Abstract Different degrees in the biological activities of Canavalia rosea had been previously reported . In this study, our group assessed the cardioprotective effects of the ethyl acetate fraction (EAcF) of the Canavalia rosea leaves. Firstly, it was confirmed, by in vitro approach, that the EAcF has high antioxidant properties due to the presence of important secondary metabolites, as flavonoids. In order to explore their potential protector against cardiovascular disorders, hearts were previously perfused with EAcF (300 μg.mL-1) and submitted to the global ischemia followed by reperfusion in Langendorff system. The present findings have demonstrated that EAcF restored the left ventricular developed pressure and decreased the arrhythmias severity index. Furthermore, EAcF significantly increased the glutathiones peroxidase activity with decreased malondialdehyde and creatine kinase levels. EAcF was effective upon neither the superoxide dismutase, glutationes reductase nor the catalase activities. In addition, the Western blot analysis revealed that ischemia-reperfusion injury significantly upregulates caspase 3 protein expression, while EAcF abolishes this effect. These results provide evidence that the EAcF reestablishes the cardiac contractility and prevents arrhythmias; it is suggested that EAcF could be used to reduce injury caused by cardiac reperfusion. However more clinical studies should be performed, before applying it in the clinic.

Abstract Pendimethalin herbicide is widely used and persists in the environment as a contaminant causing negative impacts, including for human health. Microorganisms have the capacity to remove many contaminants from the environment. Thus, the aim of this work was to evaluate the efficiency of soil bacterial species prospected by molecular modelling of cytochrome P450 in to degrade pendimethalin. Strains of Burkholderia sp. and Methylobacterium radiotolerans were cultivated in a mineral saline medium enriched with 281 mg/L pendimethalin (MSPEN) and another containing glucose 1.0 g/L as extra carbon source (MSPENGLI). Both strains were able to degrade pendimethalin under the two conditions experienced. Burkholderia sp. F7G4PR33-4 was more efficient in degrading 65% of the herbicide in MSPEN medium, with 49.3% in MSPENGLI; while Methylobacterium radiotolerans A6A1PR46-4 degraded 55.4% in MSPEN and 29.8% in MSPENGLI mediums. These findings contribute to the expansion of knowledge on the competence of isolates of these two bacterial genera in degrading herbicidal xenobiotics and biotechnological potential for pendimethalin degradation and bioremediation.

Abstract Leishmaniasis is a neglected disease caused by Leishmania. Chemotherapy remains the mainstay for leishmaniasis control; however, available drugs fail to provide a parasitological cure, and are associated with high toxicity. Natural products are promising leads for the development of novel chemotherapeutics against leishmaniasis. This work investigated the leishmanicidal properties of ethanolic extract of Croton blanchetianus (EECb) on Leishmania infantum and Leishmania amazonensis, and found that EECb, rich in terpenic compounds, was active against promastigote and amastigote forms of both Leishmania species. Leishmania infantum promastigotes and amastigotes presented IC50 values of 208.6 and 8.8 μg/mL, respectively, whereas Leishmania amazonensis promastigotes and amastigotes presented IC50 values of 73.6 and 3.1 μg/mL, respectively. Promastigotes exposed to EECb (100 µg/mL) had their body cellular volume reduced and altered to a round shape, and the flagellum was duplicated, suggesting that EECb may interfere with the process of cytokinesis, which could be the cause of the decline in the parasite multiplication rate. Regarding possible EECb targets, a marked depolarization of the mitochondrial membrane potential was observed. No cytotoxic effects of EECb were observed in murine macrophages at concentrations below 60 µg/mL, and the CC50 obtained was 83.8 µg/mL. Thus, the present results indicated that EECb had effective and selective effects against Leishmania infantum and Leishmania amazonensis, and that these effects appeared to be mediated by mitochondrial dysfunction.

