| Project/Area Number |
61430026
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| Research Category |
Grant-in-Aid for General Scientific Research (A)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | KYUSHU UNIVERSITY |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
IMOTO Taiji KYUSHU UNIVERSITY, 薬学部, 教授 (90038282)
SAKAI Kiyoshi KYUSHU UNIVERSITY, 薬学部, 教授 (90153840)
KOMORI Tetsuya KYUSHU UNIVERSITY, 薬学部, 教授 (80037572)
NISHIOKA Itsuo KYUSHU UNIVERSITY, 薬学部, 教授 (20037568)
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| Project Period (FY) |
1986 – 1987
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| Project Status |
Completed (Fiscal Year 1987)
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| Budget Amount *help |
¥26,900,000 (Direct Cost: ¥26,900,000)
Fiscal Year 1987: ¥6,000,000 (Direct Cost: ¥6,000,000)
Fiscal Year 1986: ¥20,900,000 (Direct Cost: ¥20,900,000)
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| Keywords | Drugmetabolism / Alkaloid / Tannin / Glycosphingolipid / Platelet-Activating-Factor / Lysozyme / Proton Nuclear Magnetic Resonance Spectrometry / 構造決定 / 代謝産物 / 植物ポリフェノール / 海産動物糖脂質 / 立体化学 / ストリキニーネ / スコポラミン / グリコスフインゴリピド / プロスタグランジン / FT-NMR |
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| Research Abstract |
WITH THE VIEW TO ELUCIDATING THE STEREOCHEMISTRY ON A COMPLEX STRUCTURE OF BIOLOGICALLY ACTIVE PLANT- AND ANINAL-CONSTITUENTS AND OF DRUG METABOLITES, A FOLLOWING JOINT PROJECT WAS CONDUCTED BY UTILIZING THE 270 MHz FT-NMR SPECTROMETRY. METABOLISM OF ALKALOIDS WAS ALSO INVESTIGATED. 1. METABOLISM OF TWO ALKALOIDS, STRYCHINE AND SCOPOLAMINE WAS STUDIED IN EXPERIMENTAL ANIMALS. FIVE URINARY METABOLITES OF STRYCHININE IN RATS WERE ISOLATED AND IDENTIFIED BY COMPARISON WITH AUTHENTIC SAMPLES. IN VITRO METABOLITES OF STRYCHNINE AND SCOPOLAMINE FORMED WITH LIVER MICROSOMES OF RATS WERE DETERMINED, AND EFFECT OF INDUCERS OF DRUG METABOLIZING ENZYMES WAS EXAMINED. THE STRUCTURES OF FOUR URINARY METABOLITES OF SCOPOLAMINE IN RATS AND RABBITS WERE ELUCIDATED. 2. CHEMICAL EXAMINATIONS ON TANNINS AND RELATED COMPOUNDS IN VARIOUS BEVERAGE TEAS (3 SPECIES), COMMERCIAL RHUBARBS (4 SPECIES), FAGACEOUS PLANTS (6 SPECIES) IN JAPAN AND TAIWANESE MEDICINAL PLANTS (12 SPECIES) HAVE LED TO THE ISOLATION AND
… More
CHARACTERIZATION OF TOTALLY 120 COMPOUNDS ABOUT 70 NEW TANNINGS. 3. THE ECHINODERMATA IN MARINE INVERTEBRATES WHICH IS RICH IN LIPIDS ATTRACTED A CONSIDERABLE ATTENTION AND, FROM THE STARFISH ACANTHASTER PLANCI, SIX CEREBROSIDES AND TWO DIHEXOSIDE TYPE GLYCOSPHINGOLIPIDS WERE NEWLY OBTAINED IN A PURE STATE AND CHARACTERIZED ON THE BASIS OF CHEMICAL AND SPECTROSCOPIC EVIDENCES. THE STEREOCHEMISTRY OF THE PHYTOSPHINGOSINE BASE WAS DETERMINED BY COMPARISON WITH THE SYNTHESIZED COMPOUND. 4. ASYMMETRIC SYNTHESIS OF PLATELET-ACTIVATING FACTOR (PAF) AND ITS ENANTIOMER BY USING BIOCATALYSTS WAS STUDIED. (1) ENZYME CATALYZED ASYMMETRIC HYDROLYSIS OF 1,3-DI-O-ACYL-2-O-BENZYLGLYCEROL AFFORDED OPTICALLY ACTIVE MONOACYLATE, WHICH WAS CONVERTED INTO 2,3-O-ISOPROPYRIDENE-sn-GLYCEROL. (2) MICROBIAL REDUCTION OF THE PRO-CHIRAL <alpha>-KETOESTER AFFORDED OPTICALLY PURE <alpha>-HYDROXYESTER, WHICH WAS CONVERTED INTO (+)-AND (-)-BATYL ALCOHOL, A KEY SYNTHETIC INTERMEDIATE FOR PAF. 5. NMR ANALYSIS HAVE BEEN MADE OF H-D EXCHANGE RATES OF TRYPTOPHAN INDOLE N-1 HYDROGENS IN CHEMICALLY MODIFIED LYSOZYMES. THE EXCHANGE RATES FOR TRYPTOPHAN RESIDUES REMOTE FROM THE MODIFICATION SITES ARE PERTURBED AND ARE RELATED TO THE LOCAL FLUCTUATIONS. THE CHANGE IN THE LOCAL FLUCTUATION DUE TO THE CHEMICAL MODIFICATION IS RELATED TO THE MINOR CHANGE IN THE LOCAL CONFORMATION. Less
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