A new mesoionic compound, 4-phenyl-5-(4-nitro-cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine (MI-D), is described along with some of its biological properties. Its effects on hepatic metabolism, on O 2 À and nitric oxide (NO) production, and in in vivo models for potential antinociceptive, antipyretic, and antiinflammatory activities were determined. In perfused rat liver, MI-D (25 mM) stimulated glycogenolysis (95%), and inhibited oxygen uptake (37%) with affecting glycolysis. In phorbol 12-myristate 13-acetate-stimulated macrophages, O 2 À generation was reduced (95%) by MI-D (15 mM), whereas the production of NO was unaffected. MI-D (2 mg/kg) inhibited (55%) the number of abdominal writhings induced by acetic acid. At 1 mg/kg, MI-D inhibited the febrile response (5 h) induced by lipopolysaccharide (LPS) and was also effective against a preexisting febrile response. Treatment with MI-D (1 mg/kg) reduced by 67% prostaglandin (PGE 2 ) levels in the cerebrospinal fluid of LPS-exposed mice, and at a higher dose (8 mg/kg) MI-D inhibited paw edema formation (2 h) induced by carrageenan. MI-D has a spectrum of activities similar to other nonsteroidal antiinflammatory drugs, qualifying it as a potential anti-inflammatory drug. Drug Dev.

The aqueous extract (AE) and isolated fraction (ppt-3) of Cuphea carthagenensis (Jacq.) J. F. Macbr (sete-sangrias) were tested using models of nociception and inflammation in mice. Oral administration (p.o.) of the AE (10 to 100 mg/kg) and fraction ppt-3 (0.1 to 10 mg/kg) reduced the acetic acid-induced writhing in mice by 40 to 50% and by 46 to 70% of control, respectively. At the same doses AE and ppt-3 did not affect the tail flick response. Fraction ppt-3 also reduced the carrageenininduced paw edema, but at a dose 1000 times higher than that inducing antinociception. The results indicated the presence in the plant of antinociceptive constituents devoid of antiinflammatory activity, with actions apparently mediated by non-opioid mechanisms.Plants of the genus Cuphea, family Lythraceae, are known by the generic name of "sete-sangrias" and used in the Brazilian folk medicine as hypotensive, diuretic, antipyretic, antiinflammatory and laxative 1,2 . The hypotensive activity was confirmed in previous studies showing the decrease in blood pressure induced by the aqueous extract (AE) of Cuphea aperta 3

RESUMOO objetivo deste trabalho foi avaliar a dietilpropiona (DEP), um derivado fenetilamínico utilizado como anorexígeno, e dietas de diferentes densidades calóricas, utilizando ratos de ambos os sexos. O experimento contou com 72 ratos Wistar distribuídos por sexo, bloqueados por peso inicial e alocados dois a dois em 36 gaiolas experimentais. As dietas e a água foram fornecidas ad libitum e atenderam a todas as exigências dos animais, sendo que a dieta de alta energia continha 3.700kcal de energia metabolizável (EM)/kg, a média 3.350kcal EM/kg e a baixa 3.000kcal EM/kg de ração. A droga foi administrada com uma dose diária de 20mg/kg, durante 36 dias, por via intraperitonial. A análise estatística considerou os efeitos da droga, energia da dieta, sexo, triplicata e a interação entre essas variáveis. Os resultados mostraram que houve interação entre dieta e droga (p<0,0195) e que o uso da droga diminuiu o consumo alimentar apenas em dietas de baixa e média energias. A interação entre sexo e droga (p<0,0253) mostrou que a droga reduziu o ganho de peso em ambos os sexos. Concluiu-se que a DEP reduziu o ganho de peso dos machos e das fêmeas, com redução de gordura depositada em ambos os sexos, sendo que as percentagens de deposição de gordura foram maiores nas fêmeas do que nos machos, os quais depositaram mais proteína. A DEP foi responsável pela redução no consumo de dietas de baixa e média energia metabolizável, não havendo efeito em dietas de alta energia. ABSTRACTThis aim of this work is to evaluate diethylpropion (DEP), a phenethylamine like drug used as an anorectic, and different caloric density diets using rats of both sexes. The experiment used 72 Wistar rats distributed by sex blocked by initial weight and separated two by two in 36 experimental cages. The diets and water were permitted ad libitum and attended to animal needs. The high-energy diet had 3,700kcal of metabolizable energy (ME)/kg, the medium energy diet had 3,359kcal ME/kg and the low energy diet had 3,000kcal ME/kg of feed. The drug was administered intraperitonealy daily during 36 days. The statistical analysis considered the effects of the drug, energy of the diet, sex, replicates and the interaction between these factors. There was an interaction between diet and drug (p<0.0195) and the use of the drug reduced only the food intake of low and medium energy diets. An interaction between sex and drug (p<0.0253) showed that the weight gain was reduced in both sexes. We conclude that DEP reduces the weight gain in male and in female rats, with a reduction in fat deposition in both sexes. The percentages of fat reduction were higher on females than on males while the latter had higher deposition of protein on the carcass. DEP was responsible for a reduction on food intake of low and medium energy diets, having no effect on the high energy diet.

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