RESUMO
AIMS: CYP53A15, from the sorghum pathogen Cochliobolus lunatus, is involved in detoxification of benzoate, a key intermediate in aromatic compound metabolism in fungi. Because this enzyme is unique to fungi, it is a promising drug target in fungal pathogens of other eukaryotes. METHODS AND RESULTS: In our work, we showed high antifungal activity of seven cinnamic acid derivatives against C. lunatus and two other fungi, Aspergillus niger and Pleurotus ostreatus. To elucidate the mechanism of action of cinnamic acid derivatives with the most potent antifungal properties, we studied the interactions between these compounds and the active site of C. lunatus cytochrome P450, CYP53A15. CONCLUSION: We demonstrated that cinnamic acid and at least four of the 42 tested derivatives inhibit CYP53A15 enzymatic activity. SIGNIFICANCE AND IMPACT OF THE STUDY: By identifying selected derivatives of cinnamic acid as possible antifungal drugs, and CYP53 family enzymes as their targets, we revealed a potential inhibitor-target system for antifungal drug development.
Assuntos
Antifúngicos/farmacologia , Benzoato 4-Mono-Oxigenase/antagonistas & inibidores , Cinamatos/farmacologia , Inibidores Enzimáticos/farmacologia , Antifúngicos/química , Antifúngicos/metabolismo , Ascomicetos/efeitos dos fármacos , Benzoato 4-Mono-Oxigenase/química , Benzoato 4-Mono-Oxigenase/metabolismo , Domínio Catalítico , Cinamatos/química , Cinamatos/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Fungos/enzimologia , Pleurotus/efeitos dos fármacosRESUMO
The authors analysed 79 patients with intraarticular fracture of the distal end of the humerus, treated during the past 5 years. Seventeen patients were treated by conservative methods, and 62 by surgery. Of the latter, 23 required emergency operations. In the majority of cases, open reduction was accomplished by special plates for the distal end of the humerus and by Y-plates. Screws, Kirschner wires and suture of bone fragments were rarely used. The most frequently employed approach was osteotomy of the olecranon. The results were excellent, except in 13 patients.
Assuntos
Lesões no Cotovelo , Fraturas do Úmero/cirurgia , Adulto , Articulação do Cotovelo/cirurgia , Feminino , Humanos , MasculinoRESUMO
The authors report a case of intestinal loop penetration and peritonitis caused by penetration of the tip of the fixation into the abdominal cavity after internal fixation of an unstable intertrochanteric fracture. Complete regression of acute infection was achieved by suturing the intestinal wound, removing the internal fixation device and administering systemic and local antibiotic therapy.
Assuntos
Placas Ósseas , Fixação Interna de Fraturas/instrumentação , Fraturas do Quadril/cirurgia , Íleo/lesões , Perfuração Intestinal/cirurgia , Jejuno/lesões , Complicações Pós-Operatórias/cirurgia , Idoso , Mau Alinhamento Ósseo/diagnóstico por imagem , Falha de Equipamento , Feminino , Fraturas do Quadril/diagnóstico por imagem , Humanos , Íleo/diagnóstico por imagem , Íleo/cirurgia , Perfuração Intestinal/diagnóstico por imagem , Jejuno/diagnóstico por imagem , Jejuno/cirurgia , Complicações Pós-Operatórias/diagnóstico por imagem , Radiografia , ReoperaçãoRESUMO
In our study we examined the patients with extraarticular fractures in five years period: from 1984 to 1987. Most of them were treated operatively (76%). The good results highly correlated with the early timing of operation, the best results are seen in cases, which are operated urgently or in the first week after injury.
Assuntos
Fraturas do Úmero/cirurgia , Feminino , Humanos , Fraturas do Úmero/diagnóstico por imagem , Masculino , Radiografia , Estudos RetrospectivosRESUMO
Carbon substrates used as the sole source of carbon and energy were tested for the classification and identification of species of Flavobacterium: Flavobacterium meningosepticum, F. breve, F. odoratum, F. multivorum, F. thalpophilum, and Flavobacterium sp. group IIb. Hierarchical classification and stepwise discriminant analysis revealed three F. meningosepticum, two F. breve, two F. odoratum, and two Flavobacterium sp. group IIb subgroups. Glucose, histidine, asparagine, tryptophan, maltose, citric acid, and glycine were selected as the most useful substrates to differentiate between the groups and subgroups.
Assuntos
Álcoois/metabolismo , Aminoácidos/metabolismo , Metabolismo dos Carboidratos , Ácidos Carboxílicos/metabolismo , Flavobacterium/classificação , Meios de Cultura , Flavobacterium/metabolismo , Estatística como AssuntoRESUMO
Authors present 3 cases with stable osteosynthesis of the ribs in unstable chest. An operative technique of osteosynthesis with the reconstruction by an Ao-plate and screws K-3.5 has been shown. Indications for applying of stable osteosynthesis have been stressed, and are as follows:--unstable chest following injuries--polytrauma combined bu unstable chest,--open fractures of the ribs (when the space between the fragment is not too large),--injuries of the lungs, combined with the injury of the ribs create unstability of the chest,--pseudoarthrosis of many ribs, or permanently unstable chest,--when a respirator is not available, this treatment is mandatory. Authors have experimentally examined and compared the value of OS with the plate of Judet and they described the advantages, as well as disadvantages (poor fixation, migration of the plate danger of eventual injury of intercostal arteries a.o.). The results of two patients were excellent, while the third one died 5 weeks following the surgery, due to other causes. Although the internal stabilization of the chest with the aid of the respirator is a proved method, a lasting hospitalization is frequently complicated by this treatment; all this represents a basis for a new approach: AO plate, and an emergency osteosynthesis immediately following injury; this gives the best results so that authors consider it as revolutionary progress in the treatment of such injuries.