Caryocar brasiliense peel ethanolic extract has neuroprotective potential and reduces the activation of ERK1/2 in the ischemia and reperfusion brain acute phase in the rat.

Oxidative stress induced by ischemia and reperfusion (I/R) injury results in cell death by necrosis or apoptosis and triggers the activation of different intracellular pathways, such as mitogen-activated protein activated kinases. Pequi (Caryocar brasiliense) peel, residue of a fruit from Brazilian savannah-like vegetation, has phenolic compounds that have been demonstrated to have antioxidant effects in vitro. The present study aimed to evaluate the neuroprotective effects of C. brasiliense peel ethanolic extract (CBPE) against transient global I/R injury in the rat brain. Global ischemia for 5, 20, and 45 min followed by 2 h of reperfusion caused a significant time-dependent increase in the number of ischemic neurons (p ≤ 0.05); increased immunoreactivity of cleaved caspase-3 (CASP3); and activated extracellular signal-regulated kinase (ERK) 1/2. Pretreatment with CBPE (600 mg/kg, oral) or vitamin E (0.6 mg, oral) for 30 days showed significant protection against acute brain injury induced by 20 and 45 min or 5 min of ischemia, respectively, by reducing the cortical ischemic neuron count (p ≤ 0.05) and p-ERK1/2 immunoreactivity. In addition, active c-Jun N-terminal kinase (JNK) immunoreactivity was reduced in animals not subjected to ischemia. Therefore, we suggest an association between vitamin E and CBPE, which may generate a better neuroprotective response. Interestingly, mainly in the hippocampus and oligodendrocytes, high dose CBPE increase the number of isquemic neurons and of CASP3 immunoreactive cells in animals subjected or not to ischemia, which was not verified in the vitamin E group. Therefore, additional studies are recommended to verify the safety of the continuous use of CBPE.

Variability of polyphenols and volatiles during fruit development of three pitanga (Eugenia uniflora L.) biotypes.

Changes in volatile constituents and phenolic compounds were investigated during fruit development of three pitanga biotypes. Constituents were submitted to multivariate analysis and fruit samples were differentiated by selina-1,3,7(11)-trien-8-one (38.2 ±â€¯2.9%) and its epoxide (26.4 ±â€¯7.2%) for the red-orange biotype; by curzerene (15.04 ±â€¯2.1%) and atractylone (8.47 ±â€¯2.1%) for the red biotype; and by spathulenol (3.7 ±â€¯0.8%) and germacrone (54.7 ±â€¯3.1%) for the purple biotype. Hydrolysable tannins such as mono-O-galloyl-d-glucose, 1,2,6-tri-O-galloyl-ß-d-glucose, tellimagrandin II, and eugeniflorin D2 were identified, as well as oenothein B as the major compound (32.43 ±â€¯7.1 mg/g dry fruit). During pitanga's maturation, anthocyanin content increased, while flavonoid and tannin contents decreased. Higher contents of the majority of phenolic compounds occurred in the red-orange biotype. Biosynthesis of phenolic compounds was influenced by biotype and degree of maturation, whereas chemovariation in essential oil constituents was mainly due to biotypes, thus confirming essential oil chemotypes of E. uniflora.

Protective effect and induction of DNA repair by Myrciaria cauliflora seed extract and pedunculagin on cyclophosphamide-induced genotoxicity.

Ellagitannins are well-known antioxidants in medicinal plants, foods, and edible fruits, particularly in Myrciaria cauliflora (jabuticaba). Thus, this study aimed to evaluate the protective effects of jabuticaba seed extract (JSE) and pedunculagin using in vivo micronucleus test and comet assay in mouse bone marrow cells, in combination with cyclophosphamide (CP), a bioreductive alkylating agent. The ellagitannin composition of JSE was determined by HPLC/PDA, with castalagin, vescalagin, and pedunculagin as the main compounds (124.4, 45.5, and 15.6mg/g dw, respectively). Results from pre- and co- treatments with JSE or pedunculagin clearly showed their protective action against CP-induced micronuclei and DNA damage. The effects of both tannins in post-treatments with CP suggested they influence DNA repair systems. These findings indicate that JSE and pedunculagin possess chemopreventive as well as DNA repair-inducing properties.

Genotoxicity and cytotoxicity evaluation of oenothein B and its protective effect against mitomycin C-induced mutagenic action.

