4-Hydroxy-2-pyridone alkaloids: Structures and synthetic approaches

Theanine is a non-protein amino acid that occurs naturally in the tea plant (Camellia sinensis) and contributes to the favourable taste of tea. It is also associated with effects such as the enhancement of relaxation and the improvement of concentration and learning ability. It is also linked with health benefits including the prevention of certain cancers and cardiovascular disease, the promotion of weight loss and enhanced performance of the immune system. Thus, there has been a significant rise in the demand for theanine. While theanine has been chemically and biologically synthesised, techniques to isolate theanine from natural sources remain an important area of research. In this review article, the properties and health benefits of theanine are summarised and the synthesis and isolation of theanine are reviewed and discussed. Future perspectives for the isolation of theanine from natural sources are also outlined.

L-Theanine: properties, synthesis and isolation from tea.

Pyrano[3,2-c]pyridone and pyrano[3,2-c]quinolone structural motifs are commonly found in alkaloids manifesting diverse biological activities. As part of a program aimed at structural simplification of bioactive natural products utilizing multicomponent synthetic processes, we developed compound libraries based on these privileged heterocyclic scaffolds. The selected library members display low nanomolar antiproliferative activity and induce apoptosis in human cancer cell lines. Mechanistic studies reveal that these compounds induce cell cycle arrest in the G2/M phase and block in vitro tubulin polymerization. Because of the successful clinical use of microtubule-targeting agents, these heterocyclic libraries are expected to provide promising new leads in anticancer drug design.

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Structural simplification of bioactive natural products with multicomponent synthesis. 2. Antiproliferative and antitubulin activities of pyrano[3,2-c]pyridones and pyrano[3,2-c]quinolones

Phylogenetic relationships among members of the Fusarium solani species complex in human infections and the descriptions of F. keratoplasticum sp. nov. and F. petroliphilum stat. nov.

According to an aspect of the invention, articles are provided which comprise a substrate and a ceramic coating which covers at least a portion of the substrate surface. The ceramic coating includes raised ceramic shells connected by a ceramic layer that is conformal with the substrate. According to another aspect of the present invention, carbon nanotubes are provided, which comprise a ceramic coating covering at least a portion of the carbon nanotubes.

Articles having ceramic coated surfaces

In the course of screening for drugs that suppress the Ca(2+)-mediated growth inhibition in a yeast mutant, we found that the metabolite of Fusarium sp. strain YCM1008 inhibited Ca(2+)-signaling. A novel pyrano-pyridone, YCM1008A was isolated from the fermentation broth using HLB column chromatography followed by HPLC, and the structure was elucidated by spectral analysis. YCM1008A suppressed Ca(2+)-induced growth inhibition of the Saccharomyces cerevisiae (Deltazds1Deltasyr1) mutant.

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YCM1008A, a novel Ca2+-signaling inhibitor, produced by Fusarium sp. YCM1008.

DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, wherein R1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR4 or the like; R2 represents hydrogen or COR5 ; R3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR6, with the proviso that the compound wherein R1, R2 and Z each represents hydrogen, R3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.!

DC 107 derivatives and treatment methods

Gamma-glutamylcysteine synthetase (gammaGCS, EC 6.3.2.2) catalyzes the formation of gamma-glutamylcysteine from L-glutamic acid (Glu) and L-cysteine (Cys) in an ATP-dependent manner. While gammaGCS can use various amino acids as substrate, little is known about whether it can use non-amino acid compounds in place of Cys. We determined that gammaGCS from Escherichia coli has the ability to combine Glu and amines to form gamma-glutamylamides. The reaction rate depended on the length of the methylene chain of the amines in the following order: n-propylamine > butylamine > ethylamine >> methylamine. The optimal pH for the reaction was narrower and more alkaline than for the reaction with an amino acid. The newly found catalytic ability of gammaGCS was used in the production of theanine (gamma-glutamylethylamine). The resting cells of E. coli expressing gammaGCS, in which ATP was regenerated through glycolysis, synthesized 12.1 mM theanine (18 h) from 429 mM ethylamine.

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A Novel Catalytic Ability of γ-Glutamylcysteine Synthetase of Escherichia coli and Its Application in Theanine Production

topoisomerases, we have screened cultures of actinomycetes and fungi for their ability to inhibit selectively the growth of bacteriophage TP-68 at the concentration that shows no apparent antibacterial activity against NUB3620. In the course of microbial screening, strain KYI1768 was identified to produce active metabolites. We described here production including fermentation and isolation, and biological activity of novel pyrrole-amide antitumor antibiotics, pyrronamycin A and B, produced by Streptomyces sp. The producing organism KYI 1768 was isolated from a soil sample collected in Okazaki city, Aichi prefecture, Japan and assigned to the Streptomyces sp. Fermentation was carried out at 25°C for 42 hours with appropriate aeration and agitation in 30-liter jar fermenter containing the 15 liters of culture medium consisting of glycerol 5%, dry yeast 1.5%, KH2PO4 0.05%, MgSO4-7H2O 0.05%,

Pyrronamycin A and B, novel antitumor antibiotics containing pyrrole-amide repeating unit, produced by Streptomyces sp.

Disclosed are a neural stem cell propagation accelerator which contains a compound produced by Penicillium sp. strain CND1007 (FERM BP-10917) or a pharmacologically acceptable salt thereof, a novel compound produced by Penicillium sp. strain CND1007 or a pharmacologically acceptable salt thereof as an effective component, and a method for the production of neural stem cells in which the neural stem cells are cultured and propagated in the presence of a compound produced by Penicillium sp. CND1007 or a pharmacologically acceptable salt thereof, and the neural stem cells are collected from the culture material.

Shingo Kakita

Papers

YCM1008A, a novel Ca2+-signaling inhibitor, produced by Fusarium sp. YCM1008.

DC 107 derivatives and treatment methods

A Novel Catalytic Ability of γ-Glutamylcysteine Synthetase of Escherichia coli and Its Application in Theanine Production

Pyrronamycin A and B, novel antitumor antibiotics containing pyrrole-amide repeating unit, produced by Streptomyces sp.

Nerve trunk cell propagation accelerator