The triterpenes 3ß-lup-20(29)-en-3-ol and 3ß-lup-20(29)-en-3-yl acetate and the carbohydrate 1,2,3,4,5,6-hexa-O-acetyl-dulcitol as photosynthesis light reactions inhibitors.

Three compounds were isolated from Maytenus acanthophylla Reissek (Celastraceae): the pentacyclic triterpenes lup-20(29)-en-3ß-ol (lupeol, 1) and 3ß-lup-20(29)-en-3-yl acetate (2) and the carbohydrate 1,2,3,4,5,6-hexa-O-acetyldulcitol (3); lupeol was also isolated from Xylosma flexuosa. The compounds' structures were elucidated by spectroscopic and spectrometric analysis. Compound 1 acts as an energy transfer inhibitor, interacting with isolated CF1 bound to thylakoid membrane, and dulcitol hexaacetate 3 behaves as a Hill reaction inhibitor and as an uncoupler, as determined by polarography. Chlorophyll a (Chl a) fluorescence induction kinetics from the minimum yield F0 to the maximum yield F(M )provides information of the filling up from electrons coming from water to plastoquinone pool with reducing equivalents. In this paper we have examined the effects of compounds 1 and 3 on spinach leaf discs. Compound 1 induces the appearance of a K-band, which indicates that it inhibits the water splitting enzyme. In vivo assays measuring the fluorescence of chl a in P. ixocarpa leaves sprayed with compound 1, showed the appearance of the K-band and the PSII reaction centers was transformed to "heat sinks" or silent reaction centers unable to reduce Q(A). However, 3 also induced the appearance of a K band and a new band I appears in P. ixocarpa plants, therefore it inhibits at the water splitting enzyme complex and at the PQH2 site on b6f complex. Compounds 1 and 3 did not affect chlorophyll a fluorescence of L. perenne plants.

In vitro activity of 2-pyridinecarboxylic acid against trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus / Atividade in vitro do ácido 2-piridinocarboxílico em tripanossoma do subgênero Schizotrypanum isolado do morcego Phyllostomus hastatus

The effect of 2-pyridinecarboxylic acid (picolinic acid) on trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus was determined in this study. Picolinic acid, at 50 µg mL-1, inhibited epimastigote growth by 99% after 12 days incubation. In addition, trypomastigote motility decreased by 50% after 6h and completely after 24h in the presence of 50 µg mL-1 picolinic acid. The 50% cytotoxic concentration on HEp-2 cell line was 275 µg mL-1 after 4 days incubation. Altogether, these results indicate higher toxicity against trypanosomes. The inhibitory effect of picolinic acid on epimastigote growth can be partially reversed by nicotinic acid and L-tryptophan, suggesting a competitive inhibition. Furthermore, two anti-Trypanosoma (Schizotrypanum) cruzi drugs were also evaluated with regard to bat trypanosome growth. Benznidazole, at 50 µg mL-1, inhibited epimastigote growth by 90% after 12 days incubation. Nifurtimox, at the same concentration, caused 96% growth inhibition after four days incubation. Corroborating a previous study, bat trypanosomes are a good model for screening new trypanocidal compounds. Moreover, they can be used to study many biological processes common to human pathogenic trypanosomatids.

O efeito do ácido 2-piridinocarboxílico (ácido picolínico) sobre um tripanossoma do subgênero Schizotrypanum isolado do morcego Phyllostomus hastatus foi determinado neste estudo. O ácido picolínico, na concentração de 50 µg mL-1, inibiu 99% do crescimento de epimastigotas após 12 dias de incubação. Além disso, houve um decréscimo de 50 e 100% na mobilidade dos tripomastigotas após 6 e 24h, respectivamente, em presença de ácido picolínico na concentração de 50 µg mL-1. A concentração citotóxica 50% para células HEp-2 foi de 275 µg mL-1 após quatro dias de incubação. Esses resultados indicam maior toxicidade contra os tripanossomas. O efeito inibitório do ácido picolínico sobre o crescimento de epimastigotas pode ser parcialmente revertido por ácido nicotínico e L-triptofano, sugerindo inibição competitiva. Adicionalmente, o efeito de dois fármacos com atividade anti-Trypanosoma (Schizotrypanum) cruzi foi avaliado sobre o crescimento do tripanossoma de morcego. Benzonidazol, na concentração de 50 µg mL-1, inibiu 90% do crescimento de epimastigotas após 12 dias de incubação. Nifurtimox, na mesma concentração, causou 96% de inibição do crescimento após quatro dias de incubação. Corroborando trabalhos anteriores, tripanossomas de morcegos são bons modelos para seleção inicial de novos compostos tripanocidas. Além disso, eles podem ser utilizados para estudar vários processos biológicos comuns aos tripanossomatídeos patogênicos ao homem.

Salvinia auriculata: aquatic bioindicator studied by instrumental neutron activation analysis (INAA).

Through instrumental neutron activation analysis (INAA) the elemental chemical composition of Salvinia auriculata and Ouro Preto city public water was determined. Elements Ce, Th, Cr, Hf, Sb, Sc, Rb, Fe, Zn, Co, Au, La and Br were quantified. High chromium concentration was determined in this plant. But, chromium was determined only in low concentrations in the water. The results indicate the great capacity of this plant to absorb and accumulate inorganic elements.

Anti-trypanosomal activity of pentacyclic triterpenes isolated from Austroplenckia populnea (Celastraceae).

Four pentacyclic triterpenes isolated from Austroplenckia populnea and four compounds of known anti T. cruzi or anti-malarial activity were tested. Of those triterpenes tested 20alpha-hydroxy-tingenone showed high activity, epikatonic acid was less active, while populnilic and populninic acids were inactive against the trypanosome of the subgenus Schizotrypanum tested. Benzonidazole, nifurtimox, ketoconazole and primaquine presented a remarkable dose-dependent inhibitory effect reaching practically to a total growth inhibition of the parasite at the end of incubation time. The trypanosome tested appear to be a suitable model for preliminary screen for anti T. (S.) cruzi compounds.

Anti-trypanosomal activity of pentacyclic triterpenes isolated from Austroplenckia populnea (Celastraceae)

Four pentacyclic triterpenes isolated from Austroplenckia populnea and four compounds of known anti T. cruzi or anti-malarial activity were tested. Of those triterpenes tested 20alpha-hydroxy-tingenone showed high activity, epikatonic acid was less active, while populnilic and populninic acids were inactive against the trypanosome of the subgenus Schizotrypanum tested. Benzonidazole, nifurtimox, ketoconazole and primaquine presented a remarkable dose-dependent inhibitory effect reaching practically to a total growth inhibition of the parasite at the end of incubation time. The trypanosome tested appear to be a suitable model for preliminary screen for anti T. (S.) cruzi compounds

Constituintes químicos e atividade antiespermatogênica em folhas de Austroplenckia populnea (Celastraceae)

Folhas de Austroplenckia populnea (mangabarana, marmelinho do campo) foram submetidos a estudo fitoquímico. Do extrato hexânico foram isolados e identificados três triterpenos pentacíclicos e um sesquiterpeno agarofurânico inédito. Realizou-se testes de atividade antiespermatogência utilizando parte deste extrato. Os resultados mostraram uma redução significativa do número de espermatozóides no epidídimo.