RESUMEN
The oral hygiene and oral status of children with severe disabilities with both nutritional and respiratory complications who were institutionalized at Karugamonoie (KNI), a facility for children with disabilities, were investigated in this study. Their oral hygiene management was solely dependent on caregivers and nurses at the institution. Thirty children (13 females, 17 males; average age, 7.6 years) who had a tracheotomy and feeding tube (gastrostomy, nasogastric, or jejunostomy feeding tube) were included in the study. As for oral characteristics, poor control of tongue movement, anterior open-bite, abnormal strain of facial muscles, dry mouth, and swallowing dysfunction were found in 63.3%, 63.3%, 13.3%, 20.0%, and 100.0%, of the children, respectively. The mean ± standard deviation Decayed, Missing, Filled Teeth score was 0.13 ± 0.57. The Gingival Index (GI) showed that the children had mild (53.3%) to moderate (46.7%) gingivitis. The Simplified Oral Hygiene Index was excellent in 50.0% of the children, good in 23.3%, fair in 20.0%, and poor in 6.7% of the children. These indices were satisfactory in general except for GI management, which may have been hampered by abnormal oral functions and anterior open-bite. In conclusion, oral hygiene management of children with nutritional and respiratory complications at KNI was shown to be of high quality even without on-site intervention by dental specialists.
Asunto(s)
Caries Dental , Discapacidad Intelectual , Niño , Niño Institucionalizado , Índice CPO , Femenino , Humanos , Masculino , Salud Bucal , Higiene Bucal , Índice de Higiene OralRESUMEN
This research attempts to establish a method to measure 11 kinds of oxygenated volatile organic compound (OVOC) in ambient air by using the canister collection-gas chromatography/mass spectrometry (GC/MS) method. Since several compounds such as acetone exhibited high blank concentrations due to their laboratory use, stringent quality control was conducted for the VOC-free added water and the VOC-free nitrogen gas. In order to prevent the decline of recovery rates due to lack of sufficient relative humidity, it is necessary to add VOC-free water when pressurizing and diluting the air samples. Thus, all the target compounds in ambient air were obtained from the canisters at high recovery rates without significant contamination. Furthermore, the canister collection-GC/MS method makes it possible to apply simultaneous air monitoring of OVOCs as well as volatile hazardous air pollutants without additional sampling.
RESUMEN
Conformationally restricted 3-anilino-4-(3-indolyl)maleimide derivatives were designed and synthesized aiming at discovery of novel protein kinase Cbeta (PKCbeta)-selective inhibitors possessing oral bioavailability. Among them, compounds having a fused five-membered ring at the indole 1,2-position inhibited PKCbeta2 with IC50 of nM-order and showed good oral bioavailability. One of the most potent compounds was found to be PKCbeta-selective over other 6 isozymes and exhibited ameliorative effects in a rat diabetic retinopathy model via oral route.
Asunto(s)
Maleimidas/química , Maleimidas/farmacología , Proteína Quinasa C/antagonistas & inhibidores , Administración Oral , Animales , Disponibilidad Biológica , Diabetes Mellitus Experimental/tratamiento farmacológico , Retinopatía Diabética/tratamiento farmacológico , Relación Dosis-Respuesta a Droga , Maleimidas/farmacocinética , Maleimidas/uso terapéutico , Estructura Molecular , Proteína Quinasa C/metabolismo , Proteína Quinasa C beta , Ratas , Relación Estructura-ActividadRESUMEN
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg(-1) h(-1) in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg(-1) h(-1). These results suggest that compound 2 (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent.
