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1-25 67 0

Synthesis of physiologically active compounds of quinolizidine and quinoline types

Shukhrat Rakhimov

Subjects of research: derivatives of alkaloid cytisine and l-phenyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline.
Purpose of work: development of methods for synthesis of new N-benzyl derivatives of cytisine and asymmetric bimolecular compounds on the basis of cytisine and substituted 1 -phenyl-1,2,3,4-tetrahydroisoquinolines with the purpose to obtain biologically perspective substances.
Methods of research: methods of organic synthesis, mass spectrometry, NMR spectroscopy, RSA, chromatography (TLC, column), computational methods of computer chemistry, and biological analysis methods.
The results obtained and their novelty: targeted synthesis of N-benzyl derivatives of cytisine by reaction with aromatic aldehydes has been carried out. The conditions of obtaining l-phenyl-6,7-dimethoxy-l,2,3,4-tetrahydroisoquinoline derivatives by Pictet-Spengler reaction have been found. Synthesis of bimolecular compounds using the derivatives and cytisine has been carried out for the first time. Conditions of these reactions were developed. 38 new substances have been synthesized.
Practical value: a simple method of obtaining N-benzyl derivatives of cytisine and N-(3-oxobutyl)cytisine has been suggested.
As a result of pharmacological investigations, compounds with N-cholinestimulating, N-cholinolytic, anti-inflammatory, anti-edema and spasmolytic (papaverine like) action have been found among derivatives obtained from cytisine. All the obtained compounds are low toxic. It shows new possibilities for search of medicinal preparations on the basis of these compounds.
Degree of embed and economic effectivity: as a result of the investigations, l-(4'-methoxyphenyl)-6,7-dimethoxy-l,2,3,4-tetrahydroisoquinoline has been suggested as a local anaesthetic preparation. An application for patent for compound obtaining method has been handed in.
Field of application: Organic Chemistry, Bioorganic Chemistry, Chemistry of natural compounds and physiologically active compounds, Medicine.

1-52 33 0

Synthesis of physiologically active 1-aryl-1,2,3,4-tetrahydroisoquinoline substances and their derivatives

Sherzod Jurakulov

The aim of research work is the synthesis of new physiological active 1-aryltctrahydroisoquinolinc substances mono- and bis-dcrivatives, study of their physicochemical properties and identification of promising biologically active compounds among them.
The objects of the research work arc homoveratrylaminc, a series of substituted bcnzaldchides and synthesized new l-aryl-l,2,3,4-tctrahydroisoquinolincs and their derivatives.
Scientific novelty of the research work:
an effective method for the synthesis of new mono-dcrivatives of 1-aryl-1,2,3,4-tctrahydroisoquinoline has been developed;
methods for the synthesis of new bis-tetrahydroisoquinolines with Ar-Ar and >N-CH2-N< bonds have been developed for the first time;
it was established that the interaction of l-aryl-l,2,3,4-tctrahydroisoquinolincs with paraform under normal conditions and microwave irradiation depends on the nature of the used solvent and the structure of isoquinoline;
synthesis of new 41 substances has been carried out and compounds with cytotoxic, sedative-tranquilizing and antiarrhythmic activity were found in the series of synthesized compounds and shown dependence cytotoxic activity on the structure;

1-90 58 0

Synthesis and revealing the biological activity of derivatives alkaloids and triterpenoids of oleanane series (glycyrrhizinic acid)

