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Suppression of 12-O-tetradecanoylphorbol-13-acetate-induced ornithine decarboxylase activity by resveratrol derivatives Nature Precedings
Suaib Luqman; Tamara P. Kondratyuk; Juma Hosino; Mark Cushman; John M. Pezzuto.
As demonstrated previously, resveratrol (3,4',5-trihydroxy-trans-stilbene) inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ornithine decarboxylase (ODC), the key rate limiting enzyme in mammalian polyamine synthesis. Using human bladder epithelial carcinoma HTB-24 cells in culture where resveratrol inhibits induction with an IC50 of 8.8 µM, we now report potential metabolites demonstrate greater activity [tetrabutylammonium (E)-4-(3,5-dihydroxystyryl)phenyl sulfate (IC50 1.2 µM), resveratrol tripotassium 3,5,4'-trisulfate (IC50 1.8 µM), resveratrol tripotassium 3,4'-disulfate (IC50 1.8 µM), and resveratrol tripotassium 3,5-disulfate (IC50 2.3 µM)]. Based on RT-PCR...
Tipo: Poster Palavras-chave: Cancer; Chemistry; Molecular Cell Biology; Pharmacology.
Ano: 2012 URL: http://precedings.nature.com/documents/6908/version/1
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Chemopreventive potential of natural products isolated from a alchornea glandulosa, pterogyne nitens and its semisynthetic analogs Nature Precedings
Mauro C. C. Morais; Laura E. Marler; Suaib Luqman; Tamara P. Kondratyuk; Maicon S. Petronio; Luis O. Regasini; Dulce H. S. Silva; Vanderlan S. Bolzani; Christiane P. Soares; John M. Pezzuto.
INTRODUCTION: Chemoprevention involves the use of natural or synthetic substances to reduce the risk of developing cancer. Gallic acid was found to possess several pharmacological activities, such as anti-oxidant and anti-inflammatory. Guanidine alkaloids display a broad spectrum of biological activities and its cytotoxic effect were well investigated.
OBJECTIVES: The present study evaluated the chemopreventive potential of natural products and its semi-synthetic analogs using quinone reductase (QR) induction, aromatase inhibition and the suppression of NFκB activity, which are well established strategies for screening compounds to cancer chemoprevention. 
METHODS: Gallic acid was isolated from Alchornea...
Tipo: Poster Palavras-chave: Cancer; Chemistry; Molecular Cell Biology; Pharmacology.
Ano: 2012 URL: http://precedings.nature.com/documents/6923/version/1
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Inhibiton of NFκB activation and aromatase activity by vanilloids: An in vitro and in silico study Nature Precedings
Suaib Luqman; Abha Meena; Laura E. Marler; Tamara P. Kondratyuk; John M. Pezzuto.
Target-specific drugs, including natural products, offer promise for the amelioration of cancer and other human ailments with reduced side-effects. Capsaicin, the pungent ingredient present in chillies (Capsicum annuum L.), and capsazepine, a synthetic analogue of capsaicin (collectively referred to as vanilloids), are known to possess a variety of pharmacological and physiological properties. In our continuous effort to discover cancer chemopreventive agents from natural products, we investigated the effect of vanilloids on NFκB activation with stably transfected 293/NFκB-Luc human embryonic kidney cells induced by treatment with tumor necrosis factor (TNFα), and aromatase activity. Capsaicin and capsazepine blocked...
Tipo: Poster Palavras-chave: Cancer; Molecular Cell Biology; Pharmacology; Bioinformatics.
Ano: 2012 URL: http://precedings.nature.com/documents/6913/version/1
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Suppression of TNF-α induced NFκB activity by gallic acid and its semi-synthetic alkyl-gallates: Possible role in cancer chemoprevention Nature Precedings
Suaib Luqman; Mauro C. C. Morais; Tamara P. Kondratyuk; Maicon S. Petronio; Luis O. Regasini; Dulce H. S. Silva; Vanderlan S. Bolzani; Christiane P. Soares; John M. Pezzuto.
NFκB, a transcription factor, regulates the expression of a number of genes involved in carcinogenesis. Thus, agents that can suppress NFκB activation have the potential to suppress carcinogenesis. In the present investigation, gallic acid was isolated from Alchornea glandulosa (Euphorbiaceae) and eight semi-synthetic alkyl gallates were prepared from the reaction of the corresponding alcohols with gallic acid at 80oC for 48 h in good yields (70-97%). All the compounds were evaluated against TNF-α-induced NFκB activation with stable transfected 293/NFκB-Luc human embryonic kidney cells. Treatment of cells with gallic acid and the gallate esters (20 µg/ml) significantly reduced TNF-α...
Tipo: Poster Palavras-chave: Cancer; Chemistry; Molecular Cell Biology; Pharmacology.
Ano: 2012 URL: http://precedings.nature.com/documents/6922/version/1
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