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Napolitano,H.B.; Silva,M.; Ellena,J.; Rodrigues,B.D.G.; Almeida,A.L.C.; Vieira,P.C.; Oliva,G.; Thiemann,O.H.. |
Several natural compounds have been identified for the treatment of leishmaniasis. Among them are some alkaloids, chalcones, lactones, tetralones, and saponins. The new compound reported here, 7-geranyloxycoumarin, called aurapten, belongs to the chemical class of the coumarins and has a molecular weight of 298.37. The compund was extracted from the Rutaceae species Esenbeckia febrifuga and was purified from a hexane extract starting from 407.7 g of dried leaves and followed by four silica gel chromatographic fractionation steps using different solvents as the mobile phase. The resulting compound (47 mg) of shows significant growth inhibition with an LD50 of 30 µM against the tropical parasite Leishmania major, which causes severe clinical manifestations... |
Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Coumarin; Aurapten (7-geranyloxycoumarin); X-rays; Leishmania; Inhibitor. |
Ano: 2004 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2004001200010 |
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Okubo, Kazuhiro; Yokoyama, Naoaki; Govind, Yadav; Alhassan, Andy; Igarashi, Ikuo. |
In the present study, we examined the effects of four kinds of cysteine protease inhibitors (E64, E64d, leupeptin, and ALLN) on the in vitro asexual growth of Babesia bovis. Of these, only the lipophilic inhibitors, E64d and ALLN, were found to effectively inhibit the growth of B. bovis. In further experiments, E64d, but not ALLN, significantly suppressed the parasite’s invasion of host erythrocytes, while both chemicals, especially ALLN, inhibited the parasite’s replication within the infected erythrocytes. These data suggested the presence of cysteine protease(s) derived from B. bovis, in which the protease(s) would play important roles in the erythrocyte invasion and/or replication processes of the parasite. |
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Palavras-chave: Babesia bovis; Cysteine protease; Inhibitor; Invasion; Replication. |
Ano: 2007 |
URL: http://ir.obihiro.ac.jp/dspace/handle/10322/1041 |
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Dube,Aman K.; Kumar,Maushmi S.. |
Abstract Fungi is a well-known model used to study drug metabolism and its production in in vitro condition. We aim to screen the most efficient strain of Cunninghamella sp. among C. elegans, C. echinulata and C. blakesleeana for bromhexine metabolites production. We characterized the metabolites produced using various analytical tools and compared them with mammalian metabolites in Rat liver microsomes (RLM). The metabolites were collected by two-stage fermentation of bromhexine with different strains of Cunninghamella sp. followed by extraction. Analysis was done by thin layer chromatography, high performance thin layer chromatography, Fourier transform infrared spectroscopy, high performance liquid chromatography and Liquid chromatography–mass... |
Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Cunninghamella sp.; Bromhexine; RLM; CYP3A4; Inhibitor; Metabolism. |
Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1517-83822017000200259 |
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Ji,C.; Ren,F.; Xu,M.. |
Nasopharyngeal carcinoma is a common malignancy in Southern China of uncertain etiologic origin. Diallyl trisulfide (DATS), one of the major components of garlic (Allium sativum), is highly bactericidal and fungicidal. In this study, we investigated the function of p38 mitogen-activated protein kinase (MAPK) and caspase-8 in DATS-induced apoptosis of human CNE2 cells using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide], flow cytometry assay, and Western blotting. After CNE2 cells were treated with DATS (50, 100, or 150 μM) for 24 h, cell viability rates were 75.9, 63.4 and 39.6%, and apoptosis rates were 24.5, 36.9, and 62.4%, respectively. The data showed that DATS induced CNE2 cell death in a dose-dependent manner. After human CNE2... |
Tipo: Info:eu-repo/semantics/article |
Palavras-chave: DATS; P38 MAPK; Caspase-8; Inhibitor; Apoptosis. |
Ano: 2010 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2010000900003 |
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MACHADO, R. J. A.; MONTEIRO, N. K. V.; MIGLIOLO, L.; SILVA, O. N.; PINTO, M. F. S.; OLIVEIRA, A. S.; FRANCO, O. L.; KIYOTA, S.; BEMQUERER, M. P.; UCHOA, A. F.; MORAIS, A. H. A.; SANTOS, E. A.. |
Tipo: Separatas |
Palavras-chave: Inhibitor; Seed; Erythrina velutina. |
Ano: 2013 |
URL: http://www.alice.cnptia.embrapa.br/alice/handle/doc/980468 |
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