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1.
Eur J Pharmacol ; 902: 174110, 2021 Jul 05.
Artículo en Inglés | MEDLINE | ID: mdl-33901457

RESUMEN

There is an almost unlimited interest in searching and developing new drugs, especially when we are in an era that are witnessing more and more emerging pathogens. Natural products from traditional medicines represent a large library for searching lead compounds with novel bioactivities. Sodium houttuyfonate is such one bioactive compound derived from Houttuynia cordata Thunb which has been employed in traditional medicine for treating infectious and inflammatory diseases. Sodium houttuyfonate has demonstrated multiple kinds of pharmacological effects, including antifungal, antibacterial, anti-inflammatory, and cardiovascular protective activities, which are discussed here to provide insights into our understanding of the pharmacological effects of SH and the underlying mechanisms.


Asunto(s)
Alcanos/farmacología , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Antifúngicos/farmacología , Cardiotónicos/farmacología , Sulfitos/farmacología , Alcanos/efectos adversos , Alcanos/química , Alcanos/uso terapéutico , Animales , Antibacterianos/efectos adversos , Antibacterianos/química , Antibacterianos/uso terapéutico , Antiinflamatorios/efectos adversos , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Antifúngicos/efectos adversos , Antifúngicos/química , Antifúngicos/uso terapéutico , Cardiotónicos/efectos adversos , Cardiotónicos/química , Cardiotónicos/uso terapéutico , Houttuynia/química , Humanos , Sulfitos/efectos adversos , Sulfitos/química , Sulfitos/uso terapéutico
2.
Phytochemistry ; 69(7): 1534-47, 2008 May.
Artículo en Inglés | MEDLINE | ID: mdl-18358504

RESUMEN

A defined mixture of rho iso-alpha-acids (RIAA), a modified hop extract, was evaluated for anti-inflammatory efficacy and safety. RIAA inhibited LPS-stimulated PGE(2) formation with >200-fold selectivity of COX-2 (IC(50)=1.3 microg/ml) over COX-1 (IC(50)>289 microg/ml). This occurred only when RIAA was added prior to, but not post, LPS stimulation. Consistent with this observation, RIAA produced no physiologically relevant, direct inhibition of COX-1 or COX-2 peroxidase activity. This suggests that RIAA inhibits inducible but not constitutive COX-2. In support, we found RIAA showed minimal PGE(2) inhibition (IC(50)=21mug/ml) relative to celecoxib (IC(50)=0.024 microg/ml), aspirin (IC(50)=0.52 microg/ml) or ibuprofen (IC(50)=0.57 microg/ml) in the AGS gastric mucosal model, where COX-1 and -2 are expressed constitutively. Taken together these results predict RIAA may have lower potential for gastrointestinal and cardiovascular toxicity observed with COX enzyme inhibitors. Following confirmation of bioavailable RIAA administered orally, gastrointestinal safety was assessed using the fecal calprotectin biomarker in a 14-day human clinical study; RIAA (900 mg/day) produced no change compared to naproxen (1000 mg/day), which increased fecal calprotectin 200%. Cardiovascular safety was addressed by PGI-M measurements where RIAA (1000 mg) did not reduce PGI-M or affect the urinary PGI-M/TXB(2) ratio. Drug interaction potential was evaluated against six major CYPs; of relevance, RIAA inhibited CYP2C9. Toxicity was assessed in a 21-day oral, mouse subchronic toxicity study where no dose dependent histopathological effects were noted. Clinically, RIAA (1000 mg/day) produced a 54% reduction in WOMAC Global scores in a 6-week, open-label trial of human subjects exhibiting knee osteoarthritis.


Asunto(s)
Alcanos/uso terapéutico , Antiinflamatorios/uso terapéutico , Ciclopentanos/uso terapéutico , Humulus/química , Osteoartritis/prevención & control , Extractos Vegetales/uso terapéutico , Adulto , Anciano , Alcanos/efectos adversos , Alcanos/farmacocinética , Animales , Antiinflamatorios/efectos adversos , Antiinflamatorios/farmacocinética , Disponibilidad Biológica , Peso Corporal/efectos de los fármacos , Línea Celular , Cromatografía Liquida , Inhibidores de la Ciclooxigenasa/efectos adversos , Inhibidores de la Ciclooxigenasa/farmacocinética , Inhibidores de la Ciclooxigenasa/uso terapéutico , Ciclopentanos/efectos adversos , Ciclopentanos/farmacocinética , Heces/química , Femenino , Humanos , Riñón/efectos de los fármacos , Riñón/patología , Complejo de Antígeno L1 de Leucocito/metabolismo , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Espectrometría de Masas , Ratones , Persona de Mediana Edad , Tamaño de los Órganos/efectos de los fármacos , Osteoartritis/patología , Extractos Vegetales/efectos adversos , Extractos Vegetales/farmacocinética , Prostaglandinas/orina , Resultado del Tratamiento
3.
J Eur Acad Dermatol Venereol ; 22(3): 290-6, 2008 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-18269596

