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1.
Arq. bras. med. vet. zootec. (Online) ; 72(6): 2101-2110, Nov.-Dec. 2020. tab, ilus
Artigo em Português | LILACS, VETINDEX | ID: biblio-1142286

RESUMO

O conhecimento da anatomia de qualquer animal silvestre é de fundamental importância para sua preservação e proteção. Neste contexto, o presente estudo objetivou descrever a morfologia do sistema reprodutor feminino de Alouatta belzebul. Foram utilizados seis espécimes de A. belzebul, fêmeas, adultas, e livres de lesões. Observou-se macroscopicamente que os ovários têm características morfológicas em formato ovoides, com superfície lisa, e, na análise histológica na região de córtex, evidenciou-se folículos ovarianos em diferentes estágios de desenvolvimento. As tubas uterinas anatomicamente são finas e curvilíneas, apresentando uma camada mucosa, uma muscular e outra serosa. O útero possui formato simples, com fundo globoso, com um miométrio altamente vascularizado, sendo organizado em feixes de fibras musculares lisas. A estrutura anatômica da vagina apresentou-se como um tubo muscular longo de paredes finas, onde, na região vestibular, o óstio externo da uretra é marcado por uma papila uretral bilobada e, na região de vulva, em sua porção caudal, contatou-se um clitóris bem desenvolvido. No que concerne à análise histológica da vagina, verificou-se, em região de mucosa vaginal, um extrato basal composto por epitélio estratificado pavimentoso não queratinizado atrófico. As descrições morfológicas fornecem, de forma inédita, informações importantes relativas à anatomia macroscópica e microscópica do sistema reprodutor feminino dessa espécie.(AU)


Knowledge of the anatomy of any wild animal is of fundamental importance for its preservation and protection. In this context the present study aimed to describe the morphology of the female reproductive system of A. belzebul. We used 6 specimens of A. belzebul, female, adult and free of lesions. It was macroscopically observed that the ovaries are ovoid with smooth surface and the histological analysis in cortical region showed ovarian follicles in different stages of development. The fallopian tubes are anatomically thin and curvilinear, with one mucous layer, one muscular and one serous layer. The uterus was presented in a simple format with a globular fundus, with a highly vascularized myometrium, being organized in bundles of smooth muscle fibers. The anatomical structure of the vagina presented itself as a long thin-walled muscular tube where in the vestibular region the external orifice of the urethra is marked by a bilobed urethral papilla and in the caudal portion in its caudal portion a well-developed clitoris. Regarding the histological analysis of the vagina, a basal extract composed of atrophic non-keratinized stratified squamous epithelium was found in the vaginal mucosa region. The morphological descriptions provide important information regarding the macroscopic and microscopic anatomy of the female reproductive system of this species in an unprecedented way.(AU)


Assuntos
Animais , Feminino , Ovário/anatomia & histologia , Útero/anatomia & histologia , Vagina/anatomia & histologia , Alouatta/anatomia & histologia , Tubas Uterinas/anatomia & histologia , Genitália Feminina/anatomia & histologia
2.
Interv Neuroradiol ; 23(1): 84-89, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27798328

RESUMO

Purpose Cerebral venous sinus thrombosis (CVST) is an unusual and potentially life-threatening condition with variable and nonspecific clinical symptoms and high morbimortality rates. Standard therapy consists of systemic anticoagulation; although there is no clear evidence about the best choice for treatment, intravenous heparin is used as the first-line treatment modality. Intravenous sinus thrombolysis can be an effective and relatively safe treatment for acutely deteriorating patients who have not responded to conventional therapy. This case report presents the possibility of endovascular treatment in multiple steps with mechanical thrombolysis with balloon, local pharmacological thrombolysis and stenting, in a patient with a severe form of CVST. Case summary A 67-year-old woman presented severe headache, agitation and confusion with diagnosis of venous sinus dural thrombosis in both lateral sinus and torcula. After 24 h there was neurological worsening evolving with seizures and numbness even after starting heparin, without sinus recanalization; CT scan showed left temporal intracerebral hemorrhage. We decided to take an endovascular approach in multiple steps. The first step was mechanical static thrombolysis with balloon; the second step was dynamic mechanical thrombolysis with a balloon partially deflated and "pulled"; the third step was local thrombolysis with Actilyse™; finally, the fourth step was angioplasty and reconstruction of the sinuses using multiple carotid stents and complete angiographic recanalization of both sinuses and torcula. After 24 h of endovascular treatment there was full clinical recovery and no tomographic complications. Conclusion This result shows that mechanical clot disruption, intrasinus thrombolysis and reconstruction of wall sinuses with stenting can be an endovascular option in the severe form of CVST with intracerebral hemorrhage and rapid worsening of neurological symptoms. Although this type of treatment can re-channel the occluded sinuses, further comparative and randomized studies are needed to clarify its efficacy versus other therapeutic modalities.


