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Abstract: Plants of the genus Hibiscus thrives produce a diversity of molecules with bioactive properties. In a previous study of Hibiscus tiliaceus L. methanolic extract (HME) using bacteria and yeast, as test media, it has been shown that HME strongly inhibited the mutagenic action of H2O2 or tert-butyl-hydroperoxide (t-BHP). Here, our interest is to evaluate the genotoxicity and the antigenotoxic/antimutagenic properties of HME using oxidative challenge with H2O2 and t-BHP in V79 cells. We determined cytotoxicity using clonal survival assay; evaluated DNA damage using the comet assay and the micronucleus test in binucleated cells besides of the lipid peroxidation degree and the reduced glutathione content. We examined the ability of HME in quenching hydroxyl radical by means of a HPLC-based method utilizing the hypoxanthine/xanthine oxidase assay. At concentrations ranging from 0.001 to 0.1mg/mL, HME was not cytotoxic, genotoxic or mutagenic. Treatment with non-cytotoxic concentrations of HME increased cell survival after H2O2 and t-BHP exposure and prevented DNA damage. The pre-treatment with HME also was able to decrease the mutagenic effect of these genotoxins, evaluated using the micronucleus test. HME prevented the increase in lipid peroxidation and decrease in GSH content in response to the oxidative challenge. Therefore, the ability in preventing against H2O2- and t-BHP-induced GSH depletion and lipid peroxidation was probably a major contribution to the cytoprotective effects. Moreover, HME acts as a hydroxyl radical scavenger. In summary, HME did not have a harmful or inhibitory effect on the growth of V79 cells and presented antioxidant activity, consequently, both antigenotoxic and antimutagenic effects against oxidative DNA damage. [Copyright &y& Elsevier]

Abstract: Selenium compounds display neuroprotective activities mediated at least in part by their antioxidant actions. Oxidative damage has been implicated in psychiatric disorders including schizophrenia and bipolar disorder, and an alteration in expression of selenium-binding protein-1 (SELENBP-1) has been recently reported in both the blood and brain of schizophrenic patients. In the present study we examined the effects of the organic selenium compound 3′3-ditrifluoromethyldiphenyl diselenide [(F3CPhSe)2] on apomorphine-induced stereotypy in mice, an animal model of psychosis. Systemic administration of (F3CPhSe)2 at the highest dose used (25.0μmol/kg in a 10.0ml/kg injection volume) significantly reduced apomorphine-induced stereotyped behaviors. A series of control experiments showed that the same dose of (F3CPhSe)2 did not affect open-field behavior, habituation, or aversively motivated memory. The results indicate that organic selenium compounds should be further investigated as agents with possible antipsychotic properties. [Copyright &y& Elsevier]

Abstract: Organoselenium compounds have a potential thiol peroxidase-like activity. Diphenyl diselenide (DPDS) is an electrophilic reagent used in the synthesis of a variety of pharmacologically active organic selenium compounds. Using TRAP assay of chemiluminescense we have shown that diphenyl diselenide clearly possesses a pro-oxidant property. For an investigation on the mechanisms of this property, we used mutant strains of Saccharomyces cerevisiae defective in antioxidant defenses, i.e. in superoxide dismutase, in biosynthesis of glutathione, and the transcription factor yAP-1-lacking yap1 mutant that cannot activate genes of the oxidative stress response. Exposure of growing cultures to the drug increased cell sensitivity to oxidizing agents. The pro-oxidant effect was independent of the metabolic condition or of the oxidative mutagen tested. N-acetylcysteine, a precursor of glutathione biosynthesis, could neutralize the pro-oxidant effects of diphenyl diselenide by stimulating an increase of endogenous glutathione biosynthesis or by directly binding to the drug. Vitamin E (Trolox™), a known antioxidant, was also able to protect S. cerevisiae against the pro-oxidant effect of diphenyl diselenide. In vitro assays showed that diphenyl diselenide interacts non-enzymatically with the thiol group of glutathione. [Copyright &y& Elsevier]

