Composição química e atividades biológicas das folhas de Cynara scolymus L. (alcachofra) cultivada no Brasil

The present paper describes the chemical composition and biological activities of artichoke cultivated in Brazil. Our studies demonstrated that glycosyl flavonoids (cynaroside and scolymoside), are the major constituents, along with cynaropicrin, a sesquiterpene lactone, and the triterpene lupeol. Cynarin, which is the main compound described for artichoke, was detected in very low concentration. Hexanic fraction exhibited considerable cytotoxicity and diuretic activities.

Seasonal variation of the major secondary metabolites present in the extract of Eremanthus mattogrossensis Less (Asteraceae: Vernonieae) leaves

The species Eremanthus mattogrossensis, known as "veludo do cerrado" (cerrado velvet), is native to the Brazilian Cerrado. Because the amount of metabolites present in plants may be influenced by biological and environmental factors, here we conducted an HPLC-DAD-MS/MS investigation of the metabolite concentrations found in the MeOH/H2O extract of the leaves of this species. The main compounds were identified and quantified, and the metabolites were grouped by chemical class (caffeoylquinic acids, flavonoids, and sesquiterpene lactone). Statistical analysis indicated a straight correlation between the quantity of metabolites and seasonality, suggesting that environmental properties elicit important metabolic responses.

Sesquiterpene lactones from Vernonia

Some informations about the sesquiterpene lactones isolated from Brazilian species of Vernonia are described, as well the results of tests developed with such compounds with respect to their anti-feedant, molluscicide, antimicrobial and analgesic properties.

Candida albicans PROTEIN PROFILE CHANGES IN RESPONSE TO THE BUTANOLIC EXTRACT OF Sapindus saponariaL.

Candida albicans is an opportunistic human pathogen that is capable of causing superficial and systemic infections in immunocompromised patients. Extracts of Sapindus saponaria have been used as antimicrobial agents against various organisms. In the present study, we used a combination of two-dimensional polyacrylamide gel electrophoresis (2D-PAGE) and matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS) to identify the changes in protein abundance of C. albicans after exposure to the minimal inhibitory concentration (MIC) and sub-minimal inhibitory concentration (sub-MIC) of the butanolic extract (BUTE) of S. saponaria and also to fluconazole. A total of six different proteins with greater than 1.5 fold induction or repression relative to the untreated control cells were identified among the three treatments. In general, proteins/enzymes involved with the glycolysis (GPM1, ENO1, FBA1), amino acid metabolism (ILV5, PDC11) and protein synthesis (ASC1) pathways were detected. In conclusion, our findings reveal antifungal-induced changes in protein abundance of C. albicans. By using the previously identified components of the BUTE of S. saponaria(e.g., saponins and sesquiterpene oligoglycosides), it will be possible to compare the behavior of compounds with unknown mechanisms of action, and this knowledge will help to focus the subsequent biochemical work aimed at defining the effects of these compounds.

Effects of Goyazensolide during in Vitro Cultivation of Schistosoma mansoni

Goyazensolide, a component extracted of Eremanthus goyazensis showed a significant inhibitory effect on egg-laying of Schistosoma mansoni during in vitro cultivation of this parasite. Motility of the worms was also reduced under treatment with goyazensolide and 90% of mortality was reached with concentrations up to 4mg/ml. It has found that separated worms were more susceptible than worms pairing during drug exposition and female alone was significantly more susceptible than male worm in the same conditions of in vitro cultivation. Natural products isolated from plants represent potential sources for the identification of structures useful for the design of alternative molecules to be used as new drug substances against several infectious diseases

Polygodial, the fungitoxic component from the Brazilian medicinal plant Polygonum punctatum

Polygonum punctatum (Polygonaceae) is an herb known in some regions of Brazil as "erva-de-bicho" and is used to treat intestinal disorders. The dichloromethane extract of the aerial parts of this plant showed strong activity in a bioautographic assay with the fungus Cladosporium sphaerospermum. The bioassay-guided chemical fractionation of this extract afforded the sesquiterpene dialdehyde polygodial as the active constituent. The presence of this compound with antibiotic, anti-inflammatory and anti-hyperalgesic properties in "erva-de-bicho" may account for the effects attributed by folk medicine to this plant species.

Embryonic development of human lice: rearing conditions and susceptibility to spinosad

The embryonic development of human lice was evaluated according to the changes in the morphology of the embryo observed through the transparent chorion. Based on ocular and appendage development, three stages of embryogenesis were established: early, medium, and late. Influence of temperature and relative humidity (RH) on the laboratory rearing of Pediculus humanus capitis eggs was assessed. The optimal ranges for temperature and RH were 27-31°C and 45-75%. The susceptibility of human louse eggs to insecticide spinosad (a macrocyclic lactone) was assessed by immersion method. The results showed similar susceptibility to spinosad in early, medium, and late stages of head lice eggs. In addition, this study showed similar susceptibility of head and body lice eggs to spinosad, an insecticide that has not been used as pediculicide in Argentina (lethal concentration 50: 0.01%).

