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1.
Appl Biochem Biotechnol ; 195(4): 2149-2157, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35778626

RESUMO

Tomato seeds are large waste byproducts from the processing of tomato into various food products like juice, sauce, and puree. One of the most potential uses of these tomato seeds is as a source of edible vegetable oil. The present study investigated the chemical characteristics including antioxidant activity, oxidative stability, and fatty acid composition of tomato seed extracted oil by aqueous and nonpolar (hexane) solvent. Fatty acid composition of tomato seed oils was determined by gas chromatography. Tomato seed oils were found to contain huge amount of linoleic acid, followed by oleic acid, palmitic acid, stearic acid, and linolenic acid. Polyunsaturated fatty acid and monounsaturated fatty acid content of the oil is near about 58% and 24%, respectively. Oxidative stability test of oil samples were evaluated by acid value, peroxide value, anisidine test, and TBA value. Antioxidant activity based on DPPH, FRAP, and ABTS assay of tomato seed oils was analyzed. The oil showed higher antioxidant activity-DPPH value (72-75%), FRAP value (9-11 µ mol/ml), and ABTS (37-39%). The results indicate hardly any difference in the fatty acid composition and antioxidant activity between aqueous and extracted and solvent-extracted tomato seed oil.


Assuntos
Antioxidantes , Solanum lycopersicum , Antioxidantes/química , Solventes , Ácidos Graxos , Sementes/química , Óleos de Plantas/química , Cromatografia Gasosa
2.
Food Funct ; 12(12): 5501-5523, 2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-34002192

RESUMO

There is increasing attention on the exploration of waste feedstocks as economically viable substrates for the production of prebiotic oligosaccharides, especially xylooligosaccharides, as excellent candidates for the maintenance and promotion of gut microbiota. XOS, an emerging prebiotic that has several functional attributes and beneficial health effects, is mainly produced by different processes, especially enzymatic hydrolysis through the valorisation of xylan enriched lignocellulosic materials. The present study deals with the enzymatic production of xylooligosaccharide (XOS) from xylan rich cauliflower stalk, a novel source. Delignification with alkali (NaOH) was found to be more efficient than acid and autohydrolysis, resulting in a higher extraction yield of xylan (18.42%). Alkaline extraction for 120 minutes at 1.25 M alkali concentration produced maximum xylan yield. FTIR analysis of xylan extracted from cauliflower stalk by an alkaline (NaOH) pretreatment method showed typical absorption bands at 1729 cm-1 that correspond to acetyl groups exhibiting the typical xylan specific band. Enzymatic hydrolysis was carried out with indigenously produced crude endoxylanase obtained from Aspergillus niger MTCC 9687 and the effects of substrate concentration, enzyme concentration, pH, time and temperature were investigated. High resolution MS analysis showed the presence of xylobiose as the major XOS. The major 1H spectral signals of XOS liberated from enzymatically hydrolysed alkali extracted cauliflower stalk xylan showed the presence of ß-anomeric protons in the spectral region of 4.0-4.7 ppm. Prebiotic efficacy of cauliflower stalk derived XOS alone and synbiotic combinations with known probiotic strains (Lactiplantibacillus plantarum, Bifidobacterium bifidum, Lactobacillus delbrueckii ssp. Helveticus) were evaluated. Butyrate was found to be the major short chain fatty acid produced by XOS supplemented fermentation media. All the synbiotic combinations showed significantly higher antioxidant and antimicrobial activities and reduced the viability of human bone cancer MG-63 cells. The individual profiles of antimicrobial components of XOS were identified as dihydroxy benzoic acid and aspartic acid by HPLC coupled to a photodiode array detector.


