Effect of ethyl acetate extract from husk fiber water of Cocos nucifera in Leishmania braziliensis infected hamsters

The objective of this study was to evaluate the treatment with ethyl acetate extract (EAE) from husk fiber water of Cocos nucifera L., Arecaceae, in L. braziliensis (Lb) infected hamsters. Twelve male hamsters were randomly allocated in three groups (n=4): G1 received only EAE; G2 was infected with Lb only and G3 received EAE after Lb infection. The infection was carried 28 days prior to the treatment with EAE, which was administrated (0.2 mL, 300 mg.kg-1) for 21 consecutive days. Infection was evaluated through skin lesions and infected footpad edema. Haematological evaluation was done on -28th, 0 and 21st days. Imprint footpad and lymph node weight were evaluated on 21st day. Lb infection significantly inhibited the peripheral leukocytes blood. However, neutrophils and lymphocytes values did not have significant alterations. G3 presented eosinophilia in relation to G2. The treatment with EAE did not reduce edema of infected footpad neither weight of drainage lymph node. Infected footpad imprints revealed amastigotes forms and cellular infiltration. Animals from G3 presented skin lesions on 7th day, shown a reduction of these lesions in day 14. Therefore, the treatment with EAE did not alter the etiological agent elimination in these conditions. However, EAE presents a healing activity in this experimental model.

Anti-oxidative and anti-ulcerogenic activity of Ipomoea imperati

Ipomoea imperati (Vahl) Griseb., Convolvulaceae, is used in traditional medicine for the treatment of inflammation, swelling and wounds, as well as to treat pains and stomach problems. This work evaluates the anti-oxidative activity by ESR (Electron Spin Resonance spectroscopy) and the preventive and curative actions of I. imperati in gastric ulcer animal model. Ipomoea imperati (200 mg/kg, p.o.) prevented the formation of gastric lesions in 78 percent (p<0.05) when compared with the negative control tween 80. Lanzoprazole, prevented in 85 percent the gastric lesions formation induced by ethanol (p<0.05). Therefore, the oral administration of I. imperati one hour before the ulcerogenic agent prevented the ulcer formation, conserving the citoprotection characteristics of the gastric mucosa and assuring the integrity of gastric glands and gastric fossets. The healing activity of I. imperati (200 mg/kg, p.o.) evaluated in chronic ulcer experiments induced by the acetic acid, was 72 percent (p<0.05). The positive control, ranitidine, healed 78 percent of the gastric lesions (p<0.05). The histological analysis confirmed the recovery of the mucosal layer and the muscle mucosal layer harmed by the acetic acid. Experiments in vitro with DPPH (2.2-diphenyl-1-picrylhydrazyl) of anti-oxidative activity demonstrated that I. imperati presents an IC50 of 0.73±0.01 mg/mL.

Antinociceptive activity of Ipomoea imperati (Vahl) Griseb., Convolvulaceae / Atividade antinociceptiva de Ipomoea imperati (Vahl) Griseb., Convolvulaceae

Ipomoea imperati (Vahl) Griseb., Convolvulaceae, is used in folk medicine for the treatment of inflammation, swelling and wounds, as well as to treat pains after childbirth and for stomach problems. Administration of ethanol extract, lipid and aqueous fraction of I. imperati(300, 100 and 200 mg/kg) significantly inhibited the abdominal constriction in mice induced by acetic acid; increased the sleeping time evoked by pentobarbital sodium and showed a significant activity by inhibiting formalin-induced paw edema in mice. The same dose of I. imperatialso raised the pain of mice in the hot-plate test and increased the latency at all observation times. The pre-treatment of the animals with naloxone (5 mg/kg, i.p.) suggested the participation of the opioid system in the antinociceptive effect of Ipomoea imperati.

A espécie vegetal Ipomoea imperati (Vahl) Griseb., Convolvulaceae, é usada popularmente para tratar inflamação, inchaço e feridas, bem como para tratar dor após o parto e dor estomacal. A administração do extrato etanólico e das frações lipídica e aquosa de I. imperati(300, 100 e 200 mg/kg) inibiu significativamente as contrações abdominais em camundongo induzidas por ácido acético, aumentou o tempo de sono evocado por pentobarbital sódico e mostrou significativa atividade inibitória sobre o edema de pata de camundongo induzido por formalina. As mesmas doses de I. imperati(300, 100 e 200 mg/kg) também elevou a latência de todos os tempos observados no teste da placa quente. O pré-tratamento de animais com naloxona (5 mg/kg, i.p) sugere a participação do sistema opioide no efeito anti-nociceptivo de Ipomoea imperati.

