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1.
J Nat Prod ; 68(8): 1256-8, 2005 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-16124772

RESUMO

Bioassay (P388 lymphocytic leukemia cell line and human cancer cell lines) guided separation of an extract prepared from the previously chemically uninvestigated Texas grasshopper Brachystola magna led to isolation of the cancer cell growth inhibitory pancratistatin (1), narciclasine (2), and ungeremine (3). Pancratistatin (1) was first isolated from the bulbs of Hymenocallis littoralis), and the original crystal structure was deduced by X-ray analysis of a monomethyl ether derivative. In the present study pancratistatin (1) was isolated from an extract of B. magna, which led to the X-ray crystal structure of this anticancer drug. Since isoquinoline derivatives 1-3 are previously known only as constituents of amaryllidaceous plants, some of the interesting implications of their rediscovery in the grasshopper B. magna that does not appear to utilize amaryllis family plants were discussed.


Assuntos
Antineoplásicos/isolamento & purificação , Alcaloides de Amaryllidaceae , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Gafanhotos , Humanos , Indolizinas , Isoquinolinas , Leucemia P388 , Conformação Molecular , Estrutura Molecular , Fenantridinas , Células Tumorais Cultivadas
2.
N Engl J Med ; 347(1): 13-8, 2002 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-12097535

RESUMO

BACKGROUND: The worldwide threat of arthropod-transmitted diseases, with their associated morbidity and mortality, underscores the need for effective insect repellents. Multiple chemical, botanical, and "alternative" repellent products are marketed to consumers. We sought to determine which products available in the United States provide reliable and prolonged complete protection from mosquito bites. METHODS: We conducted studies involving 15 volunteers to test the relative efficacy of seven botanical insect repellents; four products containing N,N-diethyl-m-toluamide, now called N,N-diethyl-3-methylbenzamide (DEET); a repellent containing IR3535 (ethyl butylacetylaminopropionate); three repellent-impregnated wristbands; and a moisturizer that is commonly claimed to have repellent effects. These products were tested in a controlled laboratory environment in which the species of the mosquitoes, their age, their degree of hunger, the humidity, the temperature, and the light-dark cycle were all kept constant. RESULTS: DEET-based products provided complete protection for the longest duration. Higher concentrations of DEET provided longer-lasting protection. A formulation containing 23.8 percent DEET had a mean complete-protection time of 301.5 minutes. A soybean-oil-based repellent protected against mosquito bites for an average of 94.6 minutes. The IR3535-based repellent protected for an average of 22.9 minutes. All other botanical repellents we tested provided protection for a mean duration of less than 20 minutes. Repellent-impregnated wristbands offered no protection. CONCLUSIONS: Currently available non-DEET repellents do not provide protection for durations similar to those of DEET-based repellents and cannot be relied on to provide prolonged protection in environments where mosquito-borne diseases are a substantial threat.


Assuntos
Culicidae , DEET , Mordeduras e Picadas de Insetos/prevenção & controle , Repelentes de Insetos , Insetos Vetores , Inseticidas , Plantas , beta-Alanina , beta-Alanina/análogos & derivados , Animais , DEET/administração & dosagem , Feminino , Humanos , Repelentes de Insetos/administração & dosagem , Inseticidas/administração & dosagem , Masculino , beta-Alanina/administração & dosagem
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