Assuntos
Brassica/química , Suplementos Nutricionais , Glucuronatos/farmacologia , Oligossacarídeos/farmacologia , Prebióticos , Aspergillus/enzimologia , Endo-1,4-beta-Xilanases , Fermentação , Microbioma Gastrointestinal/efeitos dos fármacos , Glucuronatos/química , Hidrólise , Lignina , Oligossacarídeos/química , Probióticos , Xilanos , Zea mays
3.
Prep Biochem Biotechnol ; 49(10): 935-948, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31407947

RESUMO

The present study investigated the operational conditions for different pretreatment approaches and subsequent enzymatic hydrolysis of cauliflower wastes (stalk and leaf) for better release of fermentable sugars. The structural analysis of raw and pretreated lignocellulosic biomasses was investigated using scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier transforms infrared (FTIR) analysis. Results demonstrated that the highest cellulose conversion rate and removal of most of the hemicellulose and lignin were obtained with organosolvent pretreatment. Using methanol in presence of sodium (Na) acetate was most effective in delignification of cauliflower wastes. In the present study, methanol (100% v/v) in presence of 0.1 M Na-acetate at 121 °C for 45 and 60 min for stalk and leaf, respectively, gave maximum reducing sugar yield. Response surface methodology was used to optimize different process parameters for enzymatic saccharification using microbial cellulase and xylanase. The optimum operation condition of enzymatic hydrolysis of organosolvent pretreated cauliflower wastes were substrate loading (2.5% w/v for both stalk and leaf), enzyme loading (15 and 10 U/g for stalk and leaf, respectively), pH (4.46 and 5.48 for stalk and leaf, respectively), at 60 °C and for 180 min.


Assuntos
Brassica , Compostos Orgânicos/química , Solventes/química , Gerenciamento de Resíduos/métodos , Biotecnologia/métodos , Metabolismo dos Carboidratos , Celulase/metabolismo , Celulose/metabolismo , Microscopia Eletrônica de Varredura , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
4.
J Genet Eng Biotechnol ; 16(2): 447-457, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30733759

RESUMO

In the domain of gene-gene network analysis, construction of co-expression networks and extraction of network modules have opened up enormous possibilities for exploring the role of genes in biological processes. Through such analysis, one can extract interesting behaviour of genes and would help in the discovery of genes participating in a common biological process. However, such network analysis methods in sequential processing mode often have been found time-consuming even for a moderately sized dataset. It is observed that most existing network construction techniques are capable of handling only positive correlations in gene-expression data whereas biologically-significant genes exhibit both positive and negative correlations. To address these problems, we propose a faster method for construction and analysis of gene-gene network and extraction of modules using a similarity measure which can identify both negatively and positively correlated co-expressed patterns. Our method utilizes General-purpose computing on graphics processing units (GPGPU) to provide fast, efficient and parallel extraction of biologically relevant network modules to support biomarker identification for breast cancer. The modules extracted are validated using p-value and q-value for both metastasis and non-metastasis stages of breast cancer. PNME has been found capable of identifying interesting biomarkers for this critical disease. We identified six genes with the interesting behaviours which have been found to cause breast cancer in homo-sapiens.

5.
J Genet Eng Biotechnol ; 16(1): 217-226, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30647725

RESUMO

Protein complexes are known to play a major role in controlling cellular activity in a living being. Identifying complexes from raw protein protein interactions (PPIs) is an important area of research. Earlier work has been limited mostly to yeast. Such protein complex identification methods, when applied to large human PPIs often give poor performance. We introduce a novel method called CSC to detect protein complexes. The method is evaluated in terms of positive predictive value, sensitivity and accuracy using the datasets of the model organism, yeast and humans. CSC outperforms several other competing algorithms for both organisms. Further, we present a framework to establish the usefulness of CSC in analyzing the influence of a given disease gene in a complex topologically as well as biologically considering eight major association factors.

