V V Gostev, O S Kalinogorskaya, A N Kruglov, S V Sidorenko
Antibiotic susceptibility of 119 coagulase-negative staphylococci isolated at hospitals of St. Petersburg and Moscow was investigated and estimated at the local laboratories as oxacillin resistant. The following species were identified: Staphylococcus epidermidis, S. haemolyticus, S. hominis, S.capitis, S. simulans, S. pettenkoferi, S. lentus, S. carnosus and S. warneri. The oxacillin resistance was confirmed in 79.8% of the isolates. The frequency of the associated resistance to non-beta-lactams was much higher in the oxacillin resistant isolates vs. the oxacillin susceptible ones. When the CLSI and EUCAST susceptibility criteria were used, 1-3% difference in the resistance levels was recorded. Among the oxacillin resistant isolates the frequency of resistance to gentamicin, ciprofloxacin, erythromycin, moxifloxacin, tetracycline and clindamycin equaled 90, 88, 88, 63, 43 and 26% respectively. Two linezolid resistant isolates of S. epidermidis with lower susceptibility to tedizolid were isolated. Eight isolates of S. epidermidis showed lower resistance to mupirocin. The MIC of ceftarolin for oxacillin resistant coagulase-negative staphylococci varied from 0.5 to 2.0 mcg/ml, while for the oxacillin susceptible ones it was lower than 0.25 mcg/ml. No resistance to tigecyclin and vancomycin was observed.
{"title":"[Antibiotic Resistance of Coagulase-Negative Staphylococci Isolated at Hospitals of St. Petersburg and Moscow].","authors":"V V Gostev, O S Kalinogorskaya, A N Kruglov, S V Sidorenko","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Antibiotic susceptibility of 119 coagulase-negative staphylococci isolated at hospitals of St. Petersburg and Moscow was investigated and estimated at the local laboratories as oxacillin resistant. The following species were identified: Staphylococcus epidermidis, S. haemolyticus, S. hominis, S.capitis, S. simulans, S. pettenkoferi, S. lentus, S. carnosus and S. warneri. The oxacillin resistance was confirmed in 79.8% of the isolates. The frequency of the associated resistance to non-beta-lactams was much higher in the oxacillin resistant isolates vs. the oxacillin susceptible ones. When the CLSI and EUCAST susceptibility criteria were used, 1-3% difference in the resistance levels was recorded. Among the oxacillin resistant isolates the frequency of resistance to gentamicin, ciprofloxacin, erythromycin, moxifloxacin, tetracycline and clindamycin equaled 90, 88, 88, 63, 43 and 26% respectively. Two linezolid resistant isolates of S. epidermidis with lower susceptibility to tedizolid were isolated. Eight isolates of S. epidermidis showed lower resistance to mupirocin. The MIC of ceftarolin for oxacillin resistant coagulase-negative staphylococci varied from 0.5 to 2.0 mcg/ml, while for the oxacillin susceptible ones it was lower than 0.25 mcg/ml. No resistance to tigecyclin and vancomycin was observed.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 9-10","pages":"23-8"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34451742","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}
The antitumor effect of L-lysine-α-oxidase from the culture fluid of Trichoderma harzianum Rifai F-180 was investigated for the first time. The in vitro studies revealed its high activity on a model of the forest-spring encephalitis virus and no activity against the Sindbis, Western Nile, Tyaginya and Dhori viruses.
{"title":"[L-Lysine-α-Oxidase in vitro Activity in Experiments on Models of Viruses Sindbis, Forest-Spring Encephalitis, Western Nile, Tyaginya and Dhori].","authors":"I P Smirnova, V F Larichev, Yu A Shneider","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The antitumor effect of L-lysine-α-oxidase from the culture fluid of Trichoderma harzianum Rifai F-180 was investigated for the first time. The in vitro studies revealed its high activity on a model of the forest-spring encephalitis virus and no activity against the Sindbis, Western Nile, Tyaginya and Dhori viruses.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 3-4","pages":"3-5"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34043125","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}
A L Akopov, E B Aleksandrova, M M Il'kovich, D V Petrov, V I Trofimov
Unlabelled: Rengalin is a release-active combination antitussive drug based on antibodies to bradykinin, to histamine and morphine. It acts at various mechanisms of cough reflex by modifying endogenous target molecules and their interaction with receptors. The drug's efficacy, as demonstrated previously in experimental and clinical studies, is mediated by specific release-activity obtained as a result of the production process.
