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Cancer is a disease with the highest mortality and morbidity rate worldwide. First-line drugs induce several side effects that drastically reduce the quality of life of people with this disease. Finding molecules to prevent it or generate less aggressiveness or no side effects is significant to counteract this problem. Therefore, this work searched for bioactive compounds of marine macroalgae as an alternative treatment. An 80% ethanol extract of dried Caulerpa sertularioides (CSE) was analyzed by HPLS-MS to identify the chemical components. CSE was utilized through a comparative 2D versus 3D culture model. Cisplatin (Cis) was used as a standard drug. The effects on cell viability, apoptosis, cell cycle, and tumor invasion were evaluated. The IC50 of CSE for the 2D model was 80.28 µg/mL versus 530 µg/mL for the 3D model after 24 h of treatment exposure. These results confirmed that the 3D model is more resistant to treatments and complex than the 2D model. CSE generated a loss of mitochondrial membrane potential, induced apoptosis by extrinsic and intrinsic pathways, upregulated caspases-3 and -7, and significantly decreased tumor invasion of a 3D SKLU-1 lung adenocarcinoma cell line. CSE generates biochemical and morphological changes in the plasma membrane and causes cell cycle arrest at the S and G2/M phases. These findings conclude that C. sertularioides is a potential candidate for alternative treatment against lung cancer. This work reinforced the use of complex models for drug screening and suggested using CSE's primary component, caulerpin, to determine its effect and mechanism of action on SKLU-1 in the future. A multi-approach with molecular and histological analysis and combination with first-line drugs must be included.
Assuntos
Caulerpa , Neoplasias Pulmonares , Humanos , Caulerpa/química , Qualidade de Vida , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Pontos de Checagem do Ciclo Celular , Neoplasias Pulmonares/metabolismo , Apoptose , Ciclo Celular , Linhagem Celular Tumoral , Proliferação de CélulasRESUMO
Temporomandibular disorder is a clinical painful condition in the temporomandibular joint (TMJ) region. The purified sulfated polysaccharide from the green marine algae Caulerpa racemosa (Cr) has provided anti-inflammatory and antinociceptive activity. This study evaluated these effects on a TMJ hypernociception model. Wistar rats (180 - 250 g) were pre-treated (i.v.) with Cr at 0.01, 0.1, or 1 mg/kg or vehicle 30 min before formalin (1.5%/50 µL, i.art.), capsaicin (1.5%/20 µL, i.art.), or serotonin (225 µg/50 µL, i.art.) in the TMJ, and nociceptive behaviors were measured for 45 or 30 min upon inflammatory stimuli. Inflammatory parameters vascular permeability assay, TNF-α, and IL-1ß by ELISA, protein expression of adhesion molecules ICAM-1 and CD55 by Western blot were assessed. The involvement of heme oxygenase-1 (HO-1) and nitric oxide (NO) pathways were assessed by pharmacological inhibition. Cr (1 mg/kg) reduced nociceptive behavior, plasmatic extravasation, TNF-α, and IL-1ß levels, as well as ICAM-1 and CD55 expression in periarticular tissues. Cr antinociceptive effect was not prevented by aminoguanidine, but ZnPP-IX did reduce its antinociceptive effect. Therefore, Cr antinociceptive and anti-inflammatory effects in this experimental model of hypernociception depended on the HO-1 pathway integrity, as well as reducing peripheral inflammatory events, e.g., TNF-α and IL-1ß cytokines levels, ICAM-1 and CD55 expression.
