1993 Fiscal Year Final Research Report Summary
Search for PAF antagonits from marine organisms
| Project/Area Number |
04453146
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| Research Category |
Grant-in-Aid for General Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | Hokkaido University |
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Principal Investigator |
KOBAYASHI Jun'ichi Hokkaido Univ. Fac. Pharm. Sci, Professor, 薬学部, 教授 (90221241)
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| Co-Investigator(Kenkyū-buntansha) |
SHIGEMORI Hideyuki Hokkaido Univ. Fac. Pha. Sci, Associate Professor, 薬学部, 助手 (70202108)
ISHIBASHI Masami Hokkaido Univ. Fac. Pha. Sci, Associate Professor, 薬学部, 助教授 (90212927)
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| Project Period (FY) |
1992 – 1993
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| Keywords | PAF antagonist / Sponge / Platelet aggregation / Marine organisms / Terpene / Alkaloid |
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| Research Abstract |
PAF(platelet activating factor, 1-0-alkyl-2(R)-(acetylglyceryl)-3-phosphorylcholine) causea platelet aggregation, chemotaxis, and degranulation of polymorphonuclear leukocytes, smooth muscle contraction, m vascular permeability, and hyupotension. Recent studies have shown that PAF may be involved in many inflammator, respiratory, and cardiovascular diseases.
In our project of search for new PAF autagonists from marine organisms, we systematically screened lipophilic extracts of Okinawan marine invertebrates and microorganisms for inhibition of PAF production due to A23817 and inhibition of PAF-induced platelet aggregation to find that several sponge metabolites such as manoalide, luffariolide A, bistheonllide A, swinholide A, niphatesine A, and heteronemin, exhibited PAF antagonistic activities with IC_<50> values of 0.05 - 5.0 mu g /mL.More powerful and specific PAF antagonistis may be fond through further studies of structure-activity relationship on the compounds (terpenes, alkaloid, etc.) described above.
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