<b>AIMb>To identify the components of acetylleucomycin and its hydrolytic products by LC-MS.

<b>METHODSb>Acetylleucomycin was separated on a Diamonsil C18 column with 0.1 mol x L(-1) ammonium acetate-acetontrile (35 : 65) as mobile phase. The LC-MS was equipped with an electorspray ion source (ESI), which was set at the positive ion mode, and the mass spectra of each component in chromatogram were obtained with difference cone voltage.

<b>RESULTSb>The components of acetylleucomycin and its hydrolytic products can be separated by HPLC. The components were identified according to the molecular weight and its major mass fragment ions. The major components identified in domastic acetylleucomycin were acetylleucomycin A4, A5; acetylleucomycin A1, A3; acetylleucomycin A6, A7, and acetylleucomycin A13. The hydrolytic products of acetylleucomycin were not kitasamycin, but some non-complete hydrolytic product.

<b>CONCLUSIONb>The method is rapid, sensitive and specific. It' s suitable to application in the fields of multi-components antibiotics analysis.

Chromatography, Liquid ; methods ; Hydrolysis ; Josamycin ; analysis ; chemistry ; Kitasamycin ; analogs & derivatives ; analysis ; chemistry ; Leucomycins ; analysis ; chemistry ; Macrolides ; analysis ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; methods

This study introduced Macrolid antibiotic class including effects, classification, pharmacokinetics, indication of treatment, and future prospects
Macrolides ; Pharmacokinetics

BACKGROUND: Although the incidence of resistance to macrolides in group A streptococci (GAS) was low in the past, high incidences have now been reported from several countries. We tried to find out trends of the incidence of erythromycin-resistant GAS in Korea before and after adopting the separation of the dispensary from medical practice in the middle of the year 2000. METHODS: Five hundred thirty two isolates from children with suspected pharyngotonsillitis from 1998 through 2002 were serotyped by T-agglutination. Minimal inhibitory concentrations of 330 out of 532 isolates were determined by agar dilution methods. RESULTS: The prevalent T-serotypes were T12 (36.1%), T4 (12.8%), T1 (10.9%), T2/28 (8.8%), and nontypable (7.1%). Resistance rates to erythromycin (EM) by year were 46.2% in 1998, 18.4% in 1999, 15.4% in 2000, 27.6% in 2001, 36.5% in 2002. T12 in 1999 and 2000 were 36.4% and 25.9%, respectively, which seem to be lower than any other year. This relative low percentage of T12 is associated with increasing percentage of T1 in the same year. The frequency of T12, T1,and T4 were high in each group of isolates of Seoul and Masan. From this viewpoint, there was a similarity between the distribution of T-serotypes of both groups of Seoul and Masan. CONCLUSION: The frequency of serotype T12 and T4 of GAS were relatively high in Korea from 1998 through 2002. The low rate of EM resistance in 1999 and 2000 seemed to be caused by a sudden increase of T1. The increasing rate of EM resistance from 2000 to 2002 seemed to be caused by the increase in consumption of new macrolides and the increase of T12.
Agar ; Child ; Erythromycin ; Humans ; Incidence* ; Korea* ; Macrolides ; Seoul

BACKGROUND: Although the incidence of resistance to macrolides in group A streptococci (GAS) was low in the past, high incidences have now been reported from several countries. We tried to find out trends of the incidence of erythromycin-resistant GAS in Korea before and after adopting the separation of the dispensary from medical practice in the middle of the year 2000. METHODS: Five hundred thirty two isolates from children with suspected pharyngotonsillitis from 1998 through 2002 were serotyped by T-agglutination. Minimal inhibitory concentrations of 330 out of 532 isolates were determined by agar dilution methods. RESULTS: The prevalent T-serotypes were T12 (36.1%), T4 (12.8%), T1 (10.9%), T2/28 (8.8%), and nontypable (7.1%). Resistance rates to erythromycin (EM) by year were 46.2% in 1998, 18.4% in 1999, 15.4% in 2000, 27.6% in 2001, 36.5% in 2002. T12 in 1999 and 2000 were 36.4% and 25.9%, respectively, which seem to be lower than any other year. This relative low percentage of T12 is associated with increasing percentage of T1 in the same year. The frequency of T12, T1,and T4 were high in each group of isolates of Seoul and Masan. From this viewpoint, there was a similarity between the distribution of T-serotypes of both groups of Seoul and Masan. CONCLUSION: The frequency of serotype T12 and T4 of GAS were relatively high in Korea from 1998 through 2002. The low rate of EM resistance in 1999 and 2000 seemed to be caused by a sudden increase of T1. The increasing rate of EM resistance from 2000 to 2002 seemed to be caused by the increase in consumption of new macrolides and the increase of T12.
Agar ; Child ; Erythromycin ; Humans ; Incidence* ; Korea* ; Macrolides ; Seoul