Assuntos
Trombólise Mecânica , Trombose dos Seios Intracranianos/diagnóstico por imagem , Trombose dos Seios Intracranianos/terapia , Stents , Terapia Trombolítica , Idoso , Angiografia Digital , Angiografia Cerebral , Diagnóstico Diferencial , Feminino , Escala de Coma de Glasgow , Humanos , Tomografia Computadorizada por Raios X
3.
Genet Mol Res ; 15(3)2016 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-27706717

RESUMO

The association between high-risk human papillomavirus (HPV) genotypes and p16 expression in indigenous women from the Xingu Indigenous Park, Brazil, was unknown. This study evaluated p16 expression in women with a histological diagnosis of cervical intraepithelial neoplasia (CIN) 3 or higher and correlated this expression with HPV genotypes to determine possible discrepancies in the expression of this marker. We evaluated 37 previously collected samples with different HPV genotypes and high-grade lesions diagnosed based on cytology, histology, and colposcopy. Immunohistochemical analysis was performed using paraffin-embedded tissue sections and the CINtec® Histology Kit. p16 protein expression was investigated by immunostaining with an anti-p16 antibody. HPV genotyping was performed by reverse hybridization. The age of the study population ranged from 22-75 years (43.81 ± 15.89 years) and parity ranged from 1-11 (5.92 ± 2.58). Thirteen different HPV genotypes were found using the INNO-LiPA kit. Single and multiple infections by HPV were found with prevalence of single infections (P = 0.029). Comparison between HPV genotype and simple or multiple infections was highly significant; it was observed more HPV 52 followed by HPV 16 in single infections (P < 0.001). p16 expression was predominantly diffuse, which was observed in 91.7% of lesions, whereas 8.3% were focal (P < 0.001). HPV 52, HPV 16 and 31 were the most prevalent HPV types in high-grade CIN in these indigenous women. Diffuse p16 expression in high-grade CIN was not influenced by the viral genotype; however, more studies are necessary to further our understanding of this restricted group.


Assuntos
Biomarcadores Tumorais/biossíntese , Inibidor p16 de Quinase Dependente de Ciclina/biossíntese , Infecções por Papillomavirus/genética , Displasia do Colo do Útero/genética , Adulto , Idoso , Biomarcadores Tumorais/genética , Brasil , Colposcopia , Inibidor p16 de Quinase Dependente de Ciclina/genética , Feminino , Regulação da Expressão Gênica , Genótipo , Papillomavirus Humano 16/genética , Papillomavirus Humano 16/isolamento & purificação , Papillomavirus Humano 16/patogenicidade , Papillomavirus Humano 31/genética , Papillomavirus Humano 31/isolamento & purificação , Papillomavirus Humano 31/patogenicidade , Humanos , Pessoa de Meia-Idade , Infecções por Papillomavirus/patologia , Infecções por Papillomavirus/virologia , Displasia do Colo do Útero/patologia , Displasia do Colo do Útero/virologia
4.
J Sports Med Phys Fitness ; 55(12): 1473-9, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25286889

RESUMO

AIM: The aim of the present study was to evaluate the effects of the temperature of ingested water on performance during a 40-km self-paced cycling trial in the heat (35º C and 60% relative humidity). METHODS: The study was randomized, counterbalanced, crossover and single-blinded. Ten well-trained male cycling athletes (cyclists, mountain bikers or triathletes) who were non-acclimatized to heat were subjected to four experimental situations divided into two sets. In the first set, the participants performed two trials, during which they were given either cold (10º C) or warm water (37º C) ad libitum. In these situations, the volume and timing of the water ingestion (when each bolus was ingested) were recorded and replicated in the second set, but the water temperature was reversed. RESULTS: The performance times were unaffected by the water intake volume (P=0.425), but the water at a temperature of 37º C tended to induce lower performance times (P=0.078) during the trials (AL10=93.0±3.5 min; AL37=94.4±4.1 min; SC10=93.4±4.0; SC37=97.4±4.3 min). The water intake was greater when the water was cold (P<0.05), but the temperature did not affect the heat storage rate, rectal temperature, mean skin temperature, heart rate, blood glucose level, sweat loss, sweat rate, perceived exertion rate or plasma volume changes. However, a significant reduction in the plasma volume change from pre- to postexercise was observed (P<0.01). CONCLUSION: The performance, thermoregulatory, cardiovascular and metabolic responses during a 40-km self-paced cycling trial in the heat were unaffected by different water temperatures.