Makhmudjon Gafurov

The topicality and relevance of the dissertation topics. Highly effective reversible inhibitors of the acetylcholinesterase (AChE) arc widely used in the world for alleviation of poisoning by organophosphorus pesticides and in the treatment of ilnesses such as Alzheimer's disease, myasthenia gravis, glaucoma, paralysis, and paresis. Therefore, the development of highly effective reversible inhibitors of AChE for the use in therapy of different pathologies of the central nervous system, a search among these preparations with antidotal action, chemical modification of the phannacon, as well as the creation of low-dose dose, watersoluble drugs with a wide range of therapeutic index by using the complexing agents arc an important issue today.
With the acquisition independence of Uzbekistan, organization of scientific-research works on creation of the low-dose, effective pharmaceuticals from local herbs for treatment of a number of diseases, and conduction of enhanced measures to provide the population with quality drugs at a high level medicine has led to a definite successes
At present, on the basis of glycyrrhizic acid (GA) by molecular encapsulation, complexes of the poorly soluble pharmakons were obtained, where the desired effect was achieved ath very small amounts of the pharmakons. This method is considered as the most effective way to reduce the side effects of many drug; on the basis of GA and its derivatives, the drugs against acquired immunodeficiency syndrome, skin and stomach cancers, as well as antiinflammatory water-soluble drugs with low doses and a wide of the therapeutic index arc created and put into practice. The research in this area is an urgent task of the bioorganic chemistry and medicine.
The present doctoral dissertation is, to some extent, an accomplishment of the tasks set in the Resolution 416 of the Cabinet of Ministers dated 14 July 2016 «On the procedures to support domestic manufacturers of medicinal drugs and medical devices» and other legislative documents related to the above mentioned activities.
The aim of the study is to develop drugs with a wide therapeutic mcdiccinal action on the basis of nitrogcn-containing organophosphorus reversible inhibitors of AChE possessing an antidote effect and anti-inflammatory drugs based on certain derivatives of glycyrrhizic acid.
The scientific novelty of the research is as follows:
based on alkaloids and some nitrogcn-containing heterocyclic compounds (piperidine, morpholine, hcxamcthylcncimine, anabasine, lupinine, cpilupinina), complex esters and salts of the methyl-, mcthylthion- and phcnyl-phosphonic acid complementary to the active surface of AChE have been synthesized; 
defined the appearance of the diastercomcric anisochronism effect in the NMR spectra of the mctylthiophosphonic acid derivatives with two or more asymmetric centers have been demonstrated;
effective reversible inhibitors of AChE was found.
the research showed the structure-activity relationships;
supramolccular complexes of GA salts with effective reversible AChE inhibitors - alkaloids Dcoxypcganinc hydrochloride (DOP HC) and galantamine in different proportions have been synthesized;
it shows that MASGA and DOP GA (2:1) has high cholinesterase active and less toxicity;
the gel formation of the aqueous solution of the obtained supramolccular complexes of GA and its salts was studied and the critical micelle concentration were determined; presumed mechanism of the process was proposed;
the intcrfcron-inducing activity of the created supramolccular complexes has beed studied; on the basis of the most effective comples, an anti-inflammatory drug, GLAS, has been created.
CONCLUSIONS
1. A series of ethers of O-alkylmcthylphosphonic, O-alkylmcthylthiophosphonic acids on the basis of N-P-hydroxycthyl- and N-P-hydroxypropylmorpholine, piperidine, anabasine, hcxamcthylcncimine, lupininc and cpilupine were synthesized. In the presence in the molecule of the O-alkylmcthylphosphonatc of two and more asymmetric centers, in the PMR spectra, the effect of a diastereoisomeric anisochronicity in the form of duplication of the proton signals of a methyl group directly bound to the phosphorus atom is observed and these properties helps to determine the structure of these kind substanses.
2. For hydrochlorides of O-alkylmcthylphosphonatcs, O-alkylmcthylthion-phosphonates and O-alkylphcnylphosphonatcs, the anticholinesterase activity towards the acetylcholinesterase of human blood erythrocytes and Bu-cholinesterasc of the horse blood serum is studied. All the studied compounds arc reversible inhibitors of the acetylcholinesterase and Bu-cholinesterase; the comparison of Kj values of the mcthylphosphonates and mcthylthiophosphonatcs of lupinine, cpilupine and N-P-hydroxyethylpipcpyridine showed that the replacement of the fragment of P=O by P=S leads to a sharp increase in the anticholinesterase activity for both AChE and BuChE (thionic effect), this is important on creation of new and effective inhibitors of AchcE.
3. O-alkyl-O-[N-(P-oxyethylpipcridinc)] - and O-alkyl-O-[N-(P-oxypropyl-hcxamcthyleniminyl)]mcthylthionic phosphonates arc the strong competitive reversible inhibitors of AChE and BuChE showing a high specificity for the acetylcholinesterase. It is established that O-alkyl-O-[N-(P-oxyethylpipcridinc)]-mcthylthionic phosphonates exhibit a profound preventive effect for the toxic action of armin. In the future it will provide for the creation of drugs arc effective antidotal properties based mcthyltionphosphonatcs.
4. Supramolccular complexes of salts of GA with hydrochlorides of dcsoxydcpcganinc, galantamine and prednisolone arc obtained; their structures arc studied by the methods of UV- and IR-spectroscopy. It is shown that the MGA: deoxydepeganine hydrochloride complex (2:1) surpasses the dcsoxydcpcganinc hydrochloride in its anticholinesterase activity by 85.3 times, and it is 8,3 times less toxic. For the immunosuppressive action, the complex of prednisolone with MGA (Gliprcd), at the doses of 2.5 and 5.0 mg/kg upon peroral administration, surpasses the effect of prednisolone alone given at the dose of 10 mg/kg. This was the basis for drug development of Dcoxypcganinc and Gliprcda.
5. For the first time, the supramolccular complexes of GA salts with SK, AA, PSK and BSK were obtained. Physicochemical constants of the complexes were determined, and their structures were studied by the methods of UV- and IR-spcctroscopies. Based on the results of spectral methods (UV and IR), the formation of new MGA complexes due to hydrophobic interactions and hydrogen bonds between host and guest molecules has been confirmed. This is important in the confirmation structures newly acquired complexes based on the GA.
6. In order to reveal the nature of the forces influencing the process of structuring of water molecules and the viscosity, the hydrodynamics of MASGA-1 (75% purity) and MASGA-2 (97% purity) solutions (at a concentration of 0,2% and below) was studied in control and in the presence of various agents, such as urea (destroying the intcrmolecular hydrogen bonds), xylose (affecting hydrophobic interactions) and KC1 (an electrolyte); as a result, it was found that the process of structuring in solutions may occur not only due to hydrogen bonds, but also via strong hydrophobic interactions. It will help to explain the formation of complexes.
7. As a result of pharmacological studies, it was established that the obtained new complex of MASGA:AA (GLAS) exhibits the interfcron-inducing, profound anti-exudative, anti-inflammatory and wound healing properties and, at the same time, it docs not exert toxic effects on an organism; the therapeutic index (LD5(/ED50) for the GLAS is higher than that for MASGA and AA alone by 4 and 52 times, respectively, whereas the toxicity is 6 times lower than toxicity of AA alone; it is shown, for the first time, that at the doses of 10 and 25 mg/kg, the proliferative effect of this complex exceeds that for AA alone twice. This was the basis for creation of the anti-inflammatory drug on the basis of the complex.
8. The temporary pharmaceutical article for GLAS substance and its dosage form (tablets) has been devised, the project of the technology of preparing the dosage form in the form of tablets (0,05 g) has been developed and the experimental batch of tablets has been prepared. Clinical trials were successfully conducted in three clinical institutions of Tashkent; the reports of the tests were submitted to GDQCMME and to the Ministry of Healthcare of the Republic of Uzbekistan for obtaining the permission for production. According to the Decision of the Presidium of Pharmacological Committee of the Ministry of Healthcare of Republic of Uzbekistan, the medicine has been approved for use in medical practice.