Methods: Efficacy and safety assessment of rengalin in the treatment of cough induced by acute upper respiratory tract infections (URIs) in comparison with a complex codeine-containing drug (codelac) was performed as part of a multicenter, randomized clinical trial involving 143 patients. All the participants presented with dry/non-productive cough caused by URIs (pharyngitis, laryngitis, tracheitis, tracheobronchitis, bronchitis). The duration of cough varied between 12 hours and 7 days. Rengalin was administered in 73 patients receiving 2 tablets 3 times daily for initial three days, and half reduced doses--for the subsequent four days; codelac was administered in 70 patients who were given 1 tablet 3 times daily for the entire treatment period (7 days). Primary efficacy endpoints were time to cough resolution and reduction in the severity of the cough (scored using a Cough Severity Scale). One patient in Rengalin group and three patients in Codelac group were withdrawn from the study. The article presents treatment outcomes obtained for 139 participants who completed the study in accordance with the protocol (Per Protokol-analysis). The data analysis was based on a non-inferiority (or comparability) statistical design for efficacy endpoints.
Results: The antitussive effect of rengalin was significantly comparable (p < 0.025) with that of codelac; the time to complete resolution of cough (both daytime and nocturnal) was 7.2 ± 1.0 days (versus 7.0 ± 1.1 in the group of codelac). Rengalin's efficacy was evidenced by a sufficiently reduced cough severity in the initial few days after treatment onset. As a result of the entire 7-day treatment, the severity score was reduced by 3.1 ± 09 (versus 3.1 ± 1.0 in the group of codelac; p < 0.05), totaling 0.2 ± 0.5 point in both groups at the end of the administration period. The frequent non-productive/dry cough was fully resolved in 76% of patients. All the participants in Rengalin group achieved either convalescent outcomes or significant improvement; none of the patients developed secondary bacterial complications. Positive changes in the patients' state over the week were finally confirmed by evaluating the total quality of life scores, including physical and mental component scores (SF-36 questionnaire), and total sleep quality scores, which were comparative between patients treated with rengalin and codelac (p < 0.025). At the end of the administration period, the effect of rengalin was rated by the physician i
{"title":"[Rengalin, a New Efficacious and Safe Antitussive Agent. Results of a Randomized, Comparative, Multicenter Clinical Trial in Patients with Acute Respiratory Tract Infections].","authors":"A L Akopov, E B Aleksandrova, M M Il'kovich, D V Petrov, V I Trofimov","doi":"","DOIUrl":"","url":null,"abstract":"<p><strong>Unlabelled: </strong>Rengalin is a release-active combination antitussive drug based on antibodies to bradykinin, to histamine and morphine. It acts at various mechanisms of cough reflex by modifying endogenous target molecules and their interaction with receptors. The drug's efficacy, as demonstrated previously in experimental and clinical studies, is mediated by specific release-activity obtained as a result of the production process.</p><p><strong>Methods: </strong>Efficacy and safety assessment of rengalin in the treatment of cough induced by acute upper respiratory tract infections (URIs) in comparison with a complex codeine-containing drug (codelac) was performed as part of a multicenter, randomized clinical trial involving 143 patients. All the participants presented with dry/non-productive cough caused by URIs (pharyngitis, laryngitis, tracheitis, tracheobronchitis, bronchitis). The duration of cough varied between 12 hours and 7 days. Rengalin was administered in 73 patients receiving 2 tablets 3 times daily for initial three days, and half reduced doses--for the subsequent four days; codelac was administered in 70 patients who were given 1 tablet 3 times daily for the entire treatment period (7 days). Primary efficacy endpoints were time to cough resolution and reduction in the severity of the cough (scored using a Cough Severity Scale). One patient in Rengalin group and three patients in Codelac group were withdrawn from the study. The article presents treatment outcomes obtained for 139 participants who completed the study in accordance with the protocol (Per Protokol-analysis). The data analysis was based on a non-inferiority (or comparability) statistical design for efficacy endpoints.