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Background: Indications for various diseases such as diabetes mellitus and metabolic syndrome, etc. of Fecal Microbiota Transplantation (FMT) have been investigated. For the establishment of the FMT therapy, the examination of the solvent has not been carried out, though the use of the physiological saline is fixed, at present. We have produced the Mr. Shimizu made ultrafine bubble water (UFB) that produces a larger number of bubbles than existing UFB.Objective: To verify the usefulness of UFB, we prepared a conventional Saline and UFB-prepared microbial preparation (Bio3); (Bio3/Saline) and (Bio3/UFB). The bacterial preparations, Bio3, contain glycated bacteria, lactic acid bacteria, and butyric acid bacteria. FMT was carried out to the diabetic model mouse using these microbial preparations, and whether the disease state was improved was examined. Cultured intestinal epithelial cells (CaCO-2) were also used to test for differentiation by UFB and Saline from variations in several receptors that recognize microbiota-mRNA. In addition, glucose uptake into cells was measured.Methods: FMT with (Bio3/UFB) and (Bio3/Saline) was performed in streptozotocin-induced diabetic mice (STZ-mice) in duplicate at 0, 7 days. Blood glucose levels (7, 14 days) and blood insulin levels (14 days) were measured. Cultured intestinal epithelial cells were also used to test for differentiation by UFB and Saline from change in several receptors that recognize microbiota-mRNA (Toll-like receptors, NOD-like receptors, and RIG-I-like receptors). In addition, glucose uptake into cells was measured using fluorescently labeled glucose analog (NBDG).Results: UFB could reduce the blood glucose level of STZ-induced diabetic model mice. However, no such effects were observed in Saline. Stimulation of serially diluted Bio3 with UFB-suspension were showed significant alteration in TLR4 and IL-1B-uPNA. The amount of glucose uptake in the (Bio3/UFB) group was significantly different at 30 min, inhibited or delayed. Conclusion: It is concluded that UFB-mediated cross-talk between intestinal bacteria and intestinal epithelial cells and inhibition or delay of intestinal epithelial glucose uptake may have been associated with the reduction of blood glucose levels in diabetic model mice. The superiority of UFB as a suspension used for the transfer of bacteria has been suggested.
Rifamycin S (1) was allowed to react with Na2SO3 under mild alkaline conditions to afford sodium rifamycin SV-3-sulfonate (3). Oxidation of 3 with MnO2 gave sodium rifamycin S-3-sulfonate (4a). The reaction of 4a with aromatic amines and aliphatic secondary amines led to 3-aminorifamycin derivatives 5a-g. A novel cleavage reaction of the ansa-ring occurred to give compounds 7a-g, when 4a was allowed to react with aliphatic primary amines having at least one hydrogen atom at the α-position.
As a lead development based on the previous quantitative structure-activity relationship (QSAR) results on cerebral vasodilating activities of 1-benzyl-4-diphenylmethylpiperazines, 1-cinnamy1-4-diphenylmethylpiperazines having electron-donating groups on the cinnamyl moiety were designed.Two methods of synthesis were developed.As expected from the QSAR results, these compounds exhibited stronger potency and longer-lasting effect than cinnarizine and flunarizine.
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAzabicycloalkanes as analgetics. 3. Structure-activity relations of 1-phenyl-6-azabicyclo[3.2.1]octanes and absolute stereochemistry of (+)-1-(3-hydroxyphenyl)-6-methyl-6-azabicyclo[3.2.1]octane and its 7-endo-methyl derivativeMikio Takeda, Hirozumi Inoue, Katsuyuki Noguchi, Yasushi Honma, Masatoshi Kawamori, Goro Tsukamoto, Yasuhiko Yamawaki, Seiichi Saito, Keiichi Aoe, and Cite this: J. Med. Chem. 1977, 20, 2, 221–228Publication Date (Print):February 1, 1977Publication History Published online1 May 2002Published inissue 1 February 1977https://doi.org/10.1021/jm00212a007RIGHTS & PERMISSIONSArticle Views170Altmetric-Citations18LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit PDF (969 KB) Get e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Eleven C-terminal fragment peptides of cholecystokinin (CCK) which contain a O-sulfated tyrosine residue [CCK (27-32), CCK (27-31), CCK (27-31) amide, CCK (27-30), CCK (27-30) amide, CCK (27-29), CCK (27-29) amide, CCK (26-27), CCK (26-27) amide, CCK (25-27) and CCK (25-27) amide] were prepared by the solution method. The syntheses of these peptides were carried out by stepwise condensation in combination with fragment condensation. Analgesic effects of these fragment peptides were measured by means of the writhing test. The ED50 value of CCK (27-32) was 9.1 mg/kg and that of CCK (25-27) was 7.5 mg/kg, but the other synthetic peptides produced no statistically significant response at a dose of 8 or 10 mg/kg.
