208 resultados para ANTI RETROVIRAL AGENTS


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Fusobacterium nucleatum is considered for its role in colonization of initial and late microorganisms in dental plaque and for its coaggregation with other bacterial species. It is known that action of different antimicrobial substances may interfere with either virulence factors or with host-bacteria interaction. The goal of this study was to examine the influence of subinhibitory concentrations of chlorhexidine, triclosan , penicillin G and metronidazole on hemolytic activity and bacteriocin-like substance production of oral F. nucleatum. A high resistance to penicillin G was observed and 63% of the isolates were β-lactamase positive. All the tested isolates were susceptible to metronidazole. F. nucleatum isolates grown with or without antimicrobials were alpha-hemolytics. Bacteriocin-like substance production was increased in isolates grown with penicillin G. Impaired production of hemolytic or antagonic substances can suggest a role in the regulation of oral microbiota.

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Chemical examination of the leaves of Styrax ferrugineus yielded 5-[3'-(β-D-glucopyranosyloxy)propyl]-7-methoxy-2-(3',4'-dime-thoxyphenyl) benzofuran, along with the known nor-lignans 5-(3'-hydroxypropyl)-7-methoxy-2-(3',4'-methylenedioxyphenyl) benzofuran, 5-(3'-hydroxypropyl)-7-methoxy-2-(3',4'-dimethoxyphenyl)benzofuran, 5-[3'-(β-D-glucopyranosyloxy)propyl]-7-methoxy-2-(3', 4'-methylenedioxyphenyl)benzofuran and the lignan, dihydrodehydrodiconiferyl alcohol. All arylpropanoids isolated showed antibacterial and antifungal activities. The structures of the isolates were established by spectroscopic analysis. (C) 2000 Elsevier Science Ltd.

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Quinolones constitute a family of compounds with a potent antibiotic activity. The enzyme DNA gyrase, responsible for the replication and transcription processes in DNA of bacteria, is involved in the mechanism of action of these drugs. In this sense, it is believed that quinolones stabilize the so-called 'cleavable complex' formed by DNA and gyrase, but the whole process is still far from being understood at the molecular level. This information is crucial in order to design new biological active products. As an approach to the problem, we have designed and synthesized low molecular weight peptide mimics of DNA gyrase. These peptides correspond to sequences of the subunit A of the enzyme from Escherichia coli, that include the quinolone resistance-determining region (positions 75-92) and a segment containing the catalytic Tyr-122 (positions 116-130). The peptide mimic of the non-mutated enzyme binds to ciprofloxin (CFX) only when DNA and Mg2+ were present (Kd = 1.6 × 10 -6 m), a result previously found with DNA gyrase. On the other hand, binding was reduced when mutations of Ser-83 to Leu-83 and Asp-87 to Asn-87 were introduced, a double change previously found in the subunit A of DNA gyrase from several CFX-resistant clinical isolates of E. coli. These results suggest that synthetic peptides designed in a similar way to that described here can be used as mimics of gyrases (topoisomerases) in order to study the binding of the quinolone to the enzyme-DNA complex as well as the mechanism of action of these antibiotics. Copyright © 2001 European Peptide Society and John Wiley & Sons, Ltd.

