Evaluation of cytogenotoxicity, antioxidant and hypoglycemiant activities of isolate compounds from Mansoa hirsuta D.C. (Bignoniaceae).

Mansoa hirsuta (Bignoniaceae) is a native plant from caatinga in Brazilian semiarid. This plant has been locally used as antimicrobial and hypoglycemiant agents, but their action mechanisms and toxicity remain largely unknown. Therefore, we evaluated the composition and antioxidant, cytoprotective and hypoglycemiant effects of raw extract, fractions and compounds from leaves of M. hirsuta. The cytogenotoxic effects of ursolic and oleanolic acids, the main phytotherapic components of this plant, were assessed. The raw extract and fractions presented steroids, saponins, flavonols, flavanonols, flavanones, xanthones, phenols, tannins, anthocyanins, anthocyanidins and flavonoids. The ethyl acetate fraction inhibited efficiently the cascade of lipid peroxidation while the hydroalcoholic fraction was richer in total phenols and more efficient in capturing 2,2-diphenyl-1-picrylhydrazyl (·DPPH) and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS·+) radicals. The isolated fraction of M. hirsuta also inhibited the α-amylase activity. Cytotoxic effects were absent in both raw extract and fractions while ursolic+oleanolic acids were efficient in protecting cells after exposure to hydrogen peroxide. Moreover, this mixture of acid shad no significant interference on the mitotic index and frequency of nuclear and/or chromosomal abnormalities in Allium cepa test. Therefore, M. hirsuta represents a potential source of phytochemicals against inflammatory and oxidative pathologies, including diabetes.

Ryanodane diterpenes from two Erythroxylum species.

Ryanodane diterpenes, named 14-O-methyl-ryanodanol and ryanodanol, were isolated from ripe fruit of Erythroxylum passerinum. Compound 2 was also found in the leaves of this species, while 1 was obtained from the leaves of E. nummularia. Compound 1 showed insecticidal activity against Aedes aegypti larvae.

Antinociceptive activity of Maytenus rigida stem bark.

Ethanol extract of Maytenus rigida stem bark and its fractions were assessed for antinociceptive activity in tail-flick test in rats. The activity was located in the chloroform, ethyl acetate and aq.methanol fractions. Phytochemical screening revealed that catechin was the only common class of compounds present on the ethanol extract as well as on the active fractions. 4'-Methylepigallocatechin, isolated from the ethyl acetate and aq.methanol fractions, showed antinociceptive effect in the tail-flick test (75 mg/kg; p.o.), which was reversed by the opiate antagonist naloxone (3 mg/kg; i.p.).

Larvicidal and cytotoxic potential of squamocin on the midgut of Aedes aegypti (Diptera: Culicidae).

Acetogenins are secondary metabolites exclusively produced by Annonaceae, which have antitumor, cytotoxic, and pesticide activities. In this study, we evaluated the larvicidal and cytotoxic effect of squamocin from Annona squamosa on Aedes aegypti (Diptera: Culicidae) midgut. The compound was solubilized in 2% Tween 20 at 10, 20, 50, 80 and 100 ppm. The assay was conducted in a completely randomized design with four replications, each with 20 third-instar larvae. Larval mortality was assessed every hour until total mortality, and the data were subjected to Probit analysis. Cellular damage was evaluated every 30 min in groups comprising five larvae subjected to squamocin at 50 and 100 ppm for 240 min. The total larval mortality occurred after 360 min following application of 50, 80, and 100 ppm squamocin, and 600 min after applying other concentrations with LC50 at 6.4 ppm. Both 50 and 100 ppm of squamocin showed cytotoxic activity in the midgut epithelium of A. aegypti after 240 min with 50 ppm resulting in midgut cells with light cytoplasm containing small vacuoles, whereas at 100 ppm were found cells with cytoplasm highly vacuolated, damaged apical surface and cell protrusion toward the gut lumen. In conclusion, squamocin has the potential to control A. aegypti.