The natural product oenothein B (OeB), a dimeric macrocyclic ellagitannin, has a wide range of biological activities, such as antioxidant, anti-inflammatory, anti-viral, antifungal, and antitumor. However, investigations concerning its genotoxicity have not been carried out. This study assessed the cytotoxicity, genotoxicity, and protective effects of oenothein B using in vitro SOS-Inductest and in vivo mouse bone marrow micronucleus (MN) assay through oral and intraperitonial routes. In both assays oenothein B did not produce genotoxic effects in any of doses tested; in contrast, cytotoxic effect in cells was detected only in mice groups treated by both routes and exposed for 24 and 48h. Antigenotoxic and anticytotoxic activities of oenothein B were evaluated using both assays in combination with mitomycin C (MMC), a bioreductive alkylating agent. In the MN assay, a significant reduction was observed in MN frequency in all groups co-treated with MMC and OeB compared to those which received only MMC. Anticytotoxicity was observed in mice groups exposed to OeB and MMC for 24 and 48h. In the SOS-Inductest, oenothein B failed to show antigenotoxic and anticytotoxic effects; thus, it undoubtedly showed an in vivo protective activity against primary DNA damage induced by mitomycin C.

Extrato hidroalcoolico da casca do pequi (Caryocar brasiliense) em ratos submetidos à aplicação de doxorrubicina / Hydro alcoholic extract of pequi peel (Caryocar brasiliense) in rats submitted to the application of doxorubicin

O objetivo deste estudo foi avaliar o efeito antioxidante do extrato hidroalcoolico da casca do pequi (EHCP) em ratos após a administração de doxorrubicina (DOX). Foram utilizados ratos da raça Wistar, distribuídos em quatro grupos, sendo que os animais do G1 (n=6) receberam água e solução salina (grupo controle), G2 (n=7) EHCP e solução salina, G3 (n=7) água e DOX e G4 (n=6) EHCP e DOX. O EHCP foi administrado por gavagem durante 10 dias aos ratos dos grupos G2 e G4 e água aos dos G1 e G3. DOX na dose de 10mg kg-1 e solução salina 0,9% foram administradas por via intravenosa no dia sete após o início do experimento aos animais de G3 e G4 e aos de G1 e G2, respectivamente. Foram avaliados peso e taxa de mortalidade. Dez dias após o início do experimento, foi avaliada a concentração sérica de creatina quinase MB (CK-MB), troponina e mioglobina, e os ratos foram submetidos à eutanásia e à avaliação anatomopatológica. Não houve diferença entre os tratamentos quanto ao peso dos animais (P<0,05). Com relação à taxa de mortalidade, houve aumento no grupo 2 (P<0,05). Os resultados do teste qualitativo para a detecção de CK-MB, troponina I e mioglobina nos quatro grupos foram negativos e não foram observadas alterações macroscópicas nos órgãos dos ratos dos diferentes grupos. Constatou-se necrose tubular aguda multifocal de intensidade moderada a acentuada nas regiões cortical e medular nos rins de todos os ratos avaliados. A DOX em dose única de 10mg kg-1 e via intravenosa não promove alterações cardíacas em ratos e o EHCP nas condições avaliadas aumenta o índice de mortalidade em ratos, o que pode estar relacionado a substâncias tóxicas presentes na casca desse fruto.

The objective of this study was to evaluate the antioxidant effect of the hydroalcoholic extract of pequi peel (HEPP) in rats after administration of doxorubicin (DOX). Were used 26 Wistar rats divided into four groups, which G1 (n=6) received water and saline solution (control group), G2 (n=7) HEPP and saline solution, G3 (n=7) water and DOX, and G4 (n=6) HEPP and DOX. The HEPP was administered by gavage for 10 days to G2 and G4 and water to G1 and G3. DOX and saline solution were administered intravenously on day seven after the start of the experiment, with the DOX (10mg kg-1) applied in G3 and G4, and saline solution 0.9% in G1 and G2. Were evaluated weight and mortality rate. Ten days after the start of the experiment were evaluated creatina kinase MB (CK-MB), troponin and myoglobin, and the rats were euthanized and evaluated morphologically. There was no difference between treatments in weight of animals (P>0.05). About the mortality rate an increase in group 2 was showed (P<0.05). The results of the qualitative test for the detection of CK-MB, troponin I and myoglobin in the four groups were negative and there were no macroscopic changes in different rat's organs of different groups. Multifocal and moderate to severe acute tubular necrosis in cortical and medullary regions of the kidneys was observed in all rats studied. DOX intravenous and in a one dose of 10mg kg-1 don't induce cardiac changes in rats and the HEPP in conditions here evaluated increase the rate of mortality of rats, which may be related to toxic substances in the peel of this fruit.