Assuntos
Analgésicos/química , Analgésicos/farmacologia , Organismos Aquáticos/química , Clorófitas/química , Polissacarídeos/química , Polissacarídeos/farmacologia , Sulfatos/química , Animais , Artralgia/tratamento farmacológico , Artralgia/etiologia , Artralgia/metabolismo , Biomarcadores , Capsaicina/efeitos adversos , Citocinas/metabolismo , Heme Oxigenase-1/metabolismo , Mediadores da Inflamação/metabolismo , Masculino , Óxido Nítrico/metabolismo , Ratos , Articulação Temporomandibular/efeitos dos fármacos , Articulação Temporomandibular/fisiopatologiaRESUMO
Abstract In Peru, Caulerpa filiformis is a marine algae listed as an invasive species. For years, its distribution has been considered to be in the north coast (Isla Lobos de Afuera and Piura) until a recent report of its distribution in the central coast (Ancash, Lima, and Ica). The present investigation aims to determine the main groups of secondary metabolites, total phenol content, and antioxidant activity of the methanolic extract of C. filiformis from Sechura Bay (Piura) and Paracas Bay (Ica). The main chemical groups were determined through phytochemical screening, the content of phenols by the Folin-Ciocalteu method, and antioxidant activity by the ABTS method (2,2-azinobis-[3-ethylbenzothiazoline-6-sulfonic acid]) and 2,2′-diphenyl-1-picrylhydrazyl (DPPH). The phytochemical screening of the methanolic extract of C. filiformis from Sechura Bay and Paracas Bay revealed the presence of carbohydrates, polyphenols, tannins, flavonoids, lipids, alkaloids, steroids, and triterpenes for both extracts. The total phenol content of the extract of C. filiformis from Sechura Bay (39.31 ± 0.39 mg of AGE/g extract) was significantly higher (p < 0.05) than that from Paracas Bay (18.78 ± 0.31 mg of AGE/g extract). In the ABTS and DPPH assays, the antioxidant capacity of the Sechura C. filiformis extract (IC50 = 3.49 ± 0.01 and 2.18 ± 0.02 mg/mL) was significantly higher (p < 0.05) than that of the Paracas C. filiformis extract (IC50 = 6.41 ± 0.02 and 2.42 ± 0.04 mg /mL). These findings suggest that the methanolic extract of C. filiformis is a source of secondary metabolites with an antioxidant potential.
Resumen En Perú, Caulerpa filiformis es una macroalga catalogada como especie invasora. Durante años, su distribución fue considerada en la costa norte (Isla Lobos de Afuera y Piura) hasta un informe reciente de su distribución en la costa central (Ancash, Lima e Ica). El objetivo de esta investigación es determinar los principales grupos de metabolitos secundarios, contenido total de fenol y actividad antioxidante del extracto metanólico de C. filiformis de Bahía de Sechura (Piura) y Bahía de Paracas (Ica). Los principales grupos químicos se determinaron mediante análisis fitoquímico, el contenido de fenoles mediante el método Folin-Ciocalteu y la actividad antioxidante mediante el método ABTS (ácido 2,2-azinobis- [3-etilbenzotiazolina-6-sulfónico]) y 2, 2′-difenil-1-picrylhydrazyl (DPPH). El examen fitoquímico del extracto metanólico de C. filiformis de ambas bahías revelaron la presencia de carbohidratos, polifenoles, taninos, flavonoides, lípidos, alcaloides, esteroides y triterpenos. El contenido total de fenol del extracto de C. filiformis de Bahía de Sechura (39.31 ± 0.39 mg de extracto de AGE / g) fue significativamente mayor (p <0.05) que el de Bahía de Paracas (18.78 ± 0.31 mg de extracto de AGE / g). En los ensayos ABTS y DPPH, la capacidad antioxidante del extracto de Sechura (IC50 = 3.49 ± 0.01 y 2.18 ± 0.02 mg / mL) fue significativamente mayor (p <0.05) que la del extracto de Paracas C. filiformis (IC50 = 6.41 ± 0.02 y 2.42 ± 0.04 mg / mL). Estos hallazgos sugieren que el extracto metanólico de C. filiformis es una fuente de metabolitos secundarios con potencial antioxidante.
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Coral populations and structural coral reefs have undergone severe reductions and losses respectively over large parts of the Galápagos Islands during and following the 1982-83 El Niño event. Coral tissue loss amounted to 95% across the Archipelago. Also at that time, all coral reefs in the central and southern islands disappeared following severe degradation and eventual collapse due primarily to intense bioerosion and low recruitment. Six sites in the southern islands have demonstrated low to moderate coral community (scattered colonies, but no carbonate framework) recovery. The iconic pocilloporid reef at Devil's Crown (Floreana Island) experienced recovery to 2007, then severe mortality during a La Niña cooling event, and is again (as of 2017) undergoing rapid recovery. Notable recovery has occurred at the central (Marchena) and northern islands (Darwin and Wolf). Of the 17 structural reefs first observed in the mid-1970s, the single surviving reef (Wellington Reef) at Darwin Island remains in a positive growth mode. The remainder either degraded to a coral community or was lost. Retrospective analyses of the age structure of corals killed in 1983, and isotopic signatures of the skeletal growth record of massive corals suggest the occurrence of robust coral populations during at least a 500-year period before 1983. The greatest potential threats to the recovery and persistence of coral reefs include: ocean warming and acidification, bioerosion, coral diseases, human population growth (increasing numbers of residents and tourists), overfishing, invasive species, pollution, and habitat destruction. Such a diverse spectrum of disturbances, acting alone or in combination, are expected to continue to cause local and archipelago-wide mortality and degradation of the coral reef ecosystem.