Iron bioavailability of common beans (Phaseolus vulgaris L.) intrinsically labeled with (59)Fe.

A radiobioassay was performed in rats with or without iron depletion to evaluate the iron bioavailability of diets enriched with common beans and with "multimixture", a nutritional supplement based on parts of foods that are not usually eaten. The full-body (59)Fe level was determined after 5h, the absorbed (59)Fe level was determined after 48 h, and the amount of (59)Fe retained was determined after 7 days. Iron bioavailability was assessed by the full-body radioactivity of the animals, determined using a solid scintillation detector. The iron bioavailability of common beans was higher in the iron-depleted animals (55.7%) than in the non-depleted animals (25.12%) because of the higher absorption rate in the iron-depleted animals. The multimixture did not influence dietary iron bioavailability. In addition, the iron bioavailability of common beans was similar to that observed in the standard source of iron for Wistar rats. Hence, common beans may be considered an adequate dietary iron source because of its high bioavailability.

Evaluation of cytogenotoxicity, antioxidant and hypoglycemiant activities of isolate compounds from Mansoa hirsuta D.C. (Bignoniaceae)

ABSTRACT Mansoa hirsuta (Bignoniaceae) is a native plant from caatinga in Brazilian semiarid. This plant has been locally used as antimicrobial and hypoglycemiant agents, but their action mechanisms and toxicity remain largely unknown. Therefore, we evaluated the composition and antioxidant, cytoprotective and hypoglycemiant effects of raw extract, fractions and compounds from leaves of M. hirsuta. The cytogenotoxic effects of ursolic and oleanolic acids, the main phytotherapic components of this plant, were assessed. The raw extract and fractions presented steroids, saponins, flavonols, flavanonols, flavanones, xanthones, phenols, tannins, anthocyanins, anthocyanidins and flavonoids. The ethyl acetate fraction inhibited efficiently the cascade of lipid peroxidation while the hydroalcoholic fraction was richer in total phenols and more efficient in capturing 2,2-diphenyl-1-picrylhydrazyl (·DPPH) and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS·+) radicals. The isolated fraction of M. hirsuta also inhibited the α-amylase activity. Cytotoxic effects were absent in both raw extract and fractions while ursolic+oleanolic acids were efficient in protecting cells after exposure to hydrogen peroxide. Moreover, this mixture of acid shad no significant interference on the mitotic index and frequency of nuclear and/or chromosomal abnormalities in Allium cepa test. Therefore, M. hirsuta represents a potential source of phytochemicals against inflammatory and oxidative pathologies, including diabetes.

Bioavailability of iron in the regional basic diet (RBD) with dietary supplement in Brazil.

The consumption of the regional basic diet (RBD) determines a state of malnutrition found in the low-income population of Northeastern Brazil. A dietary supplement known as multimixture has been used as an alternative source of iron in food for the prevention and/or treatment of anemia and for the recovery from malnutrition. The purpose of the present work was to evaluate the bioavailability of iron in the RBD supplemented with multimixture in iron-depleted and non-depleted Wistar rats. To produce iron depletion in the animals, pretest depletion diets without iron and the pretest control diet based on the AIN-93 diet were used for 8 weeks. This phase was followed by the test diets: control, AIN-93 extrinsically labeled with (59)FeCl(3); RBD, containing carioca beans intrinsically labeled with (59)Fe; and RBDMM, RBD plus multimixture, supplied in a single meal. Hemoglobin concentration, weight gain, and dietary intake were determined in the pretest phase. Iron bioavailability was determined by the determination of total-body radiation in the animals for 7 days, using a solid scintillation detector. The hemoglobin concentration, weight gain, and dietary intake were greater in the non-depleted animals than in the iron-depleted ones. The iron bioavailability of the diets did not differ significantly. It was concluded that the multimixture did not affect the bioavailability of Fe contained in the beans of the RBD.

