In an ongoing project to evaluate natural compounds isolated from plants from the Brazilian biodiversity as modulators of antibiotic resistance, kaempferol-3-O-beta-d-(6''-E-p-coumaroyl) glucopyranoside (tiliroside), isolated from Herissantia tiubae (Malvaceae) was investigated using the strain SA-1199B of Staphylococcus aureus, which overexpresses the norA gene encoding the NorA efflux protein which extrudes hydrophilic fluorquinolones and some biocides, such as benzalkonium chloride, cetrimide, acriflavine and ethidium bromide. The minimum inhibitory concentrations (MICs) of the antibiotics and biocides were determined by the microdilution assay in the absence and in the presence of sub-inhibitory concentration of tiliroside. Although tiliroside did not display relevant antibacterial activity (MIC = 256 microg/mL), it modulated the activity of antibiotics, i.e. in combination with antibiotics a reduction in the MIC was observed for norfloxacin (16-fold), ciprofloxacin (16-fold), lomefloxacin (four-fold) and ofloxacin (two-fold), and an impressive reduction in the MICs for the biocides (up to 128-fold). The results presented here represent the first report of a kaempferol glycoside as a putative efflux pump inhibitor in bacteria. The present finding indicates that H. tiubae (and broadly Malvaceae) could serve as a source of plant-derived natural products that modulate bacterial resistance, i.e. a source of potential adjuvants of antibiotics.

RESUMO:Mimosa paraibana Barneby foi submetida a um estudo fi toquímico para o isolamento de seus constituintes químicos, através de métodos cromatográfi cos usuais, e posterior identifi cação estrutural, utilizando-se métodos espectroscópicos de RMN 1 H e 13 C uni e bidimensionais, além de comparações com modelos da literatura. Deste estudo pioneiro, foram isolados e identifi cados cinco constituintes da fase clorofórmica: uma mistura dos esteróides, β-sitosterol e estigmasterol, a 151 -hidroxi-feofi tina A, a 5,7-dihidroxifl avanona, o 3,4,5-trihidroxibenzoato de etila e o ácido p-cumárico. A atividade antioxidante das fases hexânica, clorofórmica e acetato de etila foi avaliada utilizando o radical estável DPPH (1,1-difenil-2-picril-hidrazil) e os resultados comparados com o padrão ácido ascórbico. A avaliação da citotoxicidade das fases foi realizada empregando-se o ensaio de letalidade contra Artemia salina. Dos extratos avaliados, somente o hexânico mostrou baixa toxicidade Unitermos: Mimosa paraibana, Mimosaceae, Artemia salina, atividade antioxidante. ABSTRACT: "Chemical constituents, evaluation of the cytotoxic and antioxidant activities of Mimosa paraibana Barneby (Mimosaceae)". The phytochemical study of Mimosa paraibanaBarneby led to the isolation of its chemical constituents, through the usual chromatographic methods, and further structural identifi cation, using 1 H and 13 C NMR spectroscopic methods based on one and two-dimensional techniques, in addition to comparison with literature data. From this pioneering investigation with M. paraibana, fi ve constituents were isolated and identifi ed from the chloroform extract: a mixture of β-sitosterol and stigmasterol, 15 1 -hydroxy-phaeophytin A, 5,7-dihydroxyfl avanone, ethyl 3,4,5-trihydroxybenzoate and p-coumaric acid. The antioxidant activity of the hexane, chloroform and ethyl acetate extracts of M. paraibana were measured using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging assay and the results compared with standard ascorbic acid. The toxicity activity of the extracts were performed using the bioassay of Artemia salina.

RESUMO: "Propriedades anticonvulsivantes da fração dos alcalóides totais de Rauvolfi a ligustrina Roem. et Schult. em ratos machos". Rauvolfi a ligustrina Roem. et Schult. (Apocynaceae) é uma planta amplamente distribuída no Nordeste Brasileiro, rica em alcalóides indólicos, conhecida popularmente como "paratudo" e "arrebenta-boi". O presente estudo buscou avaliar a dose letal 50 % (DL 50 ) da fração de alcalóides totais (FAT) das partes aéreas da R. ligustrina e a sua possível atividade anticonvulsivantes em roedores. A FAT apresentou uma DL 50 , via intraperitoneal (i.p.), de 127,8 (112,5-145,2) mg/kg e foi efetiva, na dose de 20 mg/kg (i.p.), em proteger os animais das convulsões induzidas pelo pentilenotetrazol (PTZ) e picrotoxina (PIC) aumentando signifi cativamente (p < 0,05) a latência para o aparecimento das convulsões, sendo um indicativo de um efeito anticonvulsivante.Unitermos: Rauvolfi a ligustrina, anticonvulsivante, pentilenotetrazol, picrotoxina, eletrochoque auricular.ABSTRACT: Rauvolfi a ligustrina Roem et. Schult (Apocynaceae), commonly known as "paratudo" and "arrebenta-boi" is a small tree found in Brazilian Northeastern. Previous studies have demonstrated depressant and anticonvulsant properties of the ethanol extract of Rauvolfi a ligustrina. The aim of the present study was the determination of the lethal dose 50% (LD 50 ) and the effects of total alkaloid fraction (TAF) of the aerial parts of R. ligustrina in animal models of convulsion. It was found that the acute toxicity of TAF was 127.8 (112.5-145.2) mg/kg (i.p.) in mice. TAF (20 mg/kg, ip) signifi cantly increased (p < 0.05) the latencies of clonic seizures induced by pentylenetetrazol (PTZ) and picrotoxin (PIC). However, TAF did not protect the animals in maximal electroshock (MES) induced seizures. These results suggest that TAF of R. ligustrina possesses anticonvulsant properties.

We investigated the antinociceptive and nerve excitability effects of the N-salicyloyltryptamine (NST) NST-treated mice exhibited a significant decrease in the number of writhes when 100 and 200 mg/kg (i.p.) were administered (i.p.). This effect was not antagonized by naloxone (1.5 mg/kg, i.p.). NST inhibited the licking response of the injected paw when 100 and 200 mg/kg were administered (i.p.) to mice in the first and second phases of the formalin test. Because the antinociceptive effects could be associated with neuronal excitability inhibition, we performed the single sucrose gap technique and showed that NST (3.57 mM) significantly reduced (29.2%) amplitude of the compound action potential (CAP) suggesting a sodium channel effect induced by NST. Our results demonstrated an antinociceptive activity of the NST that could be, at least in part, associated to the reduction of the action potential amplitude. NST might represent an important tool for pain management.

ABSTRACT:The Aim of this study was to evaluated the effects of the ethanol extract of Rauvolfia ligustrina Willd. ex Roem. & Schult., Apocynaceae, roots (EER) in animal models of epilepsy. The EER increased the latency for convulsions significantly different from control (p<0,05) and in the PTZ induced convulsions test on 62,5 mg/kg (i.p.) decreased mortality. This effect was blocked by flumazenil administration, suggesting an involvement of GABAergic system in the anticonvulsant activity of EER. The EER had a moderate effect only against PIC-or STR-induced convulsions at doses 125 and 250 mg/kg. But in the MES test it did not demonstrate effect on this animal model. Therefore, the EER reduced the development of PTZ-induced kindling in both experimental groups. It also significantly (p<0.05) decreased the latency for convulsions and reduced its percentage. Our results suggest that EER owns anticonvulsant property.