Enzyme-Assisted Extraction of Bioactive Compounds from Raspberry (Rubus idaeus L.) Pomace.

Industrial processing of raspberries into juice and jam results in the production of with high content of lipophilic and hydrophilic phytochemicals. Usually considered as waste, raspberry pomace is occasionally cold-pressed to recover specialty oil. However, the resulting pomace press-cake (PPC) still contains 30% to 35% of lipophilic compounds, such as essential fatty acids, tocols, phytosterols, and ellagitannins initially present in pomace. In a perspective of sustainable development, we investigate an eco-friendly process using an aqueous enzyme-assisted extraction (AEAE) to simultaneously and effectively recover lipophilic compounds and polyphenols from the PPC. The performance of different combinations of carbohydrases and proteases was compared. After selecting the best enzymatic system, a definitive screening design involving six factors was then implemented to optimize the process. Under optimized conditions, 1.2 units of thermostable alkaline protease/100 g PPC, pH 9, 60 °C, and 2 hr hydrolysis, more than 38% of total PPC lipophilic content were recovered in the aqueous medium. The recovery of polyphenols and antioxidant activity was, respectively, 48% and 25% higher than obtained by extraction with methanol/acetone/water mixture. Such an AEAE extract might prove useful in food and nutraceutical applications. PRACTICAL APPLICATION: Raspberry pomace, a food industrial by-product, is often considered as waste. However, it is a rich source of phytochemicals, such as tocols, polyphenols, and polyunsaturated fatty acids. To overcome the drawbacks of organic solvent use, an enzyme-assisted extraction process was developed as an eco-friendly alternative to recover these bioactive compounds. Definitive screening design experimental design was used to enhance polyphenols and lipophilics extraction yields while reducing process costs. This extract is an oil-in-water emulsion, with high content in antioxidant phytochemicals, which might have potential for use in nutraceutical applications. Therefore, this green process developed for the valorization of raspberry pomace is considered as a perspective of sustainable development.

Antiproliferative and antibiofilm potentials of endolichenic fungi associated with the lichen Nephroma laevigatum.

AIMS: The objective of this study was to explore the diversity of endolichenic fungi from Nephroma laevigatum and to investigate their antiproliferative and antibiofilm potential. METHODS AND RESULTS: Forty-six isolates were obtained and identified by DNA barcoding. They belonged to genera Nemania, Daldinia, Peziza and Coniochaeta. Six strains belonging to the most represented species were selected and tested for their antiproliferative and antibiofilm activities. Extracts were analysed by reversed-phase HPLC. Activities against fungal and bacterial biofilm were evaluated using tetrazolium salt (XTT) assay and crystal violet assay respectively. Antiproliferative responses of extracts were determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Apoptosis induction by two extracts was observed in two cell lines (HT-29 and PC-3) via morphological changes, pro-apoptotic and anti-apoptotic proteins analysis (Western blotting) and DNA fragmentation. Four extracts displayed activities against Candida albicans biofilm with IC50 values ranging from 25 to 200 µg ml-1 . All extracts were inactive against Staphylococcus aureus and Pseudomonas aeruginosa biofilms. The most active isolates against human colorectal (HT-29 and HCT116) and prostate (PC-3 and DU145) cancer cell lines were Nemania serpens (NL08) and Nemania aenea var. aureolatum (NL38) with IC50 values ranging from 13 to 39 µg ml-1 . These extracts induced an apoptotic process through activation of caspases 8 and 3, poly(ADP-ribose) polymerase cleavage and DNA fragmentation. CONCLUSIONS: Selected crude fungal extracts have antiproliferative and antibiofilm activities. Data suggest that this antipoliferative effect is due to apoptosis process. This is the first report showing the effects of endolichenic fungi from N. laevigatum. SIGNIFICANCE AND IMPACT OF THE STUDY: This study highlights the therapeutic potential of endolichenic fungi metabolites as sources for drug discovery programmes.

Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard.

A new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2a-m) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.