Ministry of Education and Science of Ukraine Crimean Scientific Center of the National Academy of Sciences of Ukraine and the Ministry of. Academician of NAS of Ukraine M.O.Lozinsky Academician of NAS of Ukraine M.F.Shuba Corresponding member of NAS of Ukraine V.P.Chernykh. Doctor of Science A.M.Bugara Doctor of Science A.E.Zemlyakov Candidate of Science V.I.Grishkovets Candidate of Science V.O.Kurjanov Candidate of Science V.I.Nazarenko Candidate of Science Z.S.Protasova Candidate of Science I.N.Yurkova
It is assumed that these substances are agonists of the 1,4-benzdiazepine and antagonists of cholecystokinin CCK2 receptors as well.
THIAZOLIUM CHLORIDES
Binding of fibrinogen to activated glycoprotein IIb/IIIa (GP IIb/IIIa) on the surface of activated platelets is the final step in the platelet aggregation cascade. RGD (Arg-Gly-Asp) sequence, a fragment of fibrinogen molecule, is responsible for the binding of fibrinogen to its receptor GP IIb/IIIa. Accordingly, RGD analogs that can bind to GP IIb/IIIa receptors may act as fibrinogen antagonists.
We synthesized a series of RGD mimetics (I) based on 4-oxo-4-(piperazin-1-yl) butyric acid (as an Arg mimetic) and β-aryl-β-alanines (as an Asp-Phe mimetic).
КОНДЕНСАЦИЯ 2-ЦИАНМЕТИЛБЕНЗОЙНОЙ КИСЛОТЫ С ВТОРИЧНЫМИ АМИНАМИ КАК МЕТОД СИНТЕЗА
Thiosulfonates have a wide spectrum of antibacterial and antiprosticidal activity, some of them also anti-leukemic and anti-tumor. In order to search for biologically active compounds, we synthesized alkyl- and aryl-substituted esters of various heterocyclic and aryl-substituted thiosulfonic acids with the general formula. This communication discusses the synthesis of (2R,3R,5S)-2-(1,3-dioxolan-2-yl)-6-(E)-ethylidene-5-isopropenyl-2,3-dimethylcyclohexane-1-ene 2, which can be used for the enantioselective synthesis of clerodanes, e.g., 6-acetoxy-2-oxocolavenool 32.
Institute of Organic Chemistry, Ufa Research Center of the Russian Academy of Sciences e-mail: flmacaev@mail.md.
ИЗ 4-АМИНОБЕНЗОЙНОЙ КИСЛОТЫ - СИНТЕЗ И БИОАКТИВНОСТЬ
The synthesis of chiral dipole 1 , a potential intermediate for the preparation of enantiomerically pure isoxazolidines 2a–b , was initiated from available (+)-4α-acetyl-2-carene 35 .
FROM 4-AMINOBENZOIC ACID
NITROGEN CONTAINED DERIVATIVES OF NORAMBRENOLIDE
After heat treatment, the initial mixture of modified starch (5-9%) with water forms stable gels (stable for more than half a year after double autoclaving). The use of modified starch for growing cells or plants involves the following procedures: preparation of a mixture of modified starch with water (8-9% modified starch); treatment in an autoclave with a technology similar to the technology for the preparation of agar gels. The modified starch was shown to be similar to commercial preparations on agar in terms of gel-forming properties.
Для объединения имидазольного и хиноидного фрагментов в одну молекулу нами разработана схема реакции, основной стадией которой является реакция нуклеофильного замещения одного из атомов хлора в молекуле 2,3-дихлор-1,4-нафтохинона (1 ).
COOH R
The essence of this reaction lies in the change of the configuration of the C-13 center of steroid from 13β to 13α during the reaction of 17-ketosteroid with aromatic ortho-diamine, e.g. The manipulation of the reaction conditions, which is the essence of the authors' "know-how", makes it possible to obtain II and IV with changed or unchanged R3 on 3-hydroxy function. Some of them are intermediates in the synthesis of the new drugs with antihormonal and antitumor activity corresponding to.
The more consumed form of collaboration may include not only synthesis but also investigation of specific activity of the agreed range of the compounds.