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Introduction: The study of otolaryngologic manifestations in children HIV + can lead to early diagnosis of AIDS, allowing specific treatment, responsible by reduced morbidity and mortality. Objectives: Detect the otolaryngologic manifestations in children with AIDS and alert to the importance of the early diagnosis. Study design: Clinical prospective. Material and method: We evaluated 22 children with AIDS assisted at Faculdade de Medicina de Botucatu (São Paulo, Brasil). The medical records were reviewed and the children were submitted to otolaryngologic and hearing acuity exams. Results: We evaluated 12 boys and 10 girls, whose ages ranged from 8 months to 12 years. In B and C clinical classification were included 18 children who were using anti-retroviral medicaments. Physical examination mainly indicated cervical lymphadenopathy (18 cases), paleness of the nasal mucous membrane with abundant mucous secretion over the nasal epithelium (15 cases) and retraction of tympanic membranes (seven cases). The main otolaryngologic diagnoses were: rhinosinusitis (16 cases), oral candidiasis (13 cases), inadequate eustachian tube function (seven cases) and recurrent tonsillar infections (six cases). Conductive hearing loss were detected in 4 children. No child presented sensorineural hearing loss. Conclusions: The main otolaryngologic manifestations presented by the children with HIV virus were rhinosinusitis, oral candidiasis, inadequate eustachian tube function and recurrent tonsillar infections. The allergic aspect of the nasal mucous membrane and the cervical lymphadenopathy were frequent signs and could alert the otolaryngologyst to AIDS during the exam.

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This study evaluates the effect of subgingival irrigation with a 1% chlorhexidine collagen gel in periodontal pockets as an adjunct procedure to scaling and root planing (SRP). Thirty-seven sites with probing depth (PD) of 5-7 mm and BANA positive in 6 patients with chronic periodontal disease were selected. Sites were assigned to different treatment groups consisting of SRP only (group 1), SRP + irrigation with collagen gel (group 2), or SRP + irrigation with collagen gel containing 1% chlorhexidine (group 3). Subgingival irrigation was performed after initial SRP and at 7, 14 and 21 days. Clinical measurements including PD, plaque index (PI), gingival index (GI), gingival recession (GI), bleeding on probing (BOP) and clinical attachment level (CAL) were performed at the selected sites at baseline, 60 and 90 days and the BANA test was performed on plaque samples from the same sites at baseline and 90 days. There was an improvement in clinical parameters in all groups with a significantly greater decrease in GI and bleeding in the chlorhexidine group. There was a greater reduction of BANA positive sites in groups 2 and 3. The authors concluded that 1% chlorhexidine collagen gel is a promising adjunct to SRP in the treatment of adult periodontitis.

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The antimicrobial activity of irrigating solutions - Endoquil (castor oil detergent), 2% chlorhexidine gluconate solution, and 0.5% NaOCI solution - was evaluated against Gram-positive cocci (Micrococcus luteus, Staphylococcus aureus, Enterococcus faecalis, Staphylococcus epidermidis, Streptococcus mutans, and Streptococcus sobrinus), Gramnegative rods (Escherichia coli and Pseudomonas aeruginosa), and the yeast Candida albicans. Activity was evaluated using the two-layer agar diffusion technique. The base layer was obtained by pouring 10.0 ml of Muller Hinton Medium or 10.0 ml of Brain Heart Infusion agar in a Petri dish. After solidification a 5.0 ml seed layer of Muller Hinton Medium or Brain Heart Infusion agar with inoculum (106/ml) was added. Absorbent paper disks (6.0 mm in diameter) immersed in the solutions were placed at equidistant points. Plates were maintained at room temperature for 2 h for prediffusion of the solutions and incubated at 37°C for 24 h. The candle jar system was used for the Brain Heart Infusion agar plates. All tests were performed in duplicate. After incubation the medium was optimized with 0.05 g% triphenyltetrazolium chlorate gel and inhibition halos were measured. All bacterial strains were inhibited by 2.0% chlorhexidine gluconate. Endoquil was effective against Grampositive microorganisms, and 0.5% NaOCI was effective only against S. aureus. Copyright © 2001 by The American Association of Endodontists.

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Numerous natural compounds have a potential for therapeutic applications, but may have to be chemically modified to alter toxic side effects. We investigated structural parameters that could affect the cytotoxicity of isocoumarins similar to 9,10-dihydroxy-5,7-dimethoxy-1H-naphtho(2,3c)pyran-1-one (paepalantine 1). Paepalantine 1 has antimicrobial activity, as well as significant in vitro cytotoxic effects in the McCoy cell line. Two other natural and two semi-synthetic isocoumarins with similar structures obtained from the capitula of Paepalanthus bromelioides were tested on the same cell line by the neutral red assay. Substitution of the 9 and/or 10-OH group made these compounds less cytotoxic.