1-45 91 0

Synthesis and research of new efficient complexing ionites

Furkat Eshkurbonov

The aim of research work is synthesis of new high performance multifunctional complexing ionites and their application in the course of a sorption of noble and non-ferrous metals of ions from individual and mixed solutions.
The object of the research work are epichlorohydrin, formaldehyde, carbamide, thiourea, РЕРЛ, cyanotriamide, hydrolyzed polyacrylonitrile, orthophosphoric acid, complexing ionites on their basis, the aqueous solutions containing color, infrequent and noble ions of metals.
Scientific novelty of the research work is as follows:
obtained selective, thermochemical resistance, polyfunctional nitrogen-, phosphorus-, oxygen- and sulfur-containing complexing resins based on epichlorohydrin-urea (thiourea), and formalin-urea (thiourea) with polyethylenepolyamine, melamine, phosphoric acid and hydrolyzed polyacrylonitrile;
synthesized new effective and cheap complex-forming polyfunctional ion exchangers by the interaction of dimethylcarbodamidc and dimethylolthiourea with hydrolyzed polyacrylonitrile and orthophosphoric acid on the basis of local raw materials;
determined the dependence of the reaction rate constant, the activation energy, the physicochemical properties of the obtained ion exchangers on temperature, the concentration of the initial substances and study of the kinetic synthesis processes;
determined the dependence of the basic chemical and physical-chemical properties (sorption of metals of silver, cobalt, zinc, nickel, copper, lead, sorption capacity, the degree of dissociation of functional groups) of import-substituting, complexing ion exchangers from chemical compounds and physicochemical properties of starting materials;
developed a technology for the preparation of complexing ion exchangers based on dimethyl-carbamidc (dimethylolthiocarbamide) and diglycidyl-carbamidc (diglycidylthiourca).
Implementation of the research results. On the basis of results of a research and development of technology of synthesis of complexing ionites:
These complexing ionites are made at the Tashkent research institute of engineering chemistry at JSC Uzkimyosanoat and applied at a sewage disposal of the enterprises, (the reference No. 05-3583/M of JSC Uzkimyosanoat from 2016 on November 4). As a result the developed way of extraction of noble and rare metals with application of the synthesized new complexing ionites gives the chance to recommend them for concentrating and extraction of ions of precious metals from hydromctallurgical industry sewage.
The structure and volume of the thesis. The thesis consists of an introduction, four chapters, conclusion and bibliography. The volume of the thesis is 120 pages.

213-214 198 0

Suyultirilgan gazlarni saqlash masalalarini o'rganish

F Khudoyberdiyev, M Sobirov

Hozirgi vaqtda suyultirilgan tabiiy gaz global uglevodorod bozorida tobora muhim rol o'ynamoqda. Suyultirilgan tabiiy gaz iste'molining ko'payishi nafaqat ayrim mamlakatlar va mintaqalarda o'z energiya resurslarining yetishmasligi, balki, avvalambor, suyultirilgan tabiiy gazning boshqa energiya manbalariga nisbatan sezilarli afzalliklari bilan bog'liq. Birinchidan, suyultirilgan tabiiy gazni etkazib berish uchun gaz quvurlari tizimini, shu jumladan borish qiyin bo'lgan joylarda qurish va texnik xizmat ko'rsatishning hojati yo'q. Suyultirilgan tabiiy gazning asosiy afzalligi uni dengiz orqali uzoq masofalarga tashish, okeanlararo etkazib berishni amalga oshirish va eng past narxlarda bozorlarda sotish qobiliyatidir. Bu ayniqsa, energiya xavfsizligini mustahkamlash va gaz eksportini diversifikatsiya qilishga intilayotgan O'zbekiston uchun to'g'ri keladi. Ikkinchidan, suyultirilgan tabiiy gaz quvur liniyasiga nisbatan yuqori sifat bilan tavsiflanadi. Buning sababi shundaki, suyultirish jarayonida gaz zararli aralashmalar va oltingugurt birikmalaridan tozalanadi, shuning uchun chiqishda metan miqdori yuqori bo'lgan deyarli toza gaz olinadi. Bundan tashqari, suyultirilgan tabiiy gaz uglevodorod elektr energiyasi olishda ekologik toza manba hisoblanadi.

1-24 45 0

Study the synergetic properties and influence of inhibitors of esterase of insects of Laspeyresia Pomonella L. and Pyrausta Nubilalis Hb

Bakhtiyor Kholmuradov

Object of the research: pest insects of Laspeyresia pomonella I., and Pyrausta Nubilalis Hb.
The purpose of work: study of cholinesterase and carboxylesterase ferments of the pest insects of Laspeyresia pomonella L. and Pyrausta Nubilalis Hb. on the basis of subtract - inhibitors methods as well as synergist properties influencing on their phosphororganic inhibitors.
Methods of research: in the process of research, preparation of homogenates from cells of insects, substrate-inhibitors in studying of the activeness and properties of ferments, electrophoreses, calorimetric and Kamovsky methods as well as toxicological and synergetic methods in studying of inhibitors were used.
The obtained results and their novelty: for the first time it has been researched cholinesterase and carboxylesterase ferments of the pest insects of Laspeyresia pomonella L. and Pyrausta Nubilalis Hb. adapted to natural and pesticides and the activeness dynamics in their ontogeny development. It was established that the activeness of the best adapted populations of carboxylesterase ferments to the pesticides, carboxylesterase is produced against the activeness of the used pesticides in the organisms of insects. Moreover, on the basis of studying their properties and analyzing information of the used literature, it was established that the activeness of cholinesterase and carboxylesterase ferments in the organisms of the selected insects, these ferments exist in the cells of their bodies and their activeness degree variables according to the types of insects and plants, and the conditions where their organs meet.
The practical value: the carried out researches serve as a basis for working out scientifically proved aids on creation physiological active matters against selected insects and ruling metabolic activeness of ferments.
Degree of embed and economic efficiency: the given pesticides can be used as synergist against established inhibitors influencing highly on the activeness of carboxylesterase ferments of selected insects. Moreover, the achieved results of the dissertation can be used as a teaching material on biochemistry, nature defense and entomology as well as on special courses of enzymology in higher education institutions.
Field of application: bioorganic chemistry, ecology, entomology and agriculture.

552-558 88 0

Study of the biology of maple plants discovered in the Turkestan region

A Seytmetova, B Sagidollina

Түркістан облысының аумағы Қазақстан Республикасының оңтүстігінде шөлдер аймағында орналасқан. Ол шөл-ландшафт аймағы ретінде орташа белдеудің құрамына кіреді, солтүстіктен оңтүстікке қарай 550 км, ал батыстан шығысқа қарай 470 км-ге созылып жатыр [1].

