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Bezhan Chankvetadze - One of the best experts on this subject based on the ideXlab platform.
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separation of brombuterol enantiomers in capillary electrophoresis with cyclodextrin type chiral selectors and investigation of structure of selector selectand complexes using nuclear magnetic resonance spectroscopy
Electrophoresis, 2017Co-Authors: Ann Gogolashvili, Elene Tatunashvili, Tamas Sohajda, Lali Chankvetadze, Julianna Szemán, Antonio Salgado, Bezhan ChankvetadzeAbstract:In the present study, the enantiomer migration order (EMO) of Enilconazole in the presence of various cyclodextrins (CDs) was investigated by capillary electrophoresis (CE). Opposite EMO of Enilconazole were observed when β-CD or the sulfated heptakis(2-O-methyl-3,6-di-O-sulfo)-β-CD (HMDS-β-CD) was used as the chiral selectors. Nuclear magnetic resonance (NMR) spectroscopy was used to study the mechanism of chiral recognition between Enilconazole enantiomers and those two cyclodextrins. On the basis of rotating frame nuclear Overhauser (ROESY) experiments, the structure of an inclusion complex between Enilconazole and β-CD was derived, in which (+)-Enilconazole seemed to form a tighter complex than the (-)-enantiomer. This correlates well with the migration order of Enilconazole enantiomers observed in CE. No evidence of complexation between Enilconazole and HMDS-β-CD could be gathered due to lack of intermolecular nuclear Overhauser effect (NOE). Most likely the interaction between Enilconazole and HMDS-β-CD leads to formation of a shallow external complex that is sufficient for separation of enantiomers in CE but cannot be evidenced based on ROESY experiment. Thus, in this particular case CE documents the presence of intermolecular interactions which are at least very difficult to be evidenced by other instrumental techniques.
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Separation of brombuterol enantiomers in capillary electrophoresis with cyclodextrin‐type chiral selectors and investigation of structure of selector‐selectand complexes using nuclear magnetic resonance spectroscopy
Electrophoresis, 2017Co-Authors: Ann Gogolashvili, Elene Tatunashvili, Tamas Sohajda, Lali Chankvetadze, Antonio Salgado, Mehmet Gumustas, Sibel A. Ozkan, Bezhan ChankvetadzeAbstract:In the present study, the enantiomer migration order (EMO) of Enilconazole in the presence of various cyclodextrins (CDs) was investigated by capillary electrophoresis (CE). Opposite EMO of Enilconazole were observed when β-CD or the sulfated heptakis(2-O-methyl-3,6-di-O-sulfo)-β-CD (HMDS-β-CD) was used as the chiral selectors. Nuclear magnetic resonance (NMR) spectroscopy was used to study the mechanism of chiral recognition between Enilconazole enantiomers and those two cyclodextrins. On the basis of rotating frame nuclear Overhauser (ROESY) experiments, the structure of an inclusion complex between Enilconazole and β-CD was derived, in which (+)-Enilconazole seemed to form a tighter complex than the (-)-enantiomer. This correlates well with the migration order of Enilconazole enantiomers observed in CE. No evidence of complexation between Enilconazole and HMDS-β-CD could be gathered due to lack of intermolecular nuclear Overhauser effect (NOE). Most likely the interaction between Enilconazole and HMDS-β-CD leads to formation of a shallow external complex that is sufficient for separation of enantiomers in CE but cannot be evidenced based on ROESY experiment. Thus, in this particular case CE documents the presence of intermolecular interactions which are at least very difficult to be evidenced by other instrumental techniques.
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Enantiomeric resolution of chiral imidazole derivatives using capillary electrophoresis with cyclodextrin-type buffer modifiers
Journal of Chromatography A, 1995Co-Authors: Bezhan Chankvetadze, Gabriele Endresz, Gottfried BlaschkeAbstract:Abstract Enantiomeric resolutions of some chiral pharmaceuticals containing the imidazole (1,3-diazole) moiety were carried out using capillary electrophoresis. Various native cyclodextrins (ga-, β- and γ-cyclodextrin) and derivatized cyclodextrins (hydroxypropyl-, and sulfobutyl ether-β-cyclodextrin) were used as chiral buffer modifiers. The effects of the cavity size, the structure and the charge of the selectors on the chiral recognition ability were evaluated. The influence of the type and concentration of the organic modifier on the separation of miconazole enantiomers and the pH of the run buffer on the separation of Enilconazole enantiomers was also studied.
