Antispasmodic, cardioprotective and blood-pressure lowering properties of Gomphrena perennis L. and its mechanisms of action.

Background: Gomphrena perennis L. is a native plant of South America whose pharmacological properties have not been studied yet. Aim: To evaluate the cardiovascular and intestinal pharmacological effects of Gomphrena perennis L. leaves tincture (GphT) and the mechanisms involved. Experimental procedure: The chromatographic profile of GphT was done. Its ex vivo effects were evaluated by contractile concentration-response curves (CRCs) obtained from the agonist carbachol or calcium found in isolated rat small intestine, as well as in the relaxant CRCs. Cardiac effects were evaluated on isolated rat hearts exposed to ischemia/reperfusion (I/R). Experiments in vivo were performed to evaluate the diuretic activity in conscious rats and the hypotensive effect in anaesthetised rats. Results: Fifteen flavonoids were identified in GphT by HPLC-UV, including diosmin. GphT induced a non-competitive inhibition in both carbachol and calcium CRCs on rat small intestine. The first was not affected by indomethacin. Moreover, GphT, unlike diosmin, relaxed the contracture produced by a high-potassium solution in a dose-dependently way. Neither propranolol nor l-NAME changed it. GphT did not show diuretic activity but induced hypotension insensitive to l-NAME. While GphT perfusion of isolated hearts increased injury consequent to I/R, oral administration was cardioprotective and reversed by l-NAME. However, diosmin did not improve the post-ischemic recovery. Conclusions: This study supports the use of Gomphrena perennis L. tincture as an antispasmodic and hypotensive agent. Moreover, it has been demonstrated to be preventive of post-ischemic cardiac dysfunction. However, diosmin would not be responsible for these effects.

Lepidium meyenii (maca) and soy isoflavones reduce cardiac stunning of ischemia-reperfusion in rats by mitochondrial mechanisms.

BACKGROUND AND AIM: Phytoestrogens are traditionally used for cardiovascular risks but direct effects on the ischemic heart remain unclear. Plants with phytoestrogens are used for reducing menopausic symptoms and they could also be cardioprotectives. Here we investigated whether maca (Lepidium meyenii) contains isoflavones and prevents cardiac stunning, in comparison to soy isoflavones. EXPERIMENTAL PROCEDURE: Both products were orally and daily administered to rats during 1 week before exposing isolated hearts to ischemia/reperfusion (I/R). Young male (YM), female (YF) and aged female (AgF) rats treated with maca (MACA, 1 g/kg/day) or soy isoflavones (ISOF, 100 mg/kg/day) were compared to acute daidzein (DAZ, 5 mg/kg i.p.) and non-treated rat groups. Isolated ventricles were perfused inside a calorimeter to simultaneously measure contractile and calorimetrical signals before and during I/R. RESULTS AND CONCLUSIONS: Maca has genistein and daidzein. MACA and ISOF improved the post-ischemic contractile recovery (PICR) and muscle economy (P/Ht) in YM and YF hearts, but not in AgF hearts. DAZ improved PICR and P/Ht more in YM than in YF. The mKATP channels blockade reduced both PICR and P/Ht in DAZ-treated YM hearts, without affecting them in ISOF or MACA-treated YM hearts. In MACA treated YF hearts, the simultaneous blockade of NOS and mKATP channels, or the mNCX blockade reduced cardioprotection. Results show that subacute oral treatment with maca or with soy isoflavones was strongly preventive of cardiac ischemic dysfunction, more than the acute administration of a pure isoflavone (daidzein, genistein). Maca induced synergistic and complex mechanisms which prevented mitochondrial calcium overload.

Fucoidans from the phaeophyta Scytosiphon lomentaria: Chemical analysis and antiviral activity of the galactofucan component.