RESUMEN

AIM: MAS064D (Sebclair) is a novel steroid-free cream containing multiple active ingredients. Objective of this pilot study was to evaluate the efficacy and safety of MAS064D in the treatment of mild to moderate SD of the face. METHODS: Patients (n = 60) with SD were randomized to receive MAS064D (n = 40) or a matching vehicle (n = 20). The primary study endpoint was investigators' global assessment (IGA) score at day 28, compared with baseline. Secondary endpoints included: IGA score at day 14; investigators' assessment of erythema and scaling; patients' assessment of burning/stinging, pruritus and global response to MAS064D; resort to rescue medication; quality of life. RESULTS: Use of MAS064D for 4 weeks was associated with a higher percentage of success in the MAS064D group than in the vehicle group (approximately 68% vs 11%, P < 0.0001). The effects of MAS064D were significantly better than those of vehicle for investigator-assessed erythema and scaling, and patients' assessed pruritus and global response to MAS064D (P 0.01). No patient in the MAS064D group required rescue medication, compared with two patients in the vehicle group. Four patients (two each in the MAS064D and vehicle groups) reported a total of six non-serious adverse events. CONCLUSIONS: MAS064D appears to be an effective and well tolerated cream for the treatment of mild to moderate SD of the face. Further clinical evaluation of MAS064D in SD is warranted.


Asunto(s)
Alcanos/administración & dosificación , Alantoína/administración & dosificación , Dermatitis Seborreica/tratamiento farmacológico , Fármacos Dermatológicos/administración & dosificación , Etanolaminas/administración & dosificación , Piridonas/administración & dosificación , Sesquiterpenos/administración & dosificación , Tiazolidinas/administración & dosificación , Vitamina E/administración & dosificación , Administración Tópica , Adulto , Anciano , Alcanos/efectos adversos , Alantoína/efectos adversos , Fármacos Dermatológicos/efectos adversos , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Combinación de Medicamentos , Etanolaminas/efectos adversos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Sesquiterpenos Monocíclicos , Pomadas , Proyectos Piloto , Piridonas/efectos adversos , Calidad de Vida , Sesquiterpenos/efectos adversos , Índice de Severidad de la Enfermedad , Tiazolidinas/efectos adversos , Resultado del Tratamiento , Vitamina E/efectos adversos
4.
Arch Kriminol ; 205(1-2): 37-43, 2000.
Artículo en Alemán | MEDLINE | ID: mdl-10726174

RESUMEN

After surgical treatment of an inguinal hernia, a 26-year-old male was discharged from hospital with a well healing surgical wound. Four weeks later he was admitted again with a major localized painful swelling of the soft tissues, whereas the clinical examination revealed no further local or systemic signs of inflammation. The immediate operation disclosed no abscess formation, but a large colliquation necrosis of the subcutaneous tissue with an outstanding petroleum-like odour. On toxicological examination of the necrotic tissue, a respective petroleum distillate was found. The patient was confronted with the suspicion of having injected the petroleum preparation himself to prolong the wound healing and finally admitted the self-mutilating behaviour. The pathophysiology, clinical history and morphological findings are discussed in comparison with case reports of chemically induced self-mutilation.


Asunto(s)
Alcanos/efectos adversos , Hernia Inguinal/cirugía , Petróleo/efectos adversos , Automutilación/patología , Infección de la Herida Quirúrgica/inducido químicamente , Adulto , Alcanos/administración & dosificación , Hernia Inguinal/patología , Humanos , Inyecciones Subcutáneas , Masculino , Necrosis , Piel/efectos de los fármacos , Piel/patología , Infección de la Herida Quirúrgica/patología , Cicatrización de Heridas/efectos de los fármacos
5.
Am J Emerg Med ; 16(5): 508-11, 1998 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-9725968

RESUMEN

A 33-year-old white man injected approximately 4 cc of charcoal lighter fluid (99.4% naptha/0.6% inert ingredients) subcutaneously into his left antecubital fossa. The injection resulted in the toxic necrosis of his volar forearm skin extending proximally to mid-humerus and distally to the metacarpophalangeal joints of the left hand dorsally over a 6-day period. The patient ultimately required extensive surgical debridement, secondary operative closure, and approximately 150 cm2 of split-thickness skin grafting. This case demonstrates the potential for widespread, delayed toxic necrosis of the skin resulting from subcutaneous injection of naptha. This patient's case appears to represent the most severe and widespread case of toxic necrosis of the skin resulting from the subcutaneous injection of hydrocarbons reported in the literature. This case also demonstrates extensive toxic thrombophlebitis not reported in prior cases involving subcutaneous injection of hydrocarbons.