Francesca Mancianti - One of the best experts on this subject based on the ideXlab platform.
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Canine and feline dermatophytosis due to Microsporum gypseum: a retrospective study of clinical data and therapy outcome with griseofulvin.
Journal de mycologie medicale, 2013Co-Authors: Simona Nardoni, Linda Mugnaini, Roberto Amerigo Papini, M. Fiaschi, Francesca ManciantiAbstract:Summary Objective Microsporum gypseum is a common inhabitant of the soil, occasionally responsible for human and animal ringworm. Few reports describe the treatment of dermatologic diseases due to M. gypseum . The objective of this study was to evaluate retrospectively cases of M. gypseum infection in dogs and cats. Material and methods The occurrence of infection by this dermatophyte was retrospectively evaluated in dermatological specimens from 15,684 dogs and cats dermatologically diseased from Italy. Clinical outcome after treatment with griseofulvin combined with topical Enilconazole was evaluated in 41 dogs and, out of label, 10 cats. Furthermore, in vitro susceptibility to griseofulvin and Enilconazole was evaluated on 31 clinical isolates of M. gypseum . Results One hundred and eighty-five specimens out of 15,684 (1.1%) scored positive for M. gypseum . The treatment failed to achieve both mycological and clinical cure in 16 dogs (39%) and four cats (40%), as well as fungal isolates demonstrated a very poor in vitro sensitivity when tested versus griseofulvin: the MIC value was 150 μg/mL. The ED 50 value was calculated at 66 μg/mL. Conclusion Blind treatments with griseofulvin in ringworm due to M. gypseum should be avoided.
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Antifungal Activity of Tea Tree Oil From Melaleuca Alternifolia Against Trichophyton Equinum: An in Vivo Assay
Phytomedicine : international journal of phytotherapy and phytopharmacology, 2009Co-Authors: F. Pisseri, Simona Nardoni, Alessandra Bertoli, L. Pinto, Luisa Pistelli, Grazia Guidi, Francesca ManciantiAbstract:Dermatophytes are a group of keratinophilic and keratinolytic molds, some of which are responsible for ringworm. Among them Trichophyton equinum, which mostly infects equids, can cause extensive outbreaks in stud farms. The conventional treatment of equine trichophytosis is topic, based upon medicated shampoos to reduce the spread of infection among the animals. Nevertheless the popularity of phytotherapy is at an all-time peak, and the interest for natural alternatives or complements to conventional drug therapy is challenging both in human and veterinary field. Among herbal remedia Tea Tree Oil (TTO) shows a wide range of antimicrobial activities. A randomized open clinical trial was carried out on 60 thoroughbred breeding horses affected by equine ringworm. The animals were randomly divided into 2 groups of 30 subjects. Diagnostic criteria were the presence of clinical signs and positive T. equinum culture. Specificity control using TTO mixture in 5 not dermatophyte affected animals was achieved also. The antimycotic activity against T. equinum of a mixture containing 25% TTO in sweet almond oil, was evaluated in vivo treating 30 subjects, the others were administered Enilconazole 2% solution. The animals of both groups were topically treated twice a day for 15 days with a 25% mixture of TTO diluted in sweet almond oil and every 3 days, four times with Enilconazole rinses, respectively. The clinical and mycological outcome were evaluated at day 30 from the start of the treatments. Data analysis was performed by chi square test. All the treated animals showed complete clinical and aetiological healing. Part of control subjects also, showed an improvement and none of them exacerbate the lesions. This therapeutic protocol appears to be effective and versatile, being applicable immediately after physical examination, prior to have the laboratory response. It could be an alternative for practitioners interested in herbal medicines, contributing to fulfill the gap existing between in vitro and clinical studies.
