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Glaucoma is the leading cause of blindness worldwide. However, its surgical treatment, in particular via trabeculectomy, can be complicated by fibrosis. In current clinical practice, application of the drug, Mitomycin C, prevents or delays fibrosis, but can lead to additional side effects, such as bleb leakage and hypotony. Previous in silico drug screening and in vitro testing has identified the known antibiotic, josamycin, as a possible alternative antifibrotic medication with potentially fewer side effects. However, a suitable ocular delivery mechanism for the hydrophobic drug to the surgical site does not yet exist. Therefore, the focus of this paper is the development of an implantable drug delivery system for sustained delivery of josamycin after glaucoma surgery based on crosslinked γ-cyclodextrin. γ-Cyclodextrin is a commonly used solubilizer which was shown to complex with josamycin, drastically increasing the drug’s solubility in aqueous solutions. A simple γ-cyclodextrin crosslinking method produced biocompatible hydrogels well-suited for implantation. The crosslinked γ − cyclodextrin retained the ability to form complexes with josamycin, resulting in a 4-fold higher drug loading efficiency when compared to linear dextran hydrogels, and prolonged drug release over 4 days.

New spectrophotometric methods have been developed for the determination of josamycin in pure and dosage forms based on charge transfer reactions. Method-A was based on the complexation reaction of 1,2-naphthoquinone-4-sulphonate with josamycin. Complex absorbance was measured at 454 nm. Method-B was developed by the charge transfer reaction of the amino group of josamycin with menadione. The formed orange products showed maximum absorbance at 458 nm. Lambert Beer’s law was obeyed in the range of 1.0–28.8 μg/mL. The regression plots showed good linearity with determination coefficients of 0.9997. Molar absorptivity and Sandell’s sensitivity were calculated, with a detection limit (LOD) down to 0.28 μg/mL and quantification limits (LOQ) of 0.85–0.89 μg/mL. The validity of procedures was tested for accuracy, precision, recovery and interference and the results were in accordance with ICH guidelines, with relative standard deviation (RSD %) values less than 5.0%. Determination results of josamycin in marketed formulations were in good agreement with the labelled quantities and without any interference from excipients, indicating that they can be used for quality control purposes.

Glaucoma is the leading cause of blindness worldwide. However, its surgical treatment, in particular via trabeculectomy, can be complicated by fibrosis. In current clinical practice, application of the drug, Mitomycin C, prevents or delays fibrosis, but can lead to additional side effects, such as bleb leakage and hypotony. Previous in silico drug screening and in vitro testing has identified the known antibiotic, josamycin, as a possible alternative antifibrotic medication with potentially fewer side effects. However, a suitable ocular delivery mechanism for the hydrophobic drug to the surgical site does not yet exist. Therefore, the focus of this paper is the development of an implantable drug delivery system for sustained delivery of josamycin after glaucoma surgery based on crosslinked γ-cyclodextrin. γ-Cyclodextrin is a commonly used solubilizer which was shown to complex with josamycin, drastically increasing the drug's solubility in aqueous solutions. A simple γ-cyclodextrin crosslinking method produced biocompatible hydrogels well-suited for implantation. The crosslinked γ - cyclodextrin retained the ability to form complexes with josamycin, resulting in a 4-fold higher drug loading efficiency when compared to linear dextran hydrogels, and prolonged drug release over 4 days.

Community-acquired pneumonia remains one of the most pressing problems in pediatrics. The article presents data on its prevalence, child mortality from this disease, diagnostic criteria and approaches to therapy. In the Russian Federation, respiratory diseases in children aged 0-17 take third place in the structure of causes of death after external causes and malformations. The age characteristics of the etiological spectrum of community-acquired pneumonia in children and the problem of drug resistance of pathogens are discussed in detail. The sharp increase in resistance to macrolide antibiotics of the most common pathogen of the disease in early and pre-school age, pneumococcus, which occurred in recent years, makes it necessary to reconsider the question of the place of these drugs in pediatric practice. At the same time, macrolides remain highly active against atypical pathogens, whose etiological significance increases with age. In this regard, modern indications for prescription of macrolides, unique distinctions of 16-membered josamycin macrolide from other drugs of this series, and mechanisms of its action are reviewed and clarified in the article. Due to the peculiarities of its chemical structure, josamycin remains active against a significant part of pneumococci, which is increasingly resistant to 14- and 15-membered macrolides. The advantages of children’s dosage forms are presented, in particular, the dispersible tablet (solutab). This form, due to controlled release, provides convenience of use, maximum bioavailability (regardless of food intake), minimal frequency of side effects, and does not affect the gastrointestinal motility. Treatment of pneumonia and other respiratory tract infections, especially in young children, is not limited by antibiotics, is always complex and is based on the prevailing syndromes in the clinical picture.