Hyptis pectinata (L.) Poit., Lamiaceae, is an aromatic, abundant and broadly used plant species in Sergipe to treat oral and gastrointestinal pain and inflammation. The aim of the present study was to analyze the relation between periodontitis and changes in the corporal mass and alveolar bone structure after induction of experimental periodontal disease in rat treated or not treated with H. pectinata gel at 5% (GS5%) and 10% (GS10%), comparing their effects with doxycycline gel at 10% (D10%, positive control), vehicle gel (negative control) and a group with experimental periodontal disease, but non-treated. The gels were locally applied in the gingival region immediately after the experimental periodontal disease induction by ligature (3×/day, 11 days). Bone destruction was determined through clinical exam, histopathological analysis and cone beam computed tomography of the experimental animals (n = 36). After 11 days of periodontitis induction, all groups that received ligature presented a decrease in the corporal mass, except to the naïve group (without experimental periodontal disease) (p < 0.05). Computed tomography results have shown healthy bone structure in the group I and bone resorption for the test groups. Histopathological analysis confirmed the healthy bone structure for naïve group animals, while the test groups exhibited bone loss in several degrees. In particular, the non-treated group animals had an intense inflammatory process. When the periodontium of the animals treated with GS10% was histopathologically analyzed, insertion periodontium was preserved. The results for these groups were significantly different of the vehicle group (p < 0.05). According to the results, the gel based in the aqueous extract of H. pectinata at 10% can prevent bone loss in experimental periodontal disease similarly to doxycycline 10%.

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 LC50and 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 (LC50313 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 (LC90values 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.

Combretum duarteanum Cambess, Combretaceae, is a plant widely distributed in Northeastern Brazil and, in folk medicine, stems and leaves are used for pain treatment. We investigated the antinociceptive effects of the hexanic extract of leaves from C. duarteanum and of friedelin, its main compound, in formalin-, glutamate- and capsaicin- induced orofacial nociception models. In order to isolate friedelin from the hexanic extract, flash chromatography technique was used. Male mice (n = 8/group) were pretreated with hexanic extract, friedelin, morphine or vehicle, before the injection of algogen agents into the right upper lip (perinasal area). The test of formalin-induced orofacial nociception showed that hexanic extract and friedelin significantly reduced nociception (p < 0.001) in both phases of testing. In the glutamate and capsaicin-induced orofacial nociception tests, pre-treatment with hexanic extract produced a significant reduction of orofacial nociception (p < 0.001) at all doses tested.The results suggest the hexanic extract and friedelin possess antinociceptive effects in models of orofacial nociception in rodents.

Erythrina velutina Willd., Fabaceae, is a medicinal plant that can be found in the tropics and subtropics, including in the semi-arid northeastern Brazil. It is commonly used in folk medicine to treat anxiety, agitation and insomnia. E. velutina has been known to present analgesic, anti-inflammatory and antibacterial activities, however, it is unknown if this plant present a protective effect on DNA. We assessed the antigenotoxic effect of E. velutina against the genotoxic effects induced by MMS in the root meristem cells of Allium cepa. Three concentrations of the aqueous extract (100, 200 and 400 mg/L) of this medicinal plant were used in three different types of treatment (pre-, post- and simultaneous). The effects of the extracts on the root meristem cells of A. cepa were analyzed at both macroscopic and microscopic levels. Protective effects were observed at higher concentrations in pre-treatment and in simultaneous treatment. The results suggest that E. velutina may present antigenotoxic properties and demonstrate its chemopreventive potential.

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.

Medicinal plants are an important source of treatment for many ailments, although little is known of the potential genotoxic effects of most species. In the present study, two species from diverse and medicinally important genera - Maytenus rigida Mart., Celastraceae, and Aristolochia birostris Ducht, Aristolochiaceae - were analyzed to identify potentially significant secondary metabolites and the possible effects of their aqueous and alcoholic extracts on cell division in the onion root stem (genotoxicity test). The phytochemical testing revealed the presence of a number of potentially important secondary compounds in both species, including phenols, flavonoids, triterpenoids, steroids, and saponins. In the genotoxicity tests, no chromosomal abnormalities of any kind were observed in either species. In the case of M. rigida, a significant increase in mitotic activity was observed at the highest concentration. No significant tendency was recorded in A. birostris, although a considerable increase in the prophase was observed at all concentrations of the alcoholic extract. The triterpenoid content of both species may be especially important from a medicinal viewpoint, although recent findings on the carcinogenic potential of Aristolochia extracts demands caution in the interpretation of the results, and the need for further research.

