Anti-inflammatory activity of cubebin, a lignan from the leaves of Zanthoxyllum naranjillo Griseb.

Cubebin, a dibenzylbutyrolactone lignan isolated from the crude hexane extract of the leaves of Zanthoxyllum naranjillo, showed a significant anti-inflammatory activity by using the paw edema induced by carrageenin in rats, but did not provide a significant reduction in the cell migration for the acute carrageenin-induced inflammatory reaction in the peritoneal cavity of rats. Neither was it effective in reducing the edema induced by dextran nor the edema induced by histamine. It partially reduced the edema induced by serotonin. Moreover, it significantly reduced the edema induced by prostaglandin PGE2 and the number of writhings induced by both acetic acid and PGI2 in mice. Therefore, it may be suggested that the mechanism of action of cubebin is similar to that observed for most of the non-steroidal drugs.

Anti-inflammatory activity of the crude extract from the fruits of Pterodon emarginatus Vog.

The vegetal species Pterodon emarginatus Vog. (Leguminosae/Papilonaceae), popularly known in Brazil as 'sucupira branca', is widely used by domestic medicine as an anti-inflammatory. From these observations, the hexanic crude extract (HCE) of the fruits was obtained and submitted for assessment of its anti-inflammatory activity. For this purpose, the following tests were used: (1) Determination of ED50 and LD50; (2) Paw edema induced by carrageenin, dextran, histamine and nystatin; (3) Peritonitis caused by carrageenin and (4) Granuloma test. The ED50 (oral) in the edema induced by carrageenin was 500 mg/kg, and LD50 (oral) was 4.02 g/kg. In the edema caused by nystatin, there was a significant inhibition by 45% (P < 0.05 student's t-test) at the 6th hour following the treatment. In the granuloma test performed in animals treated with HCE, there was an inhibition of the granulomatous tissue formation by 22%. The migration of neutrophils towards the peritoneal cavity was inhibited in HCE treated animals by 43% (P < 0.05). However, in the edema caused by dextran and histamine, there was no significant response in HCE treated animals.

Anti-inflammatory activity of flavone and some of its derivates from Virola michelli Heckel.

The phytochemical study using Virola michelli Heckel (Myristicaceae) leaves allowed the isolation of a flavone named titonine (7,4'-dimethoxy-3'-hydroxyflavone). Titonine was further submitted to methylation and acetylation reactions yielding a 7,3',4'-trimethoxyflavone and a 7,3'-dimethoxy-4'-acetylflavone, respectively. These compounds were evaluated for both anti-inflammatory and analgesic activity. The anti-inflammatory activity was evaluated in rats using the paw edema test with carrageenin, while the analgesic activity was determined in mouse using the writhing test method. The different animal groups were treated with three compounds (10 mg/kg -i.p.) thirty min prior to stimuli application. The inhibition levels obtained for each compound were 22, 41 and 68%, respectively. Using the writhing test, oral doses of 5, 10 and 15 mg/kg of natural flavone reduced the acetic acid-induced contortions in a dose-dependent manner.

Investigation of anti-inflammatory and antinociceptive activities of trans-dehydrocrotonin, a 19-nor-clerodane diterpene from Croton cajucara. Part 1.

The anti-inflammatory and antinociceptive effects of trans-dehydrocrotonin, isolated from the bark of Croton cajucara (Euphorbiaceae), were investigated using several animal models. The trans-dehydrocrotonin produced a significant inhibition of carrageenin-induced paw edema and cotton pellet granuloma in rats. It also inhibited the writhings in mice induced by acetic acid, but did not show a significant effect in the hot-plate test in mice. The LD50 of t-DCTN was 555.0 mg/kg (p.o.) for mice.

Preliminary studies of analgesic and anti-inflammatory properties of Caesalpinia ferrea crude extract.

The crude aqueous extract of the fruits of Caesalpinia ferrea Mart. (Leguminosae) has been investigated for possible anti-inflammatory and analgesic properties. The carrageenan induced rat hind paw edema was significantly inhibited (P < 0.05) by oral administration of 300 mg/kg of this extract. A centrally mediated analgesic effect was not observed, however, there was a dose dependent reduction in the number of total writhes induced by acetic acid.