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a lufenuron pre treatment may enhance the effects of Enilconazole or griseofulvin in feline dermatophytosis
Journal of Feline Medicine and Surgery, 2009Co-Authors: Francesca Mancianti, Sara Dabizzi, Simona NardoniAbstract:The effectiveness of Enilconazole (4 weekly rinses with a 0.2% solution) or griseofulvin (50mg/kg twice daily for 40 days) following a pre-treatment with oral lufenuron (100mg/kg by-weekly for 8 weeks) was tested on 25 (11+14) Microsporum canis infected cats. Control animals were treated with lufenuron, griseofulvin and Enilconazole alone. At day 150 pre-treated animals were culturally negative and clinically cured. While lufenuron alone was found to be ineffective against M canis infection, an immunomodulatory effect of the drug can be suggested, as reported in literature. Its use could be reserved to long-lasting infections, unsuccessfully treated with conventional drugs. Further studies are required to clearly establish the possible adjuvant effect of this molecule when used prior to Enilconazole or griseofulvin.
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Antifungal activity of tea tree oil from Melaleuca alternifolia against Trichophyton equinum: an in vitro assay
'Elsevier BV', 2009Co-Authors: F. Pisseri, Simona Nardoni, L. Pinto, Luisa Pistelli, Grazia Guidi, Bertoli A, Francesca ManciantiAbstract:Dermatophytes are a group of keratinophilic and keratinolytic molds, some of which are responsible for ringworm. Among them Trichophyton equinum, which mostly infects equids, can cause extensive outbreaks in stud farms. The conventional treatment of equine trichophytosis is topic, based upon medicated shampoos to reduce the spread of infection among the animals. Nevertheless the popularity of phytotherapy is at an all-time peak, and the interest for natural alternatives or complements to conventional drug therapy is challenging both in human and veterinary field. Among herbal remedia Tea Tree Oil (TTO) shows a wide range of antimicrobial activities. A randomized open clinical trial was carried out on 60 thoroughbred breeding horses affected by equine ringworm. The animals were randomly divided into 2 groups of 30 subjects. Diagnostic criteria were the presence of clinical signs and positive T equinum culture. Specificity control using TTO mixture in 5 not dermatophyte affected animals was achieved also. The antimycotic activity against T equinum of a mixture containing 25% TTO in sweet almond oil, was evaluated in vivo treating 30 subjects, the others were administered Enilconazole 2% solution. The animals of both groups were topically treated twice a day for 15 days with a 25% mixture of TTO diluted in sweet almond oil and every 3 days, four times with Enilconazole rinses, respectively. The clinical and mycological outcome were evaluated at day 30 from the start of the treatments. Data analysis was performed by chi square test. All the treated animals showed complete clinical and aetiological healing. Part of control subjects also, showed an improvement and none of them exacerbate the lesions. This therapeutic protocol appears to be effective and versatile, being applicable immediately after physical examination, prior to have the laboratory response. It could be an alternative for practitioners interested in herbal medicines, contributing to fulfill the gap existing between in vitro and clinical studies. Published by Elsevier GmbH
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Susceptibility of Microsporum canis isolated from domestic animals against a commercially available Enilconazole in fumigant form
Journal De Mycologie Medicale, 2004Co-Authors: Francesca Mancianti, Simona NardoniAbstract:La contamination de l'environnement represente une source non negligeable d'infection a Microsporum canis soit pour l'animal, soit pour l'homme. Une decontamination convenable serait donc requise dans le cadre des mesures de controle des teignes animales. Cette etude porte sur l'effet antifongique du traitement par l'Enilconazole sous forme de fumigation sur 140 echantillons de spores et 72 de mycelium de M. canis d'origine animale. Le traitement se revele efficace sur 131 echantillons de spores provenant de prelevements de poils d'animaux sur 140 (93,6 %), et dans 66 echantillons de mycelium sur 72 (91,7 %). L'analyse statistique ne demontre aucune difference significative entre la sensibilite du mycelium et des spores. En conclusion, la fumigation d'Enilconazole pourrait etre utilisee pour la decontamination environnementale due a M. canis.
Marcelina Osińska - One of the best experts on this subject based on the ideXlab platform.
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Comparison of in vitro activities of 11 antifungal agents against Trichophyton verrucosum isolates associated with a variety hosts and geographical origin.
