113 resultados para Bioactive constituents


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This research deals with the effects of chemicals on, transplantation of Ficus carica L. cv. Roxo de Valinhos. Fig plants were sprayed with Transplantone (naphthaleneacetamide plusnaphtaleneacetic acid) 10 g/1 , Oed green (oxyethylene docosanol) 40 ml/1, Good-rite peps (polyethylene polysulfite) 0,6 ml/1, and Mobileaf 200 ml/1. A check treatment and aereduction to half of leaf area were also established. Reduction of leaf area and application of oxyethylene docosanol promoted higher plant survival. The chemicals did not affect the growth of transplanted plants. Auxins constituents of Transplantone increased leaf number of fig plants.

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The indices found are analysed as a whole and general conclusions are drawn from them which may be of use in understanding many of the problems offered by the local flora (Ilhéus). The first column of the tables presented indicates the biological form of the species, showing the nature of the flora and the constitution of the climax. A total of 200 species of phanerophyta were found; 69 macrophanerophyta (trees), 54 are mesophanerophyta (treelets) and 77 are nanophanerophyta (shrubs). The macrophanerophyta are consequently considered as dominants and the meso-and nanophanerophyta as codominants (the biological forms: chamaephyta, hemicriptophyta, criptophyta, geophyta, therophyta, epiphyta and hydrophyta are subdominants), the more so as the first cover 80% and the others more or less 50%. This points to a climax of trees and a local vegetation mainly composed of trees also. The smaller forms are left out as they are beyond the present scope of this sort of wort in Brazil. The third column of ecological formulae indicates the reaction of the constituent species to light (C = sciophilous, F = photophilous and I = indifferents), the biological types of vegetation (H = hygrophytes, X = xerophytes and M = mesophytes) and the fidelity of the species to the climax. Of the species studied: 25 are pioneers (P. Table I), 63 are accidentals (A. Table II), 35 are companion species (O. Table III), 19 show preferences (E. Table with vitality Vn), 44 are selective (S. Table V) and 13 exclusive species (L. Table VI). This leads to the conclusion that the vegetation of the region is in full reconstitution. As to the ecological characteristics of the 200 species studied, 89 are either pioneers (a class separated by the author) or accidentals; this means that the devastated zones are being reconstituted in the subsere both with members of the prisere and alien species. Of the remaining species, 54 are companion, or accompanying species, which appear in most subclimax, serclímax and quasiclimax associations, and 57 are real constituents of the local climax. As all the species except the pioneers, selectives and exclusives (xerophytes and mesophytes) may be considered as hygrophytes this type evidently predominantes in the region and may constitute a hygrophilous serclimax and quasiclímax. In regard to light 101 are sciophilous, 32 indiferents and 67 photophilous. This leads to the conclusion that the vegetation comprises mainly tolerant species, showing the hygrophilous and mesophilous character of the region with a vegetation composed mostly of trees. The presence a large number of sciophilous species is easy to understand as the hygrophilous and mesophilous habitats and the dominance of trees favour the germination and growth of tolerant species. The last two columns analyse the percentage of individuals present and the occurrent classes to which they belong: 92 species vary between 1 and 9%; 50 between to 10 and 19%; 36 between 20 and 29%; 14 between 30 and 39%; and 8 between 40 and 49%. Only 8 species belong to occurrence class V; 14 to classe IV; 36 to class III; 50 to class II; and 92 to class I. This leads to the conclusion that the local formation is very unsociable and very complex, though the median coverture is 80% and the number of species is very large. The analysis of the data also shows that the climax is being reconstituted in the subsere with elements drawn from the prisere and alien species introduced either by man (following desvastation) or by other consequent factors (such as brusque changes of microclimates due to total or partial destruction). This modifies the subclimax appreciably and apparently also the climax of the local regional subsere. As a final conclusion it is suggested that as in the subsere the pioneer formation is xerophilous, the prisere also beging as a xerosere; but as there are and probably always were hydrophilous formation evolving in the same climate, the local climax is composed of species with medium exactions, that is of relative mesophites.