Quimioprofilaxia da doença de Chagas: bloqueio da transmissão transfusional por produtos naturais / Chemyprophylaxis of Chagas disease: blockage of blood transfusion transmission by natural products

Em busca da solução para o serio problema da transmissão transfusional da doença de Chagas em nosso meio, realizamos a avaliação de produtos naturais corn atividade tripanosomicida. Os testes "in vitro" foram realizados incubando-se a 4°C, sangue de camundongos contendo ± 10(6)/ ml formas tripomastigotas de Trypanosoma cruzi corn os extratos vegetais. Após diferentes períodos de incubação, frações sangüíneas foram examinadas em microscopia de fase. Os extratos que apresentaram atividade tripanosomicida ate 48 horas de incubação, foram examinados em microscopia eletrônica corn intuito de verificarmos sua toxicidade contra os elementos normais do sangue. Foram testados 242 extratos obtidos de 81 vegetais a 56 demonstraram atividade.

Considering the serius problem of blood transfusion transmission of Chagas disease in our environment, we realized the evalution of natural products against Chagas diseases. The tests were realized "in vitro" by in incubation at 4ºC mouse blood having ± 10(6)/ml of Trypanosoma cruzi, sample "y" and "Colombina" with the plant extracts. After different times of incubation, blood fractions were examined by phase microscopy. The drugs that showed activity until 48 hours of incubation, were examined by electron microscopy to virify the toxicity to blood elements. The tests were realized with 242 extracts from 81 plants and 56 extracts showed activity against T. cruzi.

Genotoxicity of the natural cercaricides "sucupira" oil and eremanthine in mammalian cells in vitro and in vivo.

"Sucupira" oil and the lactone eremanthine, extracted from Pterodon pubescens and Eremanthus elaeagnus, respectively, are known for their cercaricidal action in experimental animals. Because of their biological effect, they have the potential to be used for the prophylaxis of schistosomiasis caused by Schistosoma mansoni. To test the clastogenicity of these agents, "sucupira" oil, either pure or diluted in corn oil, was tested in vivo on Wistar rat bone marrow cells following dermal application. Metaphase analysis showed that the compound did not induce a significant increase in the frequencies of chromosomal aberrations. When eremanthine was tested on BALB/c mice following gavage at doses of 100, 200, and 300 mg/kg bw, it did not induce structural or numerical chromosomal aberrations. In the in vitro treatment of human lymphocyte cultures, eremanthine also did not cause any increase in chromosomal aberrations or sister chromatid exchanges at the following concentrations in culture medium: 1.25, 2.50, and 5.00 micrograms/ml. From these results, under our experimental conditions, neither "sucupira" oil nor eremanthine showed clastogenic effects on mammalian cells in vivo or in vitro.

[Chemoprophylactic activity on Schistosomiasis mansoni of soaps containing essential oil from the fruits of Pterodon pubescens]. / Atividade quimioprofilática na esquistossomose mansoni de sabonetes contendo óleo essencial de frutos de Pterodon pubescens.

The chemoprophylactic action of the essential oil of the fruit of Pterodon pubescens Benth (Leguminosae), incorporated in different soap formulations, was studied in experimental schistosomiasis. The formulations were used locally on the tails of mice which were exposed to Schistosoma mansoni cercariae immediately, 24, 72 or 168 hours later by the method of tail immersion. Protection was evaluated 45 days after exposure when the mice were sacrificed and the worms collected by perfusion. The results showed levels of protection varying from 0.0 to 100% depending on the formulation used. A methodology that allowed the evaluation of soap protection of mice exposed to natural infection in snail infested streams on the outskirts of Belo Horizonte, MG, was also developed. Promising results were obtained in that protection of between 57.5 and 31.1% was observed in field trials when soap was applied to the animals 24 and 48 hours earlier. Preliminary studies evaluating irritation and toxicity were favorable and showed that this new prophylactic weapon could contribute to the control of schistosomiasis.

