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A series of imines derived from camptothecin-7-aldehyde (CPT-CHO) and aromatic amines were synthesised and tested for their cytotoxicity against tumour cell line H460, that expresses a high level of topoisomerase I. In general ortho-substituted compounds showed higher cytotoxic potency than the corresponding para-substituted imines. This effect was dependent on the nature of the substituent. Structure–activity relationships were studied by calculation of docking energy with a model of the ternary complex camptothecin–DNA–topoisomerase I. The ability of selected compounds to stimulate the topoisomerase I-mediated DNA cleavage and the persistence of the cleavable complex were consistent with the cytotoxic activity. [Copyright &y& Elsevier]

Highlights • Blends of Perilla seed oil (PO) and extra virgin olive oil (EVOO) were developed. • Blends were high in ω − 3 and ω − 6 fatty acids, biophenols, tocopherols, and sterols. • Blends showed higher oxidation stability than PO. • All blends reached the sensory acceptability by consumers. • Blends with 25–35% and 40–45% PO were paired respectively with raw and cooked foods. Abstract This study reports the blending at different levels (25, 30, 35, 40 and 45%) of Perilla seed oil (PO) with extra virgin olive oil (EVOO). Pure oils and blends were evaluated in terms of free acidity, peroxide value, fatty acid composition, sterols, tocopherols and biophenols content, oxidation stability, sensory acceptability and food pairing. Blends with high content of ω − 3 and ω − 6 fatty acids, biophenols, tocopherols, sterols and satisfying oxidation stability were obtained, representing products with improved nutritional properties. All blends resulted acceptable by consumers. Two groups of consumers with opposite preferences for samples with low (25–35%) and high (40–45%) levels of PO were identified. Blends containing 40–45% of PO were mainly paired to strong-flavour and cooked foods, while blends with less PO were preferably matched with raw meat and vegetables. Consequently, PO and EVOO blends showed promising potential as innovative vegetable oils with improved nutritional properties and versatile gastronomic use. [ABSTRACT FROM AUTHOR]

Understanding cross-cultural differences in food perception is a key issue of food research in order to understand consumer behaviour in different countries. The objective of this study was to explore potential cultural differences of balsamic vinegar perception between Korean and Italian consumers using the sorted napping method. Nine balsamic vinegars different in terms of ingredients, aging time, and origin were evaluated by Korean (n = 50) and Italian (n = 49) consumers using sorted napping. Familiarity and food matching were also examined. Descriptive analysis was performed to verify the attitude of the consumers in product description. The results obtained from two groups of consumers in Korea and Italy revealed a higher description attitude of the Italians (higher number of total elicited attributes, of attributes in common with the trained panel, of attributes shared with the vocabulary reported in literature, of significant specific positive product-attribute associations). Italian subjects generated various descriptors associated with the European gastronomic culture (aromatic herbs, fortified wine, dried figs, Indian fig, Parmigiano-Reggiano cheese), whereas Korean consumers used more terms related to the Asian food culture (red ginseng, Chinese medicine, Japanese apricot, teriyaki sauce, persimmon vinegar, balloon flower roots). Moreover, cultural differences of food matching were also observed: the Italians would pair the balsamic vinegars mainly with vegetables, fruits and cheese, while Koreans would combine the balsamic vinegars preferably with bread, vegetables and meat. In conclusion, familiarity resulted the main factors for cross-cultural differentiation. [ABSTRACT FROM AUTHOR]

Abstract: A series of hydroxamic acid-based histone deacetylase (HDAC) inhibitors were designed on the basis of a model of the HDAC2 binding site and synthesized. They are characterized by a cinnamic spacer, capped with a substituted phenyl group. Modifications of the spacer are also reported. In an in vitro assay with the isoenzyme HDAC2, a good correlation of the activity with the docking energy was found. In human ovarian carcinoma IGROV-1 cells, selected compounds produced significant acetylation of p53 and α-tubulin. Most compounds showed an antiproliferative activity comparable to that of SAHA. At equitoxic concentrations, the tested compounds were more effective than SAHA in inducing apoptotic cell death. Compounds selected for in vivo evaluation exhibited a significant antitumor activity on three tumor models at well tolerated doses, thus suggesting a good therapeutic index. [Copyright &y& Elsevier]

Abstract: Perilla frutescens is a food plant widely used in Asian cuisine. This plant was investigated for its interesting taste and somatosensory properties. Perillaldehyde and perillaketone are among the components of the aromatic extracts from P. Frutescens. These compounds were shown here to activate the cloned TRPA1 channel when expressed in an heterologous cell system and are therefore suggested to be responsible for the chemesthetic properties of this plant. [Copyright &y& Elsevier]

Abstract: A series of novel 9-substituted camptothecins derived from 9-formylcamptothecin were synthesized. The aldehyde was obtained from 10-hydroxycamptothecin or, better, by total synthesis. The compounds showed antiproliferative activity higher than that of the reference compound topotecan. Modelling suggested the possibility of a favourable interaction of small and polar 9-substituents with the topoisomerase I–DNA complex, which is consistent with the higher activity of these derivatives with respect to the corresponding 7-substituted camptothecins. [Copyright &y& Elsevier]