A biochemical study of cancer cell growth inhibitors from marine cyanobacteria

海洋蓝藻癌细胞生长抑制剂的生化研究

• 批准号: 21710237
• 负责人: TERUYA Toshiaki
• 金额: $ 2.91万
• 依托单位: University of the Ryukyus
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2009
• 资助国家: 日本
• 起止时间: 2009 至 2010
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21710237/
• 关键词: 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

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.

在我们持续的努力中分离出具有抗肿瘤活性的新型海洋蓝藻代谢产物，我们发现了双溴酰胺和bisselyngbyaside。双溴酰胺表现出有效的蛋白激酶抑制作用：PDGF刺激NRK细胞ERK（细胞外信号调节蛋白激酶）的磷酸化被10 ~ 0.1μM的双溴酰胺选择性抑制。双溴酰胺对10-0.1μM范围内AKT、PKD、plc - γ1和S6核糖体蛋白的磷酸化无影响。Biselyngbyaside对HeLa S_3细胞表现出不同的细胞毒性，IC_<50>值为0.1μg/mL，对中枢神经系统肿瘤SNB-78 （GI_<50> 0.036μM）和肺癌NCI H522 （GI_<50> 0.067μM）尤为敏感。Biselyngbyaside为compare阴性，表明它可能通过一种新机制抑制癌细胞增殖。

项目成果

Nobiletin improves hyperglycemia and insulin resistance in obese diabetic ob/ob mice

• DOI: 10.1016/j.bcp.2010.01.034
• 发表时间: 2010-06-01
• 期刊: BIOCHEMICAL PHARMACOLOGY
• 影响因子: 5.8
• 作者: Lee, Young-Sil;Cha, Byung-Yoon;Woo, Je-Tae
• 通讯作者: Woo, Je-Tae

Magnolol enhances adipocyte differentiation and glucose uptake in 3T3-L1 cells

• DOI: 10.1016/j.lfs.2009.04.001
• 发表时间: 2009-06-19
• 期刊: LIFE SCIENCES
• 影响因子: 6.1
• 作者: Choi, Sun-Sil;Cha, Byung-Yoon;Woo, Je-Tae
• 通讯作者: Woo, Je-Tae

シアノバクテリア由来の生物活性物質の単離と構造決定

蓝藻生物活性物质的分离和结构测定

• 发表时间: 2011
• 作者: 梶山雄司;末永聖武;大野修;照屋俊明
• 通讯作者: 照屋俊明

Unusual intramolecular N->0 acyl group migration occurring during conjugation of (-)-DHMEQ with cysteine

(-)-DHMEQ 与半胱氨酸缀合期间发生异常的分子内 N->0 酰基迁移

• 发表时间: 2009
• 期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19
• 作者: Kitamura;K.; Teruya;T.; Kuroda;T.; Kigoshi;H.; Suenaga;K.;Sun-Sil Choi;Byug-Yoon Cha;Takayuki Ogi;Hirokazu Sugiyama;Toshiaki Teruya;Md Abdus Salam;Ikuko Kozawa
• 通讯作者: Ikuko Kozawa

腫瘍細胞増殖阻害活性を示す新規ペプチド性化合物

具有肿瘤细胞增殖抑制活性的新型肽化合物

• 发表时间: 2009