Myrcene mimics the peripheral analgesic activity of lemongrass tea.

Oral administration of an infusion of lemongrass (Cymbopogon citratus) fresh leaves to rats produced a dose-dependent analgesia for the hyperalgesia induced by subplantar injections of either carrageenin or prostaglandin E2, but did not affect that induced by dibutyryl cyclic AMP. These results indicate a peripheral site of action which was confirmed with the essential oil obtained by steam distillation of the leaves. Silica gel column fractionation of the essential oil allowed the identification of myrcene as the major analgesic component in the oil. Identification of the components was made by thin-layer chromatography and checked by mass spectrometry. The peripheral analgesic effect of myrcene was confirmed by testing a standard commercial preparation on the hyperalgesia induced by prostaglandin in the rat paw test and upon the contortions induced by intraperitoneal injections of iloprost in mice. In contrast to the central analgesic effect of morphine, myrcene did not cause tolerance on repeated injection in rats. This analgesic activity supports the use of lemongrass tea as a "sedative" in folk medicine. Terpenes such as myrcene may constitute a lead for the development of new peripheral analgesics with a profile of action different from that of the aspirin-like drugs.

[Chemoprophylactic activity of soaps containing essential oil from the fruit of Pterodon pubescens in schistosomiasis mansoni]. / Atividade quimioprofilática de sabonetes contendo óleo essencial de frutos de Pterodon pubescens na esquistossomose mansoni.

It has been studied the chemoprophylactic action on experimental schistosomiasis of the essential oil from Pterodon pubescens "sucupira branca" as an additive through different formulations, in toilet soap. Immediately or 24 hours later, groups of mice were exposed by tail method to Schistosoma mansoni cercariae. After 45 days of the exposition, the protective action of these soaps were evaluated. The results showed different levels of protection, ranging from 29.0 to 100.0%. Further studies are on going with the most promising formulations.

Atividade quimioprofilática de sabonetes contendo óleo essencial de frutos de Pterodon pubescens na esquistossomose mansoni / Chemoprophylactic activity of soaps containing essential oil of Pterodon pubescens fruits in Schistosomiasis mansoni

It has been studied the chemoprophylactic action on experimental schistosomiasis of the essential oil from Pterodon pubescens "sucupira branca" as an additive through different formulations, in toilet soap. Immediately or 24 hours later, groups of mice were exposed by tail method to Schistosoma mansoni cercariae. After 45 days of the exposition, the protective action of these soaps were evaluated. The results showed different levels of protection, ranging from 29.0 to 100.0%. Further studies are on going with the most promising formulations.

[Chemoprophylaxis of schistosomiasis: molluscacidal activity of natural products--assays with adult snails and oviposition]. / Quimioprofilaxia da esquistossomose: atividade moluscicida de produtos naturais--ensaios com caramujos adultos e desovas.

Data concerning the molluscicidal activity of 159 extracts from 84 Brazilian plants on Biomphalaria glabrata, the most important intermediate host of Schistosoma mansoni in Brazil, are presented. Seventy eight extracts (49,0%) showed activity against snails or eggs, but only twenty nine (18.2%) were active on both, snails and eggs. Extracts of two species (Mikania hirsutissima and Qualea multiflora) have shown to be lethals to adult snails at 10 ppm concentration.

Quimioprofilaxia da esquistossomose: atividade moluscicida de produtos naturais - ensaios com caramulos adultos e desovas. / Chemoprophylaxis of schistosomiasis: molluscacidal activity of natural products - assays with adult snails and oviposition

Sao apresentados os dados relativos a atividade moluscicida de 159 extratos, de 84 plantas brasileiras, sobre Biomphalaria glabrata, o mais importante hospedeiro intermediario do Schistosoma mansoni no Brasil. Setenta e oito (49,0%) dos extratos mostraram atividade contra caramujos ou desovas, porem, somente vinte e nove (18,2%)foram ativos sobre ambos. Os extratos de duas especies de vegetais (Mikania hirsutissima e Qualea multiflora) foram letais aos caramujos adultos, na concentracao de 10 ppm