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[PMID]:28459659
[Au] Autor:Matsui K; Tachioka K; Onodera K; Ikeda R
[Ad] Endereço:Department of Microbial Science and Host Defense, Meiji Pharmaceutical University, Tokyo, Japan.
[Ti] Título:Topical Application of Josamycin Inhibits Development of Atopic Dermatitis-Like Skin Lesions in NC/Nga Mice.
[So] Source:J Pharm Pharm Sci;20:38-47, 2017.
[Is] ISSN:1482-1826
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Patients with atopic dermatitis (AD) have superficial skin colonization by Staphylococcus aureus and an increased number of T helper type 2 (Th2) cells in their peripheral blood. Our previous study showed that josamycin, a macrolide antibiotic, had excellent bactericidal activity against S. aureus strains isolated from AD patients and simultaneously inhibited Th1 and Th2 cell development mediated by Langerhans cells. The purpose of the present study was to evaluate the effect of topical application of josamycin on AD-like skin lesions in NC/Nga mice. METHODS: Josamycin (0.1%) was topically administered to NC/Nga mice with AD-like skin lesions induced by 2, 4, 6-trinitrochlorobenzene (TNCB). The therapeutic effects of josamycin were assessed by measurement of the skin severity scores, histological changes in the lesioned skin, serum levels of total IgE, and expression of interferon (IFN)-γ and interleukin (IL)-4 in lymph nodes and skin lesions. RESULTS: Topical treatment with josamycin significantly suppressed the increase in the skin severity score in NC/Nga mice. This suppressive effect was equal to that of betamethasone, and was associated with a decrease in the density of cellular infiltration into the dermis, the mast cell count in the dermis and the serum IgE level. Furthermore, topical application of josamycin reduced the expression of IFN-γ and IL-4 in auricular lymph node cells and the skin lesions. CONCLUSION: The present results show that topical application of josamycin inhibits the development of AD-like skin lesions in NC/Nga mice. This suggests that topical application of josamycin to AD lesions colonized by S. aureus would be beneficial for control of AD by acting on superficially located S. aureus and by inhibiting the development of Th1 and Th2 cells.This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Dermatite Atópica/tratamento farmacológico
Josamicina/farmacologia
Pele/efeitos dos fármacos
[Mh] Termos MeSH secundário: Administração Tópica
Animais
Antibacterianos/administração & dosagem
Dermatite Atópica/induzido quimicamente
Dermatite Atópica/patologia
Josamicina/administração & dosagem
Camundongos
Camundongos Endogâmicos
Testes de Sensibilidade Microbiana
Cloreto de Picrila
Pele/patologia
Staphylococcus aureus/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); HV13HFS217 (Josamycin); Z4ZG7O5SZ9 (Picryl Chloride)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171222
[Lr] Data última revisão:
171222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.18433/J3GW3D


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[PMID]:28276768
[Au] Autor:Zhao ZH; Jin LL; Xu YP; Liu C; Wang AP; Lei PS
[Ad] Endereço:a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica , Peking Union Medical College & Chinese Academy of Medical Sciences ,
[Ti] Título:Synthesis and antibacterial activities of some novel 17, 18-unsaturated carbonyl compounds derivated from josamycin.
[So] Source:J Asian Nat Prod Res;19(4):358-387, 2017 Apr.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Some novel josamycin derivatives bearing an arylalkyl-type side chain were designed and synthesized. By HWE or Wittig reaction, 16-aldehyde group of josamycin analogs were converted into unsaturated carbonyl compounds. They were evaluated for their in vitro antibacterial activities against a panel of respiratory pathogens. 8b and 8e exhibited comparable activities against a panel of respiratory pathogens, especially to resistant ones in the series of desmycarosyl josamycin analogs. Among of all the target molecules, 21 showed the best antibacterial activities.