BACKGROUND: Erythromycin (EM) or other macrolides have been used commonly for the treatment of bacterial pharyngitis. Recently, however, EM-resistant group A streptococci (GAS) are being reported with increasing frequency. The phenotypic expression of macrolide resistance is classified as constitutive, inducible, and M. EM resistance is mediated by ermB, ermTR, or mefA genes. The emm gene encoding M protein has variable sequences at 5'end terminus. METHODS: GAS was isolated from patients with acute pharyngitis at a local clinic in Jinju from November 2001 to May 2002. Antimicrobial susceptibility testing was performed using the disk diffusion method. The phenotypes of EM and clindamycin (CC) resistance were evaluated, and the frequency of ermB and mefA genes was determined by PCR. The emm genotype was identified with PCR and sequencing. RESULTS: A total of 125 strains of group A streptococci was isolated. The resistance rate to EM and CC was 44.8% and 19.2%, respectively. Constitutive resistance was observed in 42.1%, M phenotype in 57.9%, but inducible resistance was not seen. The ermB and mefA genes were positive in 39.3% and 58.9%, respectively. Most emm12 strains showed constitutive resistance, while emm18 and emm75 showed M phenotype. CONCLUSIONS: The EM and CC resistance rates of group A streptococci isolated from acute pharyngitis were remarkably high compared to the previous reports. M phenotype was more common than constitutive resistance in acute pharyngitis. The resistance pattern was variable according to the emm types, suggesting an association between the emm gene and resistant genes.
Clindamycin* ; Diffusion ; Erythromycin* ; Genotype ; Gyeongsangnam-do ; Humans ; Macrolides ; Pharyngitis* ; Phenotype ; Polymerase Chain Reaction

Macrolides antibiotics synthesized by Streptomyces strains are prescribed widely and seldom produce hypersensitivity reactions, even when administered topically. Consequently, they are considered very safe drugs. We report the case of a 32.year.old woman who developed anaphylactic shock after ingesting erythromycin, which she had taken twice before. The previous exposure to erythromycin, clinical findings, and a positive skin intradermal test with erythromycin (10 mg/mL) support the postulate that anaphylaxis was induced by erythromycin.
Anaphylaxis ; Anti-Bacterial Agents ; Erythromycin ; Female ; Humans ; Hypersensitivity ; Intradermal Tests ; Macrolides ; Skin ; Skin Tests ; Streptomyces

Erythromycin is a macrolide antibiotic and inhibits bacterial protein synthesis by stimulating the dissociation of the peptidyl-tRNA molecule from the ribosomes during elongation. The use of macrolides has increased dramatically over the last few years and has led to an increase in bacterial resistance to these antibiotics. Bacterial resistance to erythromycin is generally conferred by the ribosome methylation and/or transport (efflux) protein genes. Among the identified erythromycin-resistant genes, erm(B) (erythromycin methylation) and mef(A) (macrolide efflux) are generally detectable in erythromycin-resistant streptococcal species. The distribution of these genes in oral streptococcal isolates has been reported in studies from other countries but has not been previously examined in a Korean study. We here examined by PCR the presence of erm(B) and mef(A) in oral streptococci isolated from Korean dental plaques. Among the 57 erythromycin-resistant strains tested, 64.9% harbored erm(B) whereas 40.4% were positive for mef(A). Eleven isolates had both the erm(B) and mef(A) genes. Twenty six isolates had only erm(B) and 12 isolates had only mef(A). Eight of the 57 strains examined were negative for both genes.
Anti-Bacterial Agents ; Bacterial Proteins ; Dissociative Disorders ; Erythromycin ; Incidence ; Macrolides ; Methylation ; Polymerase Chain Reaction ; Ribosomes ; RNA, Transfer, Amino Acyl