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In recent years, one of the most significant progress in the understanding of liver diseases was the demonstration that liver fibrosis is a dynamic process resulting from a balance between synthesis and degradation of several matrix components, collagen in particular. Thus, fibrosis has been found to be a very early event during liver diseases, be it of toxic, viral or parasitic origin, and to be spontaneously reversible, either partially or totally. In liver fibrosis cell matrix interactions are dependent on the existence of the many factors (sometimes acting in combination) which produce the same events at the cellular and molecular levels. These events are: (i) the recruitment of fiber-producing cells, (ii) their proliferation, (iii) the secretion of matrix constituents of the extracellular matrix, and (iv) the remodeling and degradation of the newly formed matrix. All these events represent, at least in principle, a target for a therapeutic intervention aimed at influencing the experimentally induced hepatic fibrosis. In this context, hepatosplenic schistosomiasis is of particular interest, being an immune cell-mediated granulomatous disease and a model of liver fibrosis allowing extensive studies in human and animals as well as providing original in vitro models.

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Diverse conditions for stimulating human mononuclear cells to release thymocyte costimulatory factors were tested for their contribution to the generation of supernatants high titers of these monokines. Activity titers increased with LPS concentration, reaching a plateau between 1 and 10 microng/ml. Indomethacin did not modify the monokine, but the assay for thymocyte costimulatory activity was substantially affected by inhibitory substances produced by the monocytes in the absence of indomethacin. The use of nylon wool columns to trap the cells was shown to be effective in raising cellular densities without decreasing activity titers. As result, the yield per cell could be maintained even in the absence of serum, an important step toward the goal of purifiying bioactive from crude broths.

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Eventhough the rationale behind the use of medicinal plantes in Brazil and Chine is different, twenty four species are used in both countries. Scientific name, vulgar name and uses in both countries along with their chemical constituents are listed.

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This paper recalls the outcoming of marine natural products research and reviews a selection of marirne bioactive metabolites in current use together with promising trends in marine pharmacology.

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A series of studies has been carried out in the field of traditional medicine for searching radio-protective agents. According to the theory of traditional Chinese medicine, may prescriptions were tested with experimental animals. Some of them could raise the survival rate of dogs irradiated with lethal dose of Pi-rays by 30-40%. Some symptoms of radiation sickness could be improved. More than one thousand kinds of Chinese herbs were screened. Some of them have pronounced radioprotectice activities. A series of bioactive components wee isolated from these herbs. The mechanism of radiation protection were studied. Having the capability of hemopoietic system and immune system may be the characteristics of these Chinese herbs.

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We have recenty studied several natural product constituents which have effects on the CNS. (1) Tetrahydropalmatine (THP) and its analogues were isolated from Corydalis ambigua and various species of Stephania. (+)-THP and (-)-THP posses not only analgesic activity, but also exert sedative-tranquillizing and hypnotic actions. Results of receptor binding assay and their pre-and post-synaptic effects on dopaminergic system indicate that (-)-THP and (-)-stepholidine are dopamine receptor antagonists while (+)-THP is a selective dopamine depletor. (2) 3-Acetylaconitine (AAC) is an alkaloid isolated from Aconitum flavum. The relative potency of analgesic action of AAC was 5.1-35.6 and 1250-3912 times that of morphine and aspirin, respectively. The analgesic effect of AAC was antagonized by naloxone, but was eliminated by reserpine. In monkeys, after AAC was injected for 92 days, no abstinence syndrome was seen after sudden AAC withdrawal or when challenged with nalorphine. (3) Huperzine A (Hup-A) is an alkaloid isolated from Huperzia serrata which was found to be a selective ChE inhibitor and could improve learning and retrieval process. Preliminary clinical studies showed that Hup-A improve short-and long-term memory in patients of cerebral arteriosclerosis with memory impairment. (4) Ranamargarin is a new tetradecapeptide isolated from the skin of the Chines frog Rana margaratae. This peptide may mainly act on NK-1 receptor.