Influence of environmental factors on the concentration of phenolic compounds in leaves of Lafoensia pacari

Lafoensia pacari A. St.-Hil., Lythraceae, a plant from the Cerrado known as pacari or dedaleiro, is widely used as an antipyretic, wound healing, anti-inflammatory, antidiarrheal and in the treatment of gastritis and cancer. Notable among the metabolite groups identified in leaves of L. pacari are the polyphenols, such as tannins and flavonoids, related to the pharmacological activities of pacari. Studies on the influence of environmental factors over production of major groups of secondary metabolites in pacari are important because they contribute data for its cultivation and harvest, and establish quantitative parameters of secondary metabolites in the plant drug. The objective of this study was to evaluate the influence of environmental factors on concentrations of phenolic metabolites in the leaves of L. pacari. Compounds quantified in the leaves were: total phenols, tannins by protein precipitation, hydrolysable tannins, total flavonoids, ellagic acid and mineral nutrients, while soil fertility was also analyzed, all over a period of one year. The data were analyzed using multivariate analysis, and the results suggest that metabolite concentrations in the leaves of this plant are influenced by seasonal factors, in particular the temperature and foliar micronutrients (Cu, Fe, Mn, Zn).

Cytotoxic and genotoxic investigation on barbatimão [Stryphnodendron adstringens (Mart) Coville, 1910] extract

Stryphnodendron adstringens (Mart.) Coville, 1910 is a small tree, distributed widely throughout the Cerrado region of Brazil and named "barbatimão" by the Tupi-Guarani tribes, which presents astringent properties. Its ethnopharmacological uses comprise, among others, anti-inflammatory and wound healing action, and it is used in the treatment of diarrhea and gynecological problems. The phytotherapeutic use of 'barbatimão' is largely related to its tannin content, which is abundant in its bark. The main goal of the present study was to evaluate the cytotoxic, mutagenic, and genotoxic potential of the lyophilized solution of the stem bark of S. adstringens, using the Ames test, the SOS-Inductest and the SOS-Chromotest. S. adstringens presented cytotoxic activity in all tested systems, did not present mutagenic activity detectable by the Ames test and SOS-Chromotest, and showed some genotoxic effect on the SOS-Inductest. However, the metabolization of the extract by S9 fraction attenuated its genotoxic and cytotoxic activities.

Stryphnodendron adstringens (Mart.) Coville, 1910 é uma pequena árvore amplamente distribuída nas regiões de cerrado do Brasil, chamada de "barbatimão" pelas tribos Tupi-Guarani, que apresenta propriedade adstringente. Seu uso etnofarmacológico compreende, entre outros, efeitos antiinflamatório e cicatrizante, sendo empregada no tratamento de diarréias e problemas ginecológicos. Grande parte das aplicações do fitoterápico de barbatimão está relacionada aos taninos, abundantes em sua casca. O objetivo do presente trabalho foi avaliar os potenciais citotóxico, mutagênico e genotóxico da solução liofilizada da casca de S. adstringens, utilizando Teste de Ames, SOS-Induteste e SOS-Cromoteste. S. adstringens apresentou atividade citotóxica em todos os sistemas testados, não apresentou atividade mutagênica detectável pelo teste de Ames e SOS-Cromoteste e mostrou certo efeito genotóxico no SOS-Induteste. Porém, a metabolização do extrato pela fração S9 atenuou suas atividades genotóxica e citotóxica.

Atividade antifúngica de Caryocar brasiliensis (Caryocaraceae) sobre Cryptococcus neoformans / Antifungal activity of Caryocar brasiliensis (Caryocaraceae) against Cryptococcus neoformans

A grande incidência de criptococose em decorrência do aumento crescente de indivíduos imunodeprimidos e os efeitos colaterais aos fármacos utilizados para o tratamento desta infecçäo, tem incentivado a pesquisa de novos agentes antifúngicos. Através da técnica de diluiçäo em ágar, foi verificada a atividade antifúngica (in vitro) de diferentes constituintes de Caryocar brasiliensis sobre Cryptococcus neoformans. Verificou-se que a cera epicuticular retirada da folha, coletada em período de baixo índice pluviométrico (170,8mm de água), foi a parte mais ativa da planta, inibindo o crescimento de 91,3 por cento (21/23) dos isolados de Cryptococcus neoformans em concentraçäo <= a 250æg/mL

[Antifungal activity of Caryocar brasiliensis (Caryocaraceae) against Cryptococcus neoformans]. / Atividade antifúngica de Caryocar brasiliensis (Caryocaraceae) sobre Cryptococcus neoformans.

The widespread occurrence of cryptococcosis mainly in immunocompromised patients and the side effects of available drugs which are effective against this mycosis have led investigators to search for new antimycotic agents. Caryocar brasiliensis derived compounds were investigated against Cryptococcus neoformans using the agar dilution method. Based on MIC values, the best results were obtained with a concentration of < 250 g/mL of cuticular waxes of the Caryocar brasiliensis leaf collected during the dry period (170.8mm of precipitation) which inhibited the growth of 91.3% (21/23) Cryptococcus neoformans isolates.