СЕКЦИЯ
ПОЛУЧЕНИЕ БИОЛОГИЧЕСКИ АКТИВНЫХ ВЕЩЕСТВ ИЗ
Removal of lipophilic complexes from plant raw materials is possible by extraction with non-polar solvents. By perfecting the methods of removing natural complexes of a lipophilic nature, we offered new knowledge and experience for obtaining medicines using a high-quality extractant of liquefied Freon -12. By using Freon -12 in a high-quality extractant, we conducted research to create new phytomedicines of a lipophilic nature.
The clinical effectiveness of endobronchial injection of the extract during complex conservative treatment of patients with lung abscesses has been investigated. It was shown that endobronchial injection of the extract during the treatment of this pathology statistically improves the clinical transition of the disease and reduces the number of chronic cases. Expression of the gus reporter gene was detected on the explants from in vitro seedlings and inoculated with strains R1000 of A.
Higher levels (3.42 g/l) of total flavonoid production were identified in strains transformed by LBA 9402, compared to the untransformed control (0.2 g/l). Aerial parts (young leaves and leaves) were inoculated with Agrobacterium strains. Transformed hairy roots of G.uralensis were obtained by infection of A.rhizogenes 8196 either in aseptically grown plants. One of the established liquid culture lines produced glycyrrhizin (Fig. 1) with a yield of 4.5% of dry weight in the culture period as 30 days.
Some of the isolated glycosides (1-4) are monodesmoside and others are bisdesmoside glycosides of hederagenin (3β,23-dihydroxyolean-12-ene-28-acid). The structures of isolated glycosides are shown below. Pulegone, a monoterpene ketone, is the main component of the essential oil of the Ziziphora bungeana Jus., and its content in the essential oil is 56.3%.
БИОТЕХНОЛОГИИ БИОЛОГИЧЕСКИ АКТИВНЫХ ВЕЩЕСТВ»
CLONING AND SOME FEATURES OF THE SYNTHESIS OF MOUSE IMMUNOGLOBULIN ScFv-FRAGMENT AGAINST HUMAN α2-INTERFERON IN DIFF. The biological properties of the synthesized compounds were investigated in cultures and on laboratory animals. The basic immunobiological properties of the vaccine were investigated on laboratory animals (mice, rabbits) and liver (pig, cattle).
Wild pigs are naturally susceptible animals, except domestic pigs, so virus - the causative agent of CSF, is constantly circulating in the wild. After its partial purification and solubilization, some antigenic properties of the recombinant product were studied. Data obtained show the possibility and availability of ELISA test system development based on the recombinant protein received.
The research had financial support from the Ministry of Education and Science of Ukraine, grant N 2/671- 97. Toxicological testing of the most promising strains as well as their deposition and patenting are ongoing. Our work was aimed at the transformation of the human growth hormone from the inclusion bodies into soluble form.
Therefore, the next step of the work was the development of the conditions for the absorption of the protein on the corresponding sorbent directly from the concentrated urea solution. The expression of this gene inserted in the рЕТ-а134 plasmid under the control of the T7 promoter is carried out in E.coli BL 21 DE3 cells.
МЕДИКО-БИОЛОГИЧЕСКИЕ АСПЕКТЫ ПРИМЕНЕНИЯ БИОЛОГИЧЕСКИ
The protective properties of 7 MDP derivatives were studied in an avian mouse model of influenza virus infection. The activity of glutamine synthetase (GS; EC of phosphate-dependent glutaminase (PDG) and phosphate-independent glutaminase (PIG) was determined with a spectrophotometer in the supernatant from rat liver and tumor (10000 g × 3 min) and the level of endogenous glutamine in the liver, tumor and blood plasma of animals In the liver and tumor of animals with PC-1, the activity of GS (by 1.7-fold) and PDG (by 1.5-fold) increased in the liver.
In the liver of the rats with carcinosarcoma SM-1 during the decrease the activity of glutamine-metabolized enzymes (GS - in 2 times, PDG - in 2.5 times, PIG - in 4 times) the activation of the enzymes is detected ( GS) - in 4 times, PDG - in 3.5 times, PIG - in 7 times) in the tumor. The new succinate derivative Phensuccinal is a powerful antioxidant, which is currently in clinical trials for the prevention of diabetic nephropathy. The aim of the study was to evaluate the impact of long-term treatment with Phensuccinal on the lipid profile and activity of HDL-associated antioxidant enzyme paraoxonase in diabetic rabbits. Further addition to the Krebs solution of the blocker of NO synthesis NG-nitro-L-arginine (10-3 M) in the presence of TF has inhibition of.