The polymeric form ofjosamycin was developed by loading of the antibiotic into spherical submicron particles made of poly(DL- lactide-co-glycolide) (PLGA 50/50) by double emulsion method. The average diameter and zeta-potential of particles synthesized were less than 150 nm and -35 mV respectively. Polymeric form showed antimicrobial activity against gram-positive, gram-negative, and atypical bacteria. The highest antibacterial activity compared to substance (more than 8-fold) was detected against Enterococcus faecalis. The results of in vivo studies of specific activity of drugs on the model of staphylococcal sepsis in mice showed an increase in the efficacy of the studied polymeric form by 1.5-fold compared with the josamycin substance.

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The article describes state-of-the-art knowledge regarding etiology, epidemiology, clinical features and diagnostic criteria for respiratory infections caused by Mycoplasma pneumoniae (M. pneumoniae). It presents the characteristics of the main forms of lesions in mycoplasma infections of the respiratory tract – pharyngitis, bronchitis and pneumonia. Particular attention is paid to the differential diagnosis of community-acquired pneumonia of pneumococcal and mycoplasma etiology. The issues of rational choice of initial etiotropic therapy for the treatment of respiratory mycoplasmosis in children are discussed.

Different statistical studies showed that chronic prostatitis (CP) is the most common urological disease among men aged 20 to 40 years. The etiological nature of intracellular pathogens in the development of CP is currently finding more and more evidence. The prostate extract acting on various pathogenesis units is of particular interest, taking into account the variety of pathogenetic mechanisms of the development of CP. A study of the efficacy and safety of prostate extract (rectal suppositories) combined with josamycin was conducted. Findings. Patients with CP caused by intracellular pathogens received josamycin therapy. The prostate extract was included in the treatment (rectal suppositories) in Group I. Both groups showed a significant improvement in symptoms and quality of life on the NIH-CPSI scale, both in total and in individual domains, and the differences between the groups were statistically insignificant. The number of leukocytes in the prostate gland secret reduced more significantly in the active treatment group.Thus, the use of prostate extract increased the clinical efficacy of treatment, which correlates with data from the previous studies.

In this study, a kitasamycin (KIT) hapten was prepared through the o-carboxymethoxylamine method and used to produce a monoclonal antibody against KIT and josamycin (JOS). The half inhibition concentration for an indirect competitive enzyme-linked immunosorbent assay was 1.49 and 2.67 ng/mL, respectively. Based on this antibody, a gold immunochromatographic assay (GICA) was developed for the detection of KIT and JOS residues in milk and egg samples. A hand-held strip scanner was used for quantitative analysis, with limits of detection for KIT and JOS of 1.51 and 1.91 μg/L in milk, and 3.0 and 2.72 μg/kg in eggs. The proposed GICA was validated by LC–MS/MS, which indicated that the GICA method would be a useful tool for the on-site detection of KIT and JOS residues in milk and egg samples.

Mycoplasma genitalium is one of the obligate pathogens that cause sexually transmitted diseases. To detect this pathogen in routine practice, only molecular genetic methods are used that are also used to identify the resistance of MGE to antibiotics. The first-line drugs for the treatment of diseases caused by MGE, are tetracycline and macrolides. In recent years, many countries have increasingly recorded cases of unsuccessful therapy macrolides. Mutations that confer antibiotic resistance to macrolides for Mycoplasm genitalium are concentrated in nucleotide positions 2058 and 2059 in region V of the 23S rRNA gene. Unknown status of macrolide resistance M. genitalium can lead to the development of a persistent infection. We describe the first reported cases of clinical josamycin treatment failure from patient with ure - thritis. The reason for antibiotic resistance was a mutation in the 23S rRNA of MGE as a nucleotide substitution in position A2058G.

