RESUMO
A series of homologues of alpha-asarone (1), containing variable size and functionality on the side chain attached to the aromatic ring, has been subjected to a study of structure-activity relationship. For most of the prepared derivatives, either with a carbonyl (8a-8e), a hydroxy group (9a-9e), or with a conjugated double bond (10a-10d), significant effects on serum lipoprotein cholesterol, LDL-cholesterol, HDL-cholesterol and triglycerides were displayed. The results showed an enhancement of the hypocholesterolemic activity as the length of the chain is decreased. Theoretical conformational and electrostatic potential analyses of I and olefins 10 suggest unfavorable steric interactions in the bulky superior side-chain homologues as the deactivating biological effect.
Assuntos
Anisóis/síntese química , Anisóis/farmacologia , Hipolipemiantes/síntese química , Derivados de Alilbenzenos , Animais , Colesterol na Dieta/farmacologia , Cristalografia por Raios X , Dieta , Ingestão de Alimentos/efeitos dos fármacos , Hipolipemiantes/farmacologia , Masculino , Camundongos , Modelos Moleculares , Espectrofotometria Ultravioleta , Relação Estrutura-Atividade , Aumento de Peso/efeitos dos fármacosRESUMO
Alpha-asarone is a hypolipidaemic agent obtained from Guatteria gaumeri, a medical plant used in Mexico to treat hypercholesteraemia and cholelithiasis. alpha-Asarone has been shown to be hepatocarcinogenic and mutagenic in a human lymphocyte assay, a murine bone marrow cell assay and in an unscheduled DNA synthesis assay. In this study, alpha-asarone was tested for dominant lethal effects in male CF1 mice. The drug was given orally at doses of 0, 10 and 30 mg/kg per day for 5 days. Males were mated weekly with eight consecutive batches of naive, nulliparous female mice. Repeated matings revealed no perceptible effect of alpha-asarone on the incidence of pregnancy. Examination of surgically exposed uteri and ovaries of pregnant females on day 13-15 of gestation revealed an increased incidence of post-implantation loss. Semen examination of a separate group of mice showed a decreased concentration and motility of spermatozoa. These results suggest a dominant lethal mutation as well as direct alpha-asarone toxicity to spermatozoa by in treated mice.
Assuntos
Anisóis/toxicidade , Carcinógenos/toxicidade , Genes Dominantes , Genes Letais , Contagem de Espermatozoides/efeitos dos fármacos , Motilidade dos Espermatozoides/efeitos dos fármacos , Derivados de Alilbenzenos , Animais , DNA/efeitos dos fármacos , Perda do Embrião/induzido quimicamente , Epididimo/efeitos dos fármacos , Epididimo/patologia , Feminino , Masculino , Camundongos , Testes de Mutagenicidade , Tamanho do Órgão/efeitos dos fármacos , Gravidez , Glândulas Seminais/efeitos dos fármacos , Glândulas Seminais/patologia , Testículo/efeitos dos fármacos , Testículo/patologiaRESUMO
Thalidomide is a drug that is being used in several diseases with an immunological component, but the effects on the different immune functions have only been studied partially. Therefore, we studied the effect of thalidomide on PPD-or Con-A-induced proliferation of human mononuclear cells. We found no direct effect of thalidomide at up to 50 micrograms/ml on the cultures. Cells taken from subjects 6 h after ingestion of 200 mg of thalidomide proliferated equally well to PPD and Con-A than cells taken prior to drug administration. Plasma taken from subjects that ingested 200 mg of thalidomide 6 h before did not affect the proliferative response of their own cells when added to the cultures. Plasma from rabbits that were injected with doses 5 or 15 times higher than the dose given to humans did not diminish the proliferative response of human mononuclear cells to PPD. We conclude that neither thalidomide nor its metabolites affect the proliferative response of human mononuclear cells.