[Mh] Termos MeSH primário: Antibacterianos
Josamicina
Cetonas
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antibacterianos/farmacologia
Josamicina/análogos & derivados
Josamicina/síntese química
Josamicina/química
Josamicina/farmacologia
Cetonas/síntese química
Cetonas/química
Cetonas/farmacologia
Testes de Sensibilidade Microbiana
Estrutura Molecular
Staphylococcus aureus/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Ketones); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170412
[Lr] Data última revisão:
170412
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170310
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2016.1194834


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[PMID]:26729746
[Au] Autor:Berthe-Aucejo A; Girard D; Lorrot M; Bellettre X; Faye A; Mercier JC; Brion F; Bourdon O; Prot-Labarthe S
[Ad] Endereço:Pharmacie, Hôpital Robert-Debré, APHP, Paris, France.
[Ti] Título:Evaluation of frequency of paediatric oral liquid medication dosing errors by caregivers: amoxicillin and josamycin.
[So] Source:Arch Dis Child;101(4):359-64, 2016 Apr.
[Is] ISSN:1468-2044
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To study reconstitution and preparation dosing errors of liquid oral medications given by caregivers to children. METHODS: A prospective observational study was carried out in the departments of general paediatrics and emergency paediatrics at the Robert-Debré Children's University Hospital. An interview with caregivers involved (1) practical reconstitution and preparation of an oral liquid medication from a prescription drawn at random (amoxicillin (Clamoxyl, dosing spoon) or josamycin (Josacine, dose-weight pipette)) and (2) a questionnaire about their use. RESULTS: One hundred caregivers were included. Clamoxyl and Josacine were incorrectly reconstituted in 46% (23/50) and 56% (28/50) of cases, respectively, with a risk of underdosing of Clamoxyl (16/23) and overdosing of Josacine (23/28). Dose preparation with the dosing spoon was incorrect in 56% of cases, and in 10% of cases with the dose-weight pipette. Female sex, native French speaker, and age were significantly associated with correct reconstitution. Male sex and medication were significantly associated with correct preparation. CONCLUSIONS: This study highlights the high incidence of errors made by caregivers in reconstituting and preparing doses of these liquid oral medicines, which are associated with considerable risks of over- and underdosing. Factors associated with these errors have been identified which could help health professionals to optimise their strategy for educating families about the use of liquid oral medications and the need to check that they understand these instructions.
[Mh] Termos MeSH primário: Amoxicilina/administração & dosagem
Antibacterianos/administração & dosagem
Josamicina/administração & dosagem
Erros de Medicação/estatística & dados numéricos
[Mh] Termos MeSH secundário: Administração Oral
Adolescente
Adulto
Cuidadores
Criança
Pré-Escolar
Feminino
Hospitais Pediátricos
Seres Humanos
Incidência
Masculino
Pediatria
Estudos Prospectivos
Inquéritos e Questionários
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 804826J2HU (Amoxicillin); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160318
[Lr] Data última revisão:
160318
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160106
[St] Status:MEDLINE
[do] DOI:10.1136/archdischild-2015-309426


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[PMID]:26711765
[Au] Autor:Anton E; Muñoz T; Travería FJ; Navarro G; Font B; Sanfeliu I; Segura F
[Ad] Endereço:Department of Infectious Diseases, Corporació Sanitària Parc Taulí, Sabadell, Barcelona, Spain Universitat Autònoma de Barcelona, Barcelona, Spain eanton@tauli.cat.
[Ti] Título:Randomized Trial of Clarithromycin for Mediterranean Spotted Fever.
[So] Source:Antimicrob Agents Chemother;60(3):1642-5, 2015 Dec 28.