</p><p><strong>Results: </strong>The antitussive effect of rengalin was significantly comparable (p < 0.025) with that of codelac; the time to complete resolution of cough (both daytime and nocturnal) was 7.2 ± 1.0 days (versus 7.0 ± 1.1 in the group of codelac). Rengalin's efficacy was evidenced by a sufficiently reduced cough severity in the initial few days after treatment onset. As a result of the entire 7-day treatment, the severity score was reduced by 3.1 ± 09 (versus 3.1 ± 1.0 in the group of codelac; p < 0.05), totaling 0.2 ± 0.5 point in both groups at the end of the administration period. The frequent non-productive/dry cough was fully resolved in 76% of patients. All the participants in Rengalin group achieved either convalescent outcomes or significant improvement; none of the patients developed secondary bacterial complications. Positive changes in the patients' state over the week were finally confirmed by evaluating the total quality of life scores, including physical and mental component scores (SF-36 questionnaire), and total sleep quality scores, which were comparative between patients treated with rengalin and codelac (p < 0.025). At the end of the administration period, the effect of rengalin was rated by the physician i","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 1-2","pages":"19-26"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34284205","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}
N N Besednova, T A Kuznetsova, T S Zaporozhets, T N Zvyagintseva
At present the increase of antibiotic resistance in infection agents to antimicrobial drugs requires discovery of new antimicrobial substances with improved pharmacological properties and novel mechanisms of action, to which microorganisms do not develop resistance. Three areas are of interest for the search: recovery of new compounds from natural objects, including aquatic organisms, chemical modification of the known antibiotic molecules, discovery of compounds with antimicrobial activity among some new chemical structures which have no analogues in nature. The review is mainly concerned with discussion of antibacterial, antiviral and antifungal activity of sulfated polysaccharides (fucoidans) and extracts of brown, red and green algae, as well as of antioxidant, antiinflammatory, immunomodulatory and antiendotoxin properties that contribute to their antiinfective action. Such an activity makes fucoidans promising as a basis for developing new drugs for therapy of infectious diseases.
{"title":"[Brown Seaweeds as a Source of New Pharmaceutical Substances with Antibacterial Action].","authors":"N N Besednova, T A Kuznetsova, T S Zaporozhets, T N Zvyagintseva","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>At present the increase of antibiotic resistance in infection agents to antimicrobial drugs requires discovery of new antimicrobial substances with improved pharmacological properties and novel mechanisms of action, to which microorganisms do not develop resistance. Three areas are of interest for the search: recovery of new compounds from natural objects, including aquatic organisms, chemical modification of the known antibiotic molecules, discovery of compounds with antimicrobial activity among some new chemical structures which have no analogues in nature. The review is mainly concerned with discussion of antibacterial, antiviral and antifungal activity of sulfated polysaccharides (fucoidans) and extracts of brown, red and green algae, as well as of antioxidant, antiinflammatory, immunomodulatory and antiendotoxin properties that contribute to their antiinfective action. Such an activity makes fucoidans promising as a basis for developing new drugs for therapy of infectious diseases.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 3-4","pages":"31-41"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34043130","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}
M M Tsyganov, E O Rodionov, S V Miller, N V Litvyakov
Surgery results of II-III stage lung cancer remain unsatisfactory and the chemotherapy does not improve the survival. The main obstacle is the use of the standard clinical parameters for the treatment strategy and not sufficiently effective selection of regimens for the chemotherapy. Monoresistance genes defining the tumor cells sensitivity to the chemotherapeutic drugs play a significant role in development of the lung tumor resistance. The review examines the mechanisms of transport, activation and targets of the chemotherapeutic drugs, identifies the key markers for predicting their effectiveness and possible use in the clinical practice. Monoresistance genes, such as ABCC5, RRM1, ERCC1, TOP1, TOP2a, TUBB3 and TYMS are characteristic of lung cancer. Clinical trials demonstrating the efficiency of their use as predictive markers for the lung cancer chemotherapy are described. A prospective study with a personalized adjuvant chemotherapy for lung cancer patients will be performed.