Assuntos
Desempenho Atlético/fisiologia , Ciclismo/fisiologia , Regulação da Temperatura Corporal/fisiologia , Temperatura Corporal/fisiologia , Ingestão de Líquidos/fisiologia , Temperatura , Adulto , Atletas , Estudos Cross-Over , Humanos , Masculino , Adulto Jovem
5.
Interv Neuroradiol ; 18(4): 458-62, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23217641

RESUMO

The endovascular treatment of spontaneous dural cavernous sinus fistula (DAVF) can be accomplished by arterial approach, just with symptoms relief, or by numerous venous approaches through the inferior petrosal sinus, ophthalmic vein, anterior or posterior intercavernous sinus and facial vein. Our case suggests the approach to the cavernous sinus via the foramen ovale and emissary veins puncture as an alternative when there is no possibility of venous approach conventionally described. A 76-year-old woman presented with right conjunctival hyperemia, exophthalmos, intraocular pressure increasing and visual deficits in a period of six months. Angiographic diagnosis of spontaneous DAVF isolated from the cavernous sinus, Barrow Type C, with exclusive venous drainage through the superior ophthalmic vein. Endovascular treatment was performed under general anesthesia. Attempts to approach the cavernous sinus through the inferior petrosal sinus ipsilateral and contralateral intercavernous, facial vein and pterygoid plexus, as well as by dissection and direct puncture of the superior ophthalmic vein were not possible. An approach to the cavernous sinus was performed by puncturing the foramen ovale, catheterization of the emissary vein of the foramen ovale with occlusion of the fistula with microcoils. There was a symptomatic regression with gradual normalization of intraocular pressure, exophthalmos and conjunctival hyperemia in three months. The approach to the cavernous sinus through the foramen ovale and catheterization of the emissary cranial skull base vein is an exception and should be considered in cases of spontaneous and isolated DAVF not accessible by a conventional approach.


Assuntos
Seio Cavernoso/cirurgia , Malformações Vasculares do Sistema Nervoso Central/cirurgia , Veias Cerebrais/cirurgia , Procedimentos Endovasculares/métodos , Procedimentos Neurocirúrgicos/métodos , Idoso , Feminino , Humanos , Hiperemia/cirurgia
6.
Eur J Gynaecol Oncol ; 30(5): 512-3, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19899404

RESUMO

Over the years, there have been many deaths due to cervical cancer among indigenous women of the Parque Indigena do Xingu as a consequence of low screening coverage. Since 2005, however, the coverage index of cervical lesion screening has been high: 97.6% among at-risk women in 2005 and 92.6% in 2007. Cytological alterations occurred in 12.6% and 6% of the cases in the respective years. After complete diagnosis and treatment of uterine lesions, by staff trained in lower tract pathology, negative results were seen in all cases of high-grade lesions and invasive neoplasia and no case of invasive carcinoma was detected in 2007. We conclude, therefore, that health actions have been effective in decreasing the incidence of cytological alterations and invasive carcinoma.


Assuntos
Índios Sul-Americanos , Displasia do Colo do Útero/prevenção & controle , Neoplasias do Colo do Útero/prevenção & controle , Adolescente , Adulto , Brasil/epidemiologia , Colposcopia , Feminino , Humanos , Incidência , Programas de Rastreamento , Pessoa de Meia-Idade , Displasia do Colo do Útero/etnologia , Neoplasias do Colo do Útero/etnologia , Esfregaço Vaginal , Adulto Jovem
7.
Eur J Gynaecol Oncol ; 30(4): 415-7, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19761134

RESUMO

Results of preventive health measures, diagnosis and treatment applied to Parque Indigena do Xingu native women were studied. Thirty-seven cases of uterine cervical intraepithelial lesions and invasive neoplasias were treated in the local villages without referral to an advanced medical center. LEEPs were carried out in 32 women, three cold knife conizations, one vaginal hysterectomy and one Wertheim Meigs procedure. Results of 53.1% of LEEP surgical procedures did not have margin involvement by the lesions. Bleeding complications were seen in 15.6%. Regular follow-up with two or three cytologic and colposcopic tests in 32 women was carried out. All cases were negative for lesions. Five women were not followed-up due mainly to logistical reasons. Health endeavors adopted in the period 2005-2007 brought about a significant reduction of precursor lesions in this native aboriginal population without screening resources.


