Marine pharmacology in 2009-2011: marine compounds with antibacterial, antidiabetic, antifungal, anti-inflammatory, antiprotozoal, antituberculosis, and antiviral activities; affecting the immune and nervous systems, and other miscellaneous mechanisms of action.

The peer-reviewed marine pharmacology literature from 2009 to 2011 is presented in this review, following the format used in the 1998–2008 reviews of this series. The pharmacology of structurally-characterized compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, antifungal, antiprotozoal, antituberculosis, and antiviral pharmacological activities were reported for 102 marine natural products. Additionally, 60 marine compounds were observed to affect the immune and nervous system as well as possess antidiabetic and anti-inflammatory effects. Finally, 68 marine metabolites were shown to interact with a variety of receptors and molecular targets, and thus will probably contribute to multiple pharmacological classes upon further mechanism of action studies. Marine pharmacology during 2009–2011 remained a global enterprise, with researchers from 35 countries, and the United States, contributing to the preclinical pharmacology of 262 marine compounds which are part of the preclinical pharmaceutical pipeline. Continued pharmacological research with marine natural products will contribute to enhance the marine pharmaceutical clinical pipeline, which in 2013 consisted of 17 marine natural products, analogs or derivatives targeting a limited number of disease categories

Modulation of Barrier Properties of Monolayer Films from Blends of Polyethylene with Ethylene-co-Norbornene

Flexible monolayer films with modulated diffusional and optical properties were achieved from blends of a LDPE/LLDPE matrix and an ethylene/norbornene copolymer (COC). A significant decrease of O2 and CO2 permeability was observed for cast films with COC content from 5 to 20 wt %. SEM analysis showed that, despite the incompatibility of the blend components, good dispersion and distribution of the COC domains in the PE matrix were achieved; as a consequence, for COC content ranging from 5 to 10 wt % the film transparency results practically unchanged. The UV light transmission decreased on increasing the percentage of COC, which constitutes also a protection against UV radiations. A noticeable improvement was observed in the mechanical properties: adding only 5 wt % of COC, the elastic modulus becomes five times higher than that of the PE matrix. The rheological behaviour of the blends keeps practically unchanged with respect to the matrix, allowing to use the typical LDPE processing conditions. Sustainable inexpensive flexible films answering the packaging requirements of specific categories of food were achieved

Ptaquiloside, the major carcinogen of bracken fern, in the pooled raw milk of healthy sheep and goats: an underestimated, global concern of food safety

Bracken fern (Pteridium aquilinum) is a worldwide plant containing toxic substances, which represent an important chemical hazard for animals, including humans. Ptaquiloside, 1, a norsesquiterpenoid glucoside, is the major carcinogen of bracken detected in the food chain, particularly in the milk from farm animals. To date, ptaquiloside has been shown in the milk of cows feeding on a diet containing bracken fern. This is the first study that shows the systematic detection of ptaquiloside, 1, and reports its direct quantitation in pooled raw milk of healthy sheep and goats grazing on bracken. Ptaquiloside, 1, was detected by a sensitive method based on the chemical conversion of ptaquiloside, 1, into bromopterosine, 4, following gas chromatography–mass spectrometry (GC–MS) analysis. The presence of ptaquiloside, 1, possibly carcinogenic to humans, in the milk of healthy animals is an unknown potential health risk, thus representing a harmful and potential global concern of food safety

Effects of Azadirachta indica seed kernel extracts on early erythrocytic schizogony of Plasmodium berghei and pro-inflammatory response in inbred mice

Background: Medicinal plant research may contribute to develop new pharmacological control tools for vector borne diseases, such as malaria. Methods: The effects of methanol extracts (ME) obtained from seed kernel of ripe and unripe Azadirachta indica fruits were studied on erythrocytic proliferation of the rodent malaria parasite Plasmodium berghei strain ANKA and on mice pro-inflammatory response, as evaluated by measuring the matrix-metalloproteinase-9 (MMP-9) and tumour necrosis factor (TNF) plasma levels, in two mouse strains (C57BL/6 and BALB/c) which are considered as prototypical of Th1 and Th2 immune response, respectively. Results: ME obtained from seed kernel of unripe Azadirachta indica fruits decreased by about 30% the proportion of erythrocytes infected with the malaria parasite in C57BL/6 mice in the 4 days suppressive test. In this treatment group, MMP-9 and TNF levels were notably higher than those measured in the same mouse strain treated with the anti-malarial drug artesunate, Azadirachta indica kernel extracts from ripe fruits or solvent. In BALB/c mice, treatment with kernel extracts did not influence parasitaemia. MMP-9 and TNF levels measured in this mouse strain were notably lower than those recorded in C57BL/6 mice and did not vary among treatment groups. Conclusions: The effects of the ME on the parasite-host interactions appeared to be mouse strain-dependent, but also related to the ripening stage of the neem fruits, as only the unripe fruit seed kernel extracts displayed appreciable bioactivity