A simple, inexpensive and efficient agar diffusion bioassay, applying cylinder plate method, for determination of josamycin (JOS) in pure and pharmaceutical dosage forms was studied. Using a strain of Micrococcus luteus ATCC 9341 as the test organism, JOS at concentrations ranging from 0.1 to 0.5 μg/mL could be measured. The calibration graph was linear with good correlation coefficient (r = 0.999), and the method validation showed that it was specific and robust. The interference effects of degradation products and excipients were investigated in order to assess the method selectivity. The proposed method was successfully applied to estimate JOS content in tablets and suspension with good precision (intra-day RSD=0.87%; inter-day RSD=1.25%) and accuracy; the recovery values were between 97.74 and 101.13%. Bioassay was correlated with UV spectrophotometric and high performance liquid chromatographic techniques. The results obtained by these three methods were statistically analyzed by analysis of variance (ANOVA), which indicated that there was no significant difference among these methods. Therefore, we recommend this microbiological assay for drug analysis in routine quality control of josamycin in pharmaceuticals as an alternative to the physicochemical methods reported in the literature. [ABSTRACT FROM AUTHOR]

The article present data on current approaches to laboratory diagnostics and treatment of urogenital chlamydia infection in women. According to Russian and foreign guidelines, azithromycin, josamycin and doxycycline monohydrate belong to the most efficient antimicrobial drugs for the treatment of urogenital chlamydia infection in non-pregnant women. As for the treatment of pregnant patients suffering from this pathology, azithromycin and josamycin are the most optimal drugs in terms of safety and treatment efficacy according to both Russian and foreign guidelines.

Goal. Improving the effectiveness of anti-Helicobacter therapy by overcoming the growing resistance of H. pylori to antibacterial drugs. Methods. The study included 120 male and female patients aged 18 to 65 years with gastric ulcer and 12 duodenal ulcer associated with H. pylori infection, who had not received eradication therapy before and at the time of gastrobioptate intake and had not taken proton pump inhibitors (PPIS) fifteen days prior to the study. To compare the effectiveness of the antihelicobacteric regimens used, patients with almost identical complaints were divided into two groups of 60 patients each by random selection. For each group, appropriate combinations of drugs were used: scheme No. 1 – rabeprazole 20 mg 2 times a day + clarithromycin 500 mg 2 times a day + amoxicillin 1000 mg 2 times a day and scheme No. 2 – rabeprazole 20 mg 2 times a day + josamycin 500 mg 2 times a day + amoxicillin 1000 mg 2 times a day. A probiotic (lactobacillus rhamnosus GG-6milyard, saccharomyces boulardii-2,5 milyard, Bifidobacterium lactis Bb-12, inulin-50mq) was added to both groups to level the side effects of the antibiotics used and to improve the results of the applied ET. After the end of the 10-day course of antibiotic therapy, patients of both groups continued to receive rabeprazole for the next four weeks. The morphological picture in dynamics was studied in 40 patients from each group before and after treatment. To do this, FGDs was combined with a targeted biopsy of 5 points of the mucous membrane. Results. In patients of both groups of 40 people in each, included in the morphological study, inflammation was recorded in both the fundal and antral part of the stomach, and in the duodenal zone, the inflammatory process was observed in the first group in 17 (42.5%), and in the second in 14 (35.0%) people. In 30 (75.0%) patients of group 1, in 26 (65.0%) patients of group 2, gastritis activity was mainly more pronounced in the antrum compared to the fundal. Thus, in the fundal part of the stomach in 10 (25.0%) of the first, in 14 (35.0%) of the studied patients of the 2nd group, the activity of the process was noted. In both comparison groups, the activity of inflammation was mainly strong and moderate. The atrophic process was mainly registered in the antral part of the stomach – in the first group in 32 (26.7%) people, in the second in 30 (25.0%) patients. Fundus atrophy was observed in 8 (6.7%) patients of the first group and 5 (4.2%) people of the second group. By overcoming H. pylori resistance to antibiotics (to clarithromycin) by optimizing the classical three-component scheme with the replacement of clarithromycin with josamycin and the addition of probiotic to the approved schemes leads to an increase in the effectiveness of antiHelicobacter treatment. This fact in this study is clearly demonstrated when comparing the dynamics of endoscopic and histo-morphological pictures of the gastric mucosa and 12 – duodenum in patients of both study groups. Conclusion. The replacement of clarithromycin with josamycin in the classical three-component antihelicobacter scheme leads to a significant improvement in endoscopic and morphological parameters in patients suffering from gastric ulcer and 12-duodenal ulcer associated with H. pylori infection.

