Co-Investigator(Kenkyū-buntansha) |
ルナール 純子 東京医科大学, 講師 (90074632)
IMAKURA Yasuhiro Faculty of Pharmaceutical Sciences, The University of Tokushima, 薬学部, 助手 (10112640)
KIHARA Masaru Faculty of Pharmaceutical Sciences, The University of Tokushima, 薬学部, 助教授 (80035550)
RENARD Junko Department of Microbiology, Tokyo Medical College
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Budget Amount *help |
¥1,800,000 (Direct Cost: ¥1,800,000)
Fiscal Year 1986: ¥300,000 (Direct Cost: ¥300,000)
Fiscal Year 1985: ¥1,500,000 (Direct Cost: ¥1,500,000)
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Research Abstract |
Novel alkaloids, leucotamine, 0-demethylleucotamine, 3-0-acetylungiminorine, demethylmaritidine and (-)-N-demethyllycoramine, were isolated from Amaryllidaceae plants, namely Leucojum asetivum L. and Hymenocallis rotata. The structure of latifine isolated from Crinum latifolium was determined by its spectral data and by the synthesis of its racemate. The structures of acid A and acid B, oxidation products of lycoramine, were confirmed by their spectral data and by the synthesis of acid A. The apogalanthamine analogs were prepared by photochemical reaction of halo-N-benzyl- <beta> -phenethylamine derivatives. A novel synthesis of 4-phenyl-1,2,3,4-tetrahydro-4-isoquinolinols was carried out by cyclization of phenacylamine derivatives with zerovalent nickel. With regard to Amaryllidaceae alkaloids(biosynthesized from norbelladine <C_(15)> <H_(17)> N <O_3> ), tests for antiviral activity in a system of herpes simplex virus/ Vero cells gave the following results:(1)some activity was found in 3 groups of compounds, out of seven, namely Lycorine, Tazettine and Lycorenine. (2)Compounds with a 0.2 or less, chemotherapeutic index had as a common structure a hexahydroindole ring. (3)The activity of those alkaloids was due to their capacity to inhibit the viral multiplication. (4)The mechanism could be explained by the inhibition of DNA polymerase activity.
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