Assuntos
Antozoários/fisiologia , Recifes de Corais , Animais , Carbonatos , Clima , Ecossistema , Equador , El Niño Oscilação Sul , Humanos , Oceano Pacífico , Estudos RetrospectivosRESUMO
A galactose-specific lectin from Bauhinia monandra leaves (BmoLL) has been purified through ammonium sulfate fractionation followed by guar gel affinity chromatography column. This study aimed to evaluate the potential anti-inflammatory and antinociceptive activity of pure BmoLL in mice. Anti-inflammatory activity was evaluated by 1% carrageenan-induced inflammation in mice treated with BmoLL. Acetic acid-induced abdominal writhing and hot plate methods evaluated antinociceptive activity. BmoLL significantly inhibited the carrageenan-induced paw edema by 47% (30 mg/kg) and 60.5% (60 mg/kg); acetylsalicylic acid (ASA, 100 mg/kg) showed inhibition of 70.5%, in comparison to controls. Leukocyte migration, an immune response to the inflammation process, was significantly reduced in presence of BmoLL; in mice treated with ASA the decrease in leukocyte migration was similar to 15 mg/kg of the lectin. BmoLL at doses of 15, 30 and 60 mg/kg significantly reduced the number of animal contortions by 43.1, 50.1 and 71.3%, respectively. BmoLL leukocyte migration was significantly reduced; in mice treated with ASA the decrease in leukocyte migration was similar to 15 mg/kg of the lectin. BmoLL at doses of 15, 30 and 60 mg/kg significantly reduced the number of animal contortions by 43.1, 50.1 and 71.3%, respectively. The lectin (30 and 60 mg/kg) showed a significant effect in the hot plate assay. BmoLL anti-inflammatory and antinociceptive effects were dose-dependent. The search for new and natural compounds, with minimal side effects, to control pain and inflammation, is constantly increasing. BmoLL has great potential as a natural anti-inflammatory product that can be explored for pharmacological purposes.
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Abstract Inflammatory bowel diseases, which include Crohn's disease and ulcerative colitis, are characterized by chronic and relapsed gut inflammation. Caulerpa mexicana is a type of green marine algae that can be found in tropical areas, such as the Brazilian Coastland. These macrophytes exhibit in vitro and in vivo anti-inflammatory properties such as the ability to reduce both cell migration to different sites and edema formation induced by chemical irritants. The aim of this study was to examine the effect of the C. mexicana methanolic extract on the treatment of colitis induced by dextran sodium sulfate. Acute experimental colitis was induced in BALB/c mice by treatment with 3% dextran sodium sulfate orally for 14 days. During this 14-day period, C. mexicana methanolic extract (2 mg/kg/day) was given intravenously on alternate days. Treatment with the methanolic extract significantly attenuated body weight loss and severe clinical symptoms. This was associated with a remarkable amelioration of colonic architecture disruption and a significant reduction in pro-inflammatory cytokine production. These results suggest that the anti-inflammatory action of C. mexicana methanolic extract on colorectal sites may be a useful therapeutic approach for inflammatory bowel diseases.