Assuntos
Índios Sul-Americanos , Displasia do Colo do Útero/etnologia , Neoplasias do Colo do Útero/etnologia , Brasil , Feminino , Humanos , Infecções por Papillomavirus/diagnóstico , Infecções por Papillomavirus/etnologia , Infecções por Papillomavirus/prevenção & controle , Neoplasias do Colo do Útero/diagnóstico , Neoplasias do Colo do Útero/prevenção & controle , Neoplasias do Colo do Útero/terapia , Displasia do Colo do Útero/diagnóstico , Displasia do Colo do Útero/prevenção & controle , Displasia do Colo do Útero/terapia
8.
Food Chem Toxicol ; 45(10): 1975-8, 2007 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17574317

RESUMO

In the present work we evaluated both the mutagenicity and antimutagenicity of the Pothomorphe umbellata root extract (PUE) and its isolated active principle, the 4-nerolidylcatechol (4-NC), in bone marrow cells of mice using the micronucleus test. Swiss male mice were orally treated for 4 days with PUE (200, 100 or 50mg/kg/day) or 4-NC (50, 25 or 12.5mg/kg/day) prior to exposition with a single dose (200mg/kg) of cyclophosphamide (CP), 24h after the end of the treatment. The results demonstrated that the PUE and 4-NC did not have any mutagenic effect on mouse bone marrow cells; quite the opposite, there was a protective effect against genotoxicity induced by cyclophosphamide. Taken together, under the conditions tested herein, mice treated with PUE and 4-NC showed, in a dose-dependent manner, protective effect against CP-induced genotoxicity. Due to their ability to prevent chromosomal damage, with apparent low toxicity and cost, PUE or pure 4-NC are likely to open a field of interest concerning their possible use in clinical applications.


Assuntos
Antimutagênicos , Antineoplásicos Alquilantes/antagonistas & inibidores , Antineoplásicos Alquilantes/toxicidade , Catecóis/farmacologia , Ciclofosfamida/antagonistas & inibidores , Ciclofosfamida/toxicidade , Mutagênicos , Piperaceae/química , Animais , Aberrações Cromossômicas/efeitos dos fármacos , Relação Dose-Resposta a Droga , Eritrócitos/efeitos dos fármacos , Eritrócitos/ultraestrutura , Masculino , Camundongos , Testes para Micronúcleos , Extratos Vegetais/química , Raízes de Plantas/química
9.
Neurology ; 63(11): 2168-9, 2004 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-15596773

RESUMO

Lipoid proteinosis (LP) is an autosomal recessive disease that typically presents with papular, verrucous, poxlike, or acneiform scars and lesions and hoarseness. LP was recently mapped to the 1q21 locus and shown to result from mutations in the extracellular matrix protein 1 gene (ECM1). Epilepsy, mental retardation, and hippocampal calcifications can occur. The authors describe a patient with generalized dystonia caused by striatal calcifications.


Assuntos
Calcinose/etiologia , Distúrbios Distônicos/etiologia , Proteinose Lipoide de Urbach e Wiethe/complicações , Adulto , Calcinose/diagnóstico por imagem , Calcinose/patologia , Corpo Estriado/diagnóstico por imagem , Corpo Estriado/patologia , Proteínas da Matriz Extracelular/genética , Hipocampo/diagnóstico por imagem , Hipocampo/patologia , Rouquidão/etiologia , Humanos , Deficiência Intelectual/etiologia , Proteinose Lipoide de Urbach e Wiethe/genética , Proteinose Lipoide de Urbach e Wiethe/patologia , Masculino , Dermatopatias Papuloescamosas/etiologia , Tomografia Computadorizada por Raios X
10.
Clin Imaging ; 22(5): 371-5, 1998.
Artigo em Inglês | MEDLINE | ID: mdl-9755402

RESUMO

The presence or absence of tendon calcification was studied at six anatomic sites: Achilles, gastrocnemius, quadriceps, triceps (elbow), triceps long head (shoulder), and rotator cuff. The morphology of the calcifications was categorized in 156 patients with chondrocalcinosis in the knee. Achilles tendon, gastrocnemius, and quadriceps tendon calcifications were most common, ranging from 21%-25% of our patient population was thin linear bands. Triceps calcification at the elbow, rotator cuff calcifications, and long head of triceps tendon calcification were less common.