Caesalpinia pyramidalis Tul., Fabaceae, is a plant with an anti-inflammatory activity that is used in folk medicine. To evaluate the mechanism of action of this plant, studies were performed on its antinociceptive and anti-inflammatory properties using an ethanol extract (EE) made from the inner bark. Oral treatment of mice with the EE (100, 200, and 400 mg/kg) decreased their acetic acid-induced abdominal writhes (p<0.001) and their formalin-induced paw licking in both the first and second phases (p<0.001). This treatment increased the reaction time of mice on the hot-plate test (400 mg/kg, p<0.05); however, it did not alter their performance on the Rotarod performance test. The carrageenan-induced paw edema in the rats and the leukocyte migration into the peritoneal cavity of the mice were also reduced by the EE given at a dose of 400 mg/kg (p<0.05). In addition, the EE (100-400 mg/kg, v.o.) did not alter the arterial pressure of non-anesthetized rats. In conclusion, the EE of C. pyramidalis shows antinociceptive and anti-inflammatory activities in rodents, supporting the usage of this plant to treat various inflammatory diseases for which it has traditionally been used.

The effects of the decoction of Erythrina velutina Willd., Fabaceae, were investigated using the root meristem cells of Allium cepa L., Amaryllidaceae. Ten concentrations of the aqueous extract (0.125 to 1.25%) of this medicinal plant were analyzed at both macroscopic and microscopic levels. All concentrations showed root growth inhibition after 96 h treatment. Although there were no significant differences between the mitotic indexes of any concentration and the control, there were changes in the frequencies of cell stages at three different concentrations. Additionally, the presence of five different cells abnormalities was recorded: chromosome bridging, lagging chromosomes, chromosome fragments, disturbed metaphase and disturbed anaphase. These results suggest inhibitory and genotoxic activity of the decoction of E. velutina on Allium cepa.

Várias espécies do gênero Hyptis são utilizadas na medicina popular para tratar processos inflamatórios. Para avaliar as ações anti-inflamatória e antioxidante da Hyptis fruticosa Salzm. ex Benth., Lamiaceae, utilizou-se extrato etanólico (EE) das folhas desta planta e suas partições n-C6H14, CHCl3, AcOEt e MeOH/H2O. O tratamento oral com o EE das folhas da H. fruticosa (100, 200 e 400 mg/kg) ou suas partições n-C6H14, AcOEt e MeOH/H2O (50, 100 e 200 mg/kg) apresentou atividade inibitória sobre a formação de edema e migração leucocitária para a cavidade peritoneal induzidas pela carragenina em ratos (p<0,05). Entretanto, a partição CHCl3 não causou nenhum efeito sobre a formação de edema e migração de células peritoneais. O EE bruto e a partição AcOEt apresentaram alto potencial antioxidante (IC50 = 35,00±1,01 e 36,67±2,65 µg/mL DPPH, respectivamente), similar ao composto referência (IC50 = 16,67±1,21 µg/mL). Em conclusão, demonstrou-se que a H. fruticosa apresenta atividades anti-inflamatória e antioxidante.

Various species of Hyptis are used in folk medicine as anti-inflammatory. In order to evaluate the actions of Hyptis fruticosa Salzm. ex Benth., Lamiaceae, studies were performed on anti-inflammatory and antioxidant activities. The ethanol extract (EE) of H. fruticosa leaves and its n-CH, CHCl, EtOAc, and MeOH/HO partitions were used in the following experiments. Oral treatment with the EE of H. fruticosa leaves (100, 200, and 400 mg/kg) or its n-C6H14, EtOAc, and MeOH/H2O partitions (50, 100, and 200 mg/kg) elicited inhibitory activity (p<0.05) on carrageenan-induced oedema formation and leukocyte migration into the peritoneal cavity in rats. However, the CHCl3 partition did not show any inhibitory effect on paw oedema and peritonitis experimental models. The EE and EtOAc partition present highest antioxidant potential (IC50 = 35.00±1.01 and 36.67±2.65 µg/mL DPPH, respectively), similar to the reference compound (IC50 = 16.67±1.21 µg/mL). In conclusion, H. fruticosa shows anti-inflammatory and antioxidant activities.

Maytenus rigida Mart (Celastraceae), conhecida por "Bom-homem", "Bom-nome", "Cabelo-de-negro", "Casca-grossa" e "Pau-de-colher", é uma arvore de pequeno porte. A entrecasca do caule é empregada popularmente no Nordeste do Brasil no tratamento das dores em geral, infecções e inflamações. O presente trabalho avaliou tanto o perfil fitoquímico de M. rigida por meio de um roteiro analítico, quanto à atividade antibiótica dos extratos pelo método de Kirby-Bauer modificado. Os resultados demonstraram que os extratos etanólico, aquoso, clorofórmico, acetato de etila e hidroalcoólico de M. rigida apresentam atividade antibacteriana contra Escherichia coli, Pseudomonas aeruginosa e Staphylococcus aureus, enquanto que a fração hexânica não exibe qualquer atividade. Catequinas, quinonas, esteróides, triterpenos, saponinas, flavonóides e compostos fenólicos foram detectados na análise fitoquímica.

