Avaliação do extrato de Momordica charantia em Salmonella typhimurium: Mutagenicidade e antimutagenicidade

In the last years some natural products has been described as supressors of the mutagenic process in bacteria, the antimutagenics. The literature reference that in most of the countries, the population makes use of medicinal plants. The plant Momordica charantia (Cucurbitaceae) is original from Africa being used popularly as purgative, antirheumatic and for skin problems, burns and hemorrhoids. The present work had as objective to evaluate the mutagenic and antimutagenic activities of the ethanolic extract of M. charantia in Salmonella/microsome assays using TA100, TA98 and TA102 strains. It was verified that the extract did not present mutagenic activity when evaluated in different concentrations (0.64, 1.27, 2.55 and 3.84 mg/plate) but acted as antimutagenic agent against the mutations induced by the sodium azide (TA100,-S9), 4-nitro-phenylenediamine (TA98, -S9), daunomycin (TA102, +S9) 2-anthramine (TA100 and TA98, +S9) and 2-aminofluorene (TA102, +S9). When the metabolic activation (+S9) was used, the percentage of inhibition of the mutagenicity varied in the range of 31%-96%, while in absence of metabolizing system (-S9), the maximum percentage of inhibition of the mutagenicity was 44%. In that way, we can conclude that the metabolites found in the extract has potential to protect the genetic material against the damages induced by different chemical agents.

A program for terpenoid skeleton prediction based on botanical information

This paper describes a new program developed to the SISTEMAT expert system, the SISOCBOT program. This program employs the botanical data analysis and predicts, at the end of analysis, the probable skeleton of a compound based on the input of family or genus names. The SISOCBOT program was tested with 78 samples involving 302 substances, pertaining to 38 carbon skeletons, and showed a high hit index on skeleton prediction, thus emphasizing the potential importance of these data for structural determination of natural products. © 2002 Elsevier Science Ltd. All rights reserved.

Ativação de macrófagos por produtos naturais obtidos da Achillea millefolium L. (Asteraceae)

Plants are a valuable source of natural products for the maintenance of human health. The purpose of this paper was the study of immunologic activity of yarrow (Achillea millefolium L.), a largely used plant in popular medicine that has many different properties such as: antiinflammatory, astringent, antiseptic and antispasmodic. Macrophages stimulation was evaluated by the determination of H2O2, NO and TNF-α in supernatants of peritoneal macrophages cultures of mice in the presence of the yarrow leaves extract. The thin layer chromatography of extract was also analyzed, showing rutin. All concentrations showed a moderate release of H2O2 and the concentrations of 6, 8 and 10mg/mL had a higher release of NO. The TNF-a was produced in all concentrations, but the best result was obtained at 4mg/mL. Analyzing the results, it is suggested that the yarrow ethanolic extract can modulate the macrophages activation.

Produtos naturais como candidatos a fármacos úteis no tratamento do mal de Alzheimer

Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD and natural products have played an important role in the research for new acetylcholinesterase inhibitors.

Citotoxicidade de Styrax camporum Pohl em macrófagos peritoneais e a liberação de H2O2

The immunological response includes wide contexts involving several cells, and the macrophage is crucial in the cellular immune response. Several stimuli to macrophage membrane may induce the liberation of H2O2, contributing to antibacterial and cytotoxicical actions. Nowadays, there is a tendency to study natural products to verify their capacity of acting in the immune system. This study evaluated the citotoxicity of the bulk extract and the hexanic and acetic fractions extracted from Styrax camporum Pohl (Styracaceae) and the production of H2O2, on murine peritonal macrophages cultures exposed to fractions extracted from this plant. The results showed that the fraction HX 2 mg/ml produced the liberation of H 2O2 in high concentrations and to 4 mg/ml was observed high citotoxicity. The fractions AC did not produce the liberation of H 2O2 and EB was produced in low levels. We conclude that this HX is a potent stimulator of macrophage.

Communiols E-H: New polyketide metabolites from the coprophilous fungus Podospora communis

Communiols E-H (1-4), four new polyketide-derived natural products containing furanocyclopentane, furanocyclopentene, cyclopentene, or γ-lactone moieties, have been isolated from two geographically distinct isolates of the coprophilous fungus Podospora communis. The structures of these compounds were determined by analysis of NMR and MS data. © 2005 American Chemical Society and American Society of Pharmacognosy.

