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1.
Chem Commun (Camb) ; 52(51): 7943-6, 2016 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-27253678

RESUMO

Mono-, di- and trisaccharide derivatives of 1,2-unsaturated N-acetyl-d-glucal have been synthesized and shown to function as tight-binding inhibitors/slow substrates of representative hexosaminidases. Turnover is slow and not observed in the thioamide analogue, allowing determination of the 3-dimensional structure of the complex. Inhibition is insensitive to pH and to mutation of key catalytic residues, consistent with the uncharged character of the inhibitor. These properties could render this inhibitor class less prone to development of resistance.


Assuntos
Desoxiglucose/análogos & derivados , Inibidores Enzimáticos/farmacologia , Hexosaminidases/antagonistas & inibidores , Sítios de Ligação/efeitos dos fármacos , Biocatálise , Desoxiglucose/síntese química , Desoxiglucose/química , Desoxiglucose/farmacologia , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Hexosaminidases/metabolismo , Concentração de Íons de Hidrogênio , Modelos Moleculares , Estrutura Molecular
2.
Arq. Inst. Biol ; 80(2): 229-232, 20130000.
Artigo em Português | LILACS, VETINDEX | ID: biblio-1462222

RESUMO

The aim of this study was to evaluate the effects of physic nut and neem oil on the hatching of caterpillars of Diatraea saccharalis (Fabr., 1794). Tests were conducted in acclimatized chambers at 25 ± 2 C, RH 70 ± 10% and photophase of 12h. The treatments were: distilled water (control), aqueous solution of physic nut oil at 3%; aqueous solution of neem oil at 3%, and aqueous solution of physic nut and neem oil, both at 3%. A total of 250 eggs from D. saccharalis up to 24 hours of age were used for each treatment. Each egg mass containing 50 eggs, constituting one repetition, was immersed three times, for one second, in the respective treatments. Then the eggs were distributed in Petri dishes (5 cm diameter) containing filter paper moistened with distilled water at the bottom to prevent drying of the egg mass. Evaluations were made of the embryonic period and the percentage of hatched larvae of D. saccharalis. Differences were found that indicate that the vegetable oils had a toxic effect on the hatching of sugarcane borer larvae. In the treatment with neem oil only 42.4% of the eggs hatched. In the treatment with physic nut + neem oil 70% of the eggs hatched, and in the treatment with physic nut oil 60% of the eggs hatched. An increase in the embryonic period was also observed, particularly in the treatment with physic nut oil (7.09 days). It can be inferred that the oils of.


O objetivo deste trabalho foi verificar os efeitos dos óleos de pinhão-manso e neem na eclosão de lagartas de Diatraea saccharalis (Fabr., 1794). Os testes foram conduzidos em câmaras climatizadas a 25 ± 2 C, UR de 70 ± 10% e fotofase de 12 horas. Os tratamentos foram compostos por: água destilada (testemunha); solução aquosa de óleo de pinhão-manso a 3%; solução aquosa de óleo de neem a 3% e solução aquosa de óleo de pinhão-manso + óleo de neem a 3%. Foram utilizados 250 ovos de D. saccharalis com até 24 horas de idade, por tratamento. Cada massa de ovos contendo 50 ovos, constituindo uma repetição, foi imersa três vezes, durante um segundo, nos respectivos tratamentos. Em seguida, os ovos foram distribuídos em placas de Petri (5 cm de diâmetro) contendo no fundo papel filtro umedecido com água destilada, para evitar o ressecamento das massas de ovos. Foram avaliados o período embrionário e a porcentagem de lagartas eclodidas de D. saccharalis. Verificou-se efeito tóxico dos óleos vegetais sobre a eclosão das lagartas da broca-da-cana, constatando-se diferenças. Observou-se que, no tratamento com neem, apenas 42,4% das lagartas eclodiram. Para o tratamento de pinhão-manso + neem ocorreu 70% da eclosão das lagartas e com o óleo de pinhão-manso, 60% de lagartas eclodidas. Foi verificado também um alongamento do período embrionário, principalmente do tratamento com óleo de pinhã.


Assuntos
Inseticidas , Jatropha
3.
Mem Inst Oswaldo Cruz ; 92(4): 517-22, 1997.
Artigo em Inglês | MEDLINE | ID: mdl-9361747

RESUMO

A comparative histopathological study of three snails species--Biomphalaria glabrata, B. tenagophila and B. straminea--which had been infected with Schistosoma mansoni miracidia revealed similar qualitative features; consisting of areas of sporocyst proliferation and differentiation associated with reactive host reaction, at the time they were actively eliminating great number of cercariae. However, in specimens that were exposed to miracidia but failed to eliminate cercariae later on, different histopathological pictures were observed in different snail species. While B. glabrata exhibited frequent focal (granulomatous) proliferation of amebocytes in several organs, B. tenagophila and B. straminea only rarely showed such reactive changes, suggesting that the mechanism of resistance to miracidial infection probably follows different pathways in the snail species studied.


Assuntos
Biomphalaria/parasitologia , Schistosoma mansoni , Animais , Biomphalaria/fisiologia
4.
Hum Reprod ; 9(3): 413-6, 1994 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-8006127

RESUMO

In 18-week-old nulliparous rabbit does, ovulation was induced with 50 IU of pure urinary luteinizing hormone (LH; LH group), or 50 IU of human chorionic gonadotrophin (HCG; HCG group), in order to determine the effect of these treatments on 17 beta-oestradiol and progesterone concentrations, and on oocyte and embryo quality. Luteinizing follicles, recovered oocytes, progesterone concentration and grade 5 embryos were significantly reduced when pure urinary LH was used. Statistically significant correlations were found: (i) between oestradiol concentration and number of degenerated oocytes in both groups (positive); (ii) between oestradiol concentration and grade 1 and 2 embryos (negative), and grade 5 embryos (positive) in the HCG group; (iii) between progesterone concentration and metaphase II oocytes (negative), and between progesterone and grade 5 embryos (positive), in the HCG group; and (iv) between progesterone and oestradiol concentrations (negative) in the LH group. It seems that the oestradiol to progesterone ratio improves during the early luteal phase when ovulation is induced with LH, and that oestradiol and progesterone concentrations could play a role in determining oocyte and embryo quality.


Assuntos
Hormônio Luteinizante/farmacologia , Indução da Ovulação/métodos , Animais , Gonadotropina Coriônica/farmacologia , Estradiol/sangue , Feminino , Hormônio Luteinizante/urina , Ovário/anatomia & histologia , Progesterona/sangue , Coelhos , Útero/anatomia & histologia
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