{"title":"[Substantiation of Expressive Markers Use to Personalize Lung Cancer Chemotherapy].","authors":"M M Tsyganov, E O Rodionov, S V Miller, N V Litvyakov","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Surgery results of II-III stage lung cancer remain unsatisfactory and the chemotherapy does not improve the survival. The main obstacle is the use of the standard clinical parameters for the treatment strategy and not sufficiently effective selection of regimens for the chemotherapy. Monoresistance genes defining the tumor cells sensitivity to the chemotherapeutic drugs play a significant role in development of the lung tumor resistance. The review examines the mechanisms of transport, activation and targets of the chemotherapeutic drugs, identifies the key markers for predicting their effectiveness and possible use in the clinical practice. Monoresistance genes, such as ABCC5, RRM1, ERCC1, TOP1, TOP2a, TUBB3 and TYMS are characteristic of lung cancer. Clinical trials demonstrating the efficiency of their use as predictive markers for the lung cancer chemotherapy are described. A prospective study with a personalized adjuvant chemotherapy for lung cancer patients will be performed.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 9-10","pages":"38-45"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34355933","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}
B I Kantemirova, Kh M Galimzyanov, N A Stepanova, A Kh Chernysheva, Z A Alieva
In spite of the availability of many antituberculosis drugs all over the world the morbidity of tuberculosis does not lower. Often the tuberculosis therapy schemes are adapted to every particular patient which is mainly due to the therapy unfavourable effects requiring discontinuation of the drugs used. Polymorphism of the detoxication genes, as predictors of the response to the drug therapy, was shown to be of certain significance. The experimental data would allow to substantiate personalized management of tuberculosis patients and to increase its efficacy and safety.
{"title":"[Prospects of Pharmacogenetic Testing for Design of Algorithms for Personalized Treatment of Tuberculosis of Respiratory Organs in the Astrakhan Region].","authors":"B I Kantemirova, Kh M Galimzyanov, N A Stepanova, A Kh Chernysheva, Z A Alieva","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In spite of the availability of many antituberculosis drugs all over the world the morbidity of tuberculosis does not lower. Often the tuberculosis therapy schemes are adapted to every particular patient which is mainly due to the therapy unfavourable effects requiring discontinuation of the drugs used. Polymorphism of the detoxication genes, as predictors of the response to the drug therapy, was shown to be of certain significance. The experimental data would allow to substantiate personalized management of tuberculosis patients and to increase its efficacy and safety.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 9-10","pages":"29-32"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34452223","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}
O V Efremenkova, B F Vasiljeva, V A Zenkova, A M Korolev, Y N Lusikov, T A Efimenko, I A Malanicheva, E P Mirchink, E B Isakova, E N Bilanenko, O V Kamzolkina
The fungal strain INA 01108 producing antibiotic substances with broad spectrum of antibacterial activity was isolated from the natural environment. By the morphological characteristics and DNA analysis it was shown to belong to Ascomycetes of Sordariomycetes. In submerged culture the strain produced at least four antibiotics. The major component of them was identified as eremophilane-type sesquiterpene eremoxylarin A. Eremoxylarin A is effective in vitro against grampositive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin group glycopeptide antibiotics resistant Leuconostoc mesenteroides VKPM B-4177. The efficacy and toxicity of eremoxylarin A was determined on a murine staphylococcal sepsis model. The dose of 6.25 mg/kg provided 100% recovery and survival of the animals, while the dose of 3.12 mg/kg was close to the ED50. The chemical structure of eremoxylarin A allows to modify the antibiotic and such studies may be relevant to design a less toxic derivative without loss of the valuable antimicrobial properties.