Assuntos
Condrocalcinose/diagnóstico por imagem , Articulação do Joelho/diagnóstico por imagem , Tendões/diagnóstico por imagem , Tendões/patologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Calcinose , Feminino , Humanos , Articulação do Joelho/patologia , Masculino , Pessoa de Meia-Idade , Prevalência , Radiografia
11.
Clin Radiol ; 53(8): 574-8, 1998 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-9744582

RESUMO

OBJECTIVE: To compare partial flexion true sagittal (FS) magnetic resonance (MR) images with extension sagittal oblique (ESO) MR images with regard to delineation of the anterior cruciate ligament (ACL) in the knee. DESIGN: To establish the appropriate degree of flexion of the knee joint, two human cadaveric knee joints were used as a supplementary technique. FS and ESO images then were performed in 17 knees with an intact ACL and six knees with a torn ACL. In 22 of the 23 knees in which the MR diagnosis of intact or torn ACL corresponded to that derived from arthroscopy, the paired MR images were rated by a three-point scale. RESULTS: FS images were rated superior to ESO images in 53%, 41% and 47% of cases with regard to femoral attachment sites, midportions and tibial attachment sites of intact ACLs, respectively. FS images allowed better assessment of disrupted ACLs and residual ligamentous structures. Overall the FS images were either equal to or better than the ESO in the majority of cases. CONCLUSION: FS images are useful when the ACL is not well visualized in initial ESO images.


Assuntos
Lesões do Ligamento Cruzado Anterior , Articulação do Joelho/patologia , Adulto , Idoso , Ligamento Cruzado Anterior/anatomia & histologia , Ligamento Cruzado Anterior/patologia , Feminino , Humanos , Articulação do Joelho/anatomia & histologia , Imageamento por Ressonância Magnética/métodos , Masculino , Pessoa de Meia-Idade , Postura
12.
Chem Pharm Bull (Tokyo) ; 45(4): 733-6, 1997 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-9145508

RESUMO

Eight compounds structurally related to protein kinase C inhibitor MDL 27032 and substituted with indole moieties were synthesized. Their activities towards protein kinase C (PKC) and protein kinase A (PKA) were determined. Their effect on PKC-mediated contraction of rat tracheal smooth muscle, their antiproliferative activity on two murine tumor cell lines, melanoma B16 and leukemia P388 and their antimicrobial activity on a gram-positive bacterium Bacillus cereus were also examined. The mammalian and bacterial cell antiproliferative activity, as well as vasorelaxant effect, observed for some of them could not be correlated to PKC or PKA inhibition. Only bulky bis-indolyl compounds exhibited biological activity in these experiments. Rigid indolocarbazoles had the strongest antiproliferative activity.


Assuntos
Inibidores Enzimáticos/síntese química , Imidazóis/química , Oxazóis/química , Oxazolona/análogos & derivados , Proteína Quinase C/antagonistas & inibidores , Piridinas/química , Vasodilatadores/química , Animais , Divisão Celular/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Imidazóis/farmacologia , Camundongos , Oxazóis/farmacologia , Oxazolona/química , Oxazolona/farmacologia , Proteína Quinase C/metabolismo , Inibidores de Proteínas Quinases , Proteínas Quinases/metabolismo , Piridinas/farmacologia , Ratos , Células Tumorais Cultivadas , Vasodilatação/efeitos dos fármacos , Vasodilatadores/farmacologia
13.
J Med Chem ; 39(22): 4471-7, 1996 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-8893841