The brown seaweed Scytosiphon lomentaria produces moderate amounts of fucoidans. By cetrimide fractionation, typical heavily sulfated galactofucans are obtained, with no major signs of chemical heterogeneity, together with fractions with higher proportions of xylose, mannose and uronic acids. Anyway, fucose is the most important monosaccharide in most of the subfractions of the subsequent extracts. The fucan moieties appear to be mostly as 3-linked α-l-fucopyranosyl units, with several patterns of sulfate and branching. Galactose is mostly 6-linked, whereas mannose appears to be 2-linked, and xylose appears mostly as terminal stubs. Small amounts of 2-O-acetylated fucose units appear. A high and selective antiviral activity against HSV-1 and HSV-2 was determined for the galactofucan fractions whereas the uronofucoidans were inactive.

Especies de Ulva del Golfo San Jorge, Patagonia Argentina: variaciones bioquímicas estacionales - espaciales y su relación con la producción de metabolitos bioactivos / Ulva species from San Jorge Gulf, Patagonia argentina: seasonal and spatial biochemical variation and their relation with the production of bioactive metabolites

Objetivos: Investigar especies de Ulva del Golfo San Jorge, Patagonia Argentina, integrando aspectos bioquímicos, actividad biológica y variaciones estacionales/habitacionales que permitan determinar su potencial aplicación en Salud. Métodos: Las algas se colectaron estacionalmente en playas con y sin contaminación antrópica; se secaron, molieron y extrajeron con etanol. Los extractos se fraccionaron mediante solventes de distinta polaridad. Cada fracción fue caracterizada mediante reacciones químicas cualitativas y cromatografía. Las fracciones ricas en flavonoides se analizaron por HPLC-DAD y los lípidos, por TLC. La actividad biológica se ensayó mediante el test de citotoxicidad de Artemia salina, inhibición de la elongación radicular, inhibición de la xantino oxidasa, actividad antioxidante y antibacteriana. Resultados: Se identificaron Ulva rigida y Ulva lactuca. Ambas evidenciaron flavonoides, taninos, quinonas, lípidos, carbohidratos, esteroides. Los flavonoides resultaron mayoritarios en U. rigida (otoño e invierno) y en U. lactuca (primavera e invierno), destacándose kayaflavona. Se detectaron alcaloides en Ulva rigida (verano). Los lípidos fueron mayoritarios en verano; U. lactuca en invierno mostró monogalactosildiacilglicérido y en otoño, digalactosilacilglicérido y fosfatidilcolina. La actividad inhibitoria de la elongación radicular, que presume actividad antitumoral, fue importante y dosis dependiente, destacándose U. rigida de otoño y primavera (DE50= 480 y 520 µg/ml, respectivamente). Las demás bioactividades resultaron escasas o negativas. Conclusiones: Las variaciones metabólicas observadas muestran la importancia de considerar las condiciones espacio - temporales al planificar una colecta de ejemplares para su estudio y/o aplicación. Este primer análisis integral de especies de Ulva de la Patagonia Argentina, evidencia su potencialidad como antitumoral

Aim: To study species of Ulva from San Jorge Gulf, Patagonia Argentina, integrating biochemical aspects, biological activity and seasonal and spatial variations, to determine their potential application in health. Methods: Algae were collected seasonally on beaches with and without anthropogenic pollution, then dried and ground and the bioactive compounds extracted with ethanol. Extracts were fractionated using solvents with different polarity. Each fraction was characterized using qualitative chemical reactions and chromatography. Fractions rich in flavonoids were analyzed using HPLC-DAD, and lipids were analyzed using TLC. Biological activity was assayed by using the Artemia salina cytotoxicity test and the xanthine oxidase inhibition assay and by studying the inhibitory effect on root elongation, antioxidant activity and antibacterial activity. Results: Ulva rigida and Ulva lactuca were identified. Flavonoids, tannins, quinones, lipids, carbohydrates, and steroids were identified in both species. U. rigida showed a much greater amount of flavonoids in autumn and winter, whereas U. lactuca did so in spring and winter, especially kayaflavone. Alkaloids were detected in U. rigida (summer). Lipids were high in summer. U. lactuca showed monogalactosyldiacylglycerol in winter and digalactosylacylglyceride and phosphatidylcholine in autumn. The inhibitory effect on root elongation (assumed as antitumor activity) was significant and dose-dependent, U. rigida showed the highest values in autumn and spring (ED50 = 480 and 520 µg/ml, respectively). Other bioactivities were low or negative. Conclusions: Metabolic differences showed the importance of considering the seasonal-spatial conditions to plan collection of specimens for their study and/or application. This works is the first integral analysis of Ulva species from Patagonia Argentina and shows their potential to exert antitumor activity