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Tuberculosis (TB) resurged in the late 1980s and now kills approximately 3 million people a year. The reemergence of tuberculosis as a public health threat has created a need to develop new anti-mycobacterial agents. The shikimate pathway is an attractive target for herbicides and anti-microbial agents development because it is essential in algae, higher plants, bacteria, and fungi, but absent from mammals. Homologs to enzymes in the shikimate pathway have been identified in the genome sequence of Mycobacterium tuberculosis. Among them, the shikimate kinase I encoding gene (aroK) was proposed to be present by sequence homology. Accordingly, to pave the way for structural and functional efforts towards anti-mycobacterial agents development, here we describe the molecular modeling of M. tuberculosis shikimate kinase that should provide a structural framework on which the design of specific inhibitors may be based. © 2002 Elsevier Science (USA). All rights reserved.

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The use of natural active principals is widespread among a great proportion of the rural population, or by people who do not have easy access to medical assistance. These active principles are used as food or medicines, and even for purposes of contraception. It becomes necessary to establish a relationship between the folklore habits and current information on the nature of anti-fertility substances, and knowledge of their mechanisms. Anti-fertility agents may exert their actions in a number of areas, (hypothalamus, anterior pituitary, oviduct, uterus, and vagina), inhibiting synthesis and/or liberation of hormones (follicle-stimulating, luteinizing, and steroid hormones), ovulation, ovum transportation, and implantation process. Therefore, a review of literature was carried out, including of several plants used by women as abortifacient and anti-fertility agents to compare their effects with those obtained among laboratory animals.

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From the hexane-soluble fraction of an ethanol extract from leaves and stems of Stemodia foliosa (Scrophulariaceae), the new stearic acid 4-[(n-pentoxy)phenethyl] ester (1) was isolated. This compound exhibited antibacterial properties at 10μg/mL concentration by using disc diffusion method against Gram-positive bacteria Bacillus cereus and Bacillus subtilis and fast-acid bacterium Mycobacterium fortuitum. The structure of the new compound was elucidated by spectroscopic methods and by chemical conversion.

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Loss of function, muscle inflammation, and pain are some of the signs and symptoms of temporomandibular dysfunction (TMD). Pharmacological strategies to minimize the clinical manifestation of these disorders often focus on blocking or inhibiting the pain-causing symptom. Resources such as muscle-relaxants, anxiety-relief drugs, and splint therapy are often used to reduce muscular hyperactivity related to TMD muscle pain. This study compares the effect of a randomly ordered association of occlusal splint therapy (S), nonsteroid anti-inflammatory with a muscle-relaxant drug (orphenadrine citrate) (O), and an anxiety-relief drug (benzodiazepine) (B), to ease painful TMD muscle symptoms. Clinical and anamnestic analyses were recorded in accordance with the Helkimo TMD index and applied before and after treatments. Twenty-one group two Helkimo TMD adult female patients were treated, all of whom were subjected to the three random therapeutic associations proposed: SBO, BOS, and OSB. The same operator applied the three specific associations over a period of 21 days in the proposed sequence, seven days for each therapy. The results show that all the groups presented the best results in terms of relief from pain after the therapeutic association (28.5% showed a decrease and 47.6% showed an absence of symptoms). No significant difference was observed among association therapeutic protocols. Copyright © 2003 by CHROMA, Inc.

