Bioorganicheskaia khimiia最新文献

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[Immunoassay of nine serological tumor markers on hydrogel-based microchip]. [9种血清学肿瘤标志物在水凝胶微芯片上的免疫分析]。
Bioorganicheskaia khimiia Pub Date : 2013-11-01
Zh I Zubcova, E N Savvateeva, V I Butvilovskaia, M V Cybul'skaia, V R Chechetkin, L O Samokhina, L I Vinnitskiĭ, V V Maslennikov, Iu P Reznikov, A S Zasedatelev, A Iu Rubina
{"title":"[Immunoassay of nine serological tumor markers on hydrogel-based microchip].","authors":"Zh I Zubcova,&nbsp;E N Savvateeva,&nbsp;V I Butvilovskaia,&nbsp;M V Cybul'skaia,&nbsp;V R Chechetkin,&nbsp;L O Samokhina,&nbsp;L I Vinnitskiĭ,&nbsp;V V Maslennikov,&nbsp;Iu P Reznikov,&nbsp;A S Zasedatelev,&nbsp;A Iu Rubina","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A prototype of test-system for simultaneous quantitative assay of nine tumor markers in blood serum was developed. The main constituent of the test-system is OM-9 biochip containing immobilized antibodies against nine oncomarkers: α-fetoprotein (AFP), carcinoembryonic antigen (CEA), human chorionic gonadotropin (HCG), cancer antigen 15-3 (CA 15-3), cancer antigen 125 (CA 125), cancer antigen 19-9 (CA 19-9), prostate-specific antigen, total (PSAtot) and free (PSAfree) forms, neuron-specific enolase (NSE). The biochip-based assay procedure for carrying out simultaneous quantitative determination of nine tumor markers in patient's blood serum: two-steps sandwich-immunoassay, was proposed. The main analytical characteristics of the method were obtained. The results permit to consider the prototype of the test-system as a promising instrument for clinical application. The test-system prototype was tested using blood serum samples of oncological patients (252 samples) and healthy donors (185 samples). Increased concentrations of one or more tumor markers above the normal level were found in 76.6% cases of oncological patients and only in 6% cases of healthy donors. For colorectal cancer patients group, application of modern statistical methods of data-processing in medical researchers, i.e. ROC-analysis and logistic regression, indicted that the simultaneous assay of nine tumor markers on biochips showed much more diagnostic significance (area under the ROC-curve (AUC) reached 0.84) than traditional assay of 2 tumor markers, CEA and CA 19-9 (AUC = 0.59). The developed biochip-based test-system can be recommended both for the estimation of people's health, e.g., for standard medical examination, and for tracking of tumoral process in postsurgical period or after specific tumor treatment.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 6","pages":"693-704"},"PeriodicalIF":0.0,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33067199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Investigation of active center of deoxynucleoside monophosphate kinase of bacteriophage T5 by site-directed mutagenesis]. 噬菌体T5脱氧核苷单磷酸激酶活性中心的定点诱变研究。
Bioorganicheskaia khimiia Pub Date : 2013-11-01
G V Mikulinskaia, S A Taran, Iu S Skoblov, S A Feofanov
{"title":"[Investigation of active center of deoxynucleoside monophosphate kinase of bacteriophage T5 by site-directed mutagenesis].","authors":"G V Mikulinskaia,&nbsp;S A Taran,&nbsp;Iu S Skoblov,&nbsp;S A Feofanov","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Based on the computer model of active center of bacteriophage T5 deoxyribonucleoside monophosphate kinase amino acid residues essential for the enzyme activity were determined. As the result of site-directed mutagenesis, cloning and expression of the gene in E. coli series of proteins were obtained with single amino acid substitutions of conservative active center residues--S13A, D16N, T17N, T17S, R130K, K131E, Q134A, G137A, T138A, W150F, W150A, D170N, R172I, E176Q. Electrophoretically homogeneous preparations of mutant forms were purified using ion exchange and affinity chromatographic steps. Measuring of the specific enzyme activities of these enzymes for the natural acceptors of phosphoryl group (dAMP, dCMP, dGMP, dTMP) revealed that substitutions of charged residues of NMP-binding domain-namely, R130, R172, D170 and E176-lead to almost complete loss of enzyme activity. It was shown that presence of OH-group at position 17 is also important for catalytic activity. Based on the changes in specific activities we suppose that arginine residues at positions 130 and 172 participate in binding of γ-phosphoryl of donor and α-phosphoryl of acceptor. Also, aspartic acid at 16 position of ATP-binding site (P-loop) probably assists in the binding of acceptor, first of all dTMP. Unequal decrease in enzyme activities for different substrates of partially active mutants--G137A, T138A, T17N, Q134A, S13A, D16N--indicate that in the binding of various substrates different amino acid residues take part.