Mycoses, 2019Co-Authors: Dominik Łagowski, Aneta Nowakiewicz, Sebastian Gnat, Marcelina OsińskaAbstract:The high prevalence of dermatophytosis in animals is usually associated with extra expenditure on prevention, diagnosis and long-term treatment. Humans are usually infected from animals, also from asymptomatic carriers, through direct contact or indirectly via fungus-bearing hair, scales and fomites. Despite the medical importance of Trichophyton verrucosum infections, there are limited in vitro data on the fungal susceptibility to antifungal drugs, including new-generation triazoles, imidazoles and allyloamines. The aim of the current study was to evaluate comprehensively the in vitro activity of 11 antifungal drugs against a large collection of T. verrucosum isolates obtained in Poland, Latvia, Lithuania and Slovakia from humans and animals using a microdilution assay. In vitro susceptibility testing of 11 antifungal drugs was performed according to the Clinical and Laboratory Standards Institute (CLSI) document M38. The MICs of clotrimazole, ciclopirox, Enilconazole, miconazole, naftifine and terbinafine against all T. verrucosum isolates were below 1 μg/mL, whereas those of fluconazole, griseofulvin, itraconazole, ketoconazole and voriconazole were above 1 μg/mL. Ciclopirox was demonstrated to have superior activity against all strains in comparison with the other drugs, whereas fluconazole exerted the weakest in vitro effect and exhibited the highest MIC values. Our study has shown that drugs of different chemical origin have satisfactory antifungal activity and can be promising candidates for the treatment of T. verrucosum dermatophytosis. Moreover, no significant disparity in drug sensitivity between isolates obtained from different hosts and geographical regions have been demonstrated.
Clercx Cécile - One of the best experts on this subject based on the ideXlab platform.
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Long-term outcome in dogs with sinonasal aspergillosis treated with intranasal infusions of Enilconazole
2007Co-Authors: Schuller S., Clercx CécileAbstract:Long-term outcomes (mean 38+/-17 months) were evaluated in 27 dogs with sinonasal aspergillosis after successful medical treatment using intranasal infusions of 1% or 2% Enilconazole (1%, n=15; 2%, n=12). Long-term outcomes with both treatment protocols were good, with half of the dogs being asymptomatic throughout the follow-up period. The remaining dogs showed mild clinical signs compatible with chronic rhinitis/sinusitis. These clinical signs were interpreted as chronic lymphoplasmacytic rhinitis/sinusitis and episodes of bacterial rather than fungal infection. Three dogs had confirmed reinfection or relapse 2 to 36 months after clinical resolutionPeer reviewe
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Long-term outcome in dogs with sinonasal aspergillosis treated with intranasal infusions of Enilconazole
'American Animal Hospital Association', 2007Co-Authors: Schuller S., Clercx CécileAbstract:peer reviewedaudience: researcher, professional, studentLong-term outcomes (mean 38+/-17 months) were evaluated in 27 dogs with sinonasal aspergillosis after successful medical treatment using intranasal infusions of 1% or 2% Enilconazole (1%, n=15; 2%, n=12). Long-term outcomes with both treatment protocols were good, with half of the dogs being asymptomatic throughout the follow-up period. The remaining dogs showed mild clinical signs compatible with chronic rhinitis/sinusitis. These clinical signs were interpreted as chronic lymphoplasmacytic rhinitis/sinusitis and episodes of bacterial rather than fungal infection. Three dogs had confirmed reinfection or relapse 2 to 36 months after clinical resolutio
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Long-term outcomes in dogs with sinonasal aspergillosis treated with intranasal infusions of Enilconazole
'American Animal Hospital Association', 2007Co-Authors: Schuller S., Clercx CécileAbstract:peer reviewedaudience: researcher, professionalLong-term outcomes ( mean 38 +/- 17 months) were evaluated in 27 dogs with sinonasal aspergillosis after successful medical treatment using intranasal infusions of 1% or 2% Enilconazole ( 1%, n= 15; 2%, n= 12). Long-term outcomes with both treatment protocols were good, with half of the dogs being asymptomatic throughout the follow-up period. The remaining dogs showed mild clinical signs compatible with chronic rhinitis/sinusitis. These clinical signs were interpreted as chronic lymphoplasmacytic rhinitis/sinusitis and episodes of bacterial rather than fungal infection. Three dogs had confirmed reinfection or relapse 2 to 36 months after clinical resolution
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Update on Canine Sinonasal Aspergillosis