[Is] ISSN:1098-6596
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The classic antibiotic treatment for Mediterranean spotted fever (MSF) is based on tetracyclines or chloramphenicol, but chloramphenicol's bone marrow toxicity makes tetracyclines the treatment of choice. However, it is convenient to have alternatives available for patients who are allergic to tetracyclines, pregnant women, and children <8 years old. We conducted a randomized clinical trial to compare clarithromycin with doxycycline or josamycin in the treatment of MSF. Forty patients were evaluated (23 male; mean age, 39.87 years); 13 patients were aged <14 years. Seventeen patients received clarithromycin, and 23 received doxycycline or josamycin. The interval between the onset of symptoms and the start of treatment was 4.04 ± 1.70 days in the clarithromycin group versus 4.11 ± 1.60 days in the doxycycline/josamycin group (P = not significant [NS]). Time to the disappearance of fever after treatment was 2.67 ± 1.55 days in the clarithromycin group versus 2.22 ± 1.35 days in the doxycycline/josamycin (P = NS). The symptoms had disappeared at 4.70 ± 2.25 days in the clarithromycin group versus at 4.75 ± 3.08 days in the doxycycline/josamycin (P = NS). There were no adverse reactions to treatment or relapses in either group. In conclusion, clarithromycin is a good alternative to doxycycline or josamycin in the treatment of MSF.
[Mh] Termos MeSH primário: Antibacterianos/uso terapêutico
Febre Botonosa/tratamento farmacológico
Claritromicina/uso terapêutico
Doxiciclina/uso terapêutico
Josamicina/uso terapêutico
Rickettsia conorii/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Antibacterianos/efeitos adversos
Criança
Pré-Escolar
Claritromicina/efeitos adversos
Doxiciclina/efeitos adversos
Feminino
Seres Humanos
Lactente
Josamicina/efeitos adversos
Masculino
Meia-Idade
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); H1250JIK0A (Clarithromycin); HV13HFS217 (Josamycin); N12000U13O (Doxycycline)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151230
[St] Status:MEDLINE
[do] DOI:10.1128/AAC.01814-15


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[PMID]:26390565
[Au] Autor:Vinarov AZ; Stojlov SV; Kozyrev SV; Surikov VN; Chaban AV; Kurbatov DG; Shpilenja ES; Nejmark AI
[Ti] Título:[DOXYCYCLINE (UNIDOX SOLUTAB®) AND/OR JOSAMYCIN (WILPRAFEN®) IN TREATMENT OF PATIENTS WITH PROSTATITIS IN REAL CLINICAL PRACTICE. RESULTS OF THE TAURUS OBSERVATIONAL PROGRAM].
[So] Source:Urologiia;(3):75-8, 80-3, 2015 May-Jun.
[Is] ISSN:1728-2985
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Treatment of chronic prostatitis is a vital and complicated problem, in which a large number of stamps and "stereotyped" approaches often result in uncured patients. The increasing use of intracellular microorganisms in prostatitis etiology requires a modification in the standard approaches. TAURUS study shows high efficacy of doxycycline (Unidox Solutab®) and/or josamycin (Wilprafen®) in chronic prostatitis. Therapy, studied in this program, according to physicians, was effective in 93.2% of patients. Treatment failure was observed in 1.3% of all patients, another 5.5% of patients had insufficient data for assessment. Low incidence of adverse reactions was observed. In the study population, adverse reactions occurred in 2.6% of patients, of them serious adverse events were registered in 0.7% of patients. The most common adverse event in all treatment groups was diarrhea.
[Mh] Termos MeSH primário: Antibacterianos/uso terapêutico
Doxiciclina/uso terapêutico
Josamicina/uso terapêutico
Prostatite/tratamento farmacológico
[Mh] Termos MeSH secundário: Antibacterianos/administração & dosagem
Antibacterianos/efeitos adversos
Doxiciclina/administração & dosagem
Doxiciclina/efeitos adversos
Quimioterapia Combinada
Seres Humanos
Josamicina/administração & dosagem
Josamicina/efeitos adversos
Masculino
Estudos Prospectivos
Prostatite/microbiologia
Prostatite/psicologia
Qualidade de Vida
Inquéritos e Questionários
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); HV13HFS217 (Josamycin); N12000U13O (Doxycycline)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150923
[St] Status:MEDLINE


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[PMID]:26055628
[Au] Autor:Auzou M; Caillon J; Poyart C; Weber P; Ploy MC; Leclercq R; Cattoir V
[Ad] Endereço:Service de microbiologie et CNR associé de la résistance aux antibiotiques, CHU de Caen, 14033 Caen, France.