6.
J Food Sci Technol ; 53(4): 2017-24, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-27413229

RESUMO

Palm stearin fractionate (PSF), obtained from palm stearin by further fractionation with solvents and n-3 polyunsaturated fatty acids (n-3 PUFA) rich fish oil (FO) were subjected to interesterification at 1:1, 1:2, 1:3, 2:1 and 3:1 substrate molar ratio and catalyzed by lipase from Thermomyces lanuginosa for obtaining a product with triacylglycerol (TAG) structure similar to that of human milk fat (HMF). The parameters (molar ratio and time) of the interesterification reaction were standardized. The temperature of 60 °C and enzyme concentration of 10 % (w/w) were kept fixed as these parameters were previously optimized. The reactions were carried out in a stirred tank reactor equipped with a magnetic stirrer for 6, 12, 18 and 24 h. The blends were analyzed for fatty acid (FA) composition of both total FAs and those at the sn-2 position after pancreatic lipase hydrolysis. All the blended products were subjected to melting point determination and free fatty acid content. Finally, blend of PSF and FO at 2:1 molar ratio with 69.70 % palmitic acid (PA) content and 12 h of reaction produced the desired product with 75.98 % of PA at sn-2 position, 0.27 % arachidonic acid (AA), 3.43 % eicosapentaenoic acid (EPA) and 4.25 % docosahexaenoic acid (DHA) and with melting point of 42 °C. This study portrayed a successful preparation of TAG containing unique FA composition i.e. ≥ 70 % of the PA, by weight, were esterified at the sn-2 position which could be used in infant formulation with health benefits of n-3 PUFAs.

7.
J Food Sci Technol ; 52(8): 5188-95, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26243941

RESUMO

The study aimed to evaluate the in vitro antioxidant activity of medium chain fatty acid (MCFA) rich-rice bran oils in comparison with native rice bran oil. Different in vitro methods were used to evaluate the free radical scavenging activity, metal chelation activity, reducing acitivity, ABTS radical scavenging activity, thiobarbituric acid (TBA) value and so on at different concentrations of the oils such as 10-100 µg/mL. Inhibition of lipid peroxidation was evaluated measuring thiobarbituric acid responsive substance (TBARS) and conjugated diene formation. All the oils showed potent antioxidant activity at 100 µg/mL concentration. TBARS formation and conjugated diene formation was lower with MCFA rich oils i.e. the inhibition of lipid peroxidation was more in MCFA rich oils than original rice bran oil. Caprylic acid rich rice bran oil showed maximum antioxidant activity in comparison to capric- and lauric acid rich rice bran oils. Overall the MCFA rich rice bran oils showed to be more potent antioxidant than rice bran oil due to their lower unsaturated fatty acid content.

8.
J Food Sci Technol ; 51(4): 715-21, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24741165

RESUMO

Structured lipids were prepared from mustard oil by enzymatic acidolysis reaction with capric acid (C10) using lipase enzyme TLIM from Thermomyces lanuginosus as biocatalyst. Parameters such as substrate molar ratio, enzyme concentration, reaction temperature, stirring speed and time of maximum incorporation, were studied for the optimization of the reaction. The optimized set of process conditions was predicted by response surface methodology (RSM) and genetic algorithm (GA). The robustness of GA and RSM was evaluated using regression coefficient and p value. The R(2) found out by GA was 0.996 while from RSM was 0.973. The results proved that GA models have better performance than RSM models. From the result, it could be concluded that optimal conditions for synthesis of capric acid rich mustard oil were: Temperature = 39.5 °C ; time = 21.1 hr; Substrate ratio = 3.5; Enzyme content = 8.8%; Speed = 570.8 rpm.

9.
Int J Bioinform Res Appl ; 8(1-2): 18-37, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22450268

RESUMO

This paper presents an effective parameter-less graph based clustering technique (GCEPD). GCEPD produces highly coherent clusters in terms of various cluster validity measures. The technique finds highly coherent patterns containing genes with high biological relevance. Experiments with real life datasets establish that the method produces clusters that are significantly better than other similar algorithms in terms of various quality measures.