Electroanalytical studies of sulfentrazone in protic medium, its degradation by the electro-Fenton process, and toxicity assessment using ss-DNA.

Sulfentrazone is an herbicide used as a pre-plant incorporated or pre-emergence treatment. The electrochemical oxidation of sulfentrazone was studied, by cyclic, differential and square-wave voltammetry on unmodified and on glassy carbon nanotube-modified electrodes, and by controlled-potential coulometry and electrolysis. The voltammograms of sulfentrazone showed a main irreversible diffusion-controlled pH-dependent oxidation peak. The in situ DNA-damaging capacity of sulfentrazone was also investigated, employing double stranded ds-DNA-modified glassy carbon electrode, without evidence of interaction. On the other hand, in a solution of sulfentrazone and single stranded ss-DNA, the oxidation signals of the respective bases decreased concentration-dependently, indicating binding of sulfentrazone to guanine and adenine. The electro-Fenton method was employed to promote decontamination by eliminating the herbicide, resulting in almost 60% of mineralization.

8,15-epoxylabdane and norlabdane diterpenoids from Eragrostis viscosa.

Four labdanes with a 8alpha,15-epoxy ring (8alpha,15-epoxylabdan-16beta-oic acid; 8alpha,15-epoxy-16-norlabdan-13-one; 8alpha,15-epoxy-16-norlabdane; and 16-acetoxy-8alpha,15-epoxylabdane) and the known compound ambreinolide were isolated from the hexane extract of the aerial parts of the grass Eragrostis viscosa. The structures of all compounds were established based on spectroscopic data and the X-ray analysis of 8alpha,15-epoxy-16-norlabdan-13-one. The hexane extract presented moderate activity against the snail Biomphalaria glabrata. 8alpha,15-Epoxylabdan-16beta-oic acid showed no mutagenic activity for doses up to 1000 microg/plate and no significant clastogenic activity for doses up to 100 microg/ml.

Evaluation of the toxicity and molluscicidal and larvicidal activities of Schinopsis brasiliensis stem bark extract and its fractions

Dengue fever and schistosomiasis are major public health issues for which vector control using larvicide and molluscicide substances present in plants provides a promising strategy. This study evaluated the potential toxicity of the extract of hydroethanol Schinopsis brasiliensis Engl., Anacardiaceae, stem bark and its chloroform, hexane, ethyl acetate, and hydromethanol fractions against Artemia salina and Aedes Aegypti larvae and snails Biomphalaria glabrata. All of the assays were performed in triplicate and the mean mortality rates were used to determine the LC50 and LC90 values using the probit method. The hydroethanol hydromethanol extract and fraction were free of toxicity towards A. salina (LC50 > 1000 µg/ml), while chloroform fraction was moderately toxic (LC50 313 µg/ml); ethyl acetate and hexane fractions displayed low toxicity, with LC50 557 and 582 µg/ml, respectively. Chloroform, hexane, and ethyl acetate fractions showed larvicidal potential towards A. aegypti (LC50 values of 345, 527 and 583 µg/ml, respectively), while chloroform and ethyl acetate fractions were highly toxic to B. glabrata (LC90 values of 68 and 73 µg/ml, respectively). Based on these findings, ethyl acetate, chloroform, and hexane fractions should be further investigated for their potential use against the vectors of dengue and schistosomiasis.

