Search

The secondary metabolite pattern of Eryngium tricuspidatum has been found to be dominated by C

Malignant pleural mesothelioma is a fatal malignancy linked to asbestos exposure. The main challenge for mesothelioma treatment is to go beyond the drug resistance, in particular against cisplatin (CDDP), one of the most used chemotherapeutic drug. 3-O-methylfunicone (OMF) is a metabolite produced by the fungus Penicillium pinophilum; its antiproliferative properties have been previously studied in vitro. Particularly, OMF is able to inhibit mesothelioma cell motility. To improve the effects of CDDP by-passing the resistance of mesothelioma cells to this drug, in the present study we investigated the combined treatment of OMF with CDDP respectively in an established mesothelioma cell line (NCI) and primary mesothelioma cells (Mest). As compared to the effect of single treatments, the combination of OMF and CDDP resulted in a stronger inhibition of NCI and Mest cell proliferation. OMF combination with CDDP was also able to affect the migratory ability of NCI and Mest cells by down-regulating αv and β5 expression and reducing metalloproteinase 2 (MMP-2) production. In addition, this association was effective in modulating VEGF gene expression. This finding highlights the possibility to use OMF and CDDP together to regulate angiogenesis and tumour progression in mesothelioma.

(-)-Actisonitrile, a lipid based on a serinol ether skeleton, was isolated from the opisthobranch mollusk Actinocyclus papillatus. The structure was established by spectroscopic methods whereas the absolute configuration of the chiral centre was determined by comparing the optical properties of natural actisonitrile with those of (+)- and (-)-synthetic enantiomers, opportunely prepared. In a preliminary in vitro cytotoxicity bioassay, both (-)- and (+) -actisonitrile enantiomers showed cytotoxic activity against tumor and non tumor mammalian cells.

Postharvest heat treatments (hot water or hot air treatment) may be applied to horticultural crops to control fungal diseases, insect infestation and to reduce chilling injury in cultivars susceptible to low storage temperatures. The present study investigated the influence of hot water (53 degrees C for 60s) and hot air treatment (38 degrees C for 24h) applied to two typical Sardinian apple varieties, cvs. Miali and Caddina, on the composition of the lipophilic extracts of the peel as well as on the antioxidant activity of ethanolic extracts of both peel and pulp. The lipophilic extracts of the peel of the two varieties were almost similar and resulted to be dominated by the presence of triterpenes being ursolic and oleanoic acids the main metabolites in both analysed fruits. The chemical analysis of the extracts obtained from the different heat-treated samples for each variety revealed no significant difference in the relative distribution of triterpene components with respect to untreated control samples. This strongly suggested that heat treatment does not affect the composition of terpene metabolite profile of the fruit peel. On the other hand, the antioxidant activity of the ethanolic extracts of the peel and the pulp of heat treated was significantly different from that of control In particular, on Caddina variety the antioxidant activity levels of the peel were consistently higher than in the pulp and were affected by storage conditions. Differently, on Miali variety the antioxidant activity of heat-treated samples was higher than control sample in both peel and pulp.

Obligate marine hydrocarbonoclastic bacteria possess genetic and physiological features to use hydrocarbons as sole source of carbon and to compete for the uptake of nutrients in usually nutrient-depleted marine habitats. In the present work we have studied the siderophore-based iron uptake systems in Alcanivorax borkumensis SK2 and their functioning during biodegradation of an aliphatic hydrocarbon, tetradecane, under iron limitation conditions. The antiSMASH analysis of SK2 genome revealed the presence of two different putative operons of siderophore synthetases. Search for the predicted core structures indicated that one siderophore is clearly affiliated to the family of complex oligopeptidic siderophores possessing an Orn-Ser-Orn carboxyl motif whereas the second one is likely to belong to the family of SA (salicylic acid)–based siderophores. Analyzing the supernatant of SK2 culture, an extracellular siderophore was identified and its structure was resolved. Thus, along with the recently described membrane-associated amphiphilic tetrapeptidic siderophore amphibactin, strain SK2 additionally produces an extracellular type of iron-chelating molecule with structural similarity to pseudomonins. Comparative Q-PCR analysis of siderophore synthetases demonstrated their significant up-regulation in iron-depleted medium. Different expression patterns were recorded for two operons during the early and late exponential phases of growth, suggesting a different function of these two siderophores under iron-depleted conditions., This work was funded by the European Community Projects KILL-SPILL (FP7-KBBE-2012.3.5-01-4 Project 312139 “Integrated Biotechnological Solutions for Combating Marine Oil Spills”) and BRAAVOO (FP7-KBBE OCEAN 2013.1 “Biosensors, Reporters and Algal Autonomous Vessels for Ocean Operation”).

Four diterpenes, tritoniopsins A-D (1-4), have been isolated from the South China Sea nudibranch Tritoniopsis elegans and its prey, the soft coral Cladiella krempfi. They display an unprecedented pyran ring in the cladiellane framework, thus representing a novel cladiellane-based diterpene family. Their structures have been mainly characterized by NMR and mass spectrometric techniques, whereas the relative configuration of compound 1 was secured by X-ray analysis. Antiproliferative assays on tumor and nontumor cell lines have been carried out for the main metabolite, tritoniopsin B (2).

E stata determinata la fotoreattivita con DNA nativo di un gruppo di furocumarine per irradiazione a 365 nm. I valori ottenuti sono risultati in accordo con quelli di attivita fotosensibilizzatrice cutanea posseduti dalle stesse sostanze.

Nine linear polyoxygenated acetylenes, fulvynes A–I (1–9), exhibiting the uncommon 2-yne carboxylic acid functionality, have been isolated from the butanolic extract of the Mediterranean sponge Haliclona fulva. Their structures possess a long alkyl chain with several oxygenated carbons, and were established by detailed spectroscopic analysis. All fulvynes were found to be active against a chloramphenicol-resistant strain of Bacillus subtilis.

Biodiversity is increasingly exploited worldwide for the finding of new pharmaceuticals. In relation to a competitive aptitude developed in many and diverse environments, microorganisms are able to produce secondary metabolites with cytotoxic and antiproliferative properties that are valuable in the perspective of antitumor drug discovery. Particularly, fungal species in the genus Penicillium represent a prolific source of biologically active extrolites that in some cases have already disclosed possible relevance for an application in cancer chemotherapy. Antiproliferative, pro-apoptotic, anti-angiogenic, anti-metastatic, DNA synthesis and cell cycle inhibitory properties of these compounds are reviewed in the present paper. _____________________________________________________________________________________________________________