Antifungal activity of the naphthoquinone beta-lapachone against disseminated infection with Cryptococcus neoformans var. neoformans in dexamethasone-immunosuppressed Swiss mice

The in vivo antifungal activity of the naphthoquinone beta-lapachone against disseminated infection by Cryptococcus neoformans was investigated. Swiss mice were immunosuppressed daily with dexamethasone (0.5 mg per mouse) intraperitoneally for 3 days, the procedure was repeated 4 days later, and the animals were then challenged intravenously with C. neoformans (10(6) CFU/mL) 1 week later. Seven days after infection, the mice were divided into groups and treated daily with beta-lapachone (10 mg/kg, iv) for 7 (N = 6) and 14 days (N = 10). Amphotericin B (0.5 mg/kg) was used as comparator drug and an additional group received PBS. Treatment with beta-lapachone cleared the yeast from the spleen and liver, and the fungal burden decreased approximately 10(4) times in the lungs and brain 14 days after infection when compared to the PBS group (P < 0.05). This result was similar to that of the amphotericin B-treated group. Protection was suggestively due to in vivo antifungal activity of this drug and apparently not influenced by activation of the immune response, due to similar leukocyte cell counts among all groups. This study highlights the prospective use of beta-lapachone for treatment of disseminated cryptococcosis.

Antibacterial activity, chemical composition, and cytotoxicity of leaf's essential oil from Brazilian pepper tree (Schinus terebinthifolius, Raddi)

The antibacterial potential of leaf's essential oil (EO) from Brazilian pepper tree (Schinus terebinthifolius Raddi) against staphylococcal isolates from dogs with otitis externa was evaluated. The minimum inhibitory concentration of EO ranged from 78.1 to 1,250 fg/mL. The oil was analyzed by GC and GC/MS and cytotoxicity tests were carried out with laboratory animals.

Distribution of grasshoppers (Othoptera: Acridoidea) in the Tapacurá ecological station (São Lourenço da Mata, PE/Brazil)

Over the last five years, collection and periodic observation in the Tapacurá Ecological Station, São Lourenço da Mata, Pernambuco, Brazil, have been carried out to produce a systematic ecological inventory of grasshopper distribution within the station based on the classifying criteria for Acridoidea, providing new data on families, subfamilies, tribes, genera and species related to the various types of vegetation and environments the station affords.

Através de procedimento de coletas e observações periódicas, ao longo de cinco anos, na Estação Ecológica do Tapacurá, São Lourenço da Mata, PE, procedeu-se a um inventário sistemático-ecológico da distribuição dos gafanhotos da estação, adotando-se critérios classificatórios de Acridoidea com novos assinalamentos de famílias, subfamílias, tribos, gêneros e espécies, relacionados aos diversos tipos de vegetação e ambientes da estação.

Cytotoxic and DNA-topoisomerase effects of lapachol amine derivatives and interactions with DNA

The cytotoxic activity of amino (3a-e), aza-1-antraquinone (4a-e) lapachol derivatives against Ehrlich carcinoma and human K562 leukemia cells was investigated. Cell viability was determined using MTT assay, after 48 (Ehrlich) or 96 h (K562) of culture, and vincristine (for K562 leukemia) and quercetin (for Ehrlich carcinoma) were used as positive controls. The results showed dose-dependent growth-inhibiting activities and that the amino derivatives were active against the assayed cells, whereas the 4a-e derivatives were not. The allylamine derivative 3a was the most active against Ehrlich carcinoma, with IC50 = 16.94 ± 1.25 muM, and against K562 leukemia, with IC50 = 14.11 ± 1.39 muM. The analogous lawsone derivative, 5a, was also active against Ehrlich carcinoma (IC50 = 23.89 ± 2.3 muM), although the 5d and 5e derivatives showed lower activity. The interaction between 3a-d and calf thymus DNA was investigated by fluorimetric titration and the results showed a hyperchromic effect indicating binding to DNA as presented of ethidium bromide, used as positive control. The inhibitory action on DNA-topoisomerase II-a was also evaluated by a relaxation assay of supercoiled DNA plasmid, and the etoposide (200 muM) was used as positive control. Significant inhibitory activities were observed for 3a-d at 200 muM and a partial inhibitory action was observed for lapachol and methoxylapachol.

Estudo comparativo do óleo essencial de Eugenia punicifolia (HBK) DC. de diferentes localidades de Pernambuco / Comparative study of the essential oil of Eugenia punicifolia (HBK) DC. from diferent places of Pernambuco

O óleo essencial obtido por hidrodestilação das folhas de Eugenia punicifolia, coletados a partir de duas regiões de Matas Serranas do Estado de Pernambuco (Serra Negra e Brejo da Madre de Deus), foi analisado por CG/EM. O monoterpeno oxigenado, linalol (SN: 44,0 por cento, BMD: 61,2 por cento), foi o componente principal do óleo de ambas amostras. Cerca de 66,2 por cento da constituição dos voláteis da amostra proveniente de SN e 74,2 por cento de BMD referem-se aos monoterpenos oxigenados, enquanto 33,6 por cento da amostra de SN e 20,5 por cento de BMD são sesquiterpenos oxigenados, sendo o b-cariofileno o mais abundante (SN: 22,7 por cento, BMD: 16,2 por cento). Com exceção do a-cadinol, presente apenas no óleo proveniente do Brejo da Madre de Deus, a constituição química de ambas as amostras foi à mesma, variando apenas o percentual relativo de seus constituintes.

The essential oils obtained from the leaves of Eugenia punicifolia by hydrodistillation, which were collected from two different locations of Pernambuco (Serra Negra and Brejo da Madre de Deus), have been investigated by GC/MS. Linalol was found to be the main component of this oil from SN (44,0 percent) and BMD (61,2 percent). About 66,2 percent of the oil constituents from SN and 74,2 percent from BMD are oxygenated monoterpenes, with predominance of beta-cariofileno (SN: 22,7 and BMD: 16,2 percent). With exception of a-cadinol, present only in the oils from plants colleted in Brejo da Madre de Deus, the chemical composition of both samples was quite similar, the only difference was the relative content among their components.

Flavonóides isolados do pólen coletado pela abelha Scaptotrigona bipunctata (canudo)

Pólen de abelhas é uma mistura de pólens florais coletados pelas abelhas com ampla variação na sua composição. Investigação do pólen coletado pela abelha sem ferrão Scaptotrigona bipunctata levou a quatro agliconas de flavonóides: miricetina, dihidromiricetina, quercetina e isoramnetina. As estruturas foram estabelecidas a partir de dados espectroscópicos (NMR) das substâncias naturais.

Bee pollen is a mix of bee-collected floral pollens which varies widely in composition. Investigation of pollen collected by the stingless bee Scaptotrigona bipunctata yielded four flavonoid aglycones: myricetin, dihydromyricetin, quercetin and isorhamnetin. The structures were established from spectroscopic data (NMR) of the natural substances.