Selenium compounds display antioxidant and neuroprotective properties. Diphenyl diselenide (PhSe)2 is an organic selenium compound that affects a number of neuronal processes. The aim of the present study was to evaluate the effects of the systemic administration of (PhSe)2 on novel object recognition memory in mice. Adult male CF1 mice were given an i.p. injection of (PhSe)2 (0.2, 1.0, 5.0, or 25.0 μmol/kg) 30 min before training in an object recognition task. (PhSe)2 did not affect short-term memory or the total time exploring both objects, but induced a facilitation of retention measured 24 h after training. The present findings show that systemic administration of (PhSe)2 induces a facilitation of formation of long-term object recognition memory. [Copyright &y& Elsevier]

In this study, we use PGIS to evaluate and map stakeholders' preferences for seven Marine and Coastal Ecosystem Services (MCES) in the Peniche-Nazaré region, located on the west coast of Portugal. We develop an alternative approach based on the Shannon index to identify conflict potential without questioning stakeholders directly about perceived conflicts. The Shannon index allows us to identify not only areas with highly valued ecosystem services and thus with current conflicting interests, but also areas providing several services that, although currently less valued, may hold existence, bequest, and option values that are important to consider in future decisions. Moreover, despite the increasing use of PGIS, there are still lacking benchmarks to assess PGIS positional accuracy. In this study, we also compare the spatial data collected from stakeholders on one of the services considered - Food provisioning , with spatial data on fishing areas collected from another survey of individual fishers to assess our PGIS positional accuracy. We surveyed 27 local stakeholders representing a wide range of interests. Our results show that stakeholders value more Food provisioning and Leisure and recreation and that the places perceived more relevant for Food provisioning by the interviewed stakeholders coincide with those places that are used by fishers, showing positional accuracy for this service. The Shannon index's application proved useful in indirectly identifying conflict potential that is of utmost importance for Marine Spatial Planning. By anticipating potential conflicts, policymakers may be willing to limit the use of maritime space for particular activities. • The Shannon diversity index is useful in indirectly identifying conflict potential. • PPGIS provides positional accuracy regarding MCES mapping. • Food provisioning and Leisure and recreation are the most valued ecosystem services by stakeholders. • Deep-ocean ecosystem services are less valued by stakeholders. • There is a conflict of interests between fishers and tourism-related stakeholders. [ABSTRACT FROM AUTHOR]

Abstract: The scientific basis for the statement that plants and their active constituents play an important role in the prevention of chronic and degenerative diseases is continuously advancing. In fact, the origin of many therapeutic substances is due to secondary metabolism in the plant. The genus Hibiscus contains 220 species distributed around the world. It is an interesting source of potential bioactive molecules, as phenolic compounds, triterpene derivatives, phytosteroids, with antioxidant, cardioprotective, antihypertensive and antiproliferative activities. This work reviews the pharmacological evidence of extracts of plants from the genus Hibiscus, giving an overview of the most studied biological effects and the known phytochemical composition. Although more studies are necessary, Hibiscus spp. exhibits proven potential to become of important pharmacological interest. [Copyright &y& Elsevier]

Bombesin and its mammalian equivalent, gastrin-releasing peptide (GRP), stimulate cell proliferation and are involved in the pathogenesis of several types of human cancer. Bombesin-like peptides also display neuroendocrine activities and regulate neural function. In the present study, we evaluated the effects of the bombesin/GRP receptor antagonist (d-Tpi6, Leu13 psi[CH2NH]-Leu14) bombesin-(6–14) (RC-3095), experimental antitumor drug, on memory in rats. Adult female Wistar rats were treated with an intraperitoneal injection of RC-3095 (0.2, 1.0 or 5.0 mg/kg) 30 min before training in either inhibitory avoidance or novel object recognition tasks. Retention test trials were carried out 1.5 (short-term memory) or 24 h (long-term memory) after training. RC-3095 at the doses of 0.2 or 1.0 mg/kg, but not at the dose of 5.0 mg/kg, impaired both short- and long-term inhibitory avoidance retention, but did not affect recognition memory. The memory-impairing effect of RC-3095 could not be attributed to alterations in sensorimotor functions. The results show that the antitumor drug/GRP antagonist RC-3095 impairs formation of aversive memory. [Copyright &y& Elsevier]