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 6","pages":"680-92"},"PeriodicalIF":0.0,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33067200","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel urea and thiourea derivatives of thiazole-glutamic acid conjugate as potential inhibitors of microbes and fungi. 噻唑-谷氨酸缀合物的新型尿素和硫脲衍生物作为微生物和真菌的潜在抑制剂。
Bioorganicheskaia khimiia Pub Date : 2013-11-01
A Sharma, R Suhas, S Chandan, D C Gowda
{"title":"Novel urea and thiourea derivatives of thiazole-glutamic acid conjugate as potential inhibitors of microbes and fungi.","authors":"A Sharma,&nbsp;R Suhas,&nbsp;S Chandan,&nbsp;D C Gowda","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Since discovery and development of effective as well as safe drugs has brought a progressive era in human healthcare that is accompanied by the appearance of drug resistant bacterial strains, there is constant need of new antibacterial agent having novel mechanisms of action to act against the harmful pathogens. In the present study, several N-terminal substituted urea/thiourea derivatives were synthesized by the reaction of glutamic acid and 3-(1-piperazinyl)-1,2-benzisothiazole with various substituted phenyl isocyanates/isothiocyanates. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives were investigated for their antibacterial and antifungal activities against various pathogens of human origin by agar well diffusion method and microdilution method. The preliminary antimicrobial bioassay reveals that the compounds containing fluoro and bromo as substituents showed promising antimicrobial activity.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 6","pages":"736-44"},"PeriodicalIF":0.0,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33067697","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Mulberry (Morus L.) methionine sulfoxide rreductase gene cloning, sequence analysis, and expression in plant development and stress response. 桑树(Morus L.)蛋氨酸亚砜还原酶基因的克隆、序列分析及其在植物发育和胁迫响应中的表达。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
Wei Tong, Yinghua Zhang, Heng Wang, Feng Li, Zhaoyue Liu, Yuhua Wang, Rongjun Fang, Weiguo Zhao, Long Li
{"title":"Mulberry (Morus L.) methionine sulfoxide rreductase gene cloning, sequence analysis, and expression in plant development and stress response.","authors":"Wei Tong,&nbsp;Yinghua Zhang,&nbsp;Heng Wang,&nbsp;Feng Li,&nbsp;Zhaoyue Liu,&nbsp;Yuhua Wang,&nbsp;Rongjun Fang,&nbsp;Weiguo Zhao,&nbsp;Long Li","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Methionine sulfoxide reductase plays a regulatory role in plant growth and development, especially in scavenging reactive oxygen species by restoration of the oxidation of methionine in protein. A full-length cDNA sequence encoding methionine sulfoxide reductase (MSR) from mulberry, which we designated MMSR, was cloned based on mulberry expressed sequence tags (ESTs). Sequence analysis showed that the MMSR is 810 bp long, encoding 194 amino acids with a predicted molecular weight of 21.6 kDa and an isoelectric point of 6.78. The expression level of the MMSR gene under conditions of drought and salt stresses was quantified by qRT-PCR. The results show that the expression level changed significantly under the stress conditions compared to the normal growth environment. It helps us to get a better understanding of the molecular basis for signal transduction mechanisms underlying the stress response in mulberry.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"586-93"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33397105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[An expedient synthesis of fluorescent labeled ceramide-1-phosphate analogues]. 荧光标记的神经酰胺-1-磷酸盐类似物的一种权宜合成方法。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
I A Boldyrev, R E Braun, Iu G Molotkovskiĭ