Assuntos
Algoritmos , Análise por Conglomerados , Expressão Gênica , Bases de Dados Genéticas , Perfilação da Expressão Gênica , Análise de Sequência com Séries de Oligonucleotídeos/métodos
10.
Lipids ; 41(1): 49-54, 2006 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-16555471

RESUMO

The present study investigated the dietary effect of conjugated linolenic acid (CLnA) on lipid profiles and lipid peroxidations in alloxan-induced diabetes mellitus in rats. Diabetic rats were fed with 20% sunflower oil (diabetic control), sunflower oil supplemented with 0.5% CLnA, sunflower oil supplemented with 0.15% alpha-tocopherol, and sunflower oil containing 0.25% CLnA + 0.15% alpha-tocopherol. The results demonstrated that 0.5% CLnA, 0.15% alpha-tocopherol, and 0.25% CLnA + 0.15% alpha-tocopherol each on supplementation significantly lowered total cholesterol and non-HDL-cholesterol in comparison with the diabetic control group. The TAG level was significantly lowered in both the 0.15% alpha-tocopherol and 0.25% CLnA + 0.15% alpha-tocopherol groups. LDL-lipid peroxidation and erythrocyte membrane lipid peroxidation were reduced significantly in each of the experimental groups vs. the control group. The CLnA + alpha-tocopherol diet induced a greater reduction in membrane lipid and liver lipid peroxidation than the alpha-tocopherol diet alone. In conclusion, dietary CLnA exerts antioxidant activity as evidenced by reduced lipid peroxidation in chemically induced diabetes mellitus.


Assuntos
Diabetes Mellitus Experimental/sangue , Dieta , Ácidos Linolênicos/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Lipídeos/sangue , alfa-Tocoferol/farmacologia , Aloxano , Animais , Aterosclerose/prevenção & controle , Membrana Eritrocítica/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Ratos
11.
Indian J Exp Biol ; 43(7): 631-4, 2005 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-16053270

RESUMO

Salmonella pathogenesis is a complex phenomenon and a Type III secretion system plays a central role in the development of Salmonella-induced enteritis. One such Type III secretion protein is Salmonella outer protein E (SopE). Prevalence of sopE gene and its phenotypic expression (SopE protein) among different serovars of Salmonella enterica isolated from man and animals were investigated. Of 305 strains of S. enterica belonging to 11 serovars tested for the presence of sopE, 130 strains belonging to three serovars viz., Enteritidis, Gallinarum and Virchow were found to carry sopE gene irrespective of their source of isolation when tested by PCR amplification technique using its specific primers. Of these 130 strains, 112 strains were found to express SopE protein phenotypically as detected by Dot-ELISA using SopE antibody. Among the different serovars tested only serovars Gallinarum, Enteritidis and Virchow expressed SopE protein phenotypically in vitro. Role of SopE protein in pathogenesis of salmonellosis has been discussed.


Assuntos
Proteínas de Bactérias/genética , Genes Bacterianos , Salmonella enterica/genética , Animais , Sequência de Bases , DNA Bacteriano/genética , Humanos , Fenótipo , Salmonella enterica/classificação , Salmonella enterica/isolamento & purificação , Salmonella enterica/patogenicidade , Sorotipagem , Virulência/genética
12.
Can J Microbiol ; 47(5): 397-403, 2001 May.
Artigo em Inglês | MEDLINE | ID: mdl-11400729

RESUMO

Studies of the hydrolysis of bornyl, citronellyl, geranyl, and terpenyl acetates by commercially available lipases of Candida rugosa, Rhizopus arrhizus, and Mucor miehei are presented. The hydrolysis of these monoterpene esters is investigated at various temperatures and pHs, and the time dependence of the percentage of esters hydrolysed is studied. The catalytic activities of the lipases in hydrolysing the esters are compared and, overall, it is observed that under the experimental conditions used the nonspecific lipase from C. rugosa produces the highest yields of the monoterpene alcohols in comparison to the primary-ester specific lipases such as R. arrhizus and M. miehei. A rate kinetic model has been used to understand the time dependence of the yield of the product acid.