The prevalence of antibiotic-resistant urogenital mycoplasmas and ureaplasmas has been gradually increasing over the years, leading to greater concern for accurate diagnosis and treatment. In this study, the antimicrobial resistance trends in Greece were analyzed using 2992 Ureaplasma spp. and 371 M. hominis isolates collected between 2014 and 2022. Antibiotic sensitivity was determined using eight different antimicrobial agents (josamycin, pristinamycin, clindamycin, ofloxacin, azithromycin, tetracycline, erythromycin, and doxycycline), with the data analyzed using descriptive statistical methods. Resistance rates to clindamycin and erythromycin increased for both M. hominis and Ureaplasma spp., while remaining relatively low for Tetracycline, Doxycycline, and Ofloxacin. For Ureaplasma spp., high susceptibility was observed to pristinamycin, tetracycline, doxycycline, azithromycin, and josamycin, and intermediate susceptibility to erythromycin. However, the resistance rate for clindamycin dramatically increased from 60% in 2014 to a peak of 98.46% in 2021, and the erythromycin resistance rate increased from 9.54% in 2018 to 22.13% in 2021. M. hominis exhibited consistently high resistance rates to Erythromycin, while Azithromycin resistance significantly increased over time, from 52.78% in 2017 to 97.22% in 2022. The alarming escalation in antibiotic-resistant urogenital mycoplasmas and ureaplasmas in the Greek population is a significant concern. Antibiotic overconsumption may have played a crucial role in increasing resistance trends. The implementation of nationwide surveillance systems, proper antibiotic stewardship policies, and appropriate culture-based therapy policies are necessary to effectively control this emerging risk., (© 2023. The Author(s), under exclusive licence to the Japan Antibiotics Research Association.)

In this study, a kitasamycin (KIT) hapten was prepared through the o-carboxymethoxylamine method and used to produce a monoclonal antibody against KIT and josamycin (JOS). The half inhibition concentration for an indirect competitive enzyme-linked immunosorbent assay was 1.49 and 2.67 ng/mL, respectively. Based on this antibody, a gold immunochromatographic assay (GICA) was developed for the detection of KIT and JOS residues in milk and egg samples. A hand-held strip scanner was used for quantitative analysis, with limits of detection for KIT and JOS of 1.51 and 1.91 μg/L in milk, and 3.0 and 2.72 μg/kg in eggs. The proposed GICA was validated by LC–MS/MS, which indicated that the GICA method would be a useful tool for the on-site detection of KIT and JOS residues in milk and egg samples. [ABSTRACT FROM AUTHOR]

In this study, a new and accurate method based on ultra-high performance liquid chromatography (UHPLC) with electrospray ionisation tandem triple quadrupole mass spectrometry (MS/MS) was developed and validated for the determination of josamycin in three kinds of feeds (compound, concentrated and premix feeds). The optimised sample pretreatment procedure included extracting from the matrix with a mixture of methanol and acetonitrile (1:1, v/v) followed by drying under nitrogen and redissolving in phosphate buffer solution (pH = 8, 0.1 mol/L) followed by purifying using HLB cartridges. Validation of the method was carried out in three different matrices (compound, concentrated and premix feed) by recovery experiments, using samples spiked at concentration levels of 20, 100 and 200 μg/kg. Satisfactory recoveries from 82.4% to 93.0%, with RSDs lower than 17.4% under intermediate precision conditions were obtained in all feed matrices tested. The developed method was applied to commercially samples and josamycin was found frequently in feed containing kitasamycin. [ABSTRACT FROM AUTHOR]