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The purpose of this study was to carry out a scanning electron microscopic (SEM) analysis of the cleaning qualities and smear layer removal from root canal walls, instrumented and irrigated with 2.5% NaOCl, 2.0% chlorhexidine and saline solutions. Fifty extracted teeth were used in this study. All teeth were radiographed to determine the existence of a single canal. The crowns were cut at the cervical limit and the root canals were instrumented with K-type files up to size 45. During root canal preparation, irrigations were made with the different solutions being evaluated: Group 1: 2.5% NaOCl (10 roots); Group 2: 2.5% NaOCl and 17% EDTA for 2 minute (10 roots); Group 3: 2.0% chlorhexidine (10 roots); Group 4: 2.0% chlorhexidine and 17% EDTA for 2 minutes (10 roots); Group 5: saline solution (5 roots); Group 6: saline solution and 17% EDTA for 2 minutes (5 roots). After instrumentation, the canals were irrigated with each one of the solutions and the roots were cut in the buccolingual direction for SEM analysis, at the cervical, middle and apical thirds, to ascertain the presence or absence of smear layer and debris. SEM analysis was performed by three calibrated examiners and scores were submitted to Kruskal-Wallis test at the significance level of p = 5%. Results showed that the use of 17% EDTA decreased the smear layer significantly (p < 0.05) for all evaluated solutions in all thirds. When EDTA was not used, a significantly higher quantity of smear layer on the apical third was observed only in the NaOCl groups. The use of 17% EDTA was significant for debris removal except for the chlorhexidine groups. The following conclusion could be drawn: the use of 17% EDTA was necessary to enhance cleanness of the root canals.

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Purpose: To evaluate the effect of 2% chlorhexidine on the microtensile bond strength of composite resin to dentin treated with three dentin bonding systems. Materials and Methods: Flat dentinal surfaces were prepared in 24 extracted human third molars. Teeth were randomly divided into 8 distinct experimental groups according to the adhesive applied (Prime & Bond NT, Single Bond and Clearfil SE Bond), the application (yes/no) of chlorhexidine, and the time point at which it was applied (before or after acid etching the dentin). Composite resin blocks were built up over treated surfaces, and teeth were then stored in water at 37°C for 24 h. Samples were thermocycled, stored under the same conditions, and then vertically sectioned, thus obtaining specimens with 1.0 ± 0.1 mm2 cross-sectional area. Specimens were stressed in tension at 0.5 mm/min crosshead speed. Bond strength results were evaluated using a one-way ANOVA (p < 0.05). The modes of failures were verified using optical microscopy. Dentin disks were obtained from 3 additional teeth treated in the same manner for observation under SEM. The most representative samples of fractured specimens were also observed under SEM. Results: No statistically significant differences of bond strength values were found between any groups. Failures occurred mainly within the bond; exclusively adhesive fractures (adhesive-dentin) were not observed. Conclusion: The 2% chlorhexidine solution, applied before or after acid etching of the dentin, did not interfere with the microtensile bond strength of composite resin to the dentin treated with Prime & Bond NT, Single Bond, or Clearfil SE Bond bonding systems.

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Aim. Diclofenac sodium is a non-steroidal anti-inflammatory drug commonly used to attenuate painful inflammatory reactions in surgery. However, it may delay healing in the skin and gastrointestinal tract. The aim of this study was to evaluate the influence of Diclofenac in vascular healing. Methods. Ninety rabbits had their carotid arteries sectioned and reconstructed by end-to-end anastomosis with interrupted sutures. The animals were randomly allocated into 3 groups of 30 each and treated by intramuscular route with saline (control), 5 mg/kg/day of diclofenac sodium (DS-5), and 10 mg/kg/day of diclofenac sodium (DS-10). Treatment began on the day of surgery and lasted 4 days. Angiography, biomechanical properties (failure load, failure elongation, yield point, yield point elongation, and stiffness were obtained from the load/elongation curve), macroscopic and histological examinations (hematoxylin-eosin, Masson, Calleja, Picrossirius-red), and scanning electron microscopy were studied in both arteries on the 3rd and 15th postoperative days. Results. No significant differences in biomechanical properties were observed either in the 3 groups or the experimental times. The carotid artery healing process was similar in the 3 groups. Conclusion. Diclofenac sodium did not cause alterations nor delayed carotid artery healing.