Assuntos
Lipase/metabolismo , Terpenos/metabolismo , Acetatos/metabolismo , Candida/enzimologia , Combinação de Medicamentos , Ésteres/metabolismo , Hidrólise , Cinética , Mucor/enzimologia , Óleos , Fenóis , Rhizopus/enzimologia , Especificidade da Espécie , Especificidade por Substrato , Temperatura
13.
Appl Microbiol Biotechnol ; 55(5): 541-6, 2001 May.
Artigo em Inglês | MEDLINE | ID: mdl-11414318

RESUMO

From a study of three fungal and 15 bacterial strains, it was observed that Pseudomonas putida MTCC 1072 oxidized limonene with the highest efficiency of. Fermentation of limonene by P. putida MTCC 1072 was conducted for 120 h at 30 degrees C at a fixed pH of 5.0. Major bioconversion products were isolated and characterized by Fourier transform infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopy, and by elemental analysis. The bioconversion products were identified as perillyl alcohol and p-menth-1-ene-6,8-diol, and under optimum conditions the yields were 36% and 44%, respectively (a rate kinetic model indicated corresponding limiting yields of 44% and 56%). No further degradation of the products was observed using this bacteria.


Assuntos
Pseudomonas putida/metabolismo , Terpenos/metabolismo , Bactérias/metabolismo , Biotecnologia , Biotransformação , Cicloexenos , Fermentação , Fungos/metabolismo , Concentração de Íons de Hidrogênio , Cinética , Limoneno , Espectroscopia de Ressonância Magnética , Oxirredução , Pseudomonas putida/crescimento & desenvolvimento , Especificidade da Espécie , Espectroscopia de Infravermelho com Transformada de Fourier , Temperatura
14.
J Agric Food Chem ; 49(5): 2641-6, 2001 May.
Artigo em Inglês | MEDLINE | ID: mdl-11368648

RESUMO

The nutritional effect of diet containing decorticated sesame seed extracted with isopropanol (DSS-Iso) was evaluated on growth performance, food efficiency ratio, plasma and tissue lipid profile, plasma protein content, and erythrocyte membrane lipid profile of rats on a comparative basis with diets containing casein (control), soybean meal, and decorticated sesame seed extracted with hexane (DSS-Hex). Rats fed a DSS-Iso-based diet showed body weight gain and food efficiency ratio similar to those of the control groups fed diets prepared with casein, soybean meal, and DSS-Hex. However, dietary proteins exerted a separate effect on plasma lipid concentrations of the rats. Rats fed a DSS-Iso-based diet showed significant decreases in plasma total cholesterol (p < 0.01), triglyceride (p < 0.01), and VLDL+LDL cholesterol (p < 0.01) concentrations in comparison to the rats fed diet containing casein. No significant differences in plasma lipid concentrations were observed for the rats fed diets prepared with soybean meal, DSS-Hex, and DSS-Iso. Rats fed the different dietary proteins did not show much variation in plasma proteins, liver lipids, and erythrocyte membrane lipid concentrations, which suggests that DSS-Iso could be a suitable edible protein like casein or soybean meal.


Assuntos
Proteínas de Plantas/análise , Sementes/química , 2-Propanol , Animais , Gorduras na Dieta/análise , Membrana Eritrocítica/química , Lipídeos/sangue , Masculino , Valor Nutritivo , Proteínas de Plantas/isolamento & purificação , Ratos , Aumento de Peso
15.
Plant Foods Hum Nutr ; 55(3): 265-78, 2000.
Artigo em Inglês | MEDLINE | ID: mdl-11030480

RESUMO

This study investigated the nutritional effect of sunflower seed protein fraction (SSPF) extracted with isopropanol on growth, plasma and tissue lipid profile, protein content and erythrocyte membrane lipid profile of rats. Dehulled sunflower seeds were extracted with isopropanol at 50 +/- 1 degree C resulting in a protein fraction (71.5%) with low residual chlorogenic acid (0.07%) and fiber (3.3%) contents. Rats fed the sunflower seed protein fraction had a similar body weight gain and food efficiency ratios in comparison to those fed casein. Rats fed SSPF in contrast had a significantly higher growth and food efficiency ratio than the rats fed sunflower meal (SM), extracted with hexane. However, dietary proteins exerted a separate effect on plasma total cholesterol, low density lipoprotein (LDL)-cholesterol, low density lipoprotein to high density lipoprotein cholesterol (LDL-C/HDL-C) ratio and triglyceride content. Sunflower seed protein fraction resulted in a significant decrease in plasma cholesterol (p < 0.05) and LDL-cholesterol (p < 0.02) levels compared to the casein fed rats. Membrane phospholipid profile also showed a marked variation with the type of dietary protein. Rats fed SSPF and SM did not show much variation in plasma lipids, plasma proteins, liver and brain lipids and membrane phospholipid concentrations. Protein content, liver and brain lipid profile of the groups fed SSPF and casein were comparable, suggesting that the nutritional value of SSPF is better than SM and equivalent to that of casein.