Maynetus rigida Mart (Celastraceae), known as "Bom-homem", "Bom-nome", "Cabelo-de-negro", "Casca-grossa" and "Pau-de-colher", is a small tree. The stem bark is used by the population in the northeast of Brazil to treat aches, infections and inflammations in general. The present work evaluated both the phytochemistry of M. rigida Mart by an analytical routine, and the antimicrobial activity of the bark extracts by the Kirby-Bauer modified method. Our results showed the aqueous, methanol, chloroform, ethyl acetate and hydroalcoolic extracts of M. rigida Mart has antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus, while the hexane extract does not have any activity. Catechins, quinones, steroids, triterpenes, saponins, flavonoids and phenolic compounds were detected by the phytochemical analysis.

Egletes viscosa Less (Asteraceae), popularmente conhecida como "macela" ou "macela-da-terra", é uma planta largamente usada na medicina popular devido as suas propriedades: anti-inflamatória, bactericida, antidiarréica, mio-relaxante, anti-espasmódica, antinociceptiva, digestiva e anti-viral. Análise fitoquímica do extrato aquoso da Egletes viscosa (AEEV) mostrou elevada presença de flavonóides. Este estudo examinou o potencial antinociceptivo do AEEV em roedores usando diferentes concentrações (100, 200 and 400 mg/kg, p.o.). Os resultados mostraram significante efeito antinociceptivo quando testadas as doses (200 mg/kg-p<0.01; 400 mg/kg-p<0.05) e na segunda fase dos testes com formalina (200 and 400 mg/kg-p<0.001). Este efeito antinociceptivo foi similar ao ácido acetilsalicílico (300 mg/kg) nas doses de 200 e 400 mg/kg. Adicionalmente, estas observações sugerem que o AEEV é efetivo contra dores inflamatórias contínuas. AEEV foi bem tolerada. No teste de toxicidade aguda, utilizando uma administração oral de 5 g/kg de AEEV, não foi observado casos de mortalidade. Da mesma maneira, no estudo subcrônico nenhuma mortalidade foi observada após 30 dias de administração oral diária de 100 mg/kg do AEEV. Não houve diferença significativa entre os pesos corporal e dos órgãos isolados quando comparados grupo controle e teste tanto no estudo agudo quanto subcrônico. Ensaios histopatológicos não revelaram diferenças entre a aparência dos tecidos, assim como na estrutura celular dos órgãos dos animais do estudo agudo e subcrônico. No entanto, diferenças significativas foram verificadas entre os machos do grupo experimental e controle quanto à hemoglobina e leucócitos. Conclui-se que o extrato estudado não induziu nenhum risco na maioria dos parâmetros avaliados e, ainda, mostrou efeito antinociceptivo. No entanto, o aumento dos níveis de hemoglobina e leucócitos devem ser melhor investigados.

Egletes viscosa Less (Asteraceae), popularly known as "macela" or "macela-da-terra", is a plant widely used in popular medicine due to its anti-inflammatory, bactericidal, antidiarrhoea, mio-relaxant, antispasmodic, antinociceptive, digestive, and anti-viral properties. Phytochemical screening of aqueous extract of Egletes viscosa (AEEV) revealed the high presence of flavonoids. This study examined the oral antinociceptive potential of AEEV in rodents using different concentrations (100, 200, and 400 mg/kg, p.o.). The results showed significant antinociceptive action when tested in writhing (200 and 400 mg/kg-p<0.05) and in the second phase of formalin tests (200 mg/kg-p<0.01 and 400 mg/kg-p<0.001). The inhibition (%) of extract in the writhing test was 63.4, 56.7, and 79.2% respectively for 200, 400, and acetyl salicylic acid (300 mg/kg); for the formalin test (second phase) results were 66.1, 84.7, and 96.2% respectively for 200, 400, and acetyl salicylic acid (300 mg/kg). Collectively, these observations suggest that AEEV is effective against continuous inflammatory pain. AEEV was well tolerated. In an acute toxicity test, oral administration of 5 g/kg of AEEV was performed and no mortality rate was observed. Similarly, in a subchronic toxicity study, no mortality was observed after 30 days of daily oral administration of 100 mg/kg of AEEV. There was no significant difference in the body and organ weights between control and experimental animals in both acute and subchronic toxicity tests. Pathological assays did not reveal any evidence of detectable differences in the gross appearance, as well as in the architectural or cellular pattern characteristics of the internal organs of the animals in both acute and subchronic tests. Nevertheless, significant differences were verified between males of the experimental and control groups regarding the levels of hemoglobin and leukocytes. In conclusion, AEEV did not induce any hazardous effects on the majority of the parameters studied. Additionally, an antinociceptive activity of the extract was verified. However, the increase in the levels of hemoglobin and leukocytes should be investigated in more detail.

