| Co-Investigator(Kenkyū-buntansha) |
TSUDA Masashi Hokkaido Univ., Grad. School of Pharm. Sci., Asso. Prof., 大学院・薬学研究科, 助教授 (10261322)
SHIGEMORI Hideyuki Univ. of Tsukuba, Inst. Of App. Biochem., Asso. Prof., 応用生物化学系, 助教授 (70202108)
MORITA Hiroshi Hokkaido Univ., Grad. School of Pharm. Sci., Asso. Prof., 大学院・薬学研究科, 助教授 (70220069)
孫 歩祥 株式会社アミノアップ化学, 室長
SUN Buxiang AMINO UP Chem., Co., Ltd., Head of Lab.
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| Budget Amount *help |
¥13,500,000 (Direct Cost: ¥13,500,000)
Fiscal Year 2001: ¥13,500,000 (Direct Cost: ¥13,500,000)
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| Research Abstract |
1) A new anthracycline-derived pentacyclic metabolite, seragakinone A, and new peptides, dictyonamides A and B, were isolated from a marine-derived fungus Cocodinium sp., and the structures were determined on the basis of combination of NMR analyses, X-ray analysis, and degradation experiments. Seragakinone A showed antimicrobial activity, while dictyonamide A exhibited inhibitory activity against CDK-4.
2) Three new lycopodium alkaloids, seratezomines A 〜 C, with seco-seratinine-type, a seratenine-type, and a lycodoline-type skeletons, respectively, were isolated from the club moss Lycopodium serratum var. serratum. On the other hand, three new alkaloids, complanadine A, lyconadine A, 11-hydroxy lycodine, were isolated from lycopodium complanatum.
3) Fifteen new Daphniphyllum alkaloids, daphnezomines A 〜 G and daphnicyclidins A 〜 H were isolated from Daphniphyllum humile and D. teijsmanni. Daphnezomines A and B are novel alkaloids with aza-adamantane core, while daphnezomines F and G have a 1-azaobicyclo[5.2.2]undecene ring system. Daphnicyclidins A 〜 H possess unque fused hexa- or pentacyclic skeletons.
4) Three new bicyclic peptides, celogentins A 〜 C, were isolated together with moroidin from the seeds of Celosia argentea. Celogentins A 〜 C and moroidin inhibited the polymerization of tubulin. Structure-activity relationship study using four moroidin derivatives as well as Celogentins A 〜 C and moroidin indicated that the bicyclic ring system including non-peptide connections among β^S-Leu, Trp, and His residues with ring size and conformations suitable for interaction with tubulin would be important for their activity.
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