2000 Fiscal Year Final Research Report Summary
Development of a novel antitumor agent based on a marine alkaloid lamellarin
| Project/Area Number |
11660207
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Fisheries chemistry
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| Research Institution | Nagasaki University |
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Principal Investigator |
ISHIBASHI Fumito Nagasaki University, Faculty of Fisheries, Associate Professor, 水産学部, 助教授 (10192486)
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| Co-Investigator(Kenkyū-buntansha) |
ODA Tatsuya Nagasaki University, Faculty of Fisheries, Associate Professor, 水産学部, 助教授 (60145307)
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| Project Period (FY) |
1999 – 2000
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| Keywords | Lamellarin / Marine Natural Product / Alkaloid / Cytotoxicity / Structure-Activity Relationship |
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| Research Abstract |
The lamellarins are a group of DOPA-derived polycyclic alkaloids which were first isolated from the prosobranch mollusc Lamellaria sp.and a number of the members are known to exhibit interesting biological activities involving cytotoxicity, immunomodulatory activity, HIV-1 integrase inhibitory activity, and MDR reversal activity.
We have accomplished first total syntheses of lamellarin D (1a) and H (1b) and found that the former showed potent cytotoxicity against several cell lines. In order to obtain a basic information on the structure-activity relationship of lamellarins, ten derivatives of 1a varying the substituents on the parent ring-system were synthesized and their cytotoxicities were evaluated in terms of the inhibition of colony formation using HeLa cells.
As the result, it appeared that the hydroxyl groups at C-8 and C-20 positions of 1a were important for expression of the activity, while the hydroxyl group at C-14 position and the two methoxy groups at C-13 and C-21 positions were not essential for the activity.
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Research Products
(2 results)