Assuntos
Helianthus/química , Sementes/química , 2-Propanol , Animais , Dieta , Gorduras na Dieta/análise , Proteínas Alimentares/isolamento & purificação , Membrana Eritrocítica/química , Lipídeos/sangue , Masculino , Lipídeos de Membrana/análise , Valor Nutritivo , Ratos
16.
J Med Chem ; 43(5): 921-44, 2000 Mar 09.
Artigo em Inglês | MEDLINE | ID: mdl-10715158

RESUMO

The design of potent protein kinase C (PK-C) ligands with low nanomolar binding affinities was accomplished by the combined use of pharmacophore- and receptor-guided approaches based on the structure of the physiological enzyme activator, diacylglycerol (DAG). Earlier use of the former approach, which was based on the structural equivalence of DAG and phorbol ester pharmacophores, identified a fixed template for the construction of a semirigid "recognition domain" that contained the three principal pharmacophores of DAG constrained into a lactone ring (DAG-lactones). In the present work, the pharmacophore-guided approach was refined to a higher level based on the X-ray structure of the C1b domain of PK-Cdelta complexed with phorbol-13-O-acetate. A systematic search that involved modifying the DAG-lactone template with a combination of linear or branched acyl and alpha-alkylidene chains, which functioned as variable hydrophobic "affinity domains", helped identify compounds that optimized hydrophobic contacts with a group of conserved hydrophobic amino acids located on the top half of the C1 domain where the phorbol binds. The hydrophilic/hydrophobic balance of the molecules was estimated by the octanol/water partition coefficients (log P) calculated according to a fragment-based approach. The presence of branched alpha-alkylidene or acyl chains was of critical importance to reach low nanomolar binding affinities for PK-C. These branched chains appear to facilitate important van der Waals contacts with hydrophobic segments of the protein and help promote the activation of PK-C through critical membrane interactions. Molecular modeling of these DAG-lactones into an empty C1b domain using the program AutoDock 2.4 suggests the existence of competing binding modes (sn-1 and sn-2) depending on which carbonyl is directly involved in binding to the protein. Inhibition of epidermal growth factor (EGF) binding, an indirect PK-C mediated response, was realized with some DAG-lactones at a dose 10-fold higher than with the standard phorbol-12, 13-dibutyrate (PDBU). Through the National Cancer Institute (NCI) 60-cell line in vitro screen, DAG-lactone 31 was identified as a very selective and potent antitumor agent. The NCI's computerized, pattern-recognition program COMPARE, which analyzes the degree of similarity of mean-graph profiles produced by the screen, corroborated our principles of drug design by matching the profile of compound 31 with that of the non-tumor-promoting antitumor phorbol ester, prostratin. The structural simplicity and the degree of potency achieved with some of the DAG-lactones described here should dispel the myth that chemical complexity and pharmacological activity go hand in hand. Even as a racemate, DAG-lactone 31 showed low namomolar binding affinity for PK-C and displayed selective antitumor activity at equivalent nanomolar levels. Our present approach should facilitate the generation of multiple libraries of structurally similar DAG-lactones to help exploit molecular diversity for PK-C and other high-affinity receptors for DAG and the phorbol esters. The success of this work suggests that substantially simpler, high-affinity structures could be identified to function as surrogates of other complex natural products.