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This study was carried out in five sites along a small perennial river system in south-central Tanzania, which had been identified as the focus for transmission of intestinal schistosomiasis in the area. Malacological surveys preceding the study showed a focal distribution of Biomphalaria pfeifferi, intermediate host snail of Schistosoma mansoni, the snails being present in three sites but absent from the other two sites. The objective of this study was to evaluate to what extent chemical and/or physical-morphological factors determine the distribution of B. pfeifferi between these five sites. It was found that none of the chemical constituents in the waters examined were outside the tolerance range of B. pfeifferi snails. Moreover, the composition of water from B. pfeifferi-free sites was not different from that in those sites where snails occurred. Furthermore, none of the physical-morphological constituents seemed likely to be a determinant for the absence of B. pfeifferi. In view of these findings, and those of previous studies, it is concluded that the focal distribution of B. pfeifferi cannot be associated with a single environmental factor and is rather the result of more complex interactions of habitat factors

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We live in a "Demon-Haunted World". Human health care requires the ever increasing resistance of pathogens to be confronted by a correspondingly fast rate of discovery of novel antibiotics. One of the possible strategies towards this objective involves the rational localization of bioactive phytochemicals. The conceptual basis of the method consists in the surprisingly little known gearings of natural products with morphology, ecology and evolution of their plant source, i. e. an introspection into the general mechanisms of nature.

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Using phenotype techniques, characterization was made to species and serovar of 3,112 strains of Listeria, isolated from different sources of infection such as human (247-7.9%) and animals (239-7.6%), as well as from various routes of infection, including food (2,330-74.8%) and environmental constituents (296-9.5%), all coming from different regions of the country and collected during the period 1971-1997. The following species were recovered in the cultures analysed: L. monocytogenes (774-24.8%), L. innocua (2,269-72.9%), L. seeligeri (37-1.1%), L. welshimeri (22-0.7%), L. grayi (9-0.2%), and L. ivanovii (1-0.03%). L. monocytogenes was represented by ten serovars, the most prevalent being 4b (352-11.3%), 1/2a (162-5.2%), and 1/2b (148-4.7%). The predominant serovar in L. innocua was 6a (2,093-67.2%). Considerations about laboratory methods for diagnosis and epidemiological aspects are presented on the basis of the results obtained.

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The aim of this work was to study the larvicidal activity of Lippia sidoides essential oil against Aedes aegypti larvae. The essential oil and its hydrolate (saturated solution of essential oil in water) were obtained by vapor extraction and their chemical composition determined by GL-chromatography coupled to mass spectroscopy. Bioassays were run with the essential oil, pure and diluted hydrolate and with their main constituents thymol and carvacrol. The results obtained showed that L. sidoides essential oil and its hydrolate have larvicidal action against the mosquito A. aegypti, causing an almost instantaneous mortality. Thymol, an alkylated phenol derivative and one of the major components of L. sidoides essential oil, was identified as the active principle responsible for the larvicidal action, causing 100% larval mortality at the lowest tested concentration of 0.017% (w/v). These results suggest that the essential oil of L. sidoides is promising as larvicide against A. aegypti and could be useful in the search of newer, more selective, and biodegradable larvicidal natural compounds to be used in official combat programs and at home.

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Severe mucocutaneous (MCL) and diffuse (DCL) forms of American cutaneous leishmaniasis (ACL) are infrequent in Venezuela. Chemotherapy produces only transitory remission in DCL, and occasional treatment failures are observed in MCL. We have evaluated therapy with an experimental vaccine in patients with severe leishmaniasis. Four patients with MCL and 3 with early DCL were treated with monthly intradermal injections of a vaccine containing promastigotes of Leishmania (Viannia) braziliensis killed by pasteurization and viable Bacillus Calmette- Guerin. Clinical and immunological responses were evaluated. Integrity of protein constituents in extracts of pasteurized promastigotes was evaluated by gel electrophoresis. Complete remission of lesions occurred after 5-9 injections in patients with MCL or 7-10 injections in patients with early DCL. DCL patients developed positive skin reactions, average size 18.7 mm. All have been free of active lesions for at least 10 months. Adverse effects of the vaccine were limited to local reactivity to BCG at the injection sites and fever in 2 patients. Extracts of pasteurized and fresh promastigotes did not reveal differences in the integrity of protein components detectable by gel electrophoresis. Immunotherapy with this modified vaccine offers an effective, safe option for the treatment of patients who do not respond to immunotherapy with vaccine containing autoclaved parasites or to chemotherapy .