Cytotoxic activity of marine algae against cancerous cells

This paper presents an investigation on the cytotoxic activity in human tumor cell from dichloromethane, chloroform, methanol, ethanol, water extracts, and hexane and chloroform fractions from green, brown and red algae collected at Riacho Doce Beach, north coast of Alagoas, Brazil, against the cancer cells K562 (chronic myelocytic leukemia), HEp-2 (laryngeal epidermoid carcinoma) and NCI-H292 (human lung mucoepidermoid carcinoma) through the MTT colorimetric method. The dichloromethane extract and chloroform fraction of Hypnea musciformis showed the best cytotoxic activity against K562 (3.8±0.2 µg.mL-1 and 6.4±0.4 µg.mL-1, respectively). Dichloromethane extracts of Dictyota dichotoma (16.3±0.3 µg.mL-1) and the chloroform fraction of H. musciformis (6.0±0.03 µg.mL-1) and chloroform fraction of P. gymnospora (8.2±0.4) were more active against HEp-2 as well as ethanol extracts of P. gymnospora (15.9±2.8 µg.mL-1) and chloroform fraction of H. musciformis (15.0±1.3 µg.mL-1) against the cell NCI-H292. The constituents with higher anticancer action are present in the extracts of dichloromethane and chloroform and in the chloroform fraction of H. musciformis, Digenea simplex, P. gymnospora, and D.dichotoma. In the case of the seaweed S. vulgare, the anticancer constituents are present in the aqueous extract.

[Hepatoprotective effect of diheptanoin and tritreptanoin chronic consumption against steatosis in rats]. / Efeito hepatoprotetor do consumo crônico de dieptanoína e trieptanoína contra a esteatose em ratos.

OBJECTIVE: To evaluate the effect of chronic consumption of di- and triheptanoin on hepatic steatosis (HS) in rats. METHODOLOGY: Wistar rats were submitted to a diet AIN-93 with 0, 30 or 50% of its oil substituted with an oil rich in di- and triheptanoin, groups TAGC(7)0, TAGC(7)30 and TAGC(7)50 respectively, for nine months. The control group received Labina(R). Liver histology, hepatic lesion and function proofs, glycemia and lipid profile, were performed. Variance analyses, F-test, Dunnet s test and uni- and multivariate regression analyses were performed (p<0.05). RESULTS: TAGC(7)0, TAGC(7)30 and TAGC(7)50 developed HS; 80% of severe cases in TAGC(7)0, as against 40% in TAGC(7)50. The absolute (ALW) and relative (RLW) liver weights were higher in TAGC(7)0 and TAGC(7)30, and glycemia was greater in TAGC(7)30 and TAGC(7)50, than in the Control. Total cholesterol, LDL-c, LDL-c/HDL-c and total proteins were higher in the Control. The experimental oil reduced RLW and showed a tendency in the reduction of body weight, ALW, percentage of hepatic lipids and the severity of HS. The explanatory variables in relation to HS were final weight, glycemia, albumin, HDL-c, LDL-c, LDL-c/HDL-c, VLDL-c and alkaline phosphatase. CONCLUSIONS: It is suggested that di- and triheptanoin have a hepatoprotector effect against HS, in rats, in a dose-dependent manner.

Antinociceptive and anti-inflammatory activity of hydroalcoholic extracts and fractions from Erythrina mulungu

Erythrina mulungu Mart. ex Benth., Fabaceae, popularly known as mulungu, is used for the treatment of insomnia and disorders of the central nervous system. This study examined the antinociceptive effects of the hydroalcoholic extracts (HAE), the ethyl acetate and chloroformic fractions from E. mulungu in four experimental models of nociception using laboratory mice. The extracts and fractions were administered orally to mice at doses of 100 mg/kg. Inhibition of abdominal contractions were observed for all the extracts and fractions tested, as compared to controls. All extracts and fractions from E. mulungu reduced the nociception activity produced by formalin in the 2nd phase. In the hot plate test no significant effect was observed for any extract or fraction. In the peritonitis test induced by Zymosan, all of the tested extracts and the chloroformic fraction, except for the ethyl acetate phase, reduced cell migration of the peritoneal cavity. We concluded that E. mulungu shows antinociceptive effects, which are independent of the opioid system.