RESUMO

A series of compounds structurally related to staurosporine, rebeccamycin, and corresponding aglycones was synthesized, and their activities toward protein kinase C and topoisomerases I and II were tested together with their in vitro antitumor efficiency against murine B16 melanoma and P388 leukemia cells. Their antimicrobial activities were also examined against a Gram-negative bacterium (Escherichia coli), a yeast (Candida albicans), and three Gram-positive bacteria (Bacillus cereus, Streptomyces chartreusis, and Streptomyces griseus). To avoid side effects expected with protein kinase C inhibitors, we introduced substitution on the maleimide nitrogen and/or a sugar moiety linked to one of the indole nitrogens to obtain specific inhibitors of topoisomerase I with minimal activities on protein kinase C. As expected, these structures were inefficient on topoisomerase II, and some of them exhibited a strong activity against topoisomerase I. Generally, dechlorinated compounds were found to be more active than chlorinated analogues against both purified topoisomerase I and protein kinase C. On the other hand, opposite results were obtained in the cell antiproliferative assays. These results suggest lack of cell membrane permeability in the absence of the chlorine residue or cleavage of carbon-chlorine bonds inside the cell.


Assuntos
Antibacterianos/química , Antineoplásicos/química , Carbazóis/química , Indóis/química , Proteína Quinase C/antagonistas & inibidores , Inibidores da Topoisomerase I , Animais , Bacillus cereus , Carbazóis/farmacologia , Escherichia coli , Indóis/farmacologia , Leucemia P388/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Streptococcus , Células Tumorais Cultivadas
14.
J Antibiot (Tokyo) ; 49(4): 380-5, 1996 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-8642002

RESUMO

Indole-substituted oxazolidinones, oxazolones, pyrrolidinone, imidazolidinone and imidazolones were synthesized. Their inhibitory potencies towards protein kinase C and protein kinase A were determined and their in vitro activities against Streptomyces chartreusis, Streptomyces griseus, Bacillus cereus, Candida albicans and Escherichia coli were examined. The inhibition of Streptomyces sporulation observed for some of them could not be linked to in vitro protein kinase C inhibition. All proved inactive against C. albicans but three of them exhibited a marked activity towards E. coli. This effect extends to other Gram-negative bacteria.


Assuntos
Carbazóis/química , Carbazóis/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Imidazóis/química , Imidazóis/farmacologia , Indóis/química , Indóis/farmacologia , Proteína Quinase C/antagonistas & inibidores , Pirrolidinonas/química , Pirrolidinonas/farmacologia , Alcaloides/química , Alcaloides/farmacologia , Bacillus cereus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Carbazóis/síntese química , Proteínas Quinases Dependentes de AMP Cíclico/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Escherichia coli/efeitos dos fármacos , Imidazóis/síntese química , Indóis/síntese química , Testes de Sensibilidade Microbiana , Pirrolidinonas/síntese química , Saccharomyces/efeitos dos fármacos , Saccharomyces/crescimento & desenvolvimento , Estaurosporina , Relação Estrutura-Atividade
15.
J Antibiot (Tokyo) ; 48(8): 863-8, 1995 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-7592032

RESUMO

New compounds, structurally related to the potent protein kinase C inhibitor staurosporine, and substituted on the imide nitrogen with a functional group bearing a labile hydrogen (hydroxymethyl, amino, hydroxy), were synthesized. Their in vitro inhibitory potencies towards protein kinase C and protein kinase A showed that N-hydroxymethyl and N-hydroxy substitution, unlike alkyl substitution, can provide efficient protein kinase C inhibitors. The antimicrobial activities of these new compounds against Streptomyces chartreusis and Streptomyces griseus, Bacillus cereus, Escherichia coli, Candida albicans and Botrytis cinerea were examined. They proved to be inactive against E. coli and two fungi. The results suggest that there is no link between in vitro inhibition of protein kinase C and inhibition of growth and sporulation of the two Streptomyces tested. Unlike indolocarbazole maleimides, bis-indole maleimides are active against the two Streptomyces species.


Assuntos
Carbazóis/farmacologia , Proteínas Quinases Dependentes de AMP Cíclico/antagonistas & inibidores , Indóis/farmacologia , Proteína Quinase C/antagonistas & inibidores , Carbazóis/síntese química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/enzimologia , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/enzimologia , Indóis/síntese química , Relação Estrutura-Atividade
16.
São Paulo; SMS; s.d. 1 p. graf.
Não convencional em Português | Sec. Munic. Saúde SP, CRSLESTE-Producao, Sec. Munic. Saúde SP, Sec. Munic. Saúde SP | ID: sms-8582
17.
São Paulo; SMS; s.d. 1 p. graf.
Não convencional em Português | Coleciona SUS, CRSLESTE-Producao, Sec. Munic. Saúde SP, Sec. Munic. Saúde SP | ID: biblio-939824
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