BackgroundDue to the indiscriminate use of antimicrobial drugs, the emergence of human pathogenic microorganisms resistant to major classes of antibiotics has been increased and has caused many clinical problems in the treatment of infectious diseases. Thus, the aim of this study was to evaluate for the first time the in vitro antimicrobial activity and brine shrimp lethality of extracts and isolated compounds from Zeyheria tuberculosa (Vell.) Bur., a species used in Brazilian folk medicine for treatment of cancer and skin diseases.MethodsUsing the disc diffusion method, bioautography assay and brine shrimp toxicity test (Artemia salina Leach), we studied the antimicrobial activity and lethality of extracts and isolated compounds against three microorganisms strains, including Gram-positive (Staphylococcus aureus) and Gram-negative (Pseudomonas aeruginosa) bacteria and yeasts (Candida albicans).ResultsIn this study, the extracts inhibited S. aureus (8.0 ± 0.0 to 14.0 ± 0.0 mm) and C. albicans (15.3 ± 0.68 to 25.6 ± 0.4 mm) growth. In the brine shrimp test, only two of them showed toxic effects (LC50 29.55 to 398.05 μg/mL) and some extracts were non-toxic or showed weak lethality (LC50 705.02 to > 1000 μg/mL). From these extracts, four flavones [5,6,7,8-tetramethoxyflavone (1), 5,6,7-trimethoxyflavone (2), 4'-hydroxy-5,6,7,8-tetramethoxyflavone (3), and 4'-hydroxy-5,6,7-trimethoxyflavone (4)] were isolated through bioassay-guided fractionation and identified based on the 1D and 2D NMR spectral data. By bioautography assays, compounds 1 [S. aureus (16.0 ± 0.0 mm) and C. albicans (20.0 ± 0.0 mm)] and 3 [S. aureus (10.3 ± 0.6 mm) and C. albicans (19.7 ± 0.6 mm)] inhibited both microorganisms while 2 inhibited only S. aureus (11.7 ± 0.6 mm). Compound 4 did not restrain the growth of any tested microorganism.ConclusionOur results showed that extracts and isolated flavones from Z. tuberculosa may be particularly useful against two pathogenic microorganisms, S. aureus and C. albicans. These results may justify the popular use this species since some fractions tested had antimicrobial activity and others showed significant toxic effects on brine shrimps. However, in order to evaluate possible clinical application in therapy of infectious diseases, further studies about the safety and toxicity of isolated compounds are needed.

In an effort to find effective and affordable ways to control of Aedes aegypti L. (Diptera: Culicidae), the larvicidal activities of 94 extracts from ten plant species belonging to eight families [Guettarda grazielae and Spermacoce verticillata (Rubiaceae), Coccoloba mollis and Triplaris americana (Polygonaceae), Eschweilera ovata (Lecytidaceae), Merremia aegyptia (Convolvulaceae), Ouratea nitida (Ochnnaceae), Protium heptaphyllum (Burseraceae), Rourea doniana (Connaraceae), and Tovomita brevistaminea (Guttiferae)], widely found in the northeast of Brazil, were initially screened at 250 microg/mL. Nineteen of the 94 extracts from six plant species (C. mollis, G. grazielae, M. aegyptia, R. doniana, S. verticillata, and T. americana) showed significant activity (>75% mortality) against the fourth instar larvae. Some of these extracts showed 100% mosquito larvae mortality, with LD(50) values lower 200 microg/mL. When compared to synthetic insecticide Temephos (LD(50) 8.7 microg/mL), two of them, hexane (LD(50) 12.1 microg/mL) and ethyl acetate (LD(50) 51.6 microg/mL) extracts from stems of R. doniana and G. grazielae, respectively, were the most effective. The isolation and purification of these extracts are in progress and evaluation of these compounds will be needed to identify the active component.

This study aims to explain the effects of silicon on chlorophyll and to measure gas exchange and carbohydrate levels in two Lycopersicon esculentum cultivars that are exposed to drought. The experimental design used in this study was a randomised combination of five different water and silicon conditions (control, water deficit + 0.00 μmol Si, water deficit + 0.25 μmol Si, water deficit + 1.00 μmol Si, and water deficit + 1.75 μmol Si) applied to the two cultivars (Super Marmante and Santa Cruz). Parameters measured were gas exchanges, chlorophylls, and total soluble carbohydrates. Silicon at concentrations of 0.25, 1.00, and 1.75 μmol induced a gradual increase in the total chlorophyll levels. A correlation analysis revealed a linear, positive interaction between the leaf water potential and the total chlorophyll (r = 0.71; P < 0.05). This study confirmed the hypothesis that silicon has a beneficial effect with regard to chlorophyll. Under water-deficient conditions, both cultivars showed an increase in chlorophyll a when treated with silicon in addition to changes in the total chlorophyll levels. These results were supported by the change in leaf water potential. In addition, a reduction of the effects of water restriction was also observed in the transpiration rate, the stomatal conductance and in the levels of total carbohydrates.