Antinociceptive effects of an extract, fraction and an isolated compound of the stem bark of Maytenus rigida

The antinociceptive activity of the Maytenus rigida Mart. (Celastraceae) ethanol extract and its ethyl acetate fraction as well as of (-)-4'-methylepigallocatechin (1), a previously isolated compound, was demonstrated in vivo. ED50 for 1 in the writhing test was 14.14 mg/kg. The acetic acid-induced writhing was inhibited by 98.4, 84.4, and 58.3%, respectively, when mice were treated with the ethanol extract, ethyl acetate fraction, and 1. In the hot plate test, mice pretreated with 1 showed significantly increased reaction times (60-89%). Oral administration of 1 significantly inhibited first and second phases of the formalin-induced pain (50 and 26.5%, respectively), whereas indomethacin inhibited only the second phase of the test (41.2%). Ethanol extract and its fraction showed effects on inflammatory pain, while neurogenic and inflammatory pain suppression by 1 is a strong indication of the presence of both central and peripheral effects and suggests its analgesic and anti-inflammatory potential.

Pentacyclic triterpene 5-phenylpenta-2,4-dienoyl esters from Peltastes peltatus (Vell.) Woodson.

Two new pentacyclic triterpene esters, peltastine A [3beta-[5-phenyl-(2E,4E)-penta-2,4-dienoyloxy]-urs-12-ene] and peltastine B [3beta-[5-phenyl-(2E,4E)-penta-2,4-dienoyloxy]-lup-20(29)-ene], have been isolated from the stem of Peltastes peltatus (Vell.) Woodson along with the previously reported beta-amyrin juarezate [3-[5-phenyl-(2E,4E)-penta-2,4-dienoyloxy]-olean-12-ene]. The structures of these compounds were established by MS, 1D- and 2D-NMR experiments as well as by chemical degradation.

Atividade antimicrobiana de extratos hidroalcoólicos de Lafoensia pacari A. St.-Hil., Lythraceae, frente a bactérias multirresistentes de origem hospitalar / Antibacterial activity of the hydro-alcoholic extracts of Lafoensia pacari Saint Hil. against multiresistant bacterial strains from hospital source

Os microrganismos patogênicos multirresistentes apresentam-se como grandes responsáveis por milhões de mortes em todo o mundo, principalmente Pseudomonas aeruginosa e Staphylococcus aureus, responsáveis por grande parte das infecções hospitalares. A preocupação com estas espécies faz com que novas pesquisas busquem alternativas para controlar estes microrganismos de uma forma mais eficiente e também mais econômica. Os extratos fitoterápicos são alternativas promissoras para este fim, visto que são uma imensa fonte de compostos de ação biológica. O objetivo do trabalho foi a elucidação da atividade antimicrobiana do extrato de Lafoensia pacari A. St.-Hil., Lythraceae, frente a linhagens de bactérias multirresistentes (P. aeruginosa, S. aureus) isoladas de pacientes com múltiplas infecções internados na Unidade de Emergência de Maceió. Os testes de atividade antibacteriana foram avaliados pelo método de difusão em meio sólido (Kirby-Bauer) modificado. De acordo com os ensaios in vitro, foi constatado que 96,4 por cento das linhagens de bactérias utilizadas na pesquisa apresentaram-se sensíveis ao extrato da folha da planta, demonstrando atividade antibacteriana. Halos de inibição de crescimento de até 26 mm foram encontrados. Dessa forma, conclui-se que o extrato de Lafoensia pacari apresenta possibilidades de se encontrar substâncias úteis no combate a bactérias multirresistentes.

Multiresistant pathogenic microorganisms are responsible for million of death all the world, mainly Pseudomonas aeruginosa and Staphylococcus aureus that are responsible for great part of hospital infections. The concern with this species does new researches to find out alternatives to control these microorganisms in the way more efficient and more economic. The phytoterapic extracts are promissory alternatives for that purpose because they are an immense source of biological action. The objective of this study was to evaluate the antimicrobial activity of Lafoensia pacari A. St.-Hil., Lythraceae, extract on multiresistant bacterial strains (P. aeruginosa, S. aureus) that have been isolated from patients with multiple infections occupying an Emergency Unit from Maceió in Brazil. The antibacterial activity experiments were evaluated by agar diffusion tests. Agreeable us experiments in vitro, ascertain that 96,4 percent of bacterial strains utilized in this research have showed susceptible to the plant's leaf extract, it means an excellent antibacterial activity. Halos of bacterial inhibition until 26 mm were observed. Thus, it can be concluded that the Lafoensia pacari extract has showed as an excellent product to combat multiresistant bacterial.