Structural and biochemical characterization and evolutionary relationships of the fatty acid-binding protein 10 (Fabp10) of hake (Merluccius hubbsi).

A fatty acid-binding protein (FABP) from the liver of Argentine hake (Merluccius hubbsi) was isolated and characterized and its expression analyzed. The determination of its partial primary structures (72%) showed that it presents highest identity with Fabp10, commonly termed liver basic-type FABP. The evolutionary tree showed greater relationship between the Fabp10 of hake (Me Fabp10) and the Fabp10 and the Fabp10a of teleost fish. Me Fabp10 had low affinity for palmitic, oleic and palmitoleic acid and high affinity for bilirubin, lysophosphatidylcholine and lysophosphatidylethanolamine, all of them important in the metabolic functions of the liver. Me Fabp10 was able to bind only one cis-parinaric acid molecule and was found to be expressed only in the liver.

Antinociceptive and anti-inflammatory activities of an aqueous extract of Chiliotrichum diffusum

The flowers of the Chiliotrichum diffusum (G. Forst.) Kuntze, Asteraceae, have long been used in traditional medicine and rituals. In this study, the anti-inflammatory and antinociceptive activities of a decoction of the flowers were evaluated and a phytochemical analysis was performed by HPLC-DAD. In order to evaluate the antinociceptive activity, the acetic acid-induced abdominal writhing and hot plate tests were used. The anti-inflammatory activity was evaluated using carrageenaninduced rat paw oedema. The decoction induced a significant anti-inflammatory effect (inhibition of 56.0% at 3 h) and produced significant inhibition on nociception in the acetic acid test (ED50 35 mg/kg i.p.; ED50 709 mg/kg p.o.). In the hot plate test, the antinociceptive activity of the extract employed at 500 mg/kg i.p. was significantly suppressed by pretreatment with naloxone (5 mg/kg). HPLC analysis showed the presence of chlorogenic acid, caffeic acid, hyperoside, isoquercitrin, quercitrin, afzelin, quercetin, apigenin and kaempferol. The decoction of C. diffusum proved to have antinociceptive and anti-inflammatory effects that may be related to the presence of the flavones, flavonols and phenolic acids identified. The opiod system seems to be involved in the mechanism of antinociception of the extract.

Antiretroviral activity of fucoidans extracted from the brown seaweed Adenocystis utricularis.

Treatment of human immunodeficiency virus type 1 (HIV-1, causative agent of AIDS) infection represents a major challenge in antiviral therapeutics. Many difficulties are associated with the treatment, including toxicity, resistance and high costs. Taking this into account, research for novel compounds able to overcome these limitations is needed. Sulfated polysaccharides appear to be interesting, given their abundance as components of seaweeds. Herein, a series of fractions obtained from the brown seaweed Adenocystis utricularis was analysed for in vitro anti-HIV-1 activity. These fractions, which have anti-herpes simplex virus activity, were determined previously to belong to the family of fucoidans, sulfated polysaccharides obtained from the cell walls of brown seaweeds. Assays in human PBMC primary cell culture demonstrated that two of the five fractions analysed had potent anti-HIV-1 activity both against WT and drug-resistant HIV-1 strains. For active fractions, it was also shown that the inhibitory effect was not due to an inactivating effect on the viral particle (i.e. no virucidal activity was detected) but rather to a blockade of early events of viral replication. Given these encouraging results, these seaweed-derived fractions appear as good candidates for further studies on their potential for in vivo therapy and/or prophylaxis of HIV-1 infection.