{"title":"[Antimicrobial Properties of Eremoxylarin A Produced by Ascomycete of Sordariomycetes in Submerged Culture].","authors":"O V Efremenkova, B F Vasiljeva, V A Zenkova, A M Korolev, Y N Lusikov, T A Efimenko, I A Malanicheva, E P Mirchink, E B Isakova, E N Bilanenko, O V Kamzolkina","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The fungal strain INA 01108 producing antibiotic substances with broad spectrum of antibacterial activity was isolated from the natural environment. By the morphological characteristics and DNA analysis it was shown to belong to Ascomycetes of Sordariomycetes. In submerged culture the strain produced at least four antibiotics. The major component of them was identified as eremophilane-type sesquiterpene eremoxylarin A. Eremoxylarin A is effective in vitro against grampositive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin group glycopeptide antibiotics resistant Leuconostoc mesenteroides VKPM B-4177. The efficacy and toxicity of eremoxylarin A was determined on a murine staphylococcal sepsis model. The dose of 6.25 mg/kg provided 100% recovery and survival of the animals, while the dose of 3.12 mg/kg was close to the ED50. The chemical structure of eremoxylarin A allows to modify the antibiotic and such studies may be relevant to design a less toxic derivative without loss of the valuable antimicrobial properties.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 11-12","pages":"23-8"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34355938","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}
V V Valeev, A L Kovalenko, E V Talikova, V A Zaplutanov, T Yu Delvig-Kamenskaya
The published data on the modern concept of the biological role of succinate, an intermediate of the citric acid cycle are analysed in the review. Special interest to succinate is determined by investigations on the mitochondrial functions at different pathologies, discovery of the hypoxia-inducible factor HIF-1 and studies on the human genome, that resulted in detection of the G-protein coupled receptors, which selectively are bound with succinate. According to the published experimental data, besides participation in oxidative reactions, succinate is considered as a key contributor to physiological, metabolic and genetic processes.
{"title":"[Biological Functions of Succinate (a Review of Foreign Experimental Studies)].","authors":"V V Valeev, A L Kovalenko, E V Talikova, V A Zaplutanov, T Yu Delvig-Kamenskaya","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The published data on the modern concept of the biological role of succinate, an intermediate of the citric acid cycle are analysed in the review. Special interest to succinate is determined by investigations on the mitochondrial functions at different pathologies, discovery of the hypoxia-inducible factor HIF-1 and studies on the human genome, that resulted in detection of the G-protein coupled receptors, which selectively are bound with succinate. According to the published experimental data, besides participation in oxidative reactions, succinate is considered as a key contributor to physiological, metabolic and genetic processes.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 9-10","pages":"33-7"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34452224","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}
E N Bychkova, A M Korolev, E N Olsufyeva, E P Mirchink, E B Isakova
Amidation of the end carboxyl group of eremomycin and vancomycin by pinacolinic 4- or 3-amino methyl phenyl boron acids esters in the presence of the condensing reagent PyBOP resulted in formation of novel carboxamides of the antibiotics (IIIa-VIa). After elimination of the pinacolinic group under mild hydrolysis in weak acid aqueous medium there formed the respective derivatives with a residue of the nonprotected boric acid (III-VI). It was shown that the activity of the 4-substituted derivatives of the borole-containing eremomycin and vancomycin practically was the same as that of the initial antibiotics, while higher than that of the respective 3-substituted derivatives of the borole-containing derivatives against 8 strains of grampositive bacteria.
{"title":"[Design of Novel Carboxamides of Eremomycin and Vancomycin with 4- or 3-Amino Methyl Phenyl Boric Acid and Their Investigation].","authors":"E N Bychkova, A M Korolev, E N Olsufyeva, E P Mirchink, E B Isakova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Amidation of the end carboxyl group of eremomycin and vancomycin by pinacolinic 4- or 3-amino methyl phenyl boron acids esters in the presence of the condensing reagent PyBOP resulted in formation of novel carboxamides of the antibiotics (IIIa-VIa). After elimination of the pinacolinic group under mild hydrolysis in weak acid aqueous medium there formed the respective derivatives with a residue of the nonprotected boric acid (III-VI). It was shown that the activity of the 4-substituted derivatives of the borole-containing eremomycin and vancomycin practically was the same as that of the initial antibiotics, while higher than that of the respective 3-substituted derivatives of the borole-containing derivatives against 8 strains of grampositive bacteria.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 9-10","pages":"7-11"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34451739","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}
A clinical case of hepatocirrhosis with chronic hepatitis C termination (1b genotype) is described. Taking into account the cirrhotic stage of the disease, the extrahepatic HCV replication in the peripheral mononuclears, unfavourable HCV genotype, infavourable IL-28B gene polymorphism, inefficiency of the previous two courses of the standard antiviral therapy (PegIFN + ribavirin) and secondary immune deficiency, noninterferon antiviral therapy for 24 weeks was used in the treatment of the patient: interferon-inductive therapy with cycloferon in combination with ribavirin. There was observed by the 12th week of the treatment biochemical remission and a significant decrease of the virus load from 1 x 10(7) IU/ml to 7 x 10(5) IU/ml in the blood serum and from 1.35 x 10(7) IU/ml to 8 x 10(5) IU/m in the peripheral mononuclears. Investigation of the molecular biological markers of the viremia (PCR HCV-RNA) in the cells of peripheral mononuclears is an obligatory diagnostic technology in cases with suspected extrahepatic HCV infection. The kinetics of the virus load and the positive dynamics of the immunological indices in the patient at the cirrhotic stage of chronic virus hepatitis C are indicative of the efficient etiopathogenic approach with the use of the noninterferon treatment scheme (cycloferon + ribavirin), when recombinant interferons are contraindicated.