[Ti] Título:In vitro activity of josamycin against Streptococcus pyogenes isolated from patients with upper respiratory tract infections in France.
[So] Source:Med Mal Infect;45(7):293-6, 2015 Jul.
[Is] ISSN:1769-6690
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The primary objective of our study was to obtain susceptibility data for josamycin against Streptococcus pyogenes isolated from patients presenting with upper respiratory tract infections in France. The secondary objective was to characterize the molecular mechanism of resistance in macrolide-resistant isolates. PATIENTS AND METHODS: MICs of erythromycin, clarithromycin, azithromycin, josamycin, and clindamycin were determined by the broth microdilution method. Resistance genes erm(B), erm(TR), and mef(A) were screened by PCR. RESULTS: The MIC50 and MIC90 of josamycin against 193 isolates of S. pyogenes were 0.12 and 0.25mg/L, respectively, with a resistance rate estimated at 4.7%. Resistance was due to the erm(B) gene whereas strains harboring erm(TR) or mef(A) remained susceptible. CONCLUSIONS: Josamycin was active against >95% of S. pyogenes isolated from patients with upper respiratory tract infections, and can be used as an alternative for the treatment of pharyngitis.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Josamicina/farmacologia
Infecções Respiratórias/microbiologia
Streptococcus pyogenes/efeitos dos fármacos
Streptococcus pyogenes/isolamento & purificação
[Mh] Termos MeSH secundário: França
Seres Humanos
Testes de Sensibilidade Microbiana
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:150713
[Lr] Data última revisão:
150713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150610
[St] Status:MEDLINE


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[PMID]:25645440
[Au] Autor:Guschin A; Ryzhikh P; Rumyantseva T; Gomberg M; Unemo M
[Ti] Título:Treatment efficacy, treatment failures and selection of macrolide resistance in patients with high load of Mycoplasma genitalium during treatment of male urethritis with josamycin.
[So] Source:BMC Infect Dis;15:40, 2015 Feb 03.
[Is] ISSN:1471-2334
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Azithromycin has been widely used for Mycoplasma genitalium treatment internationally. However, the eradication efficacy has substantially declined recent decade. In Russia, josamycin (another macrolide) is the recommended first-line treatment for M. genitalium infections, however, no data regarding treatment efficacy with josamycin and resistance in M. genitalium infections have been internationally published. We examined the M. genitalium prevalence in males attending an STI clinic in Moscow, Russia from December 2006 to January 2008, investigated treatment efficacy with josamycin in male urethritis, and monitored the M. genitalium DNA eradication dynamics and selection of macrolide resistance in M. genitalium during this treatment. METHODS: Microscopy and real-time PCRs were used to diagnose urethritis and non-viral STIs, respectively, in males (n = 320). M. genitalium positive patients were treated with recommended josamycin regimen and treatment efficacy was monitored using quantitative real-time PCR. Macrolide resistance mutations were identified using sequencing of the 23S rRNA gene. RESULTS: Forty-seven (14.7%) males were positive for M. genitalium only and most (85.1%) of these had symptoms and signs of urethritis. Forty-six (97.9%) males agreed to participate in the treatment efficacy monitoring. All the pre-treatment M. genitalium specimens had wild-type 23S rRNA. The elimination of M. genitalium DNA was substantially faster in patients with lower pre-treatment M. genitalium load, and the total eradication rate was 43/46 (93.5%). Of the six patients with high pre-treatment M. genitalium load, three (50%) remained positive post-treatment and these positive specimens contained macrolide resistance mutations in the 23S rRNA gene, i.e., A2059G (n = 2) and A2062G (n = 1). CONCLUSIONS: M. genitalium was a frequent cause of male urethritis in Moscow, Russia. The pre-treatment M. genitalium load might be an effective predictor of eradication efficacy with macrolides (and possibly additional antimicrobials) and selection of macrolide resistance. Additional in vivo and in vitro data are crucial to support the recommendation of using josamycin as first-line treatment for M. genitalium infections in Russia. It would be valuable to develop international M. genitalium management guidelines, and quantitative diagnostic PCRs determining also M. genitalium load and resistance mutations (for macrolides and ideally also moxifloxacin) should ideally be recommended.
