2000 Fiscal Year Final Research Report Summary
Molecular design of anti-metastatic sugars from lipophilic anti-invasive sugar derivatives
| Project/Area Number |
09556022
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| Research Category |
Grant-in-Aid for Scientific Research (B).
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| Allocation Type | Single-year Grants |
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| Section | 展開研究 |
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| Research Field |
Bioproduction chemistry/Bioorganic chemistry
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| Research Institution | Mie University |
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Principal Investigator |
KASHIMURA Naoki Mie University, Faculty of Bioresources, Professor, 生物資源学部, 教授 (20026412)
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| Co-Investigator(Kenkyū-buntansha) |
SAIKI Ikuo Toyama Medical and Pharmaceutical University, Institute of Oriental Medicine, Professor, 和漢薬研究所, 教授 (80133776)
INAGAKI Minoru Mie University, Faculty of Bioresources, Assistant Professor, 生物資源学部, 助手 (20242935)
YOSHIDA Toshimichi Mie University, Faculty of Medicine, Professor, 医学部, 教授 (80166959)
TANIMOTO Toshiko Mukogawa Wemen's University, Faculty of Pharmaceutical Sciences, Associate Professor, 薬学部, 助教授 (10151870)
KIOKA Noriyuki Kyoto University, Faculty of Agriculture, Assistant Professor, 農学部, 助手 (90234179)
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| Project Period (FY) |
1997 – 2000
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| Keywords | lipophilic sugars / antimetstatic activities / human cancer cell lines / antiadhesive action / partially benzylated sugars / purine derivatives |
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| Research Abstract |
This project aimed to focus on the anti-metastatic action of lipophilic sugar derivatives, to make molecular design, and to find out novel lead compounds for new anti-cancer drugs, based on the previous studies on the anti-adhesive sugar derivatives. Of 500 compounds investigated, 8 derivatives were finally selected to subject to a series of in vitro and in vivo tests. Partially benzylated sugars were found to be one of the best compounds for the cadidate of new lead compounds, because of their easy availability of both various isomers and materials, nontoxicity, and effective action in in vivo tests. Especially those available from biomass such as chitin, fucoidan, and xylan, are of interest for future development. Various purine derivatives were studied on their anti-tumor activities. Several ethynylpurine derivatives were found to exhibit specific inhibitory action against the expression of adhesion molecules of human endothelial cells. It was further found that 4 compounds exhibit strong anti-growth action against more than 30 human cancer cell lines with at the concentration of less than 10^<-6>M.One of them was found to be effective in vivo.The main features of the present study include expected new mechanism, low toxicity and availability from biomass at low cost.
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