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The subaquatic vegetation of Los Petenes, Campeche, Mexico, stands out due to its considerable floristic diversity, composed of a great variety of sea grasses and several species of the genus Caulerpa sp. This is a genus of ecological relevance, with the invasive species in the Mediterranean, with negative impact on several native sub-aquatic plants; nevertheless, little is known about the demography and population dynamics of Caulerpa species and their contribution to food webs. Thus the main objective of this study was to describe the demographics of Caulerpa paspaloides var. wudermanni, using the number of stolons, complete and incomplete fronds, the diameter of the stolons and the biomass. The information was used to determine the growth rate (λ) of this species. The study was conducted in the Biosphere Reserve of Los Petenes, which is located in the Northwest of the state of Campeche. The submerged aquatic vegetation (SAV) in the Petenes Biosphere consists of monospecific and mixed populations of seagrass species (Thalassia testudinum, Halodule wrightii and Syringodium filiforme). Although chlorophytes, brown algae and red algae, are fundamental elements in the specific composition of the SAV in Petenes, several species of Caulerpa are prominent because of their coverage and abundance. In May and June of 2010, significant differences in the quantity of stolons, their diameter, incomplete and complete fronds, and the size of the stolons and rhizomes, were observed. In 2010, the finite population growth rate (λ) was 2.38±0.1571 for individuals and 1.20±0.1356 for the population, and in 2011 the values of λ were 1.80±0.3608 and 1.35±0.1571, respectively. From these results it can be concluded that the population is growing; however, growth is controlled by biotic and abiotic factors. Despite there was no apparent threat, we suggest continuing the demographic studies of C. paspaloides var. wurdemannii, as well as of other species of the same genus, not only to detect invasion or explosive growth, but also their presence indicated low oxygen levels and high sulphates. Rev. Biol. Trop. 62 (2): 729-741. Epub 2014 June 01.
La vegetación subacuática de Los Petenes, Campeche, México, se destaca por su gran diversidad florística, compuesto por una gran variedad de pastos marinos y varias especies del género Caulerpa sp. Caulerpa es un género de relevancia ecológica, con especies como la Caulerpa taxifolia, que es invasiva en el Mediterráneo, con un impacto negativo en varias plantas sub-acuáticas nativas, pero poco se sabe acerca de la demografía y la dinámica poblacional de las especies de Caulerpa y su contribución a las redes alimenticias. El objetivo general es conocer la demografía de Caulerpa sp., por medio del número de estolones, frondas completas e incompletas, el diámetro de los estolones y la biomasa. El estudio se realizó en la Reserva de la Biosfera de Los Petenes, en Campeche, México. La Vegetación Acuática Sumergida (VAS) en la Biosfera de los Petenes está constituida por poblaciones tanto monoespecíficas como mixtas de las especies de pastos marinos Thalassia testudinum, Halodule wrightii y Syringodium filiforme. Aunque las especies de algas clorófitas, feofitas y rodófitas son elementos fundamentales de la VAS, destacan por su cobertura y abundancia las especies de Caulerpa. En mayo y junio del 2010, hubo diferencias significativas de la cantidad de estolones, su diámetro, frondas completas e incompletas y el tamaño de los estolones como el de los ejes erectos. En el 2010 el valor de la tasa finita de crecimiento poblacional (l) fue de 2.38±0.15 con el método de las marcas y con el de la biomasa 1.20±0.13 y en el 2011 los valores fueron de 1.80±0.36 con las marcas y de 1.35±0.15 con la biomasa. Los resultados indican que la población está creciendo, pero es controlada por factores bióticos y abióticos. A pesar de que no se detecta la especie como una amenaza aparente, sugerimos que se continúen estos estudios demográficos sobre C. paspaloides var. wurdemannii e incluso de otras especies del mismo género. No solo para detectar una invasión o un crecimiento explosivo, sino porque la presencia de estas especies no indican condiciones bajas en oxígeno y altas en sulfatos.
Assuntos
Biodiversidade , Caulerpa/classificação , Espécies Introduzidas , México , Estações do AnoRESUMO
Bovine viral diarrhea virus (BVDV) is an etiologic agent that causes important economic losses in the world. It is endemic in cattle herds in most parts of the world. The purpose of this study was to evaluate the in vitro cytotoxic effect and antiviral properties of several marine natural products obtained from seaweeds: the indole alkaloid caulerpin (CAV, 1) and three diterpenes: 6-hydroxydichotoma-3,14-diene-1,17-dial (DA, 2), 10,18-diacetoxy-8-hydroxy-2,6-dolabelladiene (DB1, 3) and 8,10,18-trihydroxy-2,6-dolabelladiene (DB3, 4). The screening to evaluate the cytotoxicity of compounds did not show toxic effects to MDBK cells. The antiviral activity of the compounds was measured by the inhibition of the cytopathic effect on infected cells by plaque assay (PA) and EC50 values were calculated for CAV (EC=2,0± 5.8), DA (EC 2,8± 7.7), DB1 (EC 2,0±9.7), and DB3 (EC 2,3±7.4). Acyclovir (EC50 322± 5.9) was used in all experiments as the control standard. Although the results of the antiviral activity suggest that all compounds are promising as antiviral agents against BVDV, the Selectivity Index suggests that DB1 is the safest of the compounds tested.