BACKGROUND: Up to 90% of a theophylline dose is biotransformed, by interaction with one or more the variants of the cytochrome P-450 drug metabolism system. Macrolides affect the elimination of theophylline by influencing on the microsomal enzyme systems. We evaluate the effect of erythromycin and new macrolides on the serum theophylline level and clearance. METHOD: Subjects consisted of moderate asthmatic patients with normal renal and hepatic functions. All subjects were non-smokers and treated with oral theophylline 400mg per day. We randomly assigned 53 patients into four groups. Each group was treated with one macrolides, the first group erythromycin(n: 19, 500 mg bid), second roxitbromycin (n: 14. 150 mg bid), third clarithromycin (n: 10, 250 mg bid) and fourth azithromycin(n: 10, 250 mg bid). We measured the serum theophylline level and clearance at three intervals, at pretreatment, after the first and fourth week after receiving the following macrolides, erythromycin, roxithromycin and clarithromycin. When azithromycin was administered, the serum theophylline level was measured at pretreatment and after one week of treatment They were measured by a computerized program of Bayesian method. RESULTS: When compared with control, erytbromycin and roxithromycin-treated groups had a significantly elevated serum theophylline level and decreased clearance. However, there were no significant changes of the serum theophylline level and clearance in clarithromycin and azithromycin-treated groups. CONCLUSION: These results suggest that theophylline dose may need to be readjusted and have periodic drug monitoring when erythromycin or roxithromycin is administered concurrenfly.
Azithromycin ; Bayes Theorem ; Clarithromycin ; Cytochrome P-450 Enzyme System ; Drug Monitoring ; Erythromycin* ; Humans ; Macrolides* ; Metabolism ; Roxithromycin ; Theophylline*

Serological methods for the epidemiological study of Streptococcus pyogenes, such as T-, or M-typing, were replaced by emm typing in the 2000s. The frequency of emm types may differ according to ographical area and study period. Erythromycin resistance rates and the prevalence of erythromycin-resistant phenotypes in several countries are surveyed, and common emm genotypes associated with erythromycin resistance are described for each country. There is no correlation between erythromycin resistance and macrolide use in Korea. S. pyogenes is thought to cause severe illness, such as streptococcal toxic shock syndrome (STSS) and necrotizing fasciitis. The mortality rate of STSS is about 50%, and there have been several hundred victims of STSS in Japan in the last 2 decades. The resistance rate to macrolides peaked at 50% in 2002, and currently, <10% of strains exhibit macrolide resistance in Korea. However, the erythromycin resistance rate recently exceeded 90% in China. Considering increases of travel between neighboring countries, a vigilant survey to monitor these highly virulent and antibiotic-resistant strains is necessary.
China ; Epidemiologic Studies ; Erythromycin ; Fasciitis, Necrotizing ; Genotype ; Japan ; Korea ; Macrolides ; Organothiophosphorus Compounds ; Phenotype ; Prevalence ; Shock, Septic ; Streptococcus ; Streptococcus pyogenes

Diffuse panbronchiolitis (DPB) is a pulmonary disease characterized by chronic inflammation of the bronchioles and chronic infiltration of inflammatory cells in the lungs. Macrolides are effective therapeutic agents for chronic respiratory tract diseases, such as DPB. However, the mechanisms by which macrolides modulate the immune responses in patients with DPB remain unclear. To understand clinical efficacy for the treatment of DPB by macrolides, the effects of erythromycin (EM) on the expression of pro-inflammatory cytokines such as interleukin-6 (IL-6) and interleukin-8 (IL-8) by human neutrophils were examined. Pre-treatment with EM significantly decreased the expression of IL-6 and IL-8 transcripts by lipopolysaccharide (LPS)-stimulated human neutrophils. EM also reversed the enhanced survival of human neutrophils by LPS. These data indicate that EM has achieved therapeutic effect for patients with DPB, in part, through decreasing the expression of pro-inflammatory cytokines and the survival of neutrophils.
Apoptosis* ; Bronchioles ; Cytokines ; Erythromycin* ; Humans* ; Inflammation ; Interleukin-6* ; Interleukin-8* ; Lipopolysaccharides ; Lung ; Lung Diseases ; Macrolides ; Neutrophils* ; Respiratory Tract Diseases