The occurrence of patulin was investigated in 100 conventional and 69 organic fruity foodstuffs samples commercially available in Italy by using an HPLC method with a limit of quantification of 0.5 µg kg−1. Patulin was detected in 26 (26%) conventional and 31 (45%) organic products with a significantly higher (p < 0.01) mean concentration in the organic products (4.78 vs. 1.15 µg kg−1). Mean patulin concentrations in conventional apple juices, pear juices, other juices and fruits purees were 3.14, 0.22, 0.19, 0.11 µg kg−1, respectively, and 7.11, 11.46, 2.10, 0.18 µg kg−1 in the relevant organic products. Four samples of juices (one conventional and two organic apple, and one organic pear) contained patulin at concentrations above the limit of 50 µg kg−1, four at concentrations between 10 and 25 µg kg−1, and the remaining ones below 10 µg kg−1. Patulin was detected (<1 µg kg−1) in only three of the 23 fruity baby food samples tested (homogenized fruits, 11 conventional and 12 organic). Based on the available data on Italian intakes of fruit juices, the estimated daily intakes of patulin, were 0.38 and 1.57 ng kg−1 body weight (bw) from conventional and organic products, respectively. Estimated daily intakes of patulin for children were higher, 3.41 ng kg−1 bw from conventional and 14.17 ng kg−1 bw from organic products, but largely below the provisional maximum tolerable daily intake (PMTDI) of 400 ng kg−1 bw. Patulin was also found in two samples of organic apple vinegar (<5 µg kg−1) and in fresh apples with rotten spots (12 out of 24 samples) with maximum levels at 16 402 and 44 572 µg kg−1 for conventional and organic apples, respectively.
1 January 2018 in Journal of Enzyme Inhibition and Medicinal Chemistry
A new series of multifunctional hybrids, based on the structure of the donepezil (DNP) drug, have been developed and evaluated as potential anti Alzheimer’s disease (AD) agents. The rationale of this study was the conjugation of a benzylpiperidine/benzylpiperazine moiety with derivatives of bioactive heterocyclics (benzimidazole or benzofuran), to mimic the main structure of DNP and to endow the hybrids with additional relevant properties such as inhibition of amyloid beta (Aβ) peptide aggregation, antioxidant activity and metal chelation. Overall, they showed good activity for AChE inhibition (IC50=4.0–30.0 μΜ) and moderate ability for inhibition of Aβ1–42 self-mediated aggregation. The hybrids containing chelating groups showed improvement in the inhibition of Cu-induced Aβ42 aggregation and the antioxidant capacity. Moreover, neuroprotective effects of these compounds were evidenced in neuroblastoma cells after Aβ1–42 induced toxicity. Structure–activity relationship allowed the identification of some promising compounds and the main determinant structural features for the targeted properties. Graphical Abstract
25 November 2019 in Journal of Enzyme Inhibition and Medicinal Chemistry
Pursuing the widespread interest on multi-target drugs to combat Alzheimer´s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives. The BF framework aims to endow the conjugate molecules with ability for inhibition of AChE (bimodal way) and of amyloid-beta peptide aggregation, besides providing metal (Fe, Cu) chelating ability and concomitant extra anti-oxidant activity, for the hybrids with hydroxyl substitution. The new TAC-BF conjugates showed very good activity for AChE inhibition (sub-micromolar range) and good capacity for the inhibition of self- and Cu-mediated Aβ aggregation, with dependence on the linker size and substituent groups of each main moiety. Neuroprotective effects were also found for the compounds through viability assays of neuroblastoma cells, after Aβ1-42 induced toxicity. Structure-activity relationship analysis provides insights on the best structural parameters, to take in consideration for future studies in view of potential applications in AD therapy. GRAPHICAL ABSTRACT Design, synthesis and evaluation of new tacrine-benzofuran hybrids as multitargeting anti- Alzheimer’s disease agents; high AChE inhibition associated with other relevant properties; structure–activity relationship analysis
The worrying and constant increase in the quantities of food and beverage industry by-products and wastes is one of the main factors contributing to global environmental pollution. Since this is a direct consequence of continuous population growth, it is imperative to reduce waste production and keep it under control. Re-purposing agro-industrial wastes, giving them new life and new directions of use, is a good first step in this direction, and, in global food production, vegetables and fruits account for a significant percentage. In this paper, brewery waste, cocoa bean shells, banana and citrus peels and pineapple wastes are examined. These are sources of bioactive molecules such as polyphenols, whose regular intake in the human diet is related to the prevention of various diseases linked to oxidative stress. In order to recover such bioactive compounds using more sustainable methods than conventional extraction, innovative solutions have been evaluated in the past decades. Of particular interest is the use of deep eutectic solvents (DESs) and compressed solvents, associated with green techniques such as microwave-assisted extraction (MAE), ultrasonic-assisted extraction (UAE), pressurized liquid extraction (PLE) and pulsed-electric-field-assisted extraction (PEF). These novel techniques are gaining importance because, in most cases, they allow for optimizing the extraction yield, quality, costs and time.
Secondary metabolites from plants and fungi are stimulating growing interest in consumers and, consequently, in the food and supplement industries. The beneficial effects of these natural compounds are being thoroughly studied and there are frequent updates about the biological activities of old and new molecules isolated from plants and fungi. In this article, we present a review of the most recent literature regarding the recent discovery of secondary metabolites through isolation and structural elucidation, as well as the in vitro and/or in vivo evaluation of their biological effects. In particular, the possibility of using these bioactive molecules in the prevention and/or treatment of widely spread pathologies such as cardiovascular and neurodegenerative diseases is discussed.
10 September 2018 in Journal of Medicinal Chemistry