{"title":"[An expedient synthesis of fluorescent labeled ceramide-1-phosphate analogues].","authors":"I A Boldyrev,&nbsp;R E Braun,&nbsp;Iu G Molotkovskiĭ","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A synthesis for fluorescent analogs of ceramide-1-phosphate bearing 9-anthrylvinyl or 4,4-difluoro-3a,4a- diaza-s-indacene-8-yl (Me4-BODIPY) fluorophore at o-position of fatty acid residue was carried out. The key stage of the synthesis is hydrolysis of corresponding sphingomyelins catalyzed by phospholipase D from Streptomyces chromofuscus; the enzymatic yield has been raised to 50-70% by appliance of organic solvent in the incubation medium.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"604-8"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33397109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and antimicrobial activity of new heterocyclic compounds containing thieno[3,2-c] coumarin and pyrazolo[4,3-c] coumarin frameworks. 含噻吩[3,2-c]香豆素和吡唑[4,3-c]香豆素框架的新杂环化合物的合成及其抑菌活性。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
Adel M Kamal El-Dean, Remon M Zaki, Ahmed A Geies, Shaban M Radwan, Mahmoud S Tolba
{"title":"Synthesis and antimicrobial activity of new heterocyclic compounds containing thieno[3,2-c] coumarin and pyrazolo[4,3-c] coumarin frameworks.","authors":"Adel M Kamal El-Dean,&nbsp;Remon M Zaki,&nbsp;Ahmed A Geies,&nbsp;Shaban M Radwan,&nbsp;Mahmoud S Tolba","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Reaction of 4-chlorocoumarin-3-carbonitrile with ethyl thioglycolate and ethyl glycinate hydrochloride leads to a series of title products. Hydrazinolysis of amino thienocoumarin carboxylate afforded the hydrazine derivative which underwent various reactions to build new heterocyclic rings containing thienocoumarin moiety. Chloro acetylation of aminoester compound afforded the chloro acetyl amino which underwent nucleophilic substitution reactions various amines. The following treatment with formaldehyde under Mannich conditions afforded the corresponding imidazo derivatives. Reaction of Ghloroacetylamino with potassium thiocyanate yielded ethylpyrimidothieno coumarin sulfanylacetate which was used as a versatile precursor for synthesis of other heterocycles. On the other hand, reaction of chloro coumarin carbo nitrile with hydrazine gave the aminopyrazolocoumaine which reacted with bifunctionally compounds to give the substituted pyrimido derivatives. Diazotization and coupling of aminopyrazole with ethylcyanoacetate yielded ethylaminotriazinopyrazolocoumarine carboxylate. Several of the compounds obtained demonstrated considerable antifungal and antibacterial activity in the in vitro test systems.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"619-30"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33402273","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Glutathione S-transferase of alpha class from pike liver]. [派克肝中α类谷胱甘肽s -转移酶]。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
E V Borvinskaia, L P Smirnov, N N Nemova
{"title":"[Glutathione S-transferase of alpha class from pike liver].","authors":"E V Borvinskaia,&nbsp;L P Smirnov,&nbsp;N N Nemova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In this study, glutathione S-transferase (GST) was isolated from the liver of pike Esox lucius, which was homogenous according to SDS-PAGE and isoelectrofocusing. It is a homodimer with subunits mass 25235.36 Da (according to HPLC-MS/MS) and pI about 6.4. Substrate specificity, thermostability, some kinetic characteristics and optimum pH were determined. The enzyme was identified as Alpha class GST.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"558-64"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33073327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and activity of a cyclo-heptapeptide containing Lys-Gly-Asp-sequence as a novel anti-platelet agent. 新型抗血小板药物lys - gly - asp -环七肽的合成及活性研究。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
Jian Jing