1-89 74 0

Structure, biological activity of antimicrobial peptides of nigella sativa and creation of pharmaceutical composition on their basis

Yuliya Oschepkova

The urgency and relevance of the theme of dissertation. The main focus in the development of medicinal products is to create drugs based on biologically active substances derived from local herbs.
The biological variety of flora of Uzbekistan serves as the potential source of valuable bioactive substances perspective for the use in medicine and agriculture. Among the wide spectrum of endemic plants the special attention is attracted by garden fennel flower - Nigella sativa L., related to family of buttercup - Ranunculaceae.
Seeds of garden fennel flower Nigella sativa have a variety of applications: as a highly effective diuretic, choleretic, mild laxative and immunostimulatory agent. In addition, some of the components provide excellent results in the treatment of various dermatological diseases associated with histamine neurohumoral and irregularities in the body. In dermatology used in atopic dermatitis, idiosyncracies, restore skin immunity, have a powerful antioxidant effec , eliminates stagnant processes of the skin.
Research of natural connections showing antimicrobial activity has both a theoretical value - for the study of molecular components and mechanisms of resistance of plants to pathogens and large practical value in agriculture and medicine. Major application antimicrobial proteins and peptides can find in medicine, as an alternative to the traditionally used antibiotics and antimicotics. It is known that as a result of wide use of antibiotics in medical practice in the last decades, for microorganisms the mechanisms of stability were produced. As a result there were strains steady to majority used presently to the antibiotics. Antimicrobial proteins and peptides in this plan are extraordinarily perspective, as they possess the wide spectrum of action, operate quickly and effectively, does not cause negative consequences.
Chemical composition of seed of garden fennel flower is studied well enough. Isolatee and characterizes lipids, carbohydrates, phenolic compounds, however the peptides contained in seed have not been studied, therefore the search of new high active antimicrobial proteins and peptides from garden fennel flower sowing and their all-round study is perspective direction and the problem of search and selection of new similar connections is very actual.
This dissertation research to some extent serves to carry out the tasks provided in the Resolution of the Cabinet of Ministers of the Republic of Uzbekistan №404 «On measures to support domestic manufacturers of drugs and medical products» of July 14, 2006, as well as in other legal documents adopted in this area.
The aim of research works is to develop methods for the isolation of individual cysteine-containing peptides from black cumin seeds, the establishment of their application in medicine and to pharmaceutical compositions on their basis.
Scientific novelty of the research work is as follows:
for the first time a systematic study of cationic peptides in seeds and seedlings of fennel flower garden Nigella sativa',
from the seeds of fennel flower garden recovered new lipid transfer protein Ns-LTPl with a molecular weight of 9602 Da containing 8 cysteine residues, to which the primary structure is installed and the data registered in the database BLAST;
isolated and characterized in detail 6 new peptides (Ns-Dl, Ns-D2, Ns-Wl, Ns-W2, Ns-Nl andNs-Gl).
it is shown that two new peptide homologous Ns-Dl and Ns-D2 with molecular weights of 5485 and 5498 Da, possess a strong inhibitory activity against phytopathogenic fungi;
defined that peptides Ns-Wl and Ns-W2 with molecular weights of 5143 and 5070 Da contain 8 cysteine residues and homologous y-purotionins cereals;
determined that Ns-Nl peptide with a molecular weight of 5696 Da in its composition contains 8 cysteine residues, is unique in the established N-terminal amino acid sequence;
defined peptide Ns-Gl with a molecular weight of 2794 , contains six cysteines in its structure and refers to a new class cysteinrich peptides, which have no analogues in molecular weight and the number of cysteine residues among the known antimicrobial peptides;
a comparative analysis of the spectrum of peptides in seeds and seedlings and found that seedlings blackie contains lipid transfer protein Ns-LTP2 with a molecular weight of 9086 Da, and 10 peptides related to defensins В-type, absent in the seeds.
CONCLUSION
1. A method for isolation of individual AMP from black cumin seed and seedling seed Nigella sativa, including acid extraction and complex chromatographic methods - affinity, size exclusion, high performance liquid chromatography.
2. From the seeds of black cumin isolated a new lipid transfer protein Ns-LTP1 with a molecular weight of 9602 Da, containing 8 cysteine residues, set the primary structure on which revealed that it belongs to a class of proteins lipid transfer. Ns-LTPl registered in the EMBL database with the identification number r86527. Determined biological activity against phytopathogen different groups; The effect of Ns-LTPl on the conductivity of the membrane clamp technique with planar bilayer phospholipid membranes. Based on these data suggested one of the possible mechanisms fungitoxicity LTP.
3. Select two homologous peptide Ns-Dl and Ns-D2, set their complete amino acid sequence and belonging to the class of defensins, shows homology to the peptides of the family Brassicaceae. Defensin Ns-D2 showed the highest antifungal and anti-microbial activity. At a concentration of 3.4 pg/ml defensin Ns-D2 destroying plasma membrane conidia B.sorokiniana.
4. Highlight the new peptide Ns-Nl with a molecular weight of 5696 Da, containing 8 cysteine residues. Based on the determination of the partial N-terminal amino acid sequence determined that the peptide has no homology to known peptides. Pending the EMBL database for the registration of a new homologous series family Ranunculaceae, containing this peptide.
5. Highlight peptides Ns-Wl and Ns-W2 with molecular weights of 5168 and 5070 Da homologous y-purotionins cereal. Installed partial N-terminal amino acid sequence.
6. First of black cumin seeds isolated peptide Ns-Gl, containing 6 cysteines its composition and consisting of two polypeptide chains joined by intra- and interchain disulfide bonds. The peptide is unique in its structure and has no structural analogues among known cationic peptides.
7. From seedling fennel flower garden allocated lipid transfer protein Ns-LTP2 with molecular weight 9086 Da and ten peptides related to defensins B-type, which is defined molecular weight and the number of cysteines.
8. The compounding ointment "Sedanil" based on black cumin seed oil and total peptides. Conducted preclinical pharmacological tests have shown high activity of wound-healing ointment proposed.
9. Projects of TFA to "Black cumin seed Nigella sativa", "Complex polypeptides" and "Pharmaceutical composition" and executed in accordance with the requirements.

