| Project/Area Number |
21710237
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Living organism molecular science
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| Research Institution | University of the Ryukyus |
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Principal Investigator |
TERUYA Toshiaki University of the Ryukyus, 教育学部, 准教授 (90375428)
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| Project Period (FY) |
2009 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2010: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2009: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
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| Keywords | シアノバクテリア / ビセリングビアサイド / ビセブロモアミド / プロテインキナーゼ阻害 / Bisebromoamide / 細胞増殖阻害活性 / Hela S_3腫瘍細胞 / 新規鎖状ペプチド / Biselyngbyaside / 異常アミノ酸 / 鎖状ペプチド / プロテインキナーゼ阻害活性 / マクロリド配糖体 / HeLa S_3腫瘍細胞 |
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| Research Abstract |
In our ongoing efforts to isolate novel marine cyanobacterial metabolites with antitumor activity, we found bisebromoamide and biselyngbyaside. Bisebromoamide exhibited potent protein kinase inhibition: the phosphorylation of ERK (extracellular signal regulated protein kinase) in NRK cells by PDGF (platelet-derived growth factor)-stimulation was selectively inhibited by treatment with 10 to 0.1μM of bisebromoamide. Bisebromoamide had no effect on the phosphorylation of AKT, PKD, PLCγ1, or S6 ribosomal protein at 10-0.1μM. Biselyngbyaside exhibited cytotoxicity against HeLa S_3 cells with an IC_<50> value of 0.1μg/mL and exhibited differential cytotoxicities : the central nervous system cancer SNB-78 (GI_<50> 0.036μM) and lung cancer NCI H522 (GI_<50> 0.067μM) were especially sensitive. Biselyngbyaside was COMPARE-negative, indicating that it likely inhibits cancer cell proliferation through a novel mechanism.
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