Inhibition of the symbiotic fungus of leaf-cutting ants by coumarins

Leaf-cutting ants are known to be a serious pest for agriculture due to the high amounts of vegetal matter from crops used by them in order to cultivate a symbiotic fungus on which they rely for food and enzymes. The mutualism between the fungus and the ants is a point to be explored when alternative methods of control are being thought of. Considering that some plants are naturally resistant to phytophagous insects, some natural products (secondary metabolites) should be evaluated with respect to their insecticide and/or fungicide properties. In this paper we isolated eight coumarins from four different plant species and we determined their effect on the development of the symbiotic fungus of the leaf-cutting ant Atta sexdens. With the exception of clausarin, all the other coumarins were inhibitory from 64 μg mL-1 through 80 μg mL-1 and xanthyletin inhibited the fungus at 25 μ mL -1. ©2005 Sociedade Brasileira de Química.

Fast preparative separation of flavones from capitula of Eriocaulon ligulatum (Vell.) L.B.Smith (Eriocaulaceae) by High-speed countercurrent chromatography (HSCCC)

High-speed countercurrent chromatography (HSCCC) is a leading method for the fast separation of natural products from plants. It was used for the preparative isolation of two flavone monoglucosides present in the capitula of Eriocaulon ligulatum (Veil.) L.B.Smith (Eriocaulaceae). This species, known locally as botão-dourado, is exported to Europe, Japan and North America as an ornamental species, constituting an important source of income for the local population of Minas Gerais State, Brazil. The solvent system, optimized in tests prior to the HSCCC run, consisted of the two phases of the mixture ethyl acetate: n-propanol: water (140:8:80, v/v/v), which led to the successful separation of 6-methoxyluteolin-7-O-β-D-allopyranoside and 6-methoxyapigenin-7-O-β-D-allopyranoside in only 3 hours. The two flavonoids were identified by NMR (1-D and 2-D) and ESI-MS, comparing their spectra with published data.

OS produtos naturais e a química medicinal moderna

Natural products have been utilized by humans since ancient times and the relief and cure of their diseases was the first purpose for using natural products in medicine. The history of the oriental and occidental civilizations is very rich in examples of the utilization of natural products in medicine and health care. Chinese traditional medicine is one of the most important examples of how natural products can be efficient in the treatment of diseases, and it points to the importance of scientific research on natural products, concerning the discovery of new active chemical entities. The complexity, chemical diversity and biological properties of natural products always fascinated people, and during the last 200 years, this led to the discovery of important new drugs. In the last 30 years, the development of new bioassay techniques, biotechnology methods, bio-guided phytochemical studies, automated high throughput screening and high performance analytical methods, have introduced new concepts and possibilities of rational drug design and drug discovery. In this context, natural products have played an important and decisive role in the development of modern medicinal chemistry.

Ação farmacológica de Syzygium cumini (L.) skeels

Natural products have received new interest recently, maybe in men's attempt to turn into the nature for the prevention and the relief of diseases, mainly because of those untreated by the traditional medicine. Syzygium cumini (L.) Skeels, popularly known as 'jambolão, is a well-known plant by several pharmacological actions so much in the popular use as in the scientific literature. In this search antidiabetic, anti-diarrhoeal, anti-inflammatory, antioxidant and antimicrobial activities of 'jambolão' were described, among other actions.

Toxicity of Azadirachta indica to leaf-cutting ant Atta sexdens rubropilosa (Hymenoptera: Formicidae)

The leaf-cutting ants are responsible for great economical damages in cultivated areas, and because of this characteristic, they have aroused the interest of researchers around the world. Thus, extracts of neem (Azadirachta indica, A. Juss) were tested through ingestion and contact experiments to investigate their toxicity to Atta sexdens rubropilosa workers. Crude extract of neem seed oil was toxic to the ants by ingestion in all concentrations tested but no toxicity was observed in contact experiments. However, crude extract of neem seed paste produced a significant toxicity to workers by ingestion and by contact.