本文描述了一例肝硬化合并慢性丙型肝炎终止期(1b 基因型)的临床病例。考虑到患者处于肝硬化阶段、外周单核细胞中存在肝外 HCV 复制、不利的 HCV 基因型、不利的 IL-28B 基因多态性、前两个疗程的标准抗病毒疗法(PegIFN + 利巴韦林)效果不佳以及继发性免疫缺陷,该患者接受了为期 24 周的非干扰素抗病毒疗法:环形干扰素联合利巴韦林的干扰素诱导疗法。在治疗的第 12 周,患者出现了生化缓解,血清中的病毒载量从 1 x 10(7) IU/ml 降至 7 x 10(5) IU/ml,外周单核细胞中的病毒载量从 1.35 x 10(7) IU/ml 降至 8 x 10(5) IU/m。外周单核细胞中病毒血症分子生物学标志物(PCR HCV-RNA)的检测是疑似肝外 HCV 感染病例的必备诊断技术。慢性丙型病毒性肝炎肝硬化阶段患者的病毒载量动力学和免疫学指标的积极动态表明,当重组干扰素被禁用时,使用非干扰素治疗方案(环干扰素+利巴韦林)是有效的病因治疗方法。
{"title":"[Kinetics of Virus Load HCV-RNA in Blood Serum and Peripheral Mononuclear Cells in a Patient with Hepatocirrhosis and Chronic Virus Hepatitis C Termination Treated According to Noninterferon Treatment Scheme (Cycloferon + Ribavirin)].","authors":"V V Stelmah, V K Kozlov, A N Nekrasova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A clinical case of hepatocirrhosis with chronic hepatitis C termination (1b genotype) is described. Taking into account the cirrhotic stage of the disease, the extrahepatic HCV replication in the peripheral mononuclears, unfavourable HCV genotype, infavourable IL-28B gene polymorphism, inefficiency of the previous two courses of the standard antiviral therapy (PegIFN + ribavirin) and secondary immune deficiency, noninterferon antiviral therapy for 24 weeks was used in the treatment of the patient: interferon-inductive therapy with cycloferon in combination with ribavirin. There was observed by the 12th week of the treatment biochemical remission and a significant decrease of the virus load from 1 x 10(7) IU/ml to 7 x 10(5) IU/ml in the blood serum and from 1.35 x 10(7) IU/ml to 8 x 10(5) IU/m in the peripheral mononuclears. Investigation of the molecular biological markers of the viremia (PCR HCV-RNA) in the cells of peripheral mononuclears is an obligatory diagnostic technology in cases with suspected extrahepatic HCV infection. The kinetics of the virus load and the positive dynamics of the immunological indices in the patient at the cirrhotic stage of chronic virus hepatitis C are indicative of the efficient etiopathogenic approach with the use of the noninterferon treatment scheme (cycloferon + ribavirin), when recombinant interferons are contraindicated.</p>","PeriodicalId":53646,"journal":{"name":"Antibiotiki i Khimioterapiya","volume":"60 3-4","pages":"24-30"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34043129","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}