoles-3-yl)thio]-N'-R1-atsetohydrazides, the structure of which is established, using modern physical and chemical methods of
analysis (elemental analysis, IR- and NMR 1H-, NMR 13C-spectroscopy), and their personality — using TOP-MS method. Because of research, among the synthesized compounds identified substances, the level of antimicrobial and antifungal action of which is approaching, and in some cases exceeds the comparative drug — trimethoprim. In the future, it is necessary to expand the range of action of the synthesized compounds towards museums and clinical pathogens of infectious diseases and explore their toxicity.
Keywords: 1,2,4-triazoles, atsetohydrazides, IR-, NMR 1H-, NMR 13C-spectroscopy, chromatography mass spectrum, antimicrobial and antifungal activity.
Pruglo Ye. S., Panasenko O. I., Knysh Ye. G.
Zaporizhia State Medical University
Anxiolytic activity of 4-amino-5-methyl-4H-1,2,4-triazole-3-thion N-derivatives and 2-(4-amino-5-methyl-1,2,4-triazole-3-ylthio) acetic acid salts
Anxiety disorders are among the most common mental illness in most populations that lead to disease, make worse functional personality characteristics and comorbidities of chronic diseases. Thus, psychopharmacology’s urgent task is to search for not only effective drugs for the treatment of anxiety disorders or depression but also for drugs that combine efficiency and safety in the treatment of anxiety and depression. To investigate the anxiolytic activity were selected the derivatives of 5-methyl-4-amino-4H-1,2,4-triazole-3-thione. Anxiogenic and anxiolytic activities of the studied compounds in the test were explored by elevated cruciform maze (ECM). The method by S. Pellow is based on giving benefits of ex-perimental animal to dark places, natural fear of open areas and falling from height. ECM was a cruciform platform (10×10×50 cm) which diverges on the right angle from the center for four sleeves. ECM was at the height of 1 m above the floor. The results of experimental studies have shown that in the ECM test after injection of the studied compounds it were not found the substances with anxiolytic effect which would sig-nificantly exceed the activity of reference drug Gidazepam but it was discovered compound with anxiogenic action. Thus we assume that the above compounds can affect 5-НТ2-receptors. It is known that agonists of the 5-НТ2С-receptors cause panic and anxiogenic effects which disrupt sleep. The most active compound can be considered the 2-(4-amino-5-methyl-1,2,4-triazole-3-ylthio) acetic acid which increased animals stay in the illuminated sleeve at 1.44 times (p < 0.05). 29 ФАРМАКОМ 2-2017 The presence of 2-hydroxybenzaldehyde residue by the amino group of N4 nitrogen atom in the molecule of 4-((2-hy-droxybenziliden) amino)-5-methyl-4H-1,2,4-triazole-3-thione shows its anxiolytic properties. Thus by the established patterns between chemical structure and anxiolytic action it may be assumed that purposeful synthesis of 2-(((2 hydroxybenziliden)amino)-5-methyl-1,2,4-triazole-3-ylthio) acetic acid can lead to the creation of anxiolytic drug based on the aforesaid molecule.
Keywords: triazoles, anxiety, anti-anxiety agents, sedatives, rat.
Grechana O. V., Serbin A. G., Buriak V. P.