Assuntos
4-Butirolactona/análogos & derivados , Antineoplásicos/química , Isoenzimas/metabolismo , Proteína Quinase C/metabolismo , Valeratos/química , 4-Butirolactona/síntese química , 4-Butirolactona/química , 4-Butirolactona/metabolismo , 4-Butirolactona/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Ligação Competitiva , Cristalografia por Raios X , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Ativação Enzimática , Fator de Crescimento Epidérmico/antagonistas & inibidores , Fator de Crescimento Epidérmico/metabolismo , Isoenzimas/química , Ligantes , Modelos Moleculares , Proteína Quinase C/química , Proteína Quinase C-alfa , Estereoisomerismo , Relação Estrutura-Atividade , Células Tumorais Cultivadas , Valeratos/síntese química , Valeratos/metabolismo , Valeratos/farmacologia
17.
J Med Chem ; 42(20): 4129-39, 1999 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-10514283

RESUMO

A series of substituted tetrahydrofurans with an embedded glycerol backbone carrying additional tetrahydrofuranylideneacetate or tetrahydrofuranylacetate motifs were grouped into four distinct templates (I-IV) according to stereochemistry. The compounds were designed to mimic three essential pharmacophores (C(3)-C=O, C(20)-OH and C(13)-C=O) of the phorbol esters according to a new, revised model. The tetrahydrofuran ring was constructed from glycidyl 4-methoxyphenyl ether, and the structures of the isomeric templates were assigned by NMR spectroscopy, including NOE. The binding affinity for protein kinase C (PKC) was assessed in terms of the ability of the ligands to displace bound [(3)H-20]phorbol 12, 13-dibutyrate (PDBU) from a recombinant alpha isozyme of PKC. Geometric Z- and E-isomers (1 and 3, respectively) containing a tetrahydrofuranylideneacetate motif were the most potent ligands with identical K(i) values of 0.35 microM. Molecular modeling studies of the four templates showed that the rms values when fitted to a prototypical phorbol 12,13-diacetate ester correlated inversely with affinities in the following order: I approximately II > III > IV. These compounds represent the first generation of rigid glycerol templates seeking to mimic the binding of the C(13)-C=O of the phorbol esters. The binding affinities of the most potent compounds are in the same range of the diacylglycerols (DAGs) despite the lack of a phorbol ester C(9)-OH pharmacophore surrogate. This finding confirms that mimicking the binding of the C(13)-C=O pharmacophore of phorbol is a useful strategy. However, since the C(9)-OH and C(13)-C=O in the phorbol esters appear to form an intramolecular hydrogen bond that functions as a combined pharmacophore, it is possible the lack of this combined motif in the target templates restricts the compounds from reaching higher binding affinities.


Assuntos
Furanos/química , Isoenzimas/química , Ésteres de Forbol/síntese química , Proteína Quinase C/química , Furanos/síntese química , Ligantes , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Conformação Molecular , Dibutirato de 12,13-Forbol/química , Ésteres de Forbol/química , Proteína Quinase C-alfa , Proteínas Recombinantes/química , Estereoisomerismo , Relação Estrutura-Atividade
18.
Lipids ; 34(2): 109-14, 1999 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-10102236