Several studies have reported that guanylhydrazones display a variety of desirable biological properties, such as antihypertensive, antibacterial, and antimalarial behaviour. They furthermore promote anti-pneumocystosis and anti-trypanosomiasis, exhibit antitumor activity, and show significant cytotoxicity against cancer cell lines. In this work, we have evaluated the cytotoxicity, mutagenicity, and genotoxicity of two guanylhydrazones derivatives, ( E )-2-[(2,3-dimethoxyphenyl) methylene] hydrazine carboxymidamide hydrochloride (2,3-DMeB) and ( E )-2-[(3,4-dimethoxyphenyl) methylene] hydrazine carboxymidamide hydrochloride (3,4-DMeB), in different biological models. Both 2,3-DMeB and 3,4-DMeB induce weak cytotoxic and mutagenic effects in bacteria and yeast. The genotoxicity of these compounds was determined in a fibroblast cell line (V79) using alkaline comet assay, as well as a modified comet assay with bacterial enzymes formamidopyrimidine DNA-glycosylase (FPG) and endonuclease III (EndoIII). Both guanylhydrazone derivatives induced DNA damage. Treatment of V79 cells with EndoIII and FPG proteins demonstrated a significant effect of 2,3-DMeB and 3,4-DMeB with respect to oxidized bases. In addition, the derivatives induced a significant increase in the frequency of micronucleated cells at high doses. The antifungal and anti-trypanosomal properties of these guanylhydrazone derivatives were also evaluated, and the obtained results suggest that 2,3-DMeB is more effective than 3,4-DMeB. The biological activity of 2,3-DMeB and 3,4-DMeB may thus be related, at least in part, to their oxidative potential, as well as to their ability to interact with DNA. Considering the previously reported in vitro antitumor activity of guanylhydrazone derivatives in combination with the lack of acute toxicity and the fact that DNA damage is only observed at high doses should render both compounds good candidates for in vivo studies on antitumor activity. [ABSTRACT FROM AUTHOR]

Highlights: [•] Toxicological properties of dicholesteroyl diselenide (DCDS) were evaluated. [•] DCDS induced cytotoxicity, GSH depletion and elevation of lipid peroxidation. [•] Micronucleus formation, point and frameshift mutations were observed. [•] N-acetylcysteine preincubation reduced oxidative, genotoxic and mutagenic effects. [•] Cholesterol substituents in DCDS elevated the cytotoxic and genotoxic potential. [Copyright &y& Elsevier]

Abstract: Patulin, a known mycotoxin, is considered a significant contaminant in apples, apple-derived products and feeds. This study investigated the genotoxic effects of patulin in multiple organs (brain, kidney, liver and urinary bladder) of mice using an in vivo comet assay. We assessed the mechanism underlying this genotoxicity by measuring the GSH content and the thiobarbituric acid-reactive species (TBARS) level. Male CF-1 mice were given 1.0–3.75mg/kg patulin intraperitoneally. The effect of patulin was dose-dependent and the highest patulin dose induced DNA strand breaks in the brain (damage index, DI, in hippocampus increased from 36.2 in control animals to 127.5), liver (44.3–138.4) and kidneys (31.5–99); decreased levels of GSH (hippocampus – from 46.9 to 18.4nmol/mg protein); and an increase in lipid peroxidation (hippocampus – from 5.8 to 20.3 MDA equivalents/mg protein). This finding establishes an interrelationship between the pro-oxidant and genotoxic effects of patulin. Pre-treatment administration of N-acetyl-cysteine reduced patulin-induced DNA damage (hippocampus – DI from 127.5 to 39.8) and lipid peroxidation (hippocampus – 20.3 to 12.8 MDA equivalents/mg protein) by restoring cellular GSH levels, reinforcing the positive relationship between patulin-induced GSH depletion and DNA damage caused by systemic administration of this mycotoxin. [Copyright &y& Elsevier]