Rita De Pasquale

The isoflavones mixture from Trifolium pratense L. protects HCN 1-A neurons from oxidative stress.

Oxidative stress‐induced neuronal cell death has been implicated in different neurological disorders and neurodegenerative diseases such as Alzheimers disease and Parkinsons. Using the Alzheimers disease‐associated hydrogen peroxide (H2O2), we investigated the neuroprotective efficacy of a natural mixture of phytoestrogenic isoflavones (genistein, daidzein, biochanin A and formononetin) from Trifolium pratense L. (Red clover) against oxidative stress‐induced cell death in human cortical cell line HCN 1‐A maintained in culture. Neuronal viability was determined by MTT or trypan blue test and neuronal integrity by morphological analysis.

The phytoestrogenic isoflavones from Trifolium pratense L. (Red clover) protects human cortical neurons from glutamate toxicity

The endogenous steroid estrogen has been shown to affect neuronal growth, differentiation and survival. Genistein, daidzein and other isoflavones have been shown to mimic the pharmacological actions of the gonadal steroid estrogen with which they have structural similarities. Several studies have looked at the effect of isoflavones in the brain. In the present study, human cortical cell line HCN 1-A maintained in culture was used to test the neuroprotective efficacy of a natural mixture of phytoestrogenic isoflavones (genistein, daidzein, biochanin A and formononetin) from Red clover against glutamate toxicity. Neuronal viability was determined by MTT or trypan blue test and neuronal membrane damage was quantitatively measured by lactate dehydrogenase (LDH). The results obtained indicate that exposure of HCN 1-A cell cultures to glutamate resulted in concentration-dependent decreases in neuron viability. Concentration of glutamate ranging from 0.01 to 5 mM was toxic to these cultures. A 24-h pretreatment with 0.5, 1 and 2 microg/ml isoflavones enriched fraction (IEF) significantly increased cell survival and significantly decreased cellular lactate dehydrogenase release from differentiated cortical neurons, indicating that neurons treated with isoflavones were protected from the cell death induced by glutamate exposure. Moreover, the pretreatment with IEF prevented the morphological disruption caused by glutamate as shown by microscopical inspection. These findings indicate that IEF has a neuroprotective effect in human cortical neurons and that this effect might be resulted from his antioxidant and estrogenic actions.

Citrus bergamia Risso & Poiteau juice protects against renal injury of diet-induced hypercholesterolemia in rats.

The present study was designed to evaluate the protective effect of treatment with Citrus bergamia juice (1 mL/day, for 30 days) against hypercholesterolemic diet‐induced renal injury in rat.

3,3′-Di [1,3-thiazolidine-4-one] system. II. Anti-inflammatory and anti-histaminic properties in new substituted derivatives

Abstract In pursuing our search on anti-inflammatory dl and meso 3,3′-di[1,3-thiazolidine-4-one] compounds, two series of derivatives have been prepared by modifying the substitution pattern at positions 1 and 2 of the heterocyclic rings and by introducing an ethylene chain between nitrogen atoms. The anti-inflammatory activity of these compounds has been preliminarily assayed against carrageenin-induced rat paw edema: those proven to be active were also tested for analgesic, anti-pyretic and anti-histamine properties. As a whole, the obtained results suggest that some of the new derivatives possess significant anti-histamine activity. The meso forms generally are more active than dl ones in agreement with the previously emphasized SAR of the chiral systems under study.

Ageing influences haloperidol-induced changes in the permeability of the blood-brain barrier in the rat

Abstract— The effect of the dopaminergic antagonist haloperidol on the permeability of the blood‐brain barier (BBB) to [14C]α‐aminoisobutyric acid was studied in 10–12‐ and 28–30‐week old rats. Following the intraperitoneal injection of haloperidol (1 mg kg−1), an increase in the permeability of the BBB, with respect to younger animals, was observed within the occipital cortex, striatum, hippocampus and hypothalamus in the older rats. No correlation was found between haloperidol‐induced changes and age‐related differences in the permeability of the BBB. Such age‐associated increase in the vulnerability of the BBB when challenged with haloperidol might be related to a deterioration of the dopaminergic control of cerebrovascular permeability.