A bio-guided assessment of the anti-inflammatory activity of hop extracts (Humulus lupulus L. cv. Cascade) in human gastric epithelial cells

The present work aims to characterize and investigate the anti-inflammatory activity of hop extracts (cv. Cascade) in an in vitro model of gastric inflammation. The biological activities of hydroalcoholic and aqueous extracts from cones were evaluated by comparing IL-8 inhibition induced by TNF\u3b1. The hydroalcoholic extract demonstrated a higher inhibitory effect, which was just slightly affected by an in vitro simulated gastric digestion. The identification of active compounds was performed by a bio-guided fractionation which afforded 11 fractions, one of which inhibited IL-8 release in a concentration-dependent fashion in human gastric epithelial AGS cells. Phytochemical analysis revealed xanthohumol A and xanthohumol D as the main active components. The present study provides some experimental evidences that Humulus lupulus L. may exert an anti-inflammatory activity on the gastric district by the inhibition of the IL-8 secretion, partially due to its prenylated chalcones content

Potent Antioxidant and Genoprotective Effects of Boeravinone G, a Rotenoid Isolated from Boerhaavia diffusa

Background and Aims: Free radicals are implicated in the aetiology of some gastrointestinal disorders such as gastric ulcer, colorectal cancer and inflammatory bowel disease. In the present study we investigated the antioxidant and genoprotective activity of some rotenoids (i.e. boeravinones) isolated from the roots of Boerhaavia diffusa, a plant used in the Ayurvedic medicine for the treatment of diseases affecting the gastrointestinal tract. Methods/Principal Findings: Antioxidant activity has been evaluated using both chemical (Electron Spin Resonance spectroscopy, ESR) and Caco-2 cells-based (TBARS and ROS) assays. DNA damage was evaluated by Comet assay, while pERK 1/2 and phospho-NF-kB p65 levels were estimated by western blot. Boeravinones G, D and H significantly reduced the signal intensity of ESR induced by hydroxyl radicals, suggesting a scavenging activity. Among rotenoids tested, boeravinone G exerted the most potent effect. Boeravinone G inhibited both TBARS and ROS formation induced by Fenton's reagent, increased SOD activity and reduced H 2O 2-induced DNA damage. Finally, boeravinone G reduced the levels of pERK 1 and phospho-NF-kB p65 (but not of pERK 2) increased by Fenton's reagent. Conclusions: It is concluded that boeravinone G exhibits an extraordinary potent antioxidant activity (significant effect in the nanomolar range). The MAP kinase and NF-kB pathways seem to be involved in the antioxidant effect of boeravinone G. Boeravinone G might be considered as lead compound for the development of drugs potentially useful against those pathologies whose aetiology is related to ROS-mediated injuries

Glomangiopericytoma of the pterygomandibular space: An unusual case

We describe a case of glomangiopericytoma located in the pterygo-mandibular space, a rare anatomical region for this neoplasm to develop. The lesion is classified as a separate variant from the classic haemangiopericytoma, which is characterised by more aggressive biological behaviour. © 2006 The British Association of Oral and Maxillofacial Surgeons

The Sapogenins of Allium porrum L.

A chemical study of the sapogenin content has been conducted on leek, A. porrum L., sown and collected at different times. As a result of this investigation, a variability in the sapogenin composition depending from the climate was observed. In addition, a novel sapogenin named porrigenin C (1a), and its 25S epimer (1b) have been isolated, together with the previously described sapogenins 2-5 and to the known compounds agigenin, diosgenin, chlorogenin and 24-ethylcholesta-(6-acyl)-3-O-beta-D-glucoside. The chemical structure of the novel compound was elucidated by a detailed spectroscopic analysis mainly based on 1D and 2D NMR techniques. Porrigenin C showed a considerable antiproliferative activity on four tumor cell lines in vitro

Flavonoids and other aromatic compounds from Allium species

Comunicazione poste