Zaporozhye State Medical University
National University of Pharmacy
The investigation of acenocoumarol by spectrophotometric мethod
Cardiovascular diseases, namely auricle’s fibrillation, are the most frequent source of a system embolism and a cardioemboly stroke. Among 4-oxybenzopyrone’s derivatives, which are the doctors prescribed to the patient with the specified etiology of heart diseases and cardiovascular system, is rather often recommended an acenocoumarol. This medicine as anticoagulant has an indirect action and reduces risk of a stroke and its consequences approximately on two thirds. In recently years the scientists pay appreciable attention to search of new original domestic drugs which can be applied to prevention of a cardiovascular system’s embolism of the person. Development of new medicines for researching in cardiology for the purpose of decrease of embolic stroke consequences and following treatment of the residual phenomena of this disease is impossible without detailed and careful studying of UF-ranges of derivatives 4-oxybenzopyrones drugs. Nowadays the possibilities of UF-spectrophotometery allow to establish structure of again synthesized bond, dependence between structure and effect of medicines and to identify the part of a molecule which causes its pharmacological action (pharmakophore). We had been studied UF-ranges of an acenocoumarol in ten solvents, which have various polarity (water; 0.1 M NaOH; 0.1 M HCl; acetate buffered solution with рН 3.85; concentrated H2SO4; 95% ethanol; cyclohexane; 25% NaOH; dioxane and chloroform), which helped to establish the nature of absorption bands. Had been discovered the part of a molecule of the studied bond (pharmakophore) which existence cause an pharmacological action. The main optical characteristics of electron’s absorption spectrums of aсenocoumarol allowed to identify the transition of electrons in a molecule of the studied bond, and to study reactionary ability of the main chromophore.
Keywords: 4-oxycoumarin, acenocoumarol, UV spectra, pharmacophore, electron relocation.
Georgievskiy V. P., Zinchenko О. A., Kulikov A. Yu. Litvinenko V. I., Kolisnyk O.V., Popova N. V., Bobritskaya L. A.
State Enterprise «Ukrainian Scientific Pharmacopoeial Center for Quality of Medicines», Ukraine
State Enterprise «State Scientific Center for Drugs and Medical Products», Ukraine
National Technical University «Kharkiv Polytechnic Institute», Ukraine
National University of Pharmacy, Ukraine
To the question about standardization of medicinal plants during phyto-drugs manufacturing. Report 1. Estimation of immortelle flowers according to biologically active compounds content
In the presented manuscript the literature data and authors self-data investigations up to development of the medicinal plants quality parameters and drug based on immortelle inflorescence manufacturing were summarized. The obtained data was confirmed the methodology of the medicinal plant quality control and phyto-drugs based on their biological activity components, that is charged with the therapeutic
activity. The content of chalcon-flavonoid compounds of immortelle, that meets to immortelle choleretic activity, was estimated. The obtained data was confirm to the known results of home and foreign authors. It was demonstrated, that for the identification of immortelle compounds using HPTLC Silica gel F254 plates was acceptable the following mobile phases: chloroform – methanol – water (26:16:3) and isopropanol – chloroform – glacial acetic acid (15:15:0.5). The assay of biological activity compounds of immortelle appropriate leads by using spectrophotometric methods with aluminum chloride at 418 nm detection wavelength; calculation should be passed on the chalcon-glucoside izosalipurposide.
Keywords: herbal drug, Helichrysum arenarium, flavonoids, Flamin, choleretic activity, izosalipurposide, TLC, HPTLC, standartization of herbal drug.
UDC 615.1: 339.13
Оlkhovska А. B.
National University of Pharmacy
Analysis of differences of the «promotion» and «marketing communication» categorical framework of medicinal products and its improvement taking into account the specific character of the industry
In the paper the author according to the results of the content analysis of the works and developments of the foreign and Ukrainian scientists summarized and systematized, based on the certain criteria of classification, the categorical framework of the notions of «promotion» and «marketing communication», emphasized the differences between them, improved and pro- posed according to the personal vision and the newest paradigm for interpreting the notions of «promotion» and «marketing communication» of medicinal products taking into account the specific nature of the industry and modern trends of the development of the information and communication space of society. The differences between the notions of «promotion» and «marketing communication» of medicinal products were explained. Thus, the medicines promotion is a common notion, that provides for physical flow of pharmaceutical product in the market in the manufacturer-consumer chain using all element of the marketing complex, including marketing communication. Marketing communication is focused on the multiple communication-information relations of pharmaceu-
tical manufacturer with all participants of the market. Thus, marketing communication is used by the participants of the pharmaceutical sector while conducting marketing research, during the process of development and introduction of new medicinal products, delivery of goods, the study of feasibility of entrance to certain markets and segments, formation of the organization corporate identity, partnering between the en-
terprise and public. A general characteristic, uniting these two notions, is communication with targeted audiences.
Keywords: promotion, marketing communications, medicinal products.