Efeito hepatoprotetor do consumo crônico de dieptanoína e trieptanoína contra a esteatose em ratos / Hepatoprotective effect of diheptanoin and tritreptanoin chronic consumption against steatosis in rats

OBJETIVO: Avaliar o efeito do consumo crônico de di e trieptanoínas sobre a esteatose hepática (EH) em ratos. METODOLOGIA: Ratos Wistar submetidos à dieta AIN-93 com 0 por cento, 30 por cento ou 50 por cento de substituição do óleo por óleo rico em di e trieptanoína, grupos TAGC(7)0, TAGC(7)30 e TAGC(7)50, respectivamente, por nove meses. O grupo-controle recebeu ração Labina®. Analisaram-se histologia e provas de função e lesão hepática, glicemia e perfil lipídico sérico. Realizaram-se análise de variância, teste F, teste de Dunnet e análises de regressão uni e multivariadas (p < 0,05). RESULTADOS: TAGC(7)0, TAGC(7)30 e TAGC(7)50 desenvolveram EH; 80 por cento de casos graves no TAGC(7)0 contra 40 por cento no TAGC(7)50. Os pesos absoluto (PAF) e relativo do fígado (PRF) foram maiores em TAGC(7)0 e TAGC(7)30 e a glicemia foi maior em TAGC(7)30 e TAGC(7)50, que no grupo-controle. Colesterol total, LDL-c, LDL-c/HDL-c e proteínas totais foram maiores no grupo-controle. O óleo experimental reduziu o PRF e determinou tendência de redução do peso corporal, PAF, percentual de lipídios hepáticos e graus de EH (GHE). As variáveis explicativas para GHE foram peso final, glicemia, albumina, HDL-c, LDL-c, LDL-c/HDL-c, VLDL-c e fosfatase alcalina. CONCLUSÕES: Sugere-se que di e trieptanoínas exerçam efeito hepatoprotetor contra a EH, em ratos, em uma feição dose-dependente.

OBJECTIVE: to evaluate the effect of chronic consumption of di- and triheptanoin on hepatic steatosis (HS) in rats. METHODOLOGY: Wistar rats were submitted to a diet AIN-93 with 0, 30 or 50 percent of its oil substituted with an oil rich in di- and triheptanoin, groups TAGC(7)0, TAGC(7)30 and TAGC(7)50 respectively, for nine months. The control group received Labina®. Liver histology, hepatic lesion and function proofs, glycemia and lipid profile, were performed. Variance analyses, F-test, Dunnet´s test and uni- and multivariate regression analyses were performed (p<0.05). RESULTS: TAGC(7)0, TAGC(7)30 and TAGC(7)50 developed HS; 80 percent of severe cases in TAGC(7)0, as against 40 percent in TAGC(7)50. The absolute (ALW) and relative (RLW) liver weights were higher in TAGC(7)0 and TAGC(7)30, and glycemia was greater in TAGC(7)30 and TAGC(7)50, than in the Control. Total cholesterol, LDL-c, LDL-c/HDL-c and total proteins were higher in the Control. The experimental oil reduced RLW and showed a tendency in the reduction of body weight, ALW, percentage of hepatic lipids and the severity of HS. The explanatory variables in relation to HS were final weight, glycemia, albumin, HDL-c, LDL-c, LDL-c/HDL-c, VLDL-c and alkaline phosphatase. CONCLUSIONS: It is suggested that di- and triheptanoin have a hepatoprotector effect against HS, in rats, in a dose-dependant manner.