1-21 37 0

Structurally functional organization and laws expression of thyroglobulin gene at cancerogenesis in cells of the thyroid gland

Doniyor Mamatkulov

Subjects of research: samples DNA received from blood of sick and healthy donors, the thyroid glands of patients removed during operation concerning various tumors.
Purpose of work: studying structurally - functional features and laws expression TG gene at various tumors of a thyroid gland, studying of the molecular-genetic mechanism of formation of tumors of a thyroid gland, studying of infringements of regulation expression TG gene and creation of theoretical base for early diagnostics of these diseases.
Methods of researches: allocation of polyribosomes by a magnesium method, allocation total RNA, reception of immunosorbent PABC-TG:aTG, allocation high-molecular DNA, processing DNA restriction endonucleases, electrophoresis products of hydrolysis DNA by restriction endonucleases, hybridization of the nylon filters " Biodan " containing fragments DNA with 32P-marked cDNA, polymerase chain reaction.
The results obtained and their novelty: it is received immunosorbent PABC-TG:aTG. The size of a population individual TG polyribosomes is determined Is shown, that at papillary adcnocarcinomc decrease of the maintenance individual TG polyribosomes is observed. At papillary adcnocarcinomc chromosomal aberrations that leads to genetic instability arc revealed, frequency of chromosomal aberrations makes 2,8 %. It is shown, that at papillary adcnocarcinomc occur infringement of regulation expression TG gene at a level of synthesis mRNA, i.e. at a level of a transcription.
Practical value: Introduction in practice of molecular-genetic methods of researches of tumors of a thyroid gland stimulate more full understanding of the mechanism canccrogenesis, that is essential criterion of the forecast of an outcome of disease.
Degree of embed and economic effectivity: Results of researches can be used by development of approaches for early diagnostics of tumors of a thyroid gland, and also at reading rates of molecular biology and biochemistry of hormones at biological faculties of Universities, and rates endocrinology in medical institutes.
Field of application: biochemistry, molecular biology, biotechnology, medicine, endocrinology.

1-24 38 0

Sp-2 protein from soybean cake, the study of its antitumor activity

Yuliana Beresneva

Subjects of research: The object of study is the sp-2 protein complex from soybean cake.
Purpose of work. Isolation of the sp-2 protein complex from soybean cake, the study of its physical and chemical characteristics and specific anticancer activity on AKA.TOL, B-16 melanoma and breast cancer strains.
Methods of research. Column chromatography, electrophoretic studies, determination of amino acid composition and N-terminal amino acids, radiometric analysis on incorporation of 14C - thymidine, imunnchistochcmical analysis, microscopy, imunne enzyme analysis, PCR analysis.
The results obtained and their novelty. For the first time sp-2 protein complex was isolated from soybean cake and its physical and chemical properties were studied. The obtained purified protein complex consists from 5 proteins with a molecular mass of the core component of 30 kDa, isoelectric point of pl -3,8; 3,9 and 8,2. Amino acid composition: Ala, Arg, Asp, Vai, His, Glu, Gly, He, Leu, Lys, Met, Pro, Ser, Tyr, Thr, Phe. N-tcrminal amino acids: threonine, glycine, serine, proline, valine. The sp-2 protein has shown high antitumor activity in vitro and in vivo.
Practical value. Application was submitted to the State Patent Agency of the Republic of Uzbekistan №IAP 20080420 «The method of extraction of protein complex from plant material cake ». The results will help to increase fundamental knowledge of modem science regarding the mechanism and effects of proteins on tumor cells, allow to understand the new strategy for treating malignant tumors and to develop new anticancer drugs based on proteins extracted from soybean.
Application of results. In a result of the research sp-2 protein was proposed as an antitumor agent. In a framework of applied research under the grant of FA-A11-T174 on "Development of anti-tumor protein preparation from soybean cake and isolation of extra pure enzymes from local raw materials" a drug form of the preparation is being developed and the necessary technical documentation by the Temporary Pharmacopeias paper project for submission to the Pharmacopeias Committee of the Republic of Uzbekistan.
Field of application: chemistry of natural and physiologically active substances, medicine.

741-743 82 0

Sochdan DNK ajratib olish

Nozima Kholmirzaeva, Sofiya Togaeva, Mukhammadjon Mustafakulov

Soch jinoyat sodir bo‘lgan joyda topiladigan eng keng tarqalgan biologik dalillardan biri bo‘lib, sud tibbiyotida muhim rol o‘ynaydi. Ba‘zi ma’lumotlarga ko‘ra, to‘kilgan sochlar jinoyat sodir bo‘lgan joylarda to‘plangan namunalarning 90 foizini tashkil qiladi. Odam organizmidagi barcha hujayralar o‘zida irsiy axbarot saqlaganligi tufayli, hujayralardagi DNK ni ajratib olish va o‘rganish orqali shaxsning belgilarini aniqlash mumkinligi va sochlarda ham DNK mavjudligini inobatga olgan holda ulardan ham DNK ajratib olishning samarali usullarini ishlab chiqish sud tibbiyoti uchun shuningdek, qo‘rg‘oshin yoki simob kabi metallar bilan zaharlanganlikni aniqlash uchun ham qo‘llash mumkin. Ushbu tezisda sochlar va ular tarkibidan DNK ajratib olish haqida so‘z boradi.

216-217 117 0

Sholi qoldiq mahsulotlari tarkibidan biologik faol moddalarni ajratib olish

S Xabibullayeva , I Bobaev , A Normatov , N Yusupov

Sholini tozalashda maydalangan donidan glyukoza olish va uni biotexnologik yo‘l bilan ferentatsiyalab O‘zbekistonda kamyob mahsulotni turini ko‘paytirish dolzar muammolardan biri hisoblanadi.

11-13 96 0

Shambala – trigonella foenum-graecum L. medicinal properties of the plant

D Berdybaeva, D Aytimbetova

The health benefits and healing properties of herbal products have been known since ancient times. A number of epidemiological and laboratory studies conducted abroad revealed the biological effects and medicinal properties of shambala. In recent years, research on shambala has revealed a number of health benefits and physiological properties in both experimental animals and human clinical trials. In this research, we reviewed the available scientific literature on shambala.

