ABSTRACT This study assesses the anti-arthritic effect of the affinin-enriched (spilanthol, main alkamide) hexane extract from the roots of Heliopsis longipes (A. Gray) S.F. Blake, Asteraceae, on a Freund adjuvant-induced arthritis model in rodents. The extract was orally administered at a dose of 2, 6.6, or 20 mg/kg; a significant edema-inhibitory activity in the acute and chronic phases was observed with a dose of 2 and 20 mg/kg, respectively. The extract showed higher anti-inflammatory and anti-arthritic effects than the reference drug phenylbutazone (80 mg/kg). Moreover, the extract prevented the occurrence of secondary lesions associated to this pharmacological model.

The N-acylase activity and enantioselectivity of mammalian kidney acetone powders (KAP's) or their enzyme extract was demonstrated on (rac)-N-acetylmethionine; used as reference substrate. It was showed hydrolysis exclusively on the (S)-enantiomer. The biocatalyzed reaction allowed us, to categorize the KAPs regarding the animal source, sheep, pig, calf, bovine, dog and guinea pig as fast biocatalysts reaching equilibrium in around 4 to 5 h; and rat, mouse and hamster were slower biocatalysts, since they did it in around 24 h. In most of the reactions the kidney crude preparations gave a better conversion than the enzyme extract, this fact demonstrated that the longer stirring during the reaction in an aqueous medium, allowed a greater dissolution of the enzyme. These readily available and inexpensive crude biocatalysts have a great potential application in organic synthesis.

La enantioselectividad y actividad N-acilasa de los polvos acetónicos de riñón de mamíferos (KAP's) o su extracto enzimático fue demostrada sobre N-acetilmetionina racémica, la cual fue usada como substrato de referencia. La hidrólisis mostró preferencia exclusiva por el enantiómero-S. La reacción biocatalizada también permitió diferenciar los KAP's de acuerdo a la fuente animal, borrego, cerdo, ternera, res, perro y cuyo alcanzaron el equilibrio en aproximadamente 4 a 5 h; y rata, ratón y hámster lo hicieron en más de 24 h. En la mayoría de las reacciones, las preparaciones crudas de riñón dieron mejor conversión que el extracto enzimático, este hecho demostró que la agitación prolongada durante la reacción, permitió mayor disolución de la enzima. Estos biocatalizadores crudos, fácilmente disponibles y de bajo costo, tienen un gran potencial de aplicación en la síntesis orgánica.

Chiral diarylmethanols are versatile building blocks for the preparation of biologically active substances, but they are difficult to obtain in enantiopure form. We used Nocardia corallina B-276 for the oxidative kinetic resolution of (±)-4-(chlorophenyl)phenylmethanol, 1. Two experimental methods were used: 1) Suspension of cells in a phosphate buffer solution and 2) Cells in the culture media, in a 3-L bioreactor. After 36 hrs using the first method, the ketone/alcohol ratio was 56/44 and the unoxidized alcohol had an enantiomeric ratio of 93/7, predominating the R-alcohol.

Liver acetone powders (LAPs) were used as hydrolase sources to biocatalyze the hydrolysis of N-protected-2-hydroxymethylpiperidine acetates (N-Ts and N-Boc). Different reaction conditions were evaluated, like source of LAP (cat, guinea pig, chicken, dog, sheep, bovine, rat, mouse, pig and rabbit), proportion of cosolvent, type of cosolvent and pH.

Como fuente de hidrolasas se usaron polvos acetónicos de hígado (PAH), para biocatalizar la hidrólisis de los acetatos de la 2-hidroximetilpiperidina N-protegida (N-Ts y N-Boc). Se evaluaron diferentes condiciones de reacción, como la fuente del PAH (gato, cuyo, pollo, perro, borrego, res, rata, ratón, cerdo y conejo), la proporción de codisolvente, tipo de codisolvente y pH.

The esterification of phenylpropanoid and hydrophenylpropanoid acids, catalyzed by candida antarctica lipase B (CAL-B), with several alcohols has demonstrated that the substitution pattern on the aromatic ring has a very significant influence on the reactivity of the carboxyl group due, mainly, to electronic effects, when compared to the unsaturated acids with the hydrogenated acids. It is also clear that in the saturated acids there still remain some unclear effects related to the aromatic substituents.