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Aldose reductase (ALR2) is a key enzyme involved in diabetic complications and the search for new aldose reductase inhibitors (ARIs) is currently very important. The synthetic ARIs are often associated with deleterious side effects and medicinal and edible plants, containing compounds with aldose reductase inhibitory activity, could be useful for prevention and therapy of diabetic complications. Non-psychotropic phytocannabinoids exert multiple pharmacological effects with therapeutic potential in many diseases such as inflammation, cancer, diabetes. Here, we have investigated the inhibitory effects of extracts and their fractions from two Cannabis sativa L. chemotypes with high content of cannabidiol (CBD)/cannabidiolic acid (CBDA) and cannabigerol (CBG)/cannabigerolic acid (CBGA), respectively, on human recombinant and pig kidney aldose reductase activity in vitro . A molecular docking study was performed to evaluate the interaction of these cannabinoids with the active site of ALR2 compared to known ARIs. The extracts showed significant dose-dependent aldose reductase inhibitory activity (>70%) and higher than fractions. The inhibitory activity of the fractions was greater for acidic cannabinoid-rich fractions. Comparative molecular docking results have shown a higher stability of the ALR2-cannabinoid acids complex than the other inhibitors. The extracts of Cannabis with high content of non-psychotropic cannabinoids CBD/CBDA or CBG/CBGA significantly inhibit aldose reductase activity. These results may have some relevance for the possible use of C. sativa chemotypes based preparations as aldose reductase inhibitors. [ABSTRACT FROM AUTHOR]

Abstract: A synthetic approach towards a series of 3-hydroxymethyl-5-(1H-1,2,3-triazol)isoxazolidines has been reported, according to a procedure based on the cycloaddition reaction, under microwave irradiation, of a nitrone with 1-vinyl triazoles, prepared by a click reaction of azides with alkynes. Biological tests show that the synthesized compounds are able to inhibit proliferation of follicular and anaplastic human thyroid cancer cell lines, with IC50 values ranging from 3.87 to 8.76μM. The obtained compounds induce caspase-3 activation and DNA fragmentation prevalently in follicular human thyroid cancer cell lines. [Copyright &y& Elsevier]

Abstract: A series of modified N,O-nucleosides, characterized by the presence of a furopyrimidine moiety, has been synthesized by exploiting a Sonogashira cross coupling reaction of 1-isoxazolidinyl-5-iodouracil with alkynes, followed by treatment with CuI in refluxing TEA/MeOH mixture. The obtained compounds were screened against both RNA and DNA viruses. None of the compounds were endowed with antiviral activity at subtoxic concentrations. However, some of them were able to inhibit proliferation of MRC-5, Vero, BS-C-1 cells by 50% (CC50) at concentrations ranging from 0.7 to 62.5mM. [Copyright &y& Elsevier]

Relatively few studies are available in the literature on the apocarotenoids occurrence in food which are based on liquid chromatographic separation approaches and no reports are available on the apocarotenoids separation by SFC-APCI (+/−)/QqQ/MS. The dual purpose of this research was to investigate the apocarotenoids presence in red habanero peppers and to develop a novel SFC-APCI(+/−)/QqQ/MS methodology, using a novel fused-core C30 column, for the apocarotenoids detection in a fast and efficient way, for the first time. In this study, 25 different apocarotenoids were identified, 14 were free apocarotenoids and 11 were apocarotenoids fatty acids esters. The methodology allowed for all the separations to occur in less then five minutes. The detected Apo-10′-, Apo-14′- and Apo-15-capsorubinals and different Apo-8′-capsorubinal and Apo-10′-zeaxanthinals fatty acid esters had not been previously tentatively identified in any Capsicum species and, to the best of our knowledge, in any food matrix. [ABSTRACT FROM AUTHOR]

Abstract: Arenediyne–isoxazolidine conjugates have been synthesized as a new scaffold for the development of bioactive mimics. Some of the synthesized compounds are endowed with antiproliferative activity against three human cancer cell lines. Their thermal reactivity suggests that the biological activity probably could not be linked to the Bergman cyclization. [Copyright &y& Elsevier]

Abstract: Truncated phosphonated C-1′-branched N,O-nucleosides have been synthesized in good yields by 1,3-dipolar cycloaddition methodology, starting from N-methyl-C-(diethoxyphosphoryl)nitrone 7. Preliminary biological assays show that β-anomers are able to inhibit HIV in vitro infection at concentrations in the micromolar range. Higher SI values with respect to AZT indicated that the compounds were endowed with low cytotoxicity. [Copyright &y& Elsevier]

Abstract: A general, practical, and efficient reduction of four-, five-, six- and, seven-membered N-alkoxycarbonyl lactams to the aldehyde oxidation state is reported. The reduction methodology involves the hydrozirconation reaction by Cp2Zr(H)Cl under mild conditions and proceeds with very short reaction times and in excellent to good yields. The hydrozirconation of N-alkoxycarbonyl lactams with the Schwartz reagent demonstrated to be the mildest and most general method for the formation of lactamols with a high functional group tolerance. [Copyright &y& Elsevier]

The integrated approaches of Foodomics, defined as a discipline that studies food and nutrition domains through the application of advanced omic technologies, represent the new frontier to explain some critical issues in food science. Among several applications of omic sciences in food analysis, Nuclear Magnetic Resonance (NMR) spectroscopy is the most used for the instrumental sensitivity and precision. Furthermore, in the last years the NMR technique known as high-resolution magic angle spinning (HR-MAS) has been successfully applied in the field of food science. In particular, this powerful technique is unique for the analysis of talis qualis samples of food products. The results reported in this review showed the validity of this technique for food characterization and authentication but also for the comprehension of the changes in the metabolic profile due to different conditions. [ABSTRACT FROM AUTHOR]

Abstract: The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. Our goal is to modify the P3 site of this motif in order to identify the structural requirements for the interaction with the target. [Copyright &y& Elsevier]

Abstract: The effects of an extract from Citrus bergamia (BSext) and those of two products purified from the same extract, that is, nomilin and limonin, and reference compounds, towards HTLV-1 have been reported. Moreover, they were also compared with those obtained towards HIV-1. Results showed that the efficacy of both BSext and limonin in inhibiting HTLV-1 as well as HIV-1 expression in infected cells, as evaluated by comparable quantitative assays, was close to that of the effective, reference compounds, respectively. The protective effect of BSext and of the purified products was associated with the inhibition of both HTLV-1 and HIV-1 RT activities in conceptually similar, cell-free assays. The cytotoxicity of the assayed compounds of natural origin was substantially less pronounced than that of the reference compounds, thus showing a favourable selectivity index for the novel BSext product. [Copyright &y& Elsevier]