A smart, sensitive, and green turn-off fluorescence probe was developed and validated for the determination of two macrolides; spiramycin (SPM) and josamycin (JSM) at submicromolar concentration levels. The probe is based on the fluorone-based dye, eosin Y that efficiently interacts with the two compounds through ground-state ion-pair complex formation with quenching of its native fluorescence (λ ex /λ em of 524/548 nm). The Stern-Volmer relationship confirmed the static fluorescence quenching mechanism. Furthermore, the thermodynamic parameters of the reaction were explored via the van't Hoff plot. The values of the fluorescence quenching were linearly correlated to the drug concentration over the ranges of 0.12–5.93 and 0.30–9.66 μM (0.1–5.0 and 0.25–8.0 μg/mL) for SPM and JSM, respectively. Therefore, the probe was utilized for quality control of the two compounds in their tablets with mean %recoveries of 98.12 ± 1.72 and 97.22 ± 1.51% for SPM and JSM, respectively. Statistical analysis of the results by t - and F -tests showed excellent agreement with the results of the comparison methods. Moreover, the developed probe was applied for stability testing of the two compounds under oxidative condition along with ESI+-MS identification of the potential degradants. Besides, the greenness of the developed probe was ensured by different assessment metrics. Hence, the developed method is the first stability-indicating fluorimetric assay for the two compounds, and its chief merits include effortlessness, rapidness, sensitivity, cheapness and harmony with the green chemistry rules. • First fluorescence probe for determination of spiramycin and josamycin by turn-off mechanism using eosin Y. • Very rapid, simple, and green determination with LODs in nanomolar levels. • Stern-Volmer relationship revealed static quenching via ground-state complexation. • The probe is a specific stability-indicating tool in the presence of oxidative degradants. • Identification of the oxidative degradants by mass spectrometry for the first time. [ABSTRACT FROM AUTHOR]

The article provides latest information on the natural macrolide antibiotic josamycin, results of local and foreign trials of sensitivity and resistance of various kinds of pathogens to josamycin, evidence and success of using the antibiotic drug in the treatment of acute respiratory infections in children.

Aims Josamycin has immunomodulatory properties independent of its antibacterial actions. This study was designed to explore the influences and associated mechanisms of josamycin upon the generation of proinflammatory mediators in murine macrophages activated with lipopolysaccharide (LPS) from Prevotella intermedia , a pathogenic bacterium associated with periodontal disease. Main methods LPS was purified by employing phenol-water extraction protocol. Culture supernatants were analyzed for nitric oxide (NO) and interleukin (IL)-1β. Real-time PCR and immunoblotting were conducted to quantify mRNA and protein expression, respectively. The expression levels of IL-1β were analyzed by confocal laser scanning microscopy. NF-κB-dependent SEAP levels were estimated by reporter assay. Key findings Josamycin significantly attenuated NO production elicited by P . intermedia LPS as well as induction of iNOS protein and mRNA in RAW264.7 cells. While the release of IL-1β from cells stimulated by LPS was suppressed in the presence of josamycin, josamycin failed to reduce the degree of IL-1β mRNA expression. Josamycin did not reduce the stability of IL-1β mRNA induced by P . intermedia LPS, at the same time josamycin also failed to suppress the LPS-induced intracellular IL-1β expression. Josamycin augmented HO-1 induction in cells exposed to P . intermedia LPS, and SnPP, an inhibitor of HO-1 activity, reversed the suppressive impact of josamycin upon NO generation induced by LPS. Josamycin diminished NF-κB transcriptional activity induced by P . intermedia LPS. Further, josamycin enhanced SOCS1 mRNA level in cells activated with LPS. Significance Josamycin suppressed P . intermedia LPS-induced generation of NO and IL-1β in RAW264.7 macrophages via the inhibition of NF-κB activation as well as HO-1 and SOCS1 induction. Josamycin may have benefits as a host modulatory agent in treating periodontal disease. [ABSTRACT FROM AUTHOR]