Assuntos
Imunossupressores/farmacologia , Ativação Linfocitária/efeitos dos fármacos , Linfócitos/efeitos dos fármacos , Talidomida/farmacologia , Adolescente , Adulto , Animais , Concanavalina A/imunologia , Humanos , Masculino , Coelhos , Talidomida/metabolismo , Tuberculina/imunologiaRESUMO
El cancer del aparato digestivo es una causa frecuente de mortalidad, sin embargo su prevalencia en nuestro medio se desconece. En este trabajo se informan los resultados obtenidos en un analisis retrospectivo de 70,055 estudios histopatologicos; 61,533 correspondieron a material quirurgico-biopsia o pieza operatoria - de cinco anos (1975-1980), de ellos 673 (1.09%) presentaban proceso neoplasico maligno del aparato digestivo; los restantes 8, 522 correspondieron o protocolos de necropsia de 20 anos (1960-1980) en los que 352 (4.13%) presentaban igual patologia.Tanto en piezas operatorias como en necropsias la variedad histologica mas frecuente fue el carcinoma 82.6% y 92.8% respectivamente, seguida del linfoma. Por lo que hace a la localizacion del proceso los resultados varian igualmente segun el material motivo de estudio; en piezas operatorias los carcinomas mas frecuentes fueron: estomago (37.95%), vesicula y vias biliares (24.29%), colon (19.25%); mientras que al estudiar el material de necropsias la frecuencia fue: vesiculas y vias biliares (35.47%) pancreas (22.62%) y estomago (18.45%).Se senalan aspectos epidemiologicos, clinicos y terapeuticos de las neoplasias mas frecuentes informadas en esta revision
Assuntos
Humanos , Neoplasias do Sistema DigestórioRESUMO
A prospective and comparative study between the citology obtained through gastric washing and endoscopic (biopsy and brushing) for the diagnostic of the gastric neoplasias was carried at the Hospital de Especialidades del Centro Médico La Raza. Twenty one patients with benign gastric ulcer and 18 patients with gastric neoplasia (Two lymphomas and 16 adenocarcinomas) which we checked through surgery, necropsy or clinic evolution were studied. From 21 cases of gastric ulcer, the washing produced enough material for diagnosis in 17 of them (81%); in 16 of these neoplasia was excluded (94.1%) with false positive (5.9%). The endoscopic regained 100% of useful material and in a 100% ignored neoplasia. From 18 neoplasia cases, gastric washing produced material for 14 of them (77.8%); in 10 of these (71.4%) it made a diagnostic with 4 false negatives (28.6%); Endoscopic collected material in a 100% and the accuracy diagnostic was of 17 (94.4%) with one false negative (5.6%). Gastric washing has a high index of uselless for diagnostic from 39 samples, 8 were useless and from these, autolisis was the mein cause. Citology through gastric washing is usefull for neoplasm diagnosis in those cases in which endoscopy would be contraindicated or in those in which it is absent.
Assuntos
Adenocarcinoma/diagnóstico , Lavagem Gástrica , Linfoma/diagnóstico , Neoplasias Gástricas/diagnóstico , Citodiagnóstico/métodos , Gastroscopia , Humanos , Úlcera Gástrica/diagnósticoRESUMO
Biopsy of the pancreas frequently is followed by complications, this is why the transoperative aspiration biopsy has been recomended. During the last 2 years we used this procedure in 46 patients; in each case, one or several aspirations were done in the more-representative area of the pancreatic pathology. With the aspirated material a smear was fixed and treated with H-E stain. Biopsy was negative for carcinoma in 30 patients (65.2%), positive in 12 (26.0%), insuficient material results in other 4 (8.6%) we consider that the procedure was useful in the 82.6% of the cases and help to elect more adecuate surgical tecnic. There were no complications and we concluded that this is not a harmful procedure. The correct interpretation of the citology depends on the experience of the pathologyst with this method, to increase the percentage of correct diagnosis.