Asunto(s)
Alcanos/efectos adversos , Traumatismos del Brazo/inducido químicamente , Tratamiento de Urgencia , Petróleo/efectos adversos , Tromboflebitis/inducido químicamente , Adulto , Alcanos/administración & dosificación , Humanos , Inyecciones Subcutáneas , Masculino , Necrosis , Intento de Suicidio
6.
Scand J Work Environ Health ; 22(2): 124-32, 1996 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-8738891

RESUMEN

OBJECTIVE: The present investigation examined whether increased overtime work predicts impairment in cognitive performance in the domains of attention, executive function, and mood. METHODS: The behavioral and cognitive functions of 248 automotive workers were measured by a neurobehavioral test performance. Overtime, defined as number of hours worked greater than 8 h a day or greater than 5 d a week, was calculated from company payroll records for the week before the test day. The number of consecutive days worked before the test day was also determined. RESULTS: Cross-sectional data analysis by multiple linear regression, after adjustment for the effects of age, education, gender, alcohol intake, repeated grade in school, acute petroleum naphtha exposure, shift worked, job type, number of consecutive days worked before the test day, and number of hours worked on the test day before the testing, demonstrated that increased overtime was significantly associated with impaired performance on several tests of attention and executive function. Increased feelings of depression, fatigue, and confusion were also associated with increased overtime work. In addition significant interaction effects were observed for job type but not for naphtha exposure. CONCLUSIONS: The findings support the hypothesis that overtime work results in impaired cognitive performance in the areas of attention and executive function and that both overtime hours and the number of consecutive days worked prior to a test day affect mood.


Asunto(s)
Cognición , Fatiga/psicología , Carga de Trabajo/psicología , Adulto , Afecto/efectos de los fármacos , Alcanos/efectos adversos , Atención/efectos de los fármacos , Cognición/efectos de los fármacos , Fatiga/inducido químicamente , Femenino , Humanos , Industrias , Modelos Lineales , Masculino , Memoria/efectos de los fármacos , Pruebas Neuropsicológicas , Exposición Profesional/efectos adversos , Petróleo/efectos adversos , Estudios Prospectivos , Desempeño Psicomotor/efectos de los fármacos , Estrés Fisiológico/psicología , Factores de Tiempo , Prueba de Secuencia Alfanumérica , Estados Unidos , Volición/efectos de los fármacos , Recursos Humanos
7.
J Occup Med ; 33(4): 516-26, 1991 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-2037907

RESUMEN

To investigate the relationship between exposure to organic solvents and the presence of increased urinary cellular sediment, we conducted a cross-sectional study of 215 newspaper pressroom workers who were exposed to solvent and lubricant mixtures. Thirty-two compositors were surveyed as referents. Industrial hygiene measurements showed low-level airborne exposures to organic solvents (primarily naphthas) and minimal airborne exposure to glycol ethers. There was a high prevalence of solvent-related dermatitis indicating there was significant dermal exposure to these substances. Pressworkers were exposed to solvent mixtures that were associated with dose-related increases in leukocyturia alone or in urinary cellular sediment (erythrocyturia and/or leukocyturia). The presence of urinary cellular sediment was associated with increasing frequency of use of five particular organic solvent mixtures. These results suggest that the increase in urinary cellular sediment may be due, at least in part, to the effects of solvents on the kidney. Consistent with this hypothesis, 16% of pressmen and no compositors were found to have primarily low-grade albuminuria detectable by dipstick. Workers with urinary cellular sediment were significantly more likely to have detectable albuminuria. Albuminuria was more likely to occur with increased frequency of use of four particular solvent mixtures. The presence of urinary cellular sediment was less likely to occur with occasional use of analgesics suggesting a possible etiologic role for acute or chronic urinary tract inflammation.


Asunto(s)
Albuminuria/inducido químicamente , Enfermedades Profesionales/inducido químicamente , Impresión , Solventes/efectos adversos , Orina/citología , Adulto , Alcanos/efectos adversos , Distribución de Chi-Cuadrado , Estudios de Cohortes , Estudios Transversales , Hematuria/inducido químicamente , Humanos , Persona de Mediana Edad , New England , Aceites Volátiles/efectos adversos , Petróleo/efectos adversos , Análisis de Regresión , Encuestas y Cuestionarios
12.
S Afr Med J ; 59(15): 522-4, 1981 Apr 04.
Artículo en Inglés | MEDLINE | ID: mdl-6261408

RESUMEN

Eight children and adolescents with a predominantly motor neuropathy of which the most likely cause was n-hexane are described. n-Hexane is one of the impurities in highest concentration in benzine, a petroleum product freely available at most corner stores in South Africa. It is bought freely by a large number of Black children in Natal and sniffed to produce a state of euphoria. Benzine sniffing by children constitutes a major health hazard in Natal.


Asunto(s)
Alcanos/efectos adversos , Discinesia Inducida por Medicamentos/etiología , Enfermedades del Sistema Nervioso Periférico/inducido químicamente , Petróleo/efectos adversos , Adolescente , Niño , Femenino , Hexanos/efectos adversos , Humanos , Masculino , Trastornos Relacionados con Sustancias/etiología
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