It is also worth noting that TF does not block the inhibitory action of exogenous noradrenaline, despite the fact that the final inhibitory effect of the action of ATP or noradrenaline on smooth muscle is similar - activation of Ca2+-dependent small-conductance apamin-sensitive K+ channels in membrane of SMCs. The Ca 2+ concentration rose rapidly to 110 nM, and then fell slowly (over 15 min) to the basal level in the presence of high K + . SECRETION AND APPLICATION OF "CEREBRAL" TROPHINOTROPIN - THE REGULATOR OF NERVE TROPHIC FACTORS OF ACUTE HEMORRHAGIC GOUT.
SELECTIVE REGULATORY ACTION OF DRUGS ON DIFFERENT LEVELS OF THE PHAGOSIC ACTIVITY OF HUMAN BLOOD POLYMORPHONUCLEAR LEUKOCYTES. Under the same conditions, Ca2+-ATPase activity of myosin decreased independently of the concentration of PG. Studies in the presence of the nitric oxide donor - sodium nitroprusside (SNP), 5 mmol/l, which is able to inhibit ATPase activity via the essential sulfhydryl groups of the ATPase center of myosin molecule, showed that PA and PG (10 - 2 mg/ml) abolished the action of SNP on the cardiac actomyosin Mg2+-Ca2+-ATPase activity.
However, the presence of inflammatory substances such as TNF and IL-1α alone cannot explain the anti-HIV FV function in vitro. The detected activity can be related to the activity of another substance that we called antiviral factor (AVF) with m.m.
ЭКСТРАКТЫ И БИОЛОГИЧЕСКИ АКТИВНЫЕ ПИЩЕВЫЕ ДОБАВКИ»
It is used for dietary nutrition of people with diseases of the digestive organs (around duodenal or gastric ulcer, gastritis with reduced secretory function, hepatitis, cholecystitis, colitises, coloenteritis) in case of hyporexia. Alcoholism and "the morning after the night before" syndrome is one of the medical and social problems in Ukraine in connection with the expressed increasing trends of increasing alcoholism abundance, the extent of the use of alcohol in subtoxic and toxic doses, features of the alcoholic market (extremely low share of weak spirits in consumption, abundance of home-distilled vodka, large amount of counterfeit production). The stage of "the morning after the night before" syndrome is characterized by lowering mental and physical efficiency, increase in the risk of traumatism.
The preliminary study of the sedative properties of this extract was carried out in animals and volunteers. In the morning the volunteers filled out the test questionnaires for the assessment of the initial state of health, activity and mood, then in the evening they consumed alcohol in a dose of 20±4.5 U; Repeated filling of the questionnaires was carried out the next morning before and 1-1.5 hours after the treatment by the studied extract in a dose of 2.8-3.3 g. For 23.5% of the volunteers, alcohol consumption did not cause any significant changes in the HAM test.
In this group of volunteers, the extraction administration did not influence the results of the subsequent self-assessment. As a whole, the obtained total extract of the 8 species of official plants has the pronounced sobering effect and provides the perspective basis for creating an effective medicine for the elimination of the “morning after the night before” syndrome. The nutritional value of the new products for the territory of Ukraine * the dry powders of the fungi of Shii-Take, Pleurotus ostreatus and Ganoderma lucidum is determined by carbohydrates, proteins in which the composition contains all the essential amino acids (20-35%), food fiber (9-10%), lipids (3-6%), vitamins B1, B2, B12, PP, panthotenic acid and minerals (Fe, Mn, K, Ca, Mg, Cd, Cu, P, Zn, Ni) that they contain.
In view of the above, it is advisable to monitor the dosage of non-traditional biotechnological products consumed with food, such as dry powders of the highest edible fungal biomass of mycelium of Shii-Take, Pleurotus ostreatus and Ganoderma lucidum. The aim of our study was to carry out the immunopharmacological screening of the two plant extracts produced in SSCD by the laboratory of heterocyclic compounds.
