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1.
Appl Biochem Biotechnol ; 125(1): 63-75, 2005 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15834163

RESUMO

Esterification of glycerol with conjugated linoleic acid (CLA) was carried out in hexane. Lipase from Rhizomucor miehei provided a high degree of esterification (80%) in 8 h at 50 degrees C when used at 15% (w/w) in a system containing a 1:2 molar ratio of glycerol to free fatty acids. Esterification levels >80% were obtained in 8 h at 40 degrees C with 15% (w/w) lipase from Candida antarctica at the same molar ratio of reactants. The extent of esterification of CLA was >90% after 4 h of reaction at 50 degrees C with a 5% (w/w) loading of either R. miehei or C. antarctica lipase, together with a 1:1 molar ratio of substrates. Both enzymes incorporated the original CLA as acylglycerol residues in primarily 1,3-diacylglycerol and 1-monoacylglycerol. The CLA-rich acylglycerols can be employed as emulsifiers or as substitutes for natural fats and oils.


Assuntos
Diglicerídeos/biossíntese , Glicerídeos/biossíntese , Glicerol/metabolismo , Ácidos Linoleicos Conjugados/metabolismo , Lipase/metabolismo , Cromatografia Líquida de Alta Pressão , Enzimas Imobilizadas , Tecnologia de Alimentos/métodos , Glicerídeos/química , Hexanos , Rhizomucor/enzimologia , Temperatura
2.
J Org Chem ; 66(26): 8947-53, 2001 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-11749627

RESUMO

Two Candida antarctica lipases catalyze the enantioselective acylation of N-substituted trans-4-(4'-fluorophenyl)-3-hydroxymethylpiperidines in organic solvents. These two lipases show opposite stereochemical preference in these processes. Both enantiomers can be obtained in their optically pure forms. The (3S,4R) isomer, is an intermediate for the synthesis of (-)-Paroxetine.


Assuntos
Derivados de Benzeno/química , Piperidinas/química , Acetilação , Candida/enzimologia , Hidrólise , Indicadores e Reagentes , Lipase/química , Espectroscopia de Ressonância Magnética , Paroxetina/química , Solventes , Estereoisomerismo
3.
Gen Pharmacol ; 31(5): 747-51, 1998 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-9809473

RESUMO

1. The binding of 60 drugs, mainly steroids, to opioid receptors was studied in crude membrane fractions from mouse brains. 2. Competition assays with the different drugs (5 x 10(-7)-10(-4)M) were performed by labeling opiate receptors with [3H]diprenorphine (0.3-0.4 nM). 3. Only 7 drugs (alpha,5beta-tetrahydrodeoxycorticosterone, megestrol acetate, mifepristone, 17alpha-ethynylestradiol, diethylstilbestrol, clomiphene citrate and tamoxifen citrate) inhibited [3H]diprenorphine binding more than 50% at the highest concentration assayed (10(-4) M). The IC50 values ranged between 6x10(-5) M. 4. Thus, the present results show that only a limited number of steroids, from diverse classes, bind to opiate receptors.


Assuntos
Encéfalo/efeitos dos fármacos , Diprenorfina/metabolismo , Antagonistas de Entorpecentes/metabolismo , Esteroides/farmacologia , Animais , Ligação Competitiva , Encéfalo/metabolismo , Técnicas In Vitro , Masculino , Membranas , Camundongos , Esteroides/química , Esteroides/metabolismo , Relação Estrutura-Atividade
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