1-48 23 0

Secondary metabolites of subgenus Seriphidium of genus Artemisia plants

Rimma Mukhamatkhanova

The aim of research work is the isolation of secondary metabolites from plants Artemisia lehmanniana Runge, A leucotricha Krasch. ex T.adyg., A. korshinskyi Krash. ex Poljak. and A. tenuisecta Nevski., determination of their chemical structure and biological activity.
Scientific novelty of the research work:
15 terpenoids and 7 substances belonging to the class of phenolic compounds, including 1 coumarin and 6 flavonoids have been isolated from four species of plants of the genus Artemisia, subgenus Seriphidium {Artemisia lehmanniana Bunge, A. leucotricha Krasch. ex Ladyg., A. korshinskyi Krash. ex Poljak. and A. tenuisecta Nevski.) and indetified;
known substances (1 monoterpenoid, 4 sesquiterpene lactones, 5 triterpenoids, 6 flavonoids, and 1 coumarin) have been identified;
the structure of five new terpenoids (1 monoterpene aldehyde, 2 sesquiterpene lactones and 2 diterpenoid alkaloids) was established. Alkaloids from the genus Artemisia were isolated for the first time;
the high antiviral and antiarrhythmic activity of the obtained water-soluble derivatives of artekorin and a-santonin has been established.

158-161 149 0

Research of acute toxicity and medium-death dose of tannins of rumex confertus willd

Nadzhie Abrekova, Nuria Beknazarova, Farhod Atamuratov, Sardor Makhmudov, Tokhir Khudoyberdiev, Bahodir Sagdullaev
The purpose of this study was to determine the acute toxicity and moderate lethal dose of tannins obtained from the roots and aerial parts of the R. confertus Willd plant. Determination of acute toxicity and the average lethal dose of the samples was carried out according to the method of Litchfield and Wilcoxon. As a result of the studies, the death of animals in the studied doses did not occur. The tested drugs belong to the IV class of low toxic compounds. LD50 ≥5000 mg / kg.
1-63 228 0

Regioselective nitrosation of meta-, para-substituted phenols and β-naphthol derivatives

Djaloliddin Nurmukhammadov

The aim of research work The aim of the study is to regioselective nitrosation of the derivatives of meta- and para- substituted phenols and P-naphthol and to identify the field of application of the synthesized substances
The scientific novelty of the research work is as follows:
first carried out a systematic synthesis nitrosation phenol derivatives and P-naphthol having a m- and p- positions alkoxy-, alkyl-, halo-, hydroxy -, nitro, carbonyl, sulfo and carboxyl groups inorganic and organic nitrosating agents;
For the first time found that the reaction for the regioselective nitrosation of organic nitrites phenol and P- naphthol, proceed faster with electron-donating substituents, but compared with the nitrosation of inorganic nitrites;
found following series activity nitrosating agents to nitrosation example, acid Schaeffer in acidic medium: А1(МОг)з > Ba(NO2)2> NaNCh >H3o-C4H9ONO >изо-C5H11ONOH-C4H9ONO
found that synthesized o- nitrosophenols are substances high molecular weight as compared to Elias reagent, high sensitivity, most selective distinctive for reuse due to the formation of soluble compounds with d metals;
first developed a new method for the nitrosation of p - naphthol and 6-sulfonic acid at room temperature with high yield.
Found possibility of using the new o- nitrosophenols as important compounds in rapid determination of heavy and toxic metals in d-water irrigated agriculture and water management in soil and other objects;
for the first time found that the nitroso compounds derived from P-naphthol derivative dramatically reduces the time of vulcanization of rubber for comparison with foreign vulcanization accelerator «kaptaks» and improves the quality of rubber;
first it found that mikrokonsentration solution of 3-hydroxy-4-nitroso-2-naphthoic acid reagent is hypersensitive to cobalt ion (II);
found optimum conditions for the regioselective nitrosation of mono- and diyademyh phenols with different substituents in the ortho position and have developed a new technique nitrosation of phenol at room temperature.

1-23 44 0

Reception complex acting new defoliants on base chlorates sodium, possessing physiological active and insecticide’s characteristic

Djamshid Shukurov

Subjects of research: chlorate sodium, urea, diurea sodium chlorate, monoethanolamine, acetic acid, acephatus, ethanol, acetamipride, sipermetrine.
Purpose of work: physicochemical substantiation and development of fundamental technology scheme of acquisition with establishment of optimal parameters of the production of defoliants in possession of physiologically activity and insecticide activity on the basic of diurea sodium chlorate, monoethanolamine acetate, acephatus, ethanol, acetamipride and sipermetrine.
Methods of resarch: visual-polytermic, chemical, thermogravimetric, IR-spectroscopic, x-ray phase.
The results obtained and their novelty: For the first time by the method of mutual solubility of the components gained new data on heterogeneous phase balances in 13 systems consisted of water, diurea sodium chlorate, monoethanolamine acetate, acephatus, ethanol, acetamipride and sipermetrine. Data on investigation of influence recommended defoliants into oil content of cotton seeds and results of toxic behavior of defoliants, in possession of physiologically activity and insecticide activity.
Practical value: created scientific bases of production of new defoliants in possession of physiologically activity and insecticide activity, principle technological schemes of their reception are offered.
Degree of embed and economic effectivity: offered technologies are approved on integrated laboratory and experienced-production installation is produced initial lots defoliants, possessing physiological and insecticide by activity. Created defoliants possess "soft" action high defoliants and insecticide activity by activity promote efficient fall sheet, as well as 100% full destruction of vermin’s such as louse, whitefly, thripses. Under their influence the contamination of cotton filament with sticky masses and reduction of its quality should be prevented. The economic effectivity of 1 hectare of cotton plants treatment with defoliant based on magnesium chlorate and acephatus and with defoliant based on magnesium chlorate forms to 19477,9-22776,26 soums.
Field of application: Agriculture.