Effect of berberine and Berberis aetnensis C. Presl. alkaloid extract on glutamate-evoked tissue transglutaminase up-regulation in astroglial cell cultures

Berberis aetnensis C. Presl. is a bushy‐spiny shrub common on Mount Etna (Sicily, Italy), containing various alkaloids with several pharmacological properties. This study assessed the effect of berberine and of the alkaloid extract of B. aetnensis roots on the glutamate‐evoked tissue transglutaminase (TG2) up‐regulation in rat astrocyte primary cultures, used as an in vitro model of excitotoxicity. The findings show that the alkaloid extract of B. aetnensis roots consists mainly of berberine. Furthermore, berberine and the alkaloid extract of B. aetnensis roots were able to restore the oxidative status modified by glutamate and the levels of TG2 to control values. It was found that berberine or the alkaloid extract of B. aetnensis roots are able to ameliorate the excessive production of glutamate, protein misfolding and aggregation, mitochondrial fragmentation, and neurodegeneration. Thus, it is suggested that berberine and the alkaloid extract of B. aetnensis roots, may represent a natural therapeutic strategy in the neuropathological conditions associated with excitotoxicity. Copyright

Relaxing effects of Valeriana officinalis extracts on isolated human non‐pregnant uterine muscle

Objectives This study investigated the relaxing effects of Valeriana officinalis L. (Valerianaceae) on human uterine muscle. The major uses of this species in Europe are as a sedative and an anxiolytic; it is also used as a spasmolytic to treat gastrointestinal spasm.

Arecoline, but not haloperidol, induces changes in the permeability of the blood-brain barrier in the rat

Abstract— The aim of the present study was to investigate the existence of alterations of the blood‐brain barrier (BBB) permeability in rats injected with centrally acting drugs, by calculating a unidirectional blood‐to‐brain transfer constant (Ki) for the circulating tracer [14C]‐α‐aminoisobutyric acid. The intraperitoneal (i.p.) injection of the dopaminergic antagonist haloperidol (1 mg kg−1) did not modify the regional BBB permeability. When the cholinomimetic agent arecoline hydrobromide (6.25 mg kg−1) was injected i.p. into methylatropine‐pretreated rats, it induced a significant decrease of Kj values within the frontal cortex, parietal cortex, striatum and brain‐stem. Our findings emphasize two concepts: (1) centrally acting drugs, such as arecoline, can induce changes in the BBB permeability, through several mechanisms; (2) there is no predictable correlation of drug stimulation of specific brain neuronal pathways and changes in the permeability of the BBB.

Antioxidant and antimicrobial activities of branches extracts of five Juniperus species from Turkey

Context: Several Juniperus species (Cupressaceae) are utilized in folk medicine in the treatment of infections and skin diseases. Objective: This work was designed to evaluate the antioxidant and antimicrobial potential of methanol and water branches extracts of Juniperus species from Turkey: Juniperus communis L. var. communis (Jcc), Juniperus communis L. var. saxatilis Pall. (Jcs), Juniperus drupacea Labill. (Jd), Juniperus oxycedrus L. subsp. oxycedrus (Joo), Juniperus oxycedrus L. subsp. macrocarpa (Sibth. & Sm.) Ball. (Jom). Materials and methods: Total phenolics, total flavonoids and condensed tannins were spectrophotometrically determined. The antioxidant properties were examined using different in vitro systems. The toxicity was assayed by Artemia salina lethality test. The antimicrobial potential against bacteria and yeasts was evaluated using minimum inhibitory concentration and minimum bactericidal concentration (MIC/MBC) measurements. The effect on bacteria biofilms was tested by microtiter plate assay. Results: Both in the DPPH (1,1-diphenyl-2-picrylhydrazyl) and TBA (thiobarbituric acid) test Jom resulted the most active (IC50 = 0.034 ± 0.002 mg/mL and 0.287 ± 0.166 µg/mL). Joo exhibited the highest reducing power (1.78 ± 0.04 ASE/mL) and Fe2+ chelating activity (IC50 = 0.537 ± 0.006 mg/mL). A positive correlation between primary antioxidant activity and phenolic content was found. The extracts were potentially non-toxic against Artemia salina. They showed the best antimicrobial (MIC = 4.88-30.10 µg/mL) and anti-biofilm activity (60–84%) against S. aureus. Discussion and conclusion: The results give a scientific basis to the traditional utilization of these Juniperus species, also demonstrating their potential as sources of natural antioxidant and antimicrobial compounds.

Bronchodilatory effects of the aqueous extract of Gynostemma pentaphyllum and gypenosides III and VIII in anaesthetized guinea-pigs.

The bronchodilatory activity of the aqueous extract of Gynostemma pentaphyllum Makino leaves was investigated in anaesthetized guinea‐pigs and compared with two of its isolated gypenosides (III and VIII). The results showed that the intravenous administration of the decoction of G. pentaphyllum (2.5, 5 or 10 mg kg−1) decreased bronchial resistance in basal conditions and significantly (P<0.01) reduced (68% inhibition) the bronchoconstrictor action of histamine. Furthermore, the extract antagonized (80% inhibition) the bronchoconstrictor response induced by the antigen in sensitized guinea‐pigs. Gypenosides III (0.7 mg kg−1, i.v.) and VIII (0.3 mg kg−1, i.v.) caused a similar protective effect in both experimental models used; however, the duration and the intensity of the action was less than that of the extract containing corresponding quantities of gypenosides III and VIII. This study confirmed the validity of the traditional use of this plant in the treatment of asthma and other respiratory disorders.