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About 80% of the human adult population is infected with HSV-1. Although there are many anti-HSV-1 drugs available (acyclovir, ganciclovir, valaciclovir, foscarnet), their continuous use promotes the selection of resistant strains, mainly in ACV patients. In addition to resistance, the drugs also have toxicity, particularly when administration is prolonged. The study of new molecules isolated from green algae with potential antiviral activity represents a good opportunity for the development of antiviral drugs. Caulerpin, the major product from the marine algae Caulerpa Lamouroux (Caulerpales), is known for its biological activities such as antioxidant, antifungal, acetylcholinesterase inhibitor (AChE) and antibacterial activity. In this work, we show that caulerpin could be an alternative to acyclovir as an anti-HSV-1 drug that inhibits the alpha and beta phases of the replication cycle.
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Caulerpa sertularioides has been spreading in Bahía Culebra, a seasonal upwelling bay in the north Pacific of Costa Rica, since 2001. The survey was carried out from December 2003 to March 2005, in several locations around Bahía Culebra, located inside the Gulf of Papagayo. This study investigated spatial and temporal patterns, percent coverage, monthly growth rate, reproductive adaptations, and morphological variations of frond length and stolon diameter of Caulerpa sertularioides, at different environmental physical and chemical factors at the bay. The alga extended to depths of 23 m on a variety of substrates. The stolons extended quickly, with a maximum growth rate of 31.2 cm month-1. This alga grows mainly by fragmentation of its fronds and stolons; nevertheless it can also reproduce sexually by releasing gametes in the water column. These two modes of spreading promote the adaptation of this opportunistic species to environmental, chemical, and physical changes at this bay. At the same time the alga showed variations in the length of its fronds and stolons, adapting to conditions such as depth and season. Average percent cover and frond density increased during the dry season when the upwelling of nutrients and cold water occurs. In the rainy season the average percent cover and frond density decreased; however there was a peak in September, when high precipitation resulted in runoff into the bay of nutrient-rich waters. The morphological and physiological plasticity of C. sertularioides, in synergy with its predominant clonal propagation and sexual reproduction provided this species with a great adaptability to changes in temperature and nutrient concentration at Bahía Culebra.
Desde el 2001 se ha observado una propagación del alga verde Caulerpa sertularioides en Bahía Culebra, zona de afloramiento costero, en el Pacífico norte de Costa Rica. El muestreo se llevó acabo entre Diciembre 2003 a marzo 2005, en varias localidades de Bahía Culebra. En este estudio se presentan los patrones de distribución, cobertura, tasa mensual de crecimiento, adaptaciones reproductivas y variaciones morfológicas del largo de la fronda y diámetro del estolón de Caulerpa sertularioides, a diferentes factores ambientales físico-químicos en Bahía Culebra. Esta alga se extiende hasta profundidades de 23 m, en una gran variedad de sustratos. Los estolones se extienden rápidamente, con un crecimiento máximo de 31.2 cm mes-1. Esta alga se propaga principalmente por la fragmentación de sus frondas y estolones, así mismo se reproduce sexualmente liberando gametos a la columna de agua. Estos modos de reproducción promueven la adaptación de esta especie oportunista, a los cambios ambientales, tanto químicos, como físicos, de la bahía. Al mismo tiempo esta alga presenta variaciones en el largo de sus frondas y el diámetro del rizoma, adaptándose a diferentes profundidades y condiciones de la época del año. El porcentaje de cobertura y densidad de frondas aumentan durante la época seca, cuando emergen aguas frías y nutrientes por el afloramiento costero. Por otro lado, en la época lluviosa estas medidas decrecen, sin embargo se presenta un pico en setiembre, cuando la precipitación aumenta y llega una carga extra de nutrientes a la bahía por escorrentía. La plasticidad morfológica y fisiológica de C. sertularioides, en sinergia con su propagación clonal, proveen a esta alga con una gran adaptabilidad a los cambios en temperatura y nutrientes de Bahía Culebra.