1-75 71 0

QTL mapping of loci and genes regulated photoperiodic flowering in cotton

Fakhriddin Kushanov

The aim of the research work is to identify the genes of cotton flowering time, mapping of quantitative traits loci associated with the sensitivity to photopcriod of this crop using marker systems of Simple Sequence Repeats (SSR) and Cleaved Amplified Polymorphic Sequences (CAPS), and also annotate of candidate genes participating in the mechanism of photoperiodic flowering of cotton in the marked regions by in silico method.
Scientific novelty of the research is as follows:
for the first time new phytochrome (PHY) and HY5 gene-specific CAPS and dCAPS markers were designed and developed for cotton;
candidate markers for the PHYA, PHYB and HY5 flowering genes controlling and regulating the photoperiodic flowering of cotton arc characterized and mapped;
the chromosome localization of the studied molecular markers was determined using genetic linkage maps and cytogenetic collections of chromosome-substituted lines of cotton;
for the first time the cotton population segregating for photoperiodic flowering was developed by crossing a photopcriod insensitive mutant line with its pre-mutagenesis photoperiodic wild-type of the species G.darwinii Watt;
for the first time the molecular genetic maps of G.darwinii Watt were constructed using populations based on photoperiodic sensitivity and DNA markers;
for the first time using the intraspecific population G.darwinii, molecular-genetic mapping of the quantitative traits loci associated with flowering time and some other morpho-biological traits;
the genomic positions of identified QTL-loci were determined on the genome of G.hirsutum by in silico PCR method;
candidate genes associated with the photoperiodic sensitivity of cotton were identified using data bases and web-programs BLAST, AUGUSTUS.

367-369 96 0

Qandli diabetni davolashda probiotiklarning ahamiyati

Sayyora Muradova, Firangiz Hamroyeva

Ushbu maqolada qandli diabet bilan og‘rigan bemorlarni prabiotiklar faoliyati orqali organizmdagi qand miqdorini pasaytirish haqida ma’lumotlar keltirilgan.

1-61 61 0

Proteins and isoenzymes correlated with valuable agronomic traits of the cotton plant and wheat, as well their usage in the phylogenetic analyses

Илхам Курбанбаев

The aim of the research work is reveling of protein and isozyme markers, studying of their inheritance related with economically valuable traits of cotton and wheat, and their use in phylogenetic analysis (cotton).
Scientific novelty of the research is as follows:
for the first time on the basis of the data compiled for the reference spectrum of the three groups of proteins (water, buffer and sparingly soluble), allowing to describe electrophoretic passport of the individual cotton species and varieties;
determined relationship of the inheritance of protein markers with a number of agronomic characters of the cotton plant.
it shows that homology between one genomic species group is greater than the homology between species of different genomic groups.
G. raimondii species by protein composition exhibits relationship to the species with genomic groups Ai and A2;
established that frequency of occurrence of different populations of wheat varieties cultivated in different regions of the Republic, is different and may vary from year to year of cultivation, which in turn may be related to adaptability of the biotypes of intravariety populations to the specific agro-climatic conditions of the environment;
determined of the gluten content of the wheat varieties from different regions of the Republic, shown that this value is different in the studied samples, indicating about influence to this trait agro-climatic and agronomic conditions;
on the basis of the conducted researches released bread wheat variety «Pakhlavon».

1-61 52 0

Probiotic and bacteriocinogenic properties of lactobacilli, creation the antiulcer remedy on their base

Shakhlo Miralimova

The aim of the research work is determining the potential of lactobacilli effective producer of bactcriocin for developing new probiotic product.
Scientific novelty of the research is in the following:
for the first time the bactcriocinogcnic properties of local strains of mcsophilic - L. plantarum, L. paracasei, L. rhamnosus and thermophilic - L. helveticus, L. delbrueckii sp. bulgaricus, L. amylovorus lactobacilli, isolated from dairy products and fermented vegetable products have been proved;
the identification of mcsophilic and thermophilic lactobacilli through morphologic-cultural, physiologic-biochemical and genetic characteristics is completed;
for the first time the content of culture media and cultivation conditions for increase of bactcriocinogcnic activity of lactic acid bacteria has been determined. The increase of batcriocin production for 2.6 - 4 times as compared with control is achieved;
bactcriocinogcnic lactobacilli comply with probiotic criteria identified in guideline MUK 4.2.2602-10: resistance to bile and simulated gastric juice, acid pH value, have high antimicrobial activity, adhesive to intestinal cells in vivo in experimental mice and as in in vitro on CaCo-2 cell line;
for the first time the in vivo interaction of bactcriocin producing strain Lactobacillus rhamnosus 925 and Helicobacter pylori pathogen on gnotobiotic and special pathogen free mice has been investigated and the effective reduction of stomach by Helicobacter colonization, and reduction of inflammation level after injection of Lactobacillus rhamnosus 925 has been determined.

1-40 54 0

Polysaccharides of Gleditsia and Cardaria repens

Rano Rakhmanberdyeva

Subject of research: Gleditsia seeds, aerial parts of Cardaria repens
Purpose of work: comprehensive study of polysaccharides in the aerial part of Cardaria repens and seeds of Gleditsia, both grown in the local region; establishing structural features of the chemical constitution of arabinogalactan Cardaria repens and galactomannanes of unstudied species of Gleditsia, detection of their specific biological activity and ways of their use in the national economy.
Methods of research: chemical and physical (IR-, I3C, 'Н - NMR spectroscopy).
The results obtained and their novelty: New data received on the structure and properties of herbal galactomannanes of Gleditsia genus and arabinogalactan Cardaria repens with wide opportunities for their use.
Chemical and spectral methods revealed that arabinogalactan C. repens consists of P-1->6 linked galactopyranose residues, lateral branches along C-3 and C-2 are made of the residues of arabinose and galacturonic acid.
It is proved that galactomannanes of Gleditsia represent a branched polymer, the main polyglicoside chain of which consists of P-1,4 linked mannan, where a part of mannose residues is substituted by a-D-galactopyranose in 0-6 position.
For the first time, a branched arabinogalactomannan and inulin-type glucofructan are isolated from seeds of G. macracantha and their structures identified.
It is determined that galactomannanes are chemotaxonomic markers for this genus of plants and complement the database on chemosystematics of the representatives of Fabaceae family in order to identify galactomannanes.
Practical value: A biologically active supplement «glefud» is created on the basis of polysaccharide to control weight of overweight people.
A new reagent called «gledol» is developed and produced for immunological and cytological studies. It substitutes an imported synthetic medication, «ficoll».
«Gledan», a paint hardener is developed to be used in textile printing.
Degree of embed and economic effictivity: All documentation on gledol has been submitted to the Head Department of Drug and Medical Equipment Quality Control of Public Health Ministry of the Republic of Uzbekistan to register and sell the reagent.
Field of application: medicine, textile industry.