In vitro metabolism effect on genotoxicity and antigenotoxicity of Agaricus blazei organics and aqueous extracts by the comet assay

There is high interest in the natural products properties due to their use in popular medicine. Agaricus blazei Murrill ss. Heinem. (Ab) is native to Brazil and has been widely disseminated because its medicinal properties. In the present study, the genotoxic and antigenotoxic potential of Ab extracts were investigated using the comet assay. The cells utilized were the non drug-metabolizing line CHO-k1 (Chinese hamster ovary) and the drug-metabolizing line HTC (rat hepatoma). Cells were treated for 3 h in the absence of fetal bovain serum (FBS) with methanolic, hexanic and n-butanolic extracts at 50 μg/ml and 0.75% aqueous extract to test for genotoxicity. Antigenotoxic effects of extracts were determined in cells exposed to the DNA damage inducing agent ethyl methanesulfonate under simultaneous or simultaneous with 1 h pre-incubation conditions. The extracts did not show genotoxicity in HTC, while they were genotoxic in CHO-k1. No antigenotoxic effect was observed with any extract under any condition. These results demonstrate that the metabolism in presence or in absence has a direct influence on the genotoxicity of these extracts. © 2006 The Japan Mendel Society.

Efeito hipocolesterolêmico dos ácidos caféicos da própolis

Natural products have been used in tratamed of hypercholesterolemia. The bee products have been promoting up the man's interest, among them it stands out the propolis, coleted by bees, rich in polyphenols. The biggest polyphenols of propolis was flavonoids and caffeic acids, which have antioxidant power, presenting the protective action to the lipoprotein LDL-cholesterol against the lipid peroxidation. Therefore, the present work was evaluated whether the caffeic acids of the Botucatu's propolis (Botucatu-SP) affect the levels of plasma cholesterol, in rabbits submitted to the rich diet in cholesterol. The animals were divided in three groups: C (n=2) they received commercial ration and water for the whole period; S (n=2) they received normal ration and water in the first period and supplemented ration and water in the second and third periods; S+T (n=5) they received normal ration and water in the first period, supplemented ration and water in the second period and supplemented ration and extract rich in caffeic acids in the third period. The caffeic acids were administered diluted in water, being in the concentration of 0.05g caffeic acid mL -1 kg -1 of animal. Weekly, after fast of 14 hours, the samples of blood were collected from the marginal vein of the ear for determination of the plasma levels of total cholesterol and their fractions. The caffeic acids of the propolis reduced the plasma concentration of total cholesterol in 30% (280 for 199 mg dL -1) in the rabbits treated with flavonoids, while in the animals of the group S those levels were reduced discreetly (380 for 400 mg dL -1). The animals of the group C maintained this biochemical parameter in the normality range during the whole period (50 mg dL -1). Therefore, we concluded that the caffeic acids exert inhibititory activity in the metabolism of the cholesterol, being considered as a substance of action against the hypercholesterolemia.

Flavonoids with gastroprotective activity

Peptic ulcers are a common disorder of the entire gastrointestinal tract that occurs mainly in the stomach and the proximal duodenum. This disease is multifactorial and its treatment faces great difficulties due to the limited effectiveness and severe side effects of the currently available drugs. The use of natural products for the prevention and treatment of different pathologies is continuously expanding throughout the world. This is particularly true with regards to flavonoids, which represent a highly diverse class of secondary metabolites with potentially beneficial human health effects that is widely distributed in the plant kingdom and currently consumed in large amounts in the diet. They display several pharmacological properties in the gastroprotective area, acting as anti-secretory, cytoprotective and antioxidant agents. Besides their action as gastroprotectives, flavonoids also act in healing of gastric ulcers and additionally these polyphenolic compounds can be new alternatives for suppression or modulation of peptic ulcers associated with H. pylori. In this review, we have summarized the literature on ninety-five flavonoids with varying degrees of antiulcerogenic activity, confirming that flavonoids have a therapeutic potential for the more effective treatment of peptic ulcers.

Produtos naturais no comportamento defensivo de Apis mellifera L.

The goal was to investigate the influence of natural products such as lemongrass (Cymbopogon citratus), dried avocado leaves (Persea americana), coffee husk (Coffea arabica) and castor bean (Ricinus communis) in the defense of Apis mellifera, as well the effect of these products on the population development of the beehive. Defensive behavior was evaluated by time of first sting (TFS) and number of stingers (NS), and population development, by open brood area and operculated brood. It was observed that the treatment with smoke + seven castor beans presented significant increase in the TFS, for treatment without and with smoke. Regarding NS, it was verified that the treatments with smoke + seven castor bean and smoke + 20% coffee husk were different from the treatment without and with smoke. The other treatments did not differ significantly with respect to the use of smoke or its absence. The application of coffee husk and castor bean did not interfere in the development of the population, suggesting that these compounds were not toxic. It can be concluded that the use of castor bean and coffee husk in smoke may represent an important tool for the reduction of defensiveness, without promoting toxicity for A. mellifera.