A facile procedure was developed to synthesize novel N -glycoside josamycin derivatives by coupling 4′-amino-desmycarosyl josamycin derivatives with l- mycarose. A novel N -glycoside josamycin derivative 10a and a key intermediate 9a were designed and synthesized. And two rearranged compounds 9b and 10b were also got. [ABSTRACT FROM AUTHOR]

Bacterial lesion in the oropharynx is a pressing issue in otorhinolaryngology. After flu and acute respiratory infections, sore throat and chronic tonsillitis are the most common human diseases, the prevalence of which, as well as a high probability of a number of diseases of the internal organs (heart, blood vessels, kidneys, joints, etc.) which may develop as a complication of acute or chronic inflammation of the tonsils, determine the relevance of tonsillar pathology [3-5].

Respiratory infections are among the most common diseases of childhood and the main reason for seeking medical help. Most of them are known to be viral; however, a big role among upper and lower respiratory tract infections belongs to those caused by pathogens such as pneumococci, Haemophilus influenzae and pyogenic streptococci. Despite the availability of international guidelines and medical literature on antimicrobial chemotherapy, the percentage of unjustified antibiotic therapies remains high, leading to enhanced resistance of pathogens.

The economic costs of treating infertility using assisted reproductive technologies are a burden even for advanced Western countries.In infertility patients with long and unsuccessfully treatment history, where all available methods, including assisted reproductive technology are present, chronic endometritis is diagnosed in 60% of cases. Overview of research on chronic endometritis, suggests that endometrium contaminated by microorganisms with confirmed subclinical inflammation is the cause of the reduction in fertility. Identification of a microbial agent in endometritis in routine outpatient practice is not mandatory, as the international experience, including research with a high level of evidence proves the expediency of empirical therapy, based on the minimum clinical criteria, because, otherwise, the consequences for the reproductive system may be irreparable. Preventive antibiotic therapy in patients with pre-conception infertility and recurrent miscarriage is an effective way of preventing reproductive losses. Josamycin is the drug of choice for these conditions due to broad-spectrum, high efficacy against intracellular agents and anaerobic microbiota, favorable safety profile, as well as additional systemic anti-inflammatory and immunomodulatory effects.

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 theirin vitroantibacterial activities against a panel of respiratory pathogens.8band8eexhibited 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,21showed the best antibacterial activities. [ABSTRACT FROM PUBLISHER]

Background: The latest region-specific panel of mycoplasma species is often crucial for providing insights into local mycoplasma epidemiology and updating clinical practice guidance., Methods: We retrospectively reviewed reports of 4,166 female outpatients detected by the mycoplasma identification verification and antibiotic susceptibility kit from the last five years., Results: Among them, > 73.3% of cases with Ureaplasma urealyticum or Mycoplasma hominis single infection or co-infection with both species were susceptible to three tetracyclines and one macrolide (josamycin). Additionally, > 84.8%, ≤ 4.4%, and ≤ 39.6% of the U. urealyticum, M. hominis, and co-infection cases, respectively, were susceptible to clarithromycin and roxithromycin. Four quinolones (ciprofloxacin, ofloxacin, sparfloxacin, and levofloxacin) and three macrolides (azithromycin, erythromycin, and acetylspiramycin) were active against < 48.9% of the isolates. Furthermore, 77.8%, 18.4%, and 7.5% of the M. hominis, U. urealyticum, and co-infection cases, respectively, were susceptible to spectinomycin., Conclusions: Tetracyclines and josamycin were the best antibiotics for most mycoplasma-infected patients.