Effect of gossypol on survival and reproduction of the zoophytophagous stinkbug Podisus nigrispinus (Dallas)

Effect of gossypol on survival and reproduction of the zoophytophagous stinkbug Podisus nigrispinus (Dallas). Gossypol is a sesquiterpene aldehyde found in cotton plants conferring resistance against herbivory. Although the effect of this sesquiterpenoid on insect pests of cotton is known, the interaction of this compound with zoophytophagous predators such as Podisus nigrispinus (Dallas) (Hemiptera, Pentatomidae) has not been studied so far. Thus, the objective of this study was to evaluate the effect of the purified gossypol on nymphs and adults of P. nigrispinus. Nymphs and adults of this predator were fed on Tenebrio molitor pupae and supplemented with solutions of gossypol at concentrations of 0.00, 0.05, 0.10, and 0.20% (w/v) during the nymphal and adult stages or, only during the adult stage of P. nigrispinus. The nymphal stage of the predator was, on average, two days longer when suplemmented with gossypol. Emerged adults had lower fecundity and egg hatching, especially at the highest gossypol concentration (0.20%) ingested during the nymphal and adult stages. However, this predator was not affected when it ingested the compound only during the adult stage. P. nigrispinus can have delayed nymphal development and lower reproductive performance when ingesting the gossypol during the nymphal and adult stages, but only at higher concentrations of gossypol than that produced by cotton plants.

Solasodina em espécies de solanum do cerrado do distrito federal

An isolation method of the steroidal alkaloid solasodine was applied to the fruits of seven species of the Solanum genus from the Federal District. Two of these species show promising yields. The purity of the isolated alkaloid allows it to be transformed it into an intermediate for steroidal drugs production, 16-deshydropregnenolone, and to the lactone vespertiline.

Transformações químicas do (+)-10b,14-diol-allo-aromadendrano, isolado de duguetia glabriuscula r. e. fries (r. e. fries) (annonaceae) e avaliações biológicas de alguns derivados obtidos

The sesquiterpene (+)-allo-aromadendrane-10b-14-diol 1 was the lead compound to the preparation of several derivatives in order to test their biological activity against A. salina, C. sphaerospermum, E. coli and S. aureus. In this way the monoalcohols (+)-viridiflorol 4, 9 and 11 were synthesized from 1 together with the acetal 6, the ketal 7, and the ketone 8. The oxirane 3 and nitrile 5 were also prepared using as an intermediate the tosylate derivative 2.

Um novo método para agrupar parâmetros quimiotaxonômicos

This work presents a new methodology for searching the present state of chemical evolution for different taxa, grouping five classes of secondary metabolites. Ocurrences of 10370 natural products isolated from Asteraceae were used to exemplify the method. Relationships among tribes are discussed.

Gênero Physalis - uma revisão sobre vitaesteróides

This review describes results on the chemistry and spectroscopic data of some ergostane derivatives named withasteroids which have been obtained from Physalis genus. The main aim of this report is concerned with the description and characterization of Physalins. These natural product substances are C28 seco steroid lactone type compounds that have been shown biological activities against human illness such as immuno-deficiency, neoplasic tumors, inflammatory process and tropical endemic diseases. Physalins appear to be a source for new drugs to be apply as medicine.

RMN 2D: Detecção inversa e gradiente de campo na determinação estrutural de compostos orgânicos

A view of the general aspects involving the 2D NMR spectroscopy using inverse detection and field gradient techniques is presented through the analysis of a sesquiterpene.

Síntese e avaliação da atividade fitotóxica de lactonas derivadas do 2,4-dimetil-8-oxabiciclo[3.2.1]-oct-6-en-3-ona

The alkene 2,4-dimethyl-8-oxabicyclo[3.2.1]-oct-6-en-3-one (3) was converted to 1,3,10-trimethyl-8-oxabicyclo[5.3.0]-dec-3-ene-2,9-dione (7) and 1,3-dimethyl-8-oxabicyclo[5.3.0]-dec-3-ene-2,9-dione (8) with a 55% overall yield in both cases. Lactones (7) and (8) were converted in two steps to 1,3,4-trimethyl-13-methylene-6-oxatricyclo[8.3.0.0(3,7)]-trideca-2,5,12-trione (12) (63%) and 1,3-dimethyl-13-methylene-6-oxatricycle[8.3.0.0(3,7)]-trideca-2,5,12-trione (13) (45% from 8). The effect of lactones (7), (8), (12), (13) and the intermediates (5) and (6), at the concentration of 250 mug mL-1, on the growth of Cucumis sativus L. and Sorghum bicolor L. was evaluated. The best results were observed for lactone (13) that caused 100% inhibition on the root growth of C. sativus and lactone (12) that inhibited 90% of the root growth for S. bicolor.

Produtos naturais para o controle da transmissão da dengue: atividade larvicida de Myroxylon balsamum (óleo vermelho) e de terpenóides e fenilpropanóides

The bioassay-guided fractionation of the hexane extract obtained from the medicinal plant Myroxylon balsamum (red oil) was conducted in preparative thin layer chromatography on silica gel. The obtained fractions and some terpenoids and phenylpropanoids were assayed as larvicidal on third instar Aedes aegypti larvae, NPPN colony. The results indicate that the sesquiterpene nerolidol was the active constituent in the extract and that the sesquiterpenes were more active than the monoterpenes and phenylpropanoids utilized in this study. Lipophilicity seems to be an important property for the activity since the compounds with hydroxyl, carbonyl and methoxyl groups were less active. The results confirm also that essential oils can be a good tool for the control of dengue.