1-42 28 0

Physiological and biochemical peculiarities of Sorghum almum Parodi in different conditions of growth

Burkhon Avutkhonov

The aim of the research work is to determine the growth, development, physiological and biochemical peculiarities of Columbus grass (Sorghum almutn Parodi) under the introduction conditions.
Scientific novelty of the research is as follows:
for the first time, the growth, development, physiological and biochemical features of untradational fodder plant Sorghum almum Parodi were determined in the specific soil-climatic conditionsof Samarkand region;
it was proved correlation of the intensity of growth and development during the ontogenesis of plants, crop-producing powerof seeds and the green mass from different cultivation conditions;
it was revealed a difference in plastids pigments content, a leaf area and index, formation of dry substances, pure photosynthetic productivity and biochemical composition in different vegetation periods of Columbus grass;
it was substantiated the signs of drought-resistance of Columbus grass by means of study of water exchange peculiarities at cultivation conditions;
it was determined the techniques of Columbus grass cultivation in Samarkand region conditions and ways of practical application.

1-28 54 0

Photonics food dyes molecules

Salikh Astanov

The main purpose of the work is to invent the molecular association in the solution and pellicle of dyes widely using in food industry, formation of complexes and physical process which arc formed by the means of them and applying the received results to the practice. The following results and conclusions arc obtained by the result of spectroscopic researches conducted in the wide range of concentrations and temperatures (4.5 - 370 K) for dyes and related to them substances used in food industry and on practice.
1. For the molecules of studied substances the coefficient of extinction and meaning of optical activity, quantitative output of fluorescence and phototransformation, force of oscillator, frequencies of pure electronic transition were determined.
2. Structure of molecules and absorption of substances according to the properties of solvent, decrease of absorptive and fluorescent abilities, gipso and batochromic widening of the spectrum by the comparison with monomer molecules arc observed. It was determined that hypochromic effect, observed in the association of molecules was stipulated by the resonance splitting of excited electronic levels of the molecules of food dyes.
3. The formation of the luminescent associates in binary solvents of food dye molecules at the room temperature was observed. Absorption and luminescence bands of associates arc placed in side high length in comparison with those for monomer molecules.
4. It was established that the complicated associates of food dyes arc formed by their dimmers. In this case the angle between flatness of dimmers in the aggregate is 90°, and in the respect of the axis of aggregates growth is 45°.
5. It was shown that the complicated associates of food dyes have needle-shaped structure. These associates arc put under the influence of gravitational field of the Earth. Time and character of the relaxation in the ordering of the associates depends on the molecular mass of the monomer molecules.
1. Half width and position of exiton band of the associates of food dyes molecules were determined. On base of Davidov’s molecular cxitions theory the electron transition energies in dimmer and monomer, the interaction energy difference of excited and non-excitcd molecule in elementary cell of dimmer molecule, the resonant life-time of exiton and other parameters of associates were calculated.
2. Main ways of dcsactivation, and excitation energy for food days molecules and compounds related to them were established:
- for derivatives of corotinoids, arilcthilenes and arilpolienes - inner conversion, isomerization, conformation and luminescence of the molecules of sensibilizated oxygen:
- for derivatives of bctalainc and antociance - fluorescence and sensebilization of singlet oxygen;
-Fordcrivatives of flavon, difcnilbutadicnc and difcnilgecsatricnc 
- fluorescence and inner conversion.
8. Photo and tcrmodcstruction of monomer and associates of the molecules of antociane, bctalainc and flavon were defined. It was shown that quantum output of photodestruction is low for the molecules of antociane and it had big meaning for the derivatives of bctalainc. It was proved that the photodestruction of molecules of dyes pass through the sensibilized molecular oxygen.
9. It was shown, that the formation of the complexes containing different molecules. IR and laser irradiation cuse the rise of photo and thermostability offood dyes. The rise of photo and thermostability of food pigments and vitamins was achieved by pumping the molecular oxygen out of the solution, as result of this it was determined that term of the keeping of dyes increased 3-4 times.
10. Spectrophotometric cells, allowing obtaining the spectra of circular and linear dichroism in the conditions of laminar hydrodinamic stream were worked out and patented.

1-22 44 0

Peculiarities of receptor properties disorder of brain cell membrane in experimental dysfunction of thyroid gland

Dilnoza Yakubova

Subject of the inquiry: brain of 168 mongrel rats
Aim of the inquiry: to define peculiarities and mechanisms of receptor properties disorder of brain cell membrane in experimental pathology of thyroid glands. Methods of inquiry: biochemical, biophysical, morphological, statistical.
The results achieved and their novelty: for the first time, it has been shown that hyperthyroidism results in reduction, but hypothyroidism - in density increase of GAOA - benzodiazepine-binding sites on GAOA receptors as well as CPP-binding sites on glutamate receptors of NMDA-type in synaptosomes. At the same time, the density of kainite-binding sites on glutamate receptors of kainite-type in synaptosomes from different areas in hypothyroidism is decreased but in hyperthyroidism is increased.G-6-PDG and K+, Na+- ATPase activity in hypothyroidism has been decreased as far as pathology progressing, in hyperthyroidism has been increased. In rats with hypo- and hyperthyroidism there revealed disbalance in POL/AOD system which promotes the development of hyperperoxidation of lipids more marked in thyroid gland hypofunction. Hypo-and hyperthyroidism in rats result in the development of discirculatory changes of different peculiarities in all areas of brain. Histochemically, in hyperthyroidism reduction of content nerve cells of tigroid substance in cytoplasm are noted, but in hypothyroidism hyperchromia and hypertrophy are detected.
Practical value: the work mainly has fundamental character and finds out the mechanism of receptor properties disorder of brain cells conditioning peculiarities of the development of neurological manifestations in thyroid gland pathologies, their interconnection with structural and functional membrane disorders.
Degree of embed and economic effectivity: study results have been embedded into practice of CRL TMA experimental department, introduced in academic process - in delivering of lectures and practical lessons in Biochemistry. Field of application: fundamental medicine and biology.