Assuntos
Alga Marinha/classificação , Flora Aquática , Bryopsida/crescimento & desenvolvimento , Caulerpa/crescimento & desenvolvimento , Mudança Climática , Costa RicaRESUMO
The attachment of the psammophytic alga Caulerpa mexicana Sond. ex Kütz., a coenocytic green alga, to crushed CaCO3 particles was examined utilizing the scanning electron microscope and fluorescently tagged antivitronectin antibodies. Plants attached to the substrate through morphologically variable tubular rhizoidal extensions that grew from the stolon. In this study, we describe two means of attachment: (i) the rhizoid attachment to limestone gravel by thigmoconstriction, where tubular extensions of the rhizoid wrapped tightly around the substrate and changed morphology to fit tightly into crevices in the limestone, and (ii) through adhesion pads that formed in contact with the limestone granules. Flattened rhizoidal pads were observed to secrete a fibrillar material that contained vitronectin-like proteins identified through immunolocialization and that facilitated binding of the rhizoid to the substrate.
RESUMO
The regulation of the inflammatory response is essential to maintaining homeostasis. Several studies have investigated new drugs that may contribute to avoiding or minimizing excessive inflammatory process. The aim of this study was to evaluate the effect of extracts of green algae Caulerpa mexicana on models inflammation. In mice, the inflammatory peritonitis model is induced by zymosan. Previous treatment of mice with aqueous and methanolic extracts of C. mexicana was able to suppress the cell migration to the peritoneal cavity, in a time-dependent but not in a dose-dependent manner. The treatment of mice with C. mexicana extracts also decreased the xylene-induced ear edema, exerting strong inhibitory leukocyte migration elicited by zymosan into the air pouch. We concluded that administration of the extracts resulted in a reduction of cell migration to different sites as well as a decrease in edema formation induced by chemical irritants. This study demonstrates for the first time the anti-inflammatory effect of aqueous and methanolic extracts from the green marine algae Caulerpa mexicana.
Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Caulerpa/química , Movimento Celular/efeitos dos fármacos , Edema/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Células Cultivadas , Clorófitas/química , Citocinas/metabolismo , Orelha , Edema/induzido quimicamente , Macrófagos/efeitos dos fármacos , Masculino , Metanol/química , Camundongos , Camundongos Endogâmicos BALB C , Peritonite/induzido quimicamente , Peritonite/tratamento farmacológico , Fitoterapia/métodos , Extratos Vegetais/isolamento & purificação , Água/química , Xilenos/efeitos adversos , Zimosan/efeitos adversosRESUMO
Marine natural products have been the focus of discovery for new products of chemical and pharmacological interest. The aim of this study was to evaluate the antinociceptive activity of the methanolic (ME), acetate (AE), hexanic (HE) and chloroform (CE) extracts obtained from Caulerpa mexicana, and ME, CE and HE obtained from Caulerpa sertularioides. These marine algae are found all over the world, mainly in tropical regions. Models such as the writhing test, the hot plate test and formalin-induced nociception test were used to evaluate antinociceptive activity in laboratory mice. In the writhing test, all the extracts were administered orally at a concentration of 100 mg/kg, and induced high peripheral antinociceptive activity, with a reduction in the nociception induced by acetic acid above 65%. In the hot plate test, treatment with extracts from C. sertularioides (100 mg/kg, p.o.) did not significantly increase the latency of response, although the ME, AE and HE from C. mexicana showed activity in this model. This result suggests that these extracts exhibit antinociceptive activity. In the formalin test, it was observed that ME, AE and HE obtained from C. mexicana reduced the effects of formalin in both phases. On the other hand only CE from C. sertularioides induced significant inhibition of the nociceptive response in the first phase. To better assess the potential anti-inflammatory activity of the extracts, the carrageenan-induced peritonitis test was used to test Caulerpa spp. extracts on cell migration into the peritoneal cavity. In this assay, all extracts evaluated were able to significantly inhibit leukocyte migration into the peritoneal cavity in comparison with carrageenan. These data demonstrate that extracts from Caulerpa species elicit pronounced antinociceptive and anti-inflamatory activity against several nociception models. However, pharmacological and chemical studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive action and also to identify the active principles present in the Caulerpa species.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Caulerpa/química , Extratos Vegetais/farmacologia , Administração Oral , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Modelos Animais de Doenças , Feminino , Inflamação/tratamento farmacológico , Inflamação/fisiopatologia , Masculino , Camundongos , Dor/tratamento farmacológico , Dor/fisiopatologia , Solventes/químicaRESUMO
In this study, we attempted to identify the possible antinociceptive actions of n-butanolic phase, chloroformic phase, ethyl acetate phase and crude methanolic extract obtained from Caulerpa racemosa. This seaweed is cosmopolitan in world, mainly in tropical regions. The n-butanolic, chloroformic, ethyl acetate phases and crude methanolic extract, all administered orally in the concentration of 100 mg/kg, reduced the nociception produced by acetic acid by 47.39 percent, 70.51 percent, 76.11 percent and 72.24 percent, respectively. In the hotplate test the chloroformic and ethyl acetate phase were activite in this models. In the neurogenic phase on formalin test, were observed that crude methanolic extract (51.77 percent), n-butanolic phase (35.12 percent), chloroformic phase (32.70 percent) and indomethacin (32.06 percent) were effective in inhibit the nociceptive response. In the inflammatory phase, only the ethyl acetate phase (75.43 percent) and indomethacin (47.83 percent) inhibited significantly the nociceptive response. Based on these data, we can infer that the ethyl acetate phase shows a significant anti-inflammatory profile, whose power has not yet been determined. However, pharmacological and chemical studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive action and also to identify other active principles present in Caulerpa racemosa.