{"title":"Synthesis and activity of a cyclo-heptapeptide containing Lys-Gly-Asp-sequence as a novel anti-platelet agent.","authors":"Jian Jing","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Linear hepta-peptide Cys-Lys-Gly-Asp-Trp-Asp-Cys was synthesized first and then disulfide bond was formed between the Cys1 and Cys7 to develop cyclo-heptapeptide containing Lys-Gly-Asp-sequence. Structural simulation showed that Lys-Gly-Asp-motif (KDG) displayed functional conformation. The cyclo-heptapeptide exhibited potent anti-platelet aggregation activity based on specific recognition and interaction with the GPIIb-IIIa receptor on platelet cell membrane. The specific and potent anti-platelet activity makes the KGD-containing cyclo-heptapeptide a possible therapeutic agent.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"547-51"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33073326","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Lipophilic prodrugs of a triazole-containing colchicine analogue in liposomes: biological effects on human tumor cells. 脂质体中含三唑的秋水仙碱类似物的亲脂性前药:对人肿瘤细胞的生物学效应。
Bioorganicheskaia khimiia Pub Date : 2013-09-01
N R Kuznetsova, E V Svirshchevskaya, N S Sitnikov, L Abodo, H Sutorius, J Zapke, J Velder, P Thomopoulou, H Oschkinat, A Prokop, H G Schmalz, A Yu Fedorov, E L Vodovozova
{"title":"Lipophilic prodrugs of a triazole-containing colchicine analogue in liposomes: biological effects on human tumor cells.","authors":"N R Kuznetsova,&nbsp;E V Svirshchevskaya,&nbsp;N S Sitnikov,&nbsp;L Abodo,&nbsp;H Sutorius,&nbsp;J Zapke,&nbsp;J Velder,&nbsp;P Thomopoulou,&nbsp;H Oschkinat,&nbsp;A Prokop,&nbsp;H G Schmalz,&nbsp;A Yu Fedorov,&nbsp;E L Vodovozova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Colchicine site binders--blockers of tubulin polymerization--are potential antimitotic agents for anticancer therapy. To reduce their systemic toxicity and improve biodistribution, encapsulation in nanosized liposomes may be employed. Liposomes present a convenient means for preparation of injectable formulations of hydrophobic compounds, however colchicine as such is known to leak through the lipid bilayer. In this study, newly synthesized triazole-containing analogues of colchicine and allocolchicine, and their palmitic and oleic esters (lipophilic prodrugs) were tested for anti-proliferative activity and apoptosis-inducing potential. In contrast to colchicine conjugates, whose activities ranged with those of colchicine, allocolchicine derivatives exhibited drastically lower effects and were discarded. Liposomes of about 100 nm in diameter composed of egg phosphatidylcholine--yeast phosphatidylinositol--palmitic or oleic prodrug, 8 : 1: 1, by mol, were prepared by standard extrusion technique and tested in a panel of four human tumor cell lines. Liposome formulations preserved the biological activities of the parent colchicinoid the most towards human epithelial tumor cells. Moreover, liposomal form of the oleoyl bearing colchicinoid inhibited cell proliferation more efficiently than free lipophilic prodrug. Due to substantial loading capacity of the liposomes, the dispersions contain sufficient concentration of the active agent to test wide dose range in experiments on systemic administration to animals.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 5","pages":"609-18"},"PeriodicalIF":0.0,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33397110","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of new benzofuran-1,3-thiazolidin-4-one derivatives from natural sources and study of their antioxidant activity. 新型天然苯并呋喃-1,3-噻唑烷-4-酮衍生物的合成及其抗氧化活性研究。
Bioorganicheskaia khimiia Pub Date : 2013-07-01
N A Abdel Latif, S H Abdel Hafez, L M Break
{"title":"Synthesis of new benzofuran-1,3-thiazolidin-4-one derivatives from natural sources and study of their antioxidant activity.","authors":"N A Abdel Latif,&nbsp;S H Abdel Hafez,&nbsp;L M Break","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Synthesis of benzofuran-1,3-thiazolidinone derivatives is described herein. These compounds were prepared via a concise and short route by condensation reaction of khellinone with aromatic/aliphatic amines followed by cyclization using thioglycolic acid. The newly synthesized compounds were characterized using the well known spectroscopic tools (IR, 1H NMR, and mass spectroscopy), as well as microanalysis. In frames of biological screening of the compounds, antioxidant activity was assessed in vitro.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"39 4","pages":"491-6"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32242040","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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