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An effective vaccine against schistosomiasis mansoni would be a valuable control tool and the high levels of protection elicited in rodents and primates by radiation-attenuated cercariae provide proof of principle. A major obstacle to vaccine development is the difficulty of identifying the antigens that mediate protection, not least because of the size of the genome at 280Mb DNA encoding 14,000 to 20,000 genes. The technologies collectively called proteomics, including 2D electrophoresis, liquid chromatography and mass spectrometry, now permit any protein to be identified provided there is extensive DNA data, and preferably a genome sequence. Applied to soluble (cytosolic) proteins from schistosomes, proteomics reveals the great similarity in composition between life cycle stages, with several WHO vaccine candidates amongst the most abundant constituents. The proteomic approach has been successfully applied to identify the secretions used by cercaria to penetrate host skin, the gut secretions of adult worms and the proteins exposed on the tegument surface. Soluble proteins can also be separated by 2D electrophoresis before western blotting to identify the full range of antigenic targets present in a parasite preparation. The next step is to discover which target proteins represent the weak points in the worm's defences.

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The modern approach to the development of new chemical entities against complex diseases, especially the neglected endemic diseases such as tuberculosis and malaria, is based on the use of defined molecular targets. Among the advantages, this approach allows (i) the search and identification of lead compounds with defined molecular mechanisms against a defined target (e.g. enzymes from defined pathways), (ii) the analysis of a great number of compounds with a favorable cost/benefit ratio, (iii) the development even in the initial stages of compounds with selective toxicity (the fundamental principle of chemotherapy), (iv) the evaluation of plant extracts as well as of pure substances. The current use of such technology, unfortunately, is concentrated in developed countries, especially in the big pharma. This fact contributes in a significant way to hamper the development of innovative new compounds to treat neglected diseases. The large biodiversity within the territory of Brazil puts the country in a strategic position to develop the rational and sustained exploration of new metabolites of therapeutic value. The extension of the country covers a wide range of climates, soil types, and altitudes, providing a unique set of selective pressures for the adaptation of plant life in these scenarios. Chemical diversity is also driven by these forces, in an attempt to best fit the plant communities to the particular abiotic stresses, fauna, and microbes that co-exist with them. Certain areas of vegetation (Amazonian Forest, Atlantic Forest, Araucaria Forest, Cerrado-Brazilian Savanna, and Caatinga) are rich in species and types of environments to be used to search for natural compounds active against tuberculosis, malaria, and chronic-degenerative diseases. The present review describes some strategies to search for natural compounds, whose choice can be based on ethnobotanical and chemotaxonomical studies, and screen for their ability to bind to immobilized drug targets and to inhibit their activities. Molecular cloning, gene knockout, protein expression and purification, N-terminal sequencing, and mass spectrometry are the methods of choice to provide homogeneous drug targets for immobilization by optimized chemical reactions. Plant extract preparations, fractionation of promising plant extracts, propagation protocols and definition of in planta studies to maximize product yield of plant species producing active compounds have to be performed to provide a continuing supply of bioactive materials. Chemical characterization of natural compounds, determination of mode of action by kinetics and other spectroscopic methods (MS, X-ray, NMR), as well as in vitro and in vivo biological assays, chemical derivatization, and structure-activity relationships have to be carried out to provide a thorough knowledge on which to base the search for natural compounds or their derivatives with biological activity.