Neste estudo, tentamos identificar a atividade antinociceptiva do extrato metanólico bruto e das fases n-butanólica, clorofórmica e acetato de etila provenientes da alga Caulerpa racemosa. Esta alga é cosmopolita no mundo, principalmente em regiões tropicais. O extrato metanólico bruto e as fases n-butanólica, clorofórmica e acetato de etila foram administrados por via oral, na concentração de 100 mg/kg. Estes foram capazes de reduzir a nocicepção produzida pelo ácido acético, sendo 47,39 por cento, 70,51 por cento, 76,11 por cento e 72,24 por cento, respectivamente. No ensaio da placa quente as fases clorofórmica e acetato de etila foram ativas neste modelo. Na fase neurogênica do teste de formalina, foi observado que o extrato metanólico bruto (51,77 por cento), fase n-butanólica (35,12 por cento), fase clorofórmica (32,70 por cento) e indometacina (32,06 por cento) foram eficazes em inibir a resposta nociceptiva. Na fase inflamatória, apenas a fase acetato de etila (75,43 por cento) e indometacina (47,83 por cento) foram capazes de inibir significativamente a resposta nociceptiva. Com base nestes dados, podemos sugerir que o a fase acetato de etila apresenta um significativo efeito anti-inflamatório, cuja potência ainda não foi determinada. No entanto, estudos farmacológicos e químicos serão necessários, a fim de caracterizar o mecanismo responsável pela ação antinociceptiva e também para identificar outros princípios ativos presentes na alga Caulerpa racemosa.
RESUMO
The antinociceptive and anti-inflammatory activity of caulerpin was investigated. This bisindole alkaloid was isolated from the lipoid extract of Caulerpa racemosa and its structure was identified by spectroscopic methods, including IR and NMR techniques. The pharmacological assays used were the writhing and the hot plate tests, the formalin-induced pain, the capsaicin-induced ear edema and the carrageenan-induced peritonitis. Caulerpin was given orally at a concentration of 100 micromol/kg. In the abdominal constriction test caulerpin showed reduction in the acetic acid-induced nociception at 0.0945 micromol (0.0103-1.0984) and for dypirone it was 0.0426 micromol (0.0092-0.1972). In the hot plate test in vivo the inhibition of nociception by caulerpin (100 micromol/kg, p.o.) was also favorable. This result suggests that this compound exhibits a central activity, without changing the motor activity (seen in the rotarod test). Caulerpin (100 micromol/kg, p.o.) reduced the formalin effects in both phases by 35.4% and 45.6%, respectively. The possible anti-inflammatory activity observed in the second phase in the formalin test of caulerpin (100 micromol/kg, p.o.) was confirmed on the capsaicin-induced ear edema model, where an inhibition of 55.8% was presented. Indeed, it was also observed in the carrageenan-induced peritonitis that caulerpin (100 micromol/kg, p.o.) exhibited anti-inflammatory activity, reducing significantly the number of recruit cells by 48.3%. Pharmacological studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive and anti-inflammatory actions and also to identify other active principles present in Caulerpa racemosa.