Neurotoxins in the polar fraction of the seaweed Galaxaura marginata (Rhodophyta, Nemaliales) / Neurotoxinas na fração polar da alga marinha Galaxaura marginata (Rhodophyta, Nemaliales)

A atividade neurotóxica das substâncias polares extraídas da alga vermelha Galaxaura marginata foi estudada por meio de ensaios farmacológicos, utilizando-se algas coletadas no canal de São Sebastião (45º25' W; 26º49' S), litoral norte do estado de São Paulo, Brasil. Altas concentrações da fração polar (PF) e da PF filtrada em membrana de 1000 Da, injetadas intraperitonealmente em camundongos, foram letais. Induzindo os animais à ataxia, desorientação e severa atonia muscular prévias à morte. Sintomas similares foram descritos para camundongos e ratos testados com aminoácidos neuroexcitatórios (NEA), sugerindo que alguns dos componentes da PF atravessam a barreira Hematoencefálica, da mesma forma que os NEA. No entanto, a análise da PF no HPLC e no espectro de massa não mostraram a presença dos aminoácidos neuroexcitatórios conhecidos, ácido Caínico, acido Domóico e NMDA. Assim concluímos que G. marginata possui substâncias com atividade letal e neurotóxica, diferentes às antes, descritas.

Neurotoxic activity of polar substances extracted from the red seaweed Galaxaura marginata was investigated in pharmacological assays, using seaweed collected at São Sebastião channel (45º25' W; 26º49' S) in the northern coast of the State of São Paulo, Brazil. High concentration of the polar fraction (PF) and PF filtered through a membrane (1000 Da) intraperitoneally (IP) injected in mice were lethal, inducing ataxia, disorientation, and severe muscle atonia prior to death. The same symptoms preceding death were described in mice and rat tested with neuroexcitatory amino acids (NEA), suggesting that some PF components cross the blood-brain barrier, the same as NEA. However, the HPLC and mass spectrometric analysis did not show the presence of the known neuroexcitatory amino acids, kainic acid, domoic acid and NMDA. We conclude that G. marginata possess substances with neurotoxic and lethal activities.

Intracellular increase of glutamate in neuroblatoma cells induced by polar substances of Galaxaura marginata (Rhodophyta, Nemaliales) / Aumento do glutamato intracelular induzido por substâncias polares de Galaxaura marginata (Rhodophyta, Nemaliales) em células de neuroblastoma

Four substances purified by HPLC from red seaweed Galaxaura marginata (Ellis & Solander) Lamouroux showed neuroprotective and mitochondria regulatory properties in neuroblastoma NEURO-2A cells line. Under oxidative basal conditions, each substance is capable of modifying the glutamate, glutamine and alanine intracellular concentrations, without to alter the oxidative equilibrium of these cells. These substances, also, produced a biphasic activity in the mitochondrial metabolism, inhibiting, in lower concentrations and stimulating, in higher concentrations the mechanism of cellular 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction, that indicates the mitochondrial activity. These data suggest that the intracellular increase of glutamate can be related to the glutamate/glutamine cycle alterations induced by the blockade of intracellular glutamate transport. Moreover, we suggested that there are substances, exhibiting neuroprotective activity in neuroblastoma cells, protecting them from oxidative stress produced by the inhibition of the glutamate transporters.

Quatro substâncias purificadas da alga vermelha Galaxaura marginata (Ellis & Solander) Lamouroux, mediante HPLC, apresentaram propriedades neuroprotetoras e reguladoras da atividade mitocondrial quando testadas em células de neuroblastomas da cepa NEURO-2. Sob condições oxidativas basais, cada substância é capaz de modificar as concentrações intracelulares de glutamato, glutamina e alanina, sem alterar o equilíbrio oxidativo das células. Essas substâncias também produziram uma atividade bifásica no metabolismo mitocondrial, inibindo em baixas concentrações e estimulando em altas concentrações o mecanismo celular de redução do 3-(4,5-dimetiltiazol-2-il)-2,5-difeniltetrazol brometo (MTT), que indica atividade mitocondrial. Esses dados sugerem que o aumento do glutamato pode estar relacionado com a alteração do ciclo glutamato/glutamina induzido pelo bloqueio do transporte intracelular de glutamato. Além disso, nós sugerimos que essas substâncias exibem atividade neuroprotetora nas células de neuroblastoma, as protegendo do estresse oxidativo, produzido pela inibição dos transportadores de glutamato.

Topical antiedematous activity of the organic extract of Liagora farinosa algae (Rhodophyta, Nemaliales)

Liagora farinosa is a red alga found in tropical around the world. The topical antiedematous activity of its organic extract was studied by means of two experimental models: the in vivo mouse ear edema and the in vitro inhibition of bee venom-derived PLA2. The results showed that the polar and apolar fractions of L. farinosa extract were able to inhibir respectively 52.53 and 63.61 percent of the ear edema induced by croton oil. In vitro tests showed thath both fractions also inhibited the activity of PLA2, indicating that the possible machanism of action for the topical antiedematous activity is through the inactivation of this enzyme that releases arachidonic acid during the beginning of the infalmatory mediator cascade.