[Mh] Termos MeSH primário: Carga Bacteriana
Farmacorresistência Bacteriana/efeitos dos fármacos
Josamicina/uso terapêutico
Macrolídeos/farmacologia
Infecções por Mycoplasma/tratamento farmacológico
Mycoplasma genitalium/isolamento & purificação
Uretrite/tratamento farmacológico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Antibacterianos/farmacologia
Carga Bacteriana/efeitos dos fármacos
Carga Bacteriana/genética
DNA Bacteriano/análise
DNA Bacteriano/genética
Seres Humanos
Josamicina/farmacologia
Macrolídeos/uso terapêutico
Masculino
Meia-Idade
Infecções por Mycoplasma/epidemiologia
Infecções por Mycoplasma/microbiologia
Mycoplasma genitalium/efeitos dos fármacos
Mycoplasma genitalium/genética
Reação em Cadeia da Polimerase
Prevalência
Reação em Cadeia da Polimerase em Tempo Real
Federação Russa/epidemiologia
Falha de Tratamento
Resultado do Tratamento
Uretrite/epidemiologia
Uretrite/microbiologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (DNA, Bacterial); 0 (Macrolides); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:151028
[Lr] Data última revisão:
151028
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150204
[St] Status:MEDLINE
[do] DOI:10.1186/s12879-015-0781-7


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[PMID]:25220780
[Au] Autor:Ejeil AL; Thomas A; Mercier S; Moreau N
[Ad] Endereço:Bretonneau Hospital, Department of Oral Surgery, Paris, France, and Paris Descartes University, Sorbonne Paris Cité, France. Electronic address: Anne-laure.ejeil@parisdescartes.fr.
[Ti] Título:Unusual gingival swelling in a 4-year-old child.
[So] Source:Oral Surg Oral Med Oral Pathol Oral Radiol;118(6):627-31, 2014 Dec.
[Is] ISSN:2212-4411
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Doença de Crohn/diagnóstico
Doenças da Gengiva/diagnóstico
[Mh] Termos MeSH secundário: Antibacterianos/uso terapêutico
Azatioprina/uso terapêutico
Pré-Escolar
Doença de Crohn/tratamento farmacológico
Diagnóstico Diferencial
Quimioterapia Combinada
Feminino
Doenças da Gengiva/tratamento farmacológico
Seres Humanos
Imunossupressores/uso terapêutico
Josamicina/uso terapêutico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Immunosuppressive Agents); HV13HFS217 (Josamycin); MRK240IY2L (Azathioprine)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:141203
[Lr] Data última revisão:
141203
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:140916
[St] Status:MEDLINE


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[PMID]:24496145
[Au] Autor:Sugamata R; Sugawara A; Nagao T; Suzuki K; Hirose T; Yamamoto K; Oshima M; Kobayashi K; Sunazuka T; Akagawa KS; Omura S; Nakayama T; Suzuki K
[Ad] Endereço:1] Inflammation Program, Graduate School of Medicine, Chiba University, Chiba City, Japan [2] Department of Immunology, National Institute of Infectious Diseases, Shinjuku-ku, Japan.
[Ti] Título:Leucomycin A3, a 16-membered macrolide antibiotic, inhibits influenza A virus infection and disease progression.
[So] Source:J Antibiot (Tokyo);67(3):213-22, 2014 Mar.