'Elsevier BV', 2007Co-Authors: Peeters Dominique, Clercx CécileAbstract:audience: researcher, professionalSinonasal aspergillosis is a frequent cause of nasal discharge that occurs in otherwise healthy, young to middle-aged dogs. A local immune dysfunction is suspected in affected animals, and the role of increased interleukin-10 mRNA expression in the nasal mucosa of affected dogs is currently under investigation. Despite recent advances in imaging techniques, the "gold standard" for diagnosing the disease is direct visualization of fungal plaques during endoscopy or observation of fungal elements on cytology or histopathologic examination. Treatment can be challenging; however, the use of topical Enilconazole or clotrimazole through noninvasive techniques has increased the success of treatment and decreased the morbidity and duration of hospitalization
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Traitement chirurgical de l'aspergillose nasale chez le chien par rhynotomie combinée avec une infusion d'énilconazole
2006Co-Authors: Claeys Stéphanie, Lefebvre J.-b., Schuller S., Hamaide Annick, Clercx CécileAbstract:OBJECTIVES: To evaluate the effectiveness of rhinotomy and surgical debridement associated with topical administration of 2 per cent Enilconazole and oral itraconazole in dogs with severe or recurrent sinonasal aspergillosis. METHODS: A standard rhinotomy was performed on seven dogs. In the initial study, the bone flap was left attached cranially and replaced at the end of the procedure. In the main study group, the bone flap was discarded. Nasal passages were debrided and irrigated with Enilconazole solution for one hour. Oral itraconazole was administered to four dogs for one month postoperatively. Follow-up rhinoscopy was performed in all dogs. RESULTS: All three dogs in the initial study had recurrence of the disease and two dogs had a second surgery to remove the flap. The main study group included four dogs in which the flap was initially removed, and the two dogs from the initial study that required a second surgery. At follow-up rhinoscopy, five dogs were free of aspergillus but had bacterial or inflammatory rhinitis and one dog had a small aspergilloma but was subsequently asymptomatic. Telephone follow-up revealed that four dogs were asymptomatic, one dog had intermittent sneezing and serous nasal discharge, and one dog had intermittent epistaxis. CLINICAL SIGNIFICANCE: Rhinotomy with removal of the flap combined with one-hour infusion of 2 per cent Enilconazole and oral itraconazole resulted in satisfactory outcome in dogs with severe or recurrent aspergillosis.Peer reviewe
Dominik Łagowski - One of the best experts on this subject based on the ideXlab platform.
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Comparison of in vitro activities of 11 antifungal agents against Trichophyton verrucosum isolates associated with a variety hosts and geographical origin.
Mycoses, 2019Co-Authors: Dominik Łagowski, Aneta Nowakiewicz, Sebastian Gnat, Marcelina OsińskaAbstract:The high prevalence of dermatophytosis in animals is usually associated with extra expenditure on prevention, diagnosis and long-term treatment. Humans are usually infected from animals, also from asymptomatic carriers, through direct contact or indirectly via fungus-bearing hair, scales and fomites. Despite the medical importance of Trichophyton verrucosum infections, there are limited in vitro data on the fungal susceptibility to antifungal drugs, including new-generation triazoles, imidazoles and allyloamines. The aim of the current study was to evaluate comprehensively the in vitro activity of 11 antifungal drugs against a large collection of T. verrucosum isolates obtained in Poland, Latvia, Lithuania and Slovakia from humans and animals using a microdilution assay. In vitro susceptibility testing of 11 antifungal drugs was performed according to the Clinical and Laboratory Standards Institute (CLSI) document M38. The MICs of clotrimazole, ciclopirox, Enilconazole, miconazole, naftifine and terbinafine against all T. verrucosum isolates were below 1 μg/mL, whereas those of fluconazole, griseofulvin, itraconazole, ketoconazole and voriconazole were above 1 μg/mL. Ciclopirox was demonstrated to have superior activity against all strains in comparison with the other drugs, whereas fluconazole exerted the weakest in vitro effect and exhibited the highest MIC values. Our study has shown that drugs of different chemical origin have satisfactory antifungal activity and can be promising candidates for the treatment of T. verrucosum dermatophytosis. Moreover, no significant disparity in drug sensitivity between isolates obtained from different hosts and geographical regions have been demonstrated.