Atividades antimicrobiana e leishmanicida das sementes de Pterodon emarginatus Vogel / Antimicrobial and leishmanicidal activities of seeds of Pterodon emarginatus

O presente trabalho investigou as atividades antimicrobiana e leishmanicida das sementes de Pterodon emarginatus Vogel. O potencial antimicrobiano do óleo essencial (OE) obtido das sementes foi avaliado através dos testes de difusão em ágar (10, 25 e 50 mg) e determinação da concentração inibitória mínima e utilizou os microorganismos-padrão: Staphylococcus aureus ATCC 25923, Streptococcus mutans ATCC 25175, Pseudomonas aeruginosa ATCC 90271, Escherichia coli ATCC 10530 e Candida albicans ATCC 10231. A atividade leishmanicida do OE e frações (6,25 - 100 µg/mL) obtidas das sementes de P. emarginatus foram testadas, in vitro, sobre formas promastigotas de L. amazonensis e L. chagasi. O OE das sementes de P. emarginatus inibiu o crescimento somente de S. aureus (CIM = 2,5 mg/mL). As frações hexânica (IC50 = 50,06 µg/mL) e butanólica (IC50 = 46,65 µg/mL) apresentaram atividade frente às formas promastigotas de L. amazonensis, porém não apresentaram atividade frente a L. chagasi. Os resultados indicam que as moléculas bioativas presentes nas sementes de P. emarginatus podem ser utilizadas como protótipos para o desenvolvimento de fármacos e/ou como fonte de matérias-primas farmacêuticas.

The present work investigated the antimicrobial and leishmanicidal activities of seeds of Pterodon emarginatus. The tests of diffusion in agar (10, 25 and 50 mg) and determination of minimum inhibitory concentration (MIC) were performed using essential oil (EO) obtained from seeds using the standard microorganisms: Staphylococcus aureus ATCC 25923, Streptococcus mutans ATCC 25175, Pseudomonas aeruginosa ATCC 90271, Escherichia coli ATCC 10530 and Candida albicans ATCC 10231. Leishmanicidal activity of the EO and fractions (6.25 - 100 µg/ml) obtained of seeds of P. emarginatus was evaluated in vitro using L. amazonensis and L. chagasi promastigote forms. The EO inhibited the growth of S. aureus (MIC = 2.5 mg/ml). The hexane (IC50 = 50.06 µg/ ml) and butanol (IC50 = 46.65 µg/ml) fractions showed activity against L. amazonensis promastigote forms, but did not against L. chagasi promastigote forms. The results indicate that the bioactive molecules present in the seeds of P. emarginatus can be used as prototype for the development of drug and/or as source pharmaceutical material.

Preparation and antileishmanial activity of lipophilic N-alkyl diamines.

We report in this work the preparation and the in vitro antileishmanial activity of a series of long chains N-monoalkylated diamines and two pyridinediamine derivatives. Several compounds, tested for their in vitro antiproliferative activity against Leishmania amazonensis and Leishmania chagasi, displayed a good inhibition of parasite growth, with IC(50) below 10 microM. Compounds 10 (N-dodecyl-1,2-ethanediamine), 15 (N-decyl-1,3-propanediamine) and 20 (N-dodecyl-1,4-butanediamine) were 7.3, 2.6 and 3.6 times, respectively, more active than the reference drug amphotericin B against L. chagasi promastigote forms.

Modulatory effects of 6-carboxymethylthiopurine on activated murine macrophages.

The immunological activity of macrophages against pathogens in hosts includes the phagocytosis and the production of nitric oxide. We report herein the investigation of the effect of 6-carboxymethylthiopurine on nitric oxide production by murine macrophages as well as its effect on the cell viability and proliferation after stimulus with Mycobacterium bovis bacille Calmette-Guérin, interferon-gamma or a combination of both. J774A.1 macrophages stimulated or not by bacille Calmette-Guérin (20 microg/mL), interferon-gamma or both, were cultured in the presence of 6-carboxymethylthiopurine (125, 250 and 500 microm). Nitric oxide production was measured by the Griess method and cell viability/proliferation by the diphenyltetrazolium assay [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide]. We observed an increase of J774A.1 cell proliferation after stimulus with bacille Calmette-Guérin at 125, 250 and 500 microm (69.1, 124.0 and 89.7%, respectively) and with interferon-gamma at 125 and 250 microm (64.8% and 61.7%, respectively) (p < 0.05). In all cultures treated with 6-carboxymethylthiopurine, interferon-gamma-activated nitric oxide production by J774A.1 cells decreased as well as when subjected to interferon-gamma plus bacille Calmette-Guérin stimuli at 500 microm (p < 0.05). Altogether these data point to an anti-inflammatory effect of 6-carboxymethylthiopurine on stimulated macrophages.

Antileishmanial and antifungal activity of plants used in traditional medicine in Brazil.

The antileishmanial and antifungal activity of 24 methanol extracts from 20 plants, all of them used in the Brazilian traditional medicine for the treatment of several infectious and inflammatory disorders, were evaluated against promastigotes forms of two species of Leishmania (L. amazonensis and L. chagasi) and two yeasts (Candida albicans and Cryptococcus neoformans). Among the 20 tested methanolic extracts, those of Vernonia polyanthes was the most active against L. amazonensis (IC(50) of 4 microg/ml), those of Ocimum gratissimum exhibited the best activity against L. chagasi (IC(50) of 71 microg/ml). Concerning antifungical activity, Schinus terebintifolius, O. gratissimum, Cajanus cajan, and Piper aduncum extracts were the most active against C. albicans (MIC of 1.25 mg/ml) whereas Bixa orellana, O. gratissimum and Syzygium cumini exhibited the best activity against C. neoformans (MIC of 0.078 mg/ml).