Neste trabalho foram estudados os efeitos do extrato aquoso (EA) obtido das folhas da Hyptis pectinata sobre o sistema nervoso central de roedores. Os seguintes modelos experimentais foram utilizados em camundongos, machos e fêmeas, da linhagem Wistar: "screening" farmacológico, campo aberto, nado forçado, hipotermia induzida por apomorfina, labirinto em cruz elevado e tempo de sono induzido por tiopental. O extrato foi administrado por via oral em dose única, 30 minutos antes de cada teste. No "screening" farmacológico o EA (400 mg/kg, p.o., n = 3) diminuiu a freqüência do comportamento de auto-limpeza. No teste do campo aberto o EA diminuiu o tempo gasto em auto-limpeza (AE400: 51,3 ± 8,8, q = 5,513, P < 0.01, n = 10) de maneira similar ao diazepam (control: 107,3 ± 14,2; diazepam: 15,4 ± 4,3, q = 9,049, P < 0.001, n = 10). No teste do nado forçado o EA (400 mg/kg) diminuiu o tempo de imobilidade (con: 181,3 ± 7,2 s; imip: 91,6 ± 8,9 s, q = 7,958, P < 0,001; AE400: 111,6 ± 14,5 s, q = 6,193, P < 0,001, n = 9) indicando um possível efeito antidepressivo. Isto foi confirmado no modelo de hipotermia induzida pela apomorfina onde o EA (200 mg/kg) antagonizou o efeito da apomorfina (AE200: -0,27 ºC, q = 5,588, P < 0,001, n = 10) de maneira similar à imipramina (5 mg/kg) (control: -1,08 ºC; imipramine: 0,02 ºC, q = 7,589, P < 0,001, n = 10). Nenhum efeito do EA foi observado nos testes do labirinto em cruz elevado e do tempo de sono induzido por tiopental. Nossos resultados sugerem um possível efeito antidepressivo do extrato aquoso obtido das folhas da Hyptis pectinata.

The effects of the aqueous extract (AE) from Hyptis pectinata leaves was studied on rodent central nervous system (CNS). Pharmacological screening, open field, forced swimming, apomorphine-induced hypothermia, elevated plus maze and thiopental-induced sleep tests were used in male and female Swiss mice and Wistar rats. The AE was admnistered orally in single doses 30 minutes before each test. In the screening test the AE (400 mg/kg, p.o., n =3) decreased the frequency of grooming behavior. In the open field test it decreased the amount of time rats spent grooming (AE400: 51.3 ± 8.8, q = 5.513, P < 0.01, n = 10), similarly to diazepam (control: 107.3 ± 14.2; diazepam: 15.4 ± 4.3, q = 9.049, P < 0.001, n = 10). In the forced swimming test the AE (400 mg/kg) decreased the immobility time (con: 181.3 ± 7.2 s; imip: 91.6 ± 8.9 s, q = 7.958, P < 0.001; AE400: 111.6 ± 14.5 s, q = 6.193, P < 0.001, n = 9), indicating a possible antidepressive effect. This was confirmed in the apomorphine-induced hypothermia model where the extract (200 mg/kg) antagonized the apomorphine effect (AE200: -0.27 ºC, q = 5.588, P < 0.001, n = 10), similarly to imipramine (imipramine: 5 mg/kg) (control: -1.08 ºC; imipramine: 0.02 ºC, q = 7.589, P < 0.001, n = 10). No effect of the AE was detected in the elevated plus maze and in the sleeping time induced by thiopental models. Our results suggest a possible antidepressive effect of the aqueous extract obtained from the leaves of Hyptis pectinata.