Aim. To study clinical efficacy and antihelicobacter activity of combined treatment of duodenal ulcer (DU) with famotidin (qamatel), metronidasol (trichopol) and jozamycin (walpraphen). Material and methods. A total of 96 patients with uncomplicated DU have been treated (mean age 42.5 ± 1.5 years). The examination included standard tests, endoscopy, pH-metry (on the treatment days 1, 15 and 28), biopsies and prints from the antral stomach and its body. The sections were stained by Gimsefor morphological assessment of duodenal mucosa and detection of Helicobacter pylori (HP). Gastric acid-producing function was examined with intragastric pH-metry. The patients were divided into 3 groups: group 1 received monotherapy with famotidin (20 mg twice a day); group 2 received combined treatment with famotidin (40 mg/day), metronidasol (500 mg twice a day), josamycin (300 mg in 3 doses) for a week with following intake of famotidin alone (40 mg/day) for 3 weeks; group 3 received the same treatment plus clarythromycin. Group 1 patients benefited from the treatment but elimination of pain and dyspeptic syndromes was longer than in groups 2 and 3 (p < 0.05). Ulcer healing to treatment day 28 was observed in 71.8, 90.0 and 88.2%, respectively. Side effects occurred in 0, 10 and 16.7% cases, respectively. Conclusion. 1-week schemes of combined treatment with famotidin, metronidasol, josamycin or clarythromycin are highly effective in DU and their side effect rates are not very high.

We have previously demonstrated the excellent bactericidal activity of josamycin against Staphylococcus aureus isolated from patients with atopic dermatitis (AD), with therapeutic efficacy equal to that of betamethasone. The present study was designed to evaluate the effectiveness of combination therapy with betamethasone and josamycin for AD. Betametasone (0.1%) and josamycin (0.1%) were topically administered to NC/Nga mice with severe AD-like skin lesions. Skin severity scores, histological changes in skin lesions, and serum immunoglobulin E (IgE) levels were assessed as indicators of therapeutic efficacy. Topical treatment with both drugs suppressed the skin severity score to a greater degree than betamethasone alone. This was associated with a reduction of epidermal thickening, a reduced density of dermal cellular infiltration, a decreased mast cell count in the dermis, and a reduced serum IgE level. In addition, both drugs in combination markedly reduced the expression of interferon (IFN)-γ and interleukin (IL)-4 in auricular lymph node cells, as well as the S. aureus count on the lesioned skin. These results show that simultaneous topical application of both drugs can ameliorate severe AD-like skin lesions in NC/Nga mice. It is suggested that combination therapy with betamethasone and josamycin would be beneficial for control of severe AD lesions colonized by S. aureus by inhibiting the development of both T helper (Th) type 1 (Th1) and Th2 cells and also through elimination of superficially located S. aureus.

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. [ABSTRACT FROM AUTHOR]

Background Tylosin and Josamycin are macrolide antibiotics. They are used in the treatment of pneumonia, arthritis and mastitis in cattle, and mycoplasma infections in poultry. The incorrect use of antibiotics has lead to the presence of antibiotic residues in foods. The residues cause toxic effects on consumers. Results A simple and sensitive method was optimized and validated for the analysis of tylosin and josamycin residues in food samples. Analytical separation was performed in less than 10 min using a RP C18 monolithic column with time-programmed UV detection at 287 nm and 232 nm and a micellar solution of 0.17 M sodium dodecyl sulphate, 14% methanol and 0.3% triethylamine in 0.02 M phosphoric acid buffered at pH 4 as the mobile phase. The method was fully validated in accordance with ICH guidelines. The micellar method was successfully applied to quantitatively determine tylosin and josamycin residues in spiked chicken muscles, chicken liver, bovine muscles, liver, milk and eggs. It was also extended to the determination of tylosin and josamycin residues in chicken-based baby food and baby formulae. The compounds were separated by a monolithic column which, on account of its particular structure, could bear higher flow rates than usually found for this kind of analysis. High extraction efficiency for tylosin and josamycin was obtained without matrix interference in the extraction process and in the subsequent chromatographic determination. No organic solvent was used during the pretreatment step. Hence, it is considered an interesting technique for "green" chemistry. Conclusion The proposed method was validated and successfully applied for the determination of tylosin and josamycin residues in spiked chicken muscles, chicken liver, bovine muscles, liver, milk and eggs. It was also extended to the determination of tylosin and josamycin residues in chicken-based baby food and baby formulae. [ABSTRACT FROM AUTHOR]

Abstract: 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). [Copyright &y& Elsevier]