Sabicea species are used in the Amazon for treatment of fever and malaria, which suggests that its chemical constituents may have some effect on pain and inflammation. Phytochemical analysis of the hexane fraction obtained from the crude ethanol extract from Sabicea grisea var. grisea Cham. & Schltdl (Rubiaceae), an endemic plant in Brazil, resulted in the isolation of octacosanol. This study investigated the antinociceptive and anti-inflammatory effects of the octacosanol in different experimental models. The crude ethanolic extract and hexane fraction obtained from the leaves of S. grisea produced an inhibition of acetic acid-induced pain. Moreover, octacosanol isolated from the hexane fraction produced a significant inhibition of pain response elicited by acetic acid. Pre-treatment with yohimbine, an alpha 2-adrenergic receptor antagonist, notably reversed the antinociceptive activity induced by octacosanol in the abdominal constriction test. Furthermore, mice treated with octacosanol did not exhibit any behavioral alteration during the hot plate and rota-rod tests, indicating non-participation of the supraspinal components in the modulation of pain by octacosanol with no motor abnormality. In the formalin test, octacosanol did not inhibit the licking time in first phase (neurogenic pain), but significantly inhibited the licking time in second phase (inflammatory pain) of mice. The anti-inflammatory effect of octacosanol was evaluated using carrageenan-induced pleurisy. The octacosanol significantly reduced the total leukocyte count and neutrophils influx, as well as TNF-α levels in the carrageenan-induced pleurisy. This study revealed that the mechanism responsible for the antinociceptive and anti-inflammatory effects of the octacosanol appears to be partly associated with an inhibition of alpha 2-adrenergic transmission and an inhibition of pathways dependent on pro-inflammatory cytokines. Finally, these results demonstrated that the octacosanol from the leaves of S. grisea possesses antinociceptive and anti-inflammatory activities, which could be of relevance for the pharmacological control of pain and inflammatory processes.

RESUMO:O presente trabalho descreve o isolamento de quatro triterpenos (taraxerol, ácido ursólico, ácido 3β,19α,23-triidroxiurs-12-en-28-óico e ácido 2α,3α,19α,23-tetraidroxiurs-12-en-28-óico) e um fi toesteróide (espinasterol), bem como a avaliação do potencial antimalárico (cepa NK-65 do Plasmodium berghei), larvicida (larvas do 4º instar do Aedes aegypti), anti-radicalar (2,2-difenil-1-picril-hidrazila, DPPH) e anticolinesterásico de extratos das folhas, cascas do caule e caule de Pouteria venosa (Mart.) Baehni. Todos os compostos isolados estão sendo descritos pela primeira vez nesta espécie e foram identifi cados com base na análise de dados espectrais (IV e RMN, incluindo APT e DEPT), bem como pela comparação com dados descritos na literatura.Unitermos: Pouteria venosa, terpenóides, anticolinesterase, anti-radicalar, malária, larvicida.ABSTRACT: "Terpenoids and evaluation of the antimalarial, larvicidal, anti-radicalar and anticholinesterase potential of Pouteria venosa (Sapotaceae)". This work describes the isolation of four triterpenes (taraxerol, ursolic acid, 3β,19α,23-trihydroxyurs-12-en-28-oic acid and 2α,3α,19α,23-tetrahydroxyurs-12-en-28-oic acid) and a phytosteroid (spinasterol), as well as a preliminary evaluation of antimalarial (NK-65 strains of Plasmodium berghei), larvicidal (4 th instar of Aedes aegypti), anti-radicalar (2,2-diphenyl-1-pycryl-hydrazyl, DPPH) and anticholinesterase activities of Pouteria venosa (Mart.) Baehni extracts from leaves, stem barks and stems. All isolated compounds are being described for the fi rst time in this species and were identifi ed on basis of the spectral data (IR and NMR, including APT, DEPT), as well as by comparison with literature data