Evaluation on the leishmanicidal activity of 2-N,N'-dialkylamino-1,4-naphthoquinone derivatives.

Parasites of the Leishmania genus are the causative agents of leishmaniasis in humans, a disease that affects more than 12 million people worldwide. In this study was evaluated in vitro leishmanicidal activity of 2-N,N'-dialkylamino-1,4-naphthoquinone derivatives, covering a series of fourteen 2-N-morpholino-, 2-N-thiomorpholino, 2-N-piperidino, 2-N-(N4-methyl)-piperazino naphthoquinones (1a-n) derived from nor-lapachol and lawsone, belong to some other di-alkyaminoderivatives. At the cytotoxicity assay on peritoneal macrophages, the compounds possessing larger alkyl groups and N-methyl-piperazino moiety (1d, 1h, 1i and 1k), showed toxic effects similar to the standard drug used pentamidine. However, the other compounds of the series showed no deleterious effect on the host cell. Meanwhile, these cytotoxic derivatives (1d, 1h and 1i) had pronounced leishmanicidal activity against L. amazonensis promastigotes, and treatments with six other compounds (1d, 1e, 1f, 1h, 1k and 1n) had significant effect leishmanicidal against L. chagasi promastigotes. In the assay against L. chagasi amastigotes, eight compounds (1a, 1b, 1c, 1d, 1h, 1i, 1k and 1m) showed significant activity. Moreover, the compounds (1a, 1b, 1c, and 1m) showed effect against amastigotes of L. chagasi and not being toxic to the host cell. These data show the derivatives as promising substances for research leishmanicidal activity.

Croton grewioides Baill. (Euphorbiaceae) Shows Antidiarrheal Activity in Mice.

UNLABELLED: Based on chemotaxonomy, we decided to investigate the possible antidiarrheal activity in mice of a crude ethanolic extract obtained from aerial parts of Croton grewioides (CG-EtOH). We tested for any possible toxicity in rat erythrocytes and acute toxicity in mice. Antidiarrheal activity was assessed by determining the effect of CG-EtOH on defecation frequency, liquid stool, intestinal motility and intestinal fluid accumulation. CG-EtOH showed no in vitro cytotoxicity and was not orally lethal. In contrast, the extract given intraperitoneally (at 2000 mg/kg) was lethal, but only in females. CG-EtOH produced a significant and equipotent antidiarrheal activity, both in defecation frequency (ED50 = 106.0 ± 8.1 mg/kg) and liquid stools (ED50 = 105.0 ± 9.2 mg/kg). However, CG-EtOH (125 mg/kg) decreased intestinal motility by only 22.7% ± 4.4%. Moreover, extract markedly inhibited the castor oil-induced intestinal contents (ED50 = 34.6 ± 5.4 mg/kg). We thus conclude that CG-EtOH is not orally lethal and contains active principles with antidiarrheal activity, and this effect seems to involve mostly changes in intestinal secretion. SUMMARY: CG-EtOH showed no in vitro cytotoxicity and was not orally lethal. In contrast, the extract given intraperitoneally (at 2000 mg/kg) was lethal, but only in females.CG-EtOH probably contains active metabolites with antidiarrheal activity.CG-EtOH reduced the frequency and number of liquid stools.Metabolites presents in the CG-EtOH act mainly by reducing intestinal fluid and, to a lesser extent, reducing intestinal motility. Abbreviations Used: CG-EtOH: crude ethanolic extract obtained from the aerial parts of C. grewioides; WHO: World Health Organization; ED50: dose of a drug that produces 50% of its maximum effect; Emax: maximum effect.

Peso dos recém-nascidos normais de termo do Hospital Universitário de Joäo Pessoa / Weight of normal newborn infants at term of the Hospital Universitário de Joäo Pessoa

Os autores estudaram o peso de recém-nascidos normais de termo (37 - 41 semanas) de 604 nascimentos únicamente normais, ocorridos na Maternidade do Hospital Universitário da UFPb, no período de 1980 a 1984. Determinaram o peso médio, e se fez comparaçöes entre os pesos médios dos neonatos em cada semana de nascimento. Discutiram as conveniências da utilizaçäo clínica do peso médio, e recomendaram a elaboraçäo e utilizaçäo de cartas de crescimento ponderal intra-uterino compatíveis com as características sócio-econômicas, biológicas e geográficas da populaçäo trabalhada. No momento atual, já näo se aceita o conceito de prematuridade baseado apenas no peso dos infantes ao nascer. Apesar de durante muito tempo o peso ter sido empregado como critério para o diagnóstico de prematuridade, longe vai o tempo em que se aceitava sem discussöes a proposiçäo de Ylppo feita em 1920 e aprovada por Comité Internacional em 1937, a qual afirmava que o peso crítico abaixo do qual um recém-nascido deveria ser classificado como prematuro era de 2500g. Com o tempo verificou-se que o padräo sugerido por Ylppo näo era aplicável para todas as regiöes do globo, e que em algumas ele era totalmente errôneo. Com o aprofundamento dos estudos sobre a questäo, constatou-se que a utilizaçäo do peso como parâmetro único para o diagnóstico de prematuridade, era inconveniente, estabelecendo-se que o limite entre a prematuridade e maturidade seria uma linha que incidiria nas 37 semanas completas, calculadas a partir do 1§ dia do último período menstrual. Sendo, portanto, prematuro, todos os infantes nascidos antes de 37 semanas completas de gestaçäo, independente do peso ao nascer. A partir do momento, em que verificou-se que o peso ao nascer, näo está necessariamente relacionado com a prematuridade, procurou-se o significado verdadeiro do peso dos recém-nascidos, chegando-se à conclusäo que é um bom índice de desenvolvimento intra-uterino...