RESUMO

The present study examined the antioxidant activity of conjugated octadecatrienoic fatty acid (9 cis,11 trans,13 trans-18:3), alpha-eleostearic acid, of karela seed (Momordica charantia), fed to rats for 4 wk. The growth pattern of rats and the effect on plasma cholesterol and high density lipoprotein (HDL) cholesterol and peroxidation of plasma lipid, lipoprotein, eryhrocyte membrane, and liver lipid were measured. Rats were raised on diets containing sunflower oil mixed with three different levels of conjugated trienoic fatty acid (9c,11t,3t-18:3) 0.5, 2, and 10% by weight; the control group was raised with sunflower oil as dietary oil as the source of linoleic acid (9c,12c-18:2). The growth pattern of the three experimental groups of rats showed no significant difference compared to the control group of rats, but the group with 10% 9c,11t,13t-18:3 had slightly higher body weight than the control group of rats. Concentrations of total cholesterol, HDL-cholesterol, and non-HDL-cholesterol in plasma were similar in all four groups. Plasma lipid peroxidation was significantly lower in the case of 0.5% 9c,11t,13t-18:3 group than the control group and the 2 and 10% 9c,11t,13t-18:3 dietary groups as well. Lipoprotein oxidation susceptibility test with 0.5, 2, and 10% 9c,11t,13t-18:3 dietary groups was significantly less susceptible to lipoprotein peroxidation when compared with sunflower oil dietary group, and the dietary group with 0.5% 9c,11t,13t-18:3 showed least susceptibility. There was significant lowering in erythrocyte ghost membrane lipid peroxidation in the 0.5, 2, and 10% 9c,11t,13t-18:3 dietary groups compared to the sunflower oil groups. Nonenzymatic liver tissue lipid peroxidation was significantly lower in the group of rats raised on 0.5% 9c,11t,13t-18:3, but the groups on 2 and 10% 9c,11t,13t-18:3 acid did not show any significant difference compared with the control group of rats.


Assuntos
Antioxidantes/farmacologia , Ácidos Linolênicos/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Animais , Membrana Eritrocítica/efeitos dos fármacos , Membrana Eritrocítica/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Ratos , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo
19.
Ann Nutr Metab ; 42(5): 290-6, 1998.
Artigo em Inglês | MEDLINE | ID: mdl-9812020

RESUMO

The nutritive value of conjugated octadecatrienoic fatty acid (C18:3 Delta9,11,13alpha-elaeostearic acid) as occurs in karela seed (Momordica charantia) oil was studied. When rats were fed at the 20% level for 6 weeks, the growth pattern of rats and the food efficiency ratio showed a slightly significant difference compared to the group raised on linseed oil with non-conjugated octadecatrienoic acid (C18:3 Delta9,12,15alpha-linolenic acid) as control. The concentrations of total cholesterol, triglyceride, VLDL-cholesterol, LDL-cholesterol and LDL/HDL-cholesterol in serum were significantly higher in karela oil than in linseed oil. The liver lipid profile showed no difference. The total lipid as well as phospholipid concentrations of heart lipid were significantly higher in karela oil. The brain weight of the linseed oil group was significantly higher than the karela group. The brain phospholipid concentration of the karela oil group was significantly higher than that of the linseed oil group.


Assuntos
Gorduras Insaturadas na Dieta/administração & dosagem , Ácidos Linolênicos/administração & dosagem , Valor Nutritivo , Animais , Encéfalo/metabolismo , Colesterol/sangue , HDL-Colesterol/sangue , LDL-Colesterol/sangue , VLDL-Colesterol/sangue , Metabolismo dos Lipídeos , Lipídeos/sangue , Fígado/metabolismo , Masculino , Miocárdio/metabolismo , Ratos , Aumento de Peso
20.
Appl Radiat Isot ; 49(3): 215-26, 1998 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-9451776

RESUMO

This article considers a number of key issues in the disposal of waste containing enhanced levels of naturally occurring radioactive material (NORM), including gaseous, liquid and solid media. A brief review is made of sources of natural radioactivity in the biosphere and of anthropogenic enhancement of the concentration of NORM in the various media. The factors controlling the mobility of radionuclide activity in the environment are examined and disposal options are considered, comparison also being made with disposal of nuclear fuel cycle materials, in particular the tailings of uranium mining. Current and proposed disposal practices and policies for NORM are cited, reference being made to experiences in a number of countries.


Assuntos
Radiação de Fundo , Resíduos Radioativos , Radioisótopos/química , Eliminação de Resíduos/normas , Eliminação de Resíduos Líquidos/normas , Exposição Ambiental , Humanos , Mineração/normas , Radioisótopos/metabolismo , Eliminação de Resíduos/métodos , Tório , Urânio , Eliminação de Resíduos Líquidos/métodos , Microbiologia da Água
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