[Is] ISSN:0021-8820
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Severe respiratory disease arising from influenza virus infection has a high fatality rate. Neutrophil myeloperoxidase (MPO) has been implicated in the pathogenesis of severe influenza-induced pneumonia because extracellularly released MPO mediates the production of hypochlorous acid, a potent tissue injury factor. To search for candidate anti-influenza compounds, we screened leucomycin A3 (LM-A3), spiramycin (SPM), an erythromycin derivative (EM900, in which anti-bacterial activity has been eliminated), and clarithromycin (CAM), by analyzing their ability to inhibit MPO release in neutrophils from mice and humans. When each candidate was injected into mice infected with a lethal dose of A/H1N1 influenza virus (PR-8), LM-A3 produced the highest survival rate (80.9%). We found that LM-A3 induced beneficial effects on lung pathology and viral proliferation involved in the regulatory activity of MPO release, pro-inflammatory cytokines and interferon-α production in the lung. SPM and EM900 also induced positive survival effects in the infected mice, whereas CAM did not. We further found that these compounds inhibit virus proliferation in human pneumonia epithelial A549 cells in vitro. LM-A3 showed effective action against influenza A virus infection with high anti-viral activity in human host cells, indicating the possibility that LM-A3 is a prospective lead compound for the development of a drug for human influenza. The positive survival effect induced by EM900 suggests that pharmacological architectures between anti-bacterial and anti-influenza virus activities can be dissociated in macrolide derivatives. These observations provide valuable evidence for the potential development of novel macrolide derivatives that have strong anti-viral but no anti-bacterial activity.
[Mh] Termos MeSH primário: Antivirais/farmacologia
Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos
Influenza Humana/tratamento farmacológico
Josamicina/farmacologia
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Claritromicina/farmacologia
Citocinas/metabolismo
Modelos Animais de Doenças
Progressão da Doença
Desenho de Drogas
Células Epiteliais/virologia
Eritromicina/análogos & derivados
Eritromicina/farmacologia
Feminino
Seres Humanos
Influenza Humana/virologia
Pulmão/citologia
Pulmão/virologia
Camundongos
Camundongos Endogâmicos BALB C
Neutrófilos/efeitos dos fármacos
Neutrófilos/metabolismo
Peroxidase/efeitos dos fármacos
Peroxidase/metabolismo
Espiramicina/farmacologia
Taxa de Sobrevida
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 ((8R,9S)-8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A); 0 (Antiviral Agents); 0 (Cytokines); 63937KV33D (Erythromycin); 8025-81-8 (Spiramycin); EC 1.11.1.7 (Peroxidase); H1250JIK0A (Clarithromycin); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1405
[Cu] Atualização por classe:140327
[Lr] Data última revisão:
140327
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140206
[St] Status:MEDLINE
[do] DOI:10.1038/ja.2013.132


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[PMID]:24374276
[Au] Autor:Zhao Z; Jin L; Xu Y; Zhu D; Liu Y; Liu C; Lei P
[Ad] Endereço:State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijin
[Ti] Título:Synthesis and antibacterial activity of a series of novel 9-O-acetyl- 4'-substituted 16-membered macrolides derived from josamycin.
[So] Source:Bioorg Med Chem Lett;24(2):480-4, 2014 Jan 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of novel 9-O-acetyl-4'-substituted 16-membered macrolides derived from josamycin has been designed and synthesized by cleavage of the mycarose of josamycin and subsequent modification of the 4'-hydroxyl group. These derivatives were evaluated for their in vitro antibacterial activities against a panel of Staphylococcus aureus and Staphylococcus epidermidis. 15 (4'-O-(3-Phenylpropanoyl)-9-O-acetyl-desmycarosyl josamycin) and 16 (4'-O-butanoyl-9-O-acetyl-desmycarosyl josamycin) exhibited comparable activities to josamycin against S. aureus (MSSA) and S. epidermidis (MSSE).
[Mh] Termos MeSH primário: Antibacterianos/síntese química
Josamicina/síntese química
Josamicina/farmacologia
Staphylococcus aureus/efeitos dos fármacos
Staphylococcus epidermidis/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antibacterianos/farmacologia
Cristalografia por Raios X
Josamicina/análogos & derivados
Macrolídeos/síntese química
Macrolídeos/farmacologia
Testes de Sensibilidade Microbiana/métodos
Staphylococcus aureus/fisiologia
Staphylococcus epidermidis/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Macrolides); HV13HFS217 (Josamycin)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:140113
[Lr] Data última revisão:
140113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131231
[St] Status:MEDLINE



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