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1.
J Enzyme Inhib Med Chem ; 39(1): 2318830, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38488135

RESUMEN

The urgent demand for effective countermeasures against metallo-ß-lactamases (MBLs) necessitates development of novel metallo-ß-lactamase inhibitors (MBLIs). This study is dedicated to identifying critical chemical moieties within previously developed MBLIs, and critical MBLs should serve as the target in MBLI evaluations. Using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA), a systematic literature analysis was conducted, and the NCBI RefSeq genome database was exploited to access the abundance profile and taxonomic distribution of MBLs and their variant types. Through the implementation of two distinct systematic approaches, we elucidated critical chemical moieties of MBLIs, providing pivotal information for rational drug design. We also prioritised MBLs and their variant types, highlighting the imperative need for comprehensive testing to ensure the potency and efficacy of the newly developed MBLIs. This approach contributes valuable information to advance the field of antimicrobial drug discovery.


Asunto(s)
Inhibidores de beta-Lactamasas , beta-Lactamasas , Inhibidores de beta-Lactamasas/farmacología , Antibacterianos/farmacología , Diseño de Fármacos
2.
Int J Mol Sci ; 24(20)2023 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-37894890

RESUMEN

Pseudomonas aeruginosa is the primary opportunistic human pathogen responsible for a range of acute and chronic infections; it poses a significant threat to immunocompromised patients and is the leading cause of morbidity and mortality for nosocomial infections. Its high resistance to a diverse array of antimicrobial agents presents an urgent health concern. Among the mechanisms contributing to resistance in P. aeruginosa, the horizontal acquisition of antibiotic resistance genes (ARGs) via mobile genetic elements (MGEs) has gained recognition as a substantial concern in clinical settings, thus indicating that a comprehensive understanding of ARG dissemination within the species is strongly required for surveillance. Here, two approaches, including a systematic literature analysis and a genome database survey, were employed to gain insights into ARG dissemination. The genome database enabled scrutinizing of all the available sequence information and various attributes of P. aeruginosa isolates, thus providing an extensive understanding of ARG dissemination within the species. By integrating both approaches, with a primary focus on the genome database survey, mobile ARGs that were linked or correlated with MGEs, important sequence types (STs) carrying diverse ARGs, and MGEs responsible for ARG dissemination were identified as critical factors requiring strict surveillance. Although human isolates play a primary role in dissemination, the importance of animal and environmental isolates has also been suggested. In this study, 25 critical mobile ARGs, 45 critical STs, and associated MGEs involved in ARG dissemination within the species, are suggested as critical factors. Surveillance and management of these prioritized factors across the One Health sectors are essential to mitigate the emergence of multidrug-resistant (MDR) and extensively resistant (XDR) P. aeruginosa in clinical settings.


Asunto(s)
Antibacterianos , Pseudomonas aeruginosa , Animales , Humanos , Farmacorresistencia Microbiana/genética , Antibacterianos/farmacología , Antibacterianos/uso terapéutico
3.
Child Psychiatry Hum Dev ; 44(4): 549-55, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-23242708

RESUMEN

This study investigated childhood psychopathology and Internet addiction in adolescents. Initial assessment data were obtained from 1998 to 1999, and a follow-up assessment was performed in 2006, when the original subjects entered middle school. Personal information for the 524 male subjects was obtained from the original data. The subjects were evaluated with the Korean version of the child behavior checklist, which was administered to the children's parents. Demographic and psychosocial factors were also evaluated. Children were reassessed with the self-reported Korea Internet Addiction Scale. Our results indicated that 3.6 % of the subjects had Internet addiction, and revealed a significant relationship between withdrawal and anxiety/depression and future Internet addiction. The results suggest that withdrawal and anxiety/depression during childhood should be considered in the etiology of problematic Internet use in boys. Accordingly, clinicians should consider anxiety/depression and withdrawal during childhood to prevent Internet addiction.