Asunto(s)
Inhibidores del Factor Xa , Fibrinolíticos/síntesis química , Isoquinolinas/síntesis química , Piperidinas/síntesis química , Piridinas/síntesis química , Tetrahidroisoquinolinas/síntesis química , Administración Oral , Animales , Arteriopatías Oclusivas/complicaciones , Infarto Encefálico/tratamiento farmacológico , Infarto Encefálico/etiología , Infarto Encefálico/patología , Enfermedades Arteriales Cerebrales/complicaciones , Factor Xa/química , Fibrinolíticos/química , Fibrinolíticos/farmacología , Humanos , Inyecciones Intravenosas , Isoquinolinas/química , Isoquinolinas/farmacología , Macaca fascicularis , Arteria Cerebral Media , Modelos Moleculares , Piperidinas/química , Piperidinas/farmacología , Piridinas/química , Piridinas/farmacología , Ratas , Relación Estructura-Actividad , Tetrahidroisoquinolinas/química , Tetrahidroisoquinolinas/farmacología , Trombosis de la Vena/tratamiento farmacológicoRESUMEN
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent inhibitory activity against FXa and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkey, and showed a dose-dependent antithrombotic effect in a rat model of venous thrombosis.
Asunto(s)
Inhibidores del Factor Xa , Inhibidores de Serina Proteinasa/farmacología , Tetrahidroisoquinolinas/farmacología , Animales , Ratas , Inhibidores de Serina Proteinasa/uso terapéutico , Tetrahidroisoquinolinas/uso terapéutico , Trombosis de la Vena/tratamiento farmacológico , Trombosis de la Vena/enzimologíaRESUMEN
OBJECTIVE: To investigate how the increase in survival rate in extremely low birth weight (a birth weight of 1,000 g or less) infants had affected the incidence of retinopathy of prematurity (ROP) and the frequency of laser treatment. METHODS: We retrospectively reviewed the medical records of 122 surviving premature infants with birthweights less than 1,000 g to determine the severity of ROP observed at 16 neonatal intensive care units in Tokyo between April and October 2002. RESULTS: The survival rate was 85.6%. The mean gestational age was 26.74 weeks and the mean birth weight was 782.25 g. One-hundred-and-five infants (86.1%) developed ROP, fifty (41.0%) received laser treatment, and six (4.9%) had retinal detachment. The median postmenstrual age (gestational age at birth plus chronological age in weeks, PMA) at the onset of ROP was 32.5 weeks, and the first laser treatment was performed at the median PMA of 35.7 weeks. CONCLUSIONS: In these extremely low birth weight infants, there was an increase in the survival rate and in the incidence of severe ROP that progressed to the stage that required treatment.
Asunto(s)
Recién Nacido de muy Bajo Peso , Retinopatía de la Prematuridad/epidemiología , Peso al Nacer , Edad Gestacional , Humanos , Incidencia , Recién Nacido , Unidades de Cuidado Intensivo Neonatal/estadística & datos numéricos , Terapia por Láser , Retinopatía de la Prematuridad/terapia , Estudios Retrospectivos , Tasa de Supervivencia , Factores de Tiempo , Tokio/epidemiologíaRESUMEN
We report herein synthesis of PKCbeta-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide. Several compounds of this series exhibited IC50's as low as 50 nM against human PKCbeta2. One of the most potent compounds, 6l, inhibited PKCbeta1 and PKCbeta2 with IC50 of 21 and 5 nM, respectively, and exhibited selectivity of more than 60-fold in favor of PKCbeta2 relative to other PKC isozymes (PKCalpha, PKCgamma, and PKCepsilon).
Asunto(s)
Compuestos de Anilina/síntesis química , Indoles/síntesis química , Maleimidas/síntesis química , Proteína Quinasa C/antagonistas & inhibidores , Compuestos de Anilina/química , Humanos , Indoles/química , Isoenzimas/antagonistas & inhibidores , Isoenzimas/química , Maleimidas/química , Proteína Quinasa C/química , Proteína Quinasa C beta , Relación Estructura-ActividadRESUMEN
A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. Compounds with substituted aminocarbonylmethyl groups as the side chain showed potent FXa inhibitory activity. Compounds 1 and 2 exhibited most potent inhibitory activity and were effective as anticoagulants in a DIC model.