The Pd-catalyzed cross coupling of racemic tertiary allylic carbonates and allyl boronates is described. This reaction generates all-carbon quaternary centers in a highly regioselective and enantioselective fashion. The outcome of these reactions is consistent with a process that proceeds by way of 3,3’-reductive elimination of bis(η1-allyl)palladium intermediates. Strategies for distinguishing the product alkenes and application to the synthesis of cuparenone are also described.
A far-infrared radiation (FIR) catalytic laboratory dryer was designed by us and used to dry tomato. The kinetics of drying of tomato slices with FIR energy was dependent on both the distance from the heat source and the sample thickness. Numerical evaluation of the simplified Fick’s law for Fourier number showed that the effective moisture diffusivity increased from 0.193×10<sup>–9</sup> to 1.893×10<sup>–9</sup> m<sup>2</sup>/s, from 0.059×10<sup>–9</sup> to 2.885×10<sup>–9</sup> m<sup>2</sup>/s, and, from 0.170×10<sup>–9</sup> to 4.531×10<sup>–9</sup> m<sup>2</sup>/s for the 7, 9, and 11 mm thick slices as moisture content decreased. Application of FIR enhanced the flavour of the dried tomatoes by 36.6% when compared with the raw ones. The results demonstrate that in addition to shorter drying times, the flavour of the products can be enhanced with FIR. Therefore, FIR drying should be considered as an efficient drying method for tomato with respect to minimization of processing time, enhancement in flavour, and improvements in the quality and functional property of dried tomatoes.
We previously constructed a collection of fission yeast strains that express various mammalian cyclic nucleotide phosphodiesterases (PDEs) and developed a cell-based high throughput screen (HTS) for small molecule PDE inhibitors. Here we describe a compound, BC54, that is a selective inhibitor of enzymes from the cAMP-specific PDE4 and PDE7 families. Consistent with the biological effect of other PDE4 and PDE7 inhibitors, BC54 displays potent anti-inflammatory properties and is superior to a combination of rolipram (a PDE4 inhibitor) and BRL50481 (a PDE7A inhibitor) for inducing apoptosis in chronic lymphocytic leukemia (CLL) cells. We further exploited PKA-regulated growth phenotypes in fission yeast to isolate two mutant alleles of the human PDE4B2 gene that encode enzymes possessing single amino acid changes that confer partial resistance to BC54. We confirm this resistance to both BC54 and rolipram via yeast-based assays and, for PDE4B2T407A, in vitro enzyme assays. Thus, we are able to use this system for both chemical screens to identify biologically-active PDE inhibitors and molecular genetic studies to characterize the interaction of these molecules with their target enzymes. Based on its potency, selectivity, and effectiveness in cell culture, BC54 should be a useful tool to study biological processes regulated by PDE4 and PDE7 enzymes.
Edible and medicinal fungi (mushrooms) are widely applied to functional foods and nutraceutical products because of their proven nutritive and medicinal properties. Phellinus sensu lato is a well-known medicinal mushroom that has long been used in preventing ailments, including gastroenteric dysfunction, diarrhea, hemorrhage, and cancers, in oriental countries, particularly in China, Japan, and Korea. Polysaccharides represent a major class of bioactive molecules in Phellinus s. l., which have notable antitumor, immunomodulatory, and medicinal properties. Polysaccharides that were isolated from fruiting bodies, cultured mycelia, and filtrates of Phellinus s. l. have not only activated different immune responses of the host organism but have also directly suppressed tumor growth and metastasis. Studies suggest that polysaccharides from Phellinus s. l. are promising alternative anticancer agents or synergizers for existing antitumor drugs. This review summarizes the recent development of polysaccharides from Phellinus s. l., including polysaccharide production, extraction and isolation methods, chemical structure, antitumor activities, and mechanisms of action.
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