Synthesis and anticonvulsant activities of 3,3-dialkyl- and 3-alkyl-3-benzyl-2-piperidinones (delta-valerolactams) and hexahydro-2H-azepin-2-ones (epsilon-caprolactams).

A series of 3-substituted 2-piperidinone (delta-valerolactam) and hexahydro-2H-azepin-2-one (epsilon-caprolactam) derivatives were prepared and evaluated as anticonvulsants in mice. In the 2-piperidinone series, 3,3-diethyl compound 7b is the most effective anticonvulsant against pentylenetetrazole-induced seizures (ED50, 37 mg/kg; PI (TD50/ED50), 4.46), and 3-benzyl compound 4c (ED50, 41 mg/kg; PI, 7.

Polymorphonuclear leukocytes and human colostrum: effects of in vivo and in vitro exposure.

Polymorphonuclear leukocytes (PMN) from human colostrum were compared with blood and oral exudate PMN from the same donors for their locomotive, respiratory burst, phagocytic, and shape change (polarization) capabilities. Blood PMN were functionally superior to PMN from other sites. Colostrum PMN were similar to oral exudate PMN in all areas except locomotive responses.

The effects of treatment with PIXY321 (GM-CSF/IL-3 fusion protein) on human polymorphonuclear leukocyte function.

During a phase I trial of the genetically engineered hematopoietic growth factor PIXY321 (granulocyte-macrophage colony-stimulating factor/interleukin-3 [IL-3] fusion protein), we examined the effects of PIXY321 treatment on human polymorphonuclear leukocyte (PMN) locomotive, respiratory burst, and phagocytic responses. PIXY321 treatment was associated with transient suppression of both unstimulated locomotion and chemotaxis responses to multiple stimuli, as well as significant transient enhancement of formyl peptide-stimulated H2O2 production. No effects on opsonic phagocytosis of Staphylococcus aureus were observed.

The effects of interleukin-1 therapy on peripheral blood granulocyte function in humans.

During a phase I trial of interleukin-1 alpha (IL-1 alpha) in patients with ovarian carcinomas, the effects of this treatment on blood granulocyte respiratory burst and locomotive responses were examined. Differences in baseline granulocyte function in patients as well as dose-related effects of IL-1 alpha treatment were observed. Patients enrolled early in the trial (low-dose patients) had significantly lower locomotive responses before treatment than their paired controls; these low responses normalized after 5 days of continuous-infusion IL-1 alpha treatment.

Colostral antioxidants: separation and characterization of two activities in human colostrum.

Human colostrum contains several antioxidants which prevent the detection of human polymorphonuclear leukocyte (PMN) respiratory burst products. Using column chromatography to fractionate colostrum, two peaks of antioxidant activity were resolved away from colostral proteins and further characterized. One peak contained both cytochrome c-reducing activity and H2O2-depleting activity.