Synthetic Studies of Maitotoxin to Elucidate Mode-of-Action
| Project/Area Number |
24245009
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Organic chemistry
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| Research Institution | Kyushu University |
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Principal Investigator |
Oishi Tohru 九州大学, 理学(系)研究科(研究院), 教授 (90241520)
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| Co-Investigator(Kenkyū-buntansha) |
KONOKI Keiichi 東北大学, 大学院農学研究科, 准教授 (40292825)
TORIKAI Kohei 九州大学, 大学院理学研究院, 助教 (20456990)
EBINE Makoto 九州大学, 大学院理学研究院, 助教 (70545574)
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| Project Period (FY) |
2012-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥46,930,000 (Direct Cost: ¥36,100,000、Indirect Cost: ¥10,830,000)
Fiscal Year 2015: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2014: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2013: ¥9,100,000 (Direct Cost: ¥7,000,000、Indirect Cost: ¥2,100,000)
Fiscal Year 2012: ¥27,430,000 (Direct Cost: ¥21,100,000、Indirect Cost: ¥6,330,000)
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| Keywords | マイトトキシン / 梯子状ポリエーテル / 化学合成 / カルシウムイオン流入活性 / 部分構造 / 生物活性 / カルシウムイオン / 有機合成化学 / 構造活性相関 / 分子プローブ / 作用標的タンパク質 |
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| Outline of Final Research Achievements |
Maitotoxin (MTX) is a marine toxin produced by the dinoflagellate. The structure-activity relationship of MTX was studied by using synthetic partial structures of MTX. MTX induced Ca2+ influx activity was inhibited by the hydrophobic part corresponding to the C’-F’ and QRS ring, and the IC50 values were estimated to be ca.50 microM, respectively. The inhibitory activity of the QR(S) ring in which the seven-membered S-ring was substituted with six-membered ring, was reduced in ca. six times. However, the NOPQR(S) ring possessing both hydrophobic and hydrophilic moiety was not active. The inhibitory activity of the LMNO ring corresponding to the hydrophilic moiety was less active than that of the hydrophobic part, and there was no significant difference between the enantiomers.
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Report
(5 results)
Research Products
(47 results)
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[Journal Article] A Novel Sperm-Activating and Attracting Factor (SAAF) from the Ascidian Ascidia sydneiensis.2013
Author(s)
Matsumori, N., Hiradate, Y., Shibata, H., Oishi, T., Simma, S., Toyoda, M., Hayashi, F., Yoshida, M, Murata, M, and Morisawa, M.
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Journal Title
Organic Letters
Volume: 15
Issue: 2
Pages: 294-297
DOI
Related Report
Peer Reviewed
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