The distribution of total phenolics and main betacyanins in red beetroot (Beta vulgaris) root was determined. Also, the subsequent effects of cold storage on the content of total phenolics, main betacyanins (betanin and isobetanin), and the main known ferulic acid ester (beta-D-fructofuranosyl-alpha-D-(6-O-(E)-feruloylglucopyranoside) were determined in the peel, which is the root part containing the largest amount of total phenolics. The content of total phenolics in the red beetroot water extracts was determined according to a modification of the Folin-Ciocalteu method and expressed as gallic acid equivalents (GAE). The compounds of interest were identified by HPLC-ESI-MS and NMR techniques, and the contents of compounds were determined by HLPC analyses. The total phenolic contents in various root parts were found to decrease in the order peel, crown, flesh. Significant differences in the contents of total phenolics and individual compounds were found when the effect of cold storage (5 degrees C, 0-196 days) on the constituents of the peel from intact roots was examined. In addition to the betacyanins of red beetroot peel found in our earlier study, tentative identifications of betanidin and feruloylamaranthin were made.
Since prostate-specific membrane antigen (PSMA) is up-regulated in nearly all stages of prostate cancer (PCa), PSMA can be considered as a viable diagnostic biomarker and treatment target in PCa. This project is focused on the development and evaluation of a series of compounds directed against PSMA. The modifications to the linker are designed to improve the binding potential and pharmacokinetics for theranostic application. In addition, the results help to further elucidate the structure-activity relationships (SAR) of the resulting PSMA inhibitors. Both in vitro and in vivo experiments of 18 synthesized PSMA inhibitor variants showed that systematic chemical modification of the linker has a significant impact on the tumor-targeting and pharmacokinetic properties. This approach can lead to an improved management of patients suffering from recurrent prostate cancer by the use of one radiolabeling precursor, which can be radiolabeled either with (68)Ga for diagnosis or with (177)Lu or (225)Ac for therapy.
Chiral sulfoxides are in extremely high demand in nearly every sector of the chemical industry concerned with the design and development of new synthetic reagents, drugs, and functional materials. The primary objective of this review is to update readers on the latest developments from the past five years (2011-2016) in the preparation of optically active sulfoxides. Methodologies covered include catalytic asymmetric sulfoxidation using either chemical, enzymatic, or hybrid biocatalytic means; kinetic resolution involving oxidation to sulfones, reduction to sulfides, modification of side chains, and imidation to sulfoximines; as well as various other methods including nucleophilic displacement at the sulfur atom for the desymmetrization of achiral sulfoxides, enantioselective recognition and separation based on either metal-organic frameworks (MOF's) or host-guest chemistry, and the Horner-Wadsworth-Emmons reaction. A second goal of this work concerns a critical discussion of the problem of the accurate determination of the stereochemical outcome of a reaction due to the self-disproportionation of enantiomers (SDE) phenomenon, particularly as it relates to chiral sulfoxides. The SDE is a little-appreciated phenomenon that can readily and spontaneously occur for scalemic samples when subjected to practically any physicochemical process. It has now been unequivocally demonstrated that ignorance in the SDE phenomenon inevitably leads to erroneous interpretation of the stereochemical outcome of catalytic enantioselective reactions, in particular, for the synthesis of chiral sulfoxides. It is hoped that this two-pronged approach to covering the chemistry of chiral sulfoxides will be appealing, engaging, and motivating for current research-active authors to respond to in their future publications in this exciting area of current research.
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