Asunto(s)
Ansiedad/psicología , Conducta Adictiva/psicología , Depresión/psicología , Internet , Adolescente , Niño , Humanos , Estudios Longitudinales , Masculino , Estudios Prospectivos
4.
Planta Med ; 70(11): 1027-32, 2004 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-15549657

RESUMEN

In the present study, syringin, isolated by activity-guided fractionation of the ethyl acetate (EtOAc) extracts of the stem bark of Magnolia sieboldii, and sinapyl alcohol, the hydrolysate of syringin, were evaluated for anti-inflammatory and antinociceptive activities. Sinapyl alcohol (20, 30 mg/kg/day, p. o.) inhibited increased vascular permeability by acetic acid in mice and reduced acute paw edema by carrageenan in rats more so than syringin. When analgesic activity was measured using the acetic acid-induced writhing test and the hot plate test, sinapyl alcohol was much more potent than syringin in a mouse model. In addition, sinapyl alcohol more potently inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E2 (PGE2), and tumor necrosis factor (TNF)-alpha production by macrophages than syringin. Consistent with these observations, the expression levels of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 was reduced by sinapyl alcohol in a concentration-dependent manner. These results suggest that the anti-inflammatory and antinociceptive effects of syringin after oral administration may be attributed to its in vivo transformation to sinapyl alcohol.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Glucósidos/farmacología , Fenilpropionatos/farmacología , Fitoterapia , Ácido Acético , Administración Oral , Analgésicos/administración & dosificación , Analgésicos/uso terapéutico , Animales , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/uso terapéutico , Carragenina , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Edema/prevención & control , Glucósidos/administración & dosificación , Glucósidos/uso terapéutico , Magnolia , Masculino , Ratones , Ratones Endogámicos ICR , Fenilpropionatos/administración & dosificación , Fenilpropionatos/uso terapéutico , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
5.
Planta Med ; 69(7): 610-6, 2003 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-12898415

RESUMEN

In the present study, liriodendrin isolated by activity-guided fractionation from the ethyl acetate (EtOAc) extracts of the stem bark of Acanthopanax senticosus, was evaluated for anti-inflammatory and antinociceptive activities. Liriodendrin (5, 10 mg/kg/day, p. o.) significantly inhibited the increase of vascular permeability induced by acetic acid in mice and reduced an acute paw edema induced by carrageenan in rats. When the analgesic activity was measured by the acetic acid-induced writhing test and hot plate test, liriodendrin showed a dose-dependent inhibition in animal models. In addition, syringaresinol, the hydrolysate of liriodendrin, more potently inhibited the LPS-induced production of NO, PGE 2 and TNF-alpha production of macrophages than liriodendrin. Consistent with these observations, the expression level of iNOS and COX-2 enzyme was decreased by syringaresinol in a concentration-dependent manner. These results suggest that the anti-inflammatory and antinociceptive effects of liriodendrin after oral administration were attributable to the in vivo transformation to syringaresinol, which may function as the active constituent.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Eleutherococcus/química , Furanos/farmacología , Glucósidos/farmacología , Animales , Fraccionamiento Químico , Ciclooxigenasa 2 , Dinoprostona/biosíntesis , Furanos/antagonistas & inhibidores , Furanos/aislamiento & purificación , Glucósidos/aislamiento & purificación , Isoenzimas/biosíntesis , Corea (Geográfico) , Lignanos/antagonistas & inhibidores , Lipopolisacáridos/antagonistas & inhibidores , Masculino , Ratones , Ratones Endogámicos ICR , Óxido Nítrico/biosíntesis , Óxido Nítrico Sintasa/biosíntesis , Óxido Nítrico Sintasa de Tipo II , Dimensión del Dolor , Corteza de la Planta/química , Tallos de la Planta/química , Prostaglandina-Endoperóxido Sintasas/biosíntesis , Ratas , Ratas Sprague-Dawley , Factor de Necrosis Tumoral alfa/biosíntesis
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