『徳島大学 教育・研究者情報データベース (EDB)』---[学外] /
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EID=338503EID:338503, Map:0, LastModified:2018年11月29日(木) 16:47:26, Operator:[大家 隆弘], Avail:TRUE, Censor:0, Owner:[宇都 義浩], Read:継承, Write:継承, Delete:継承.
種別 (必須): 学術レター (ショートペーパー) [継承]
言語 (必須): 英語 [継承]
招待 (推奨):
審査 (推奨): Peer Review [継承]
カテゴリ (推奨): 研究 [継承]
共著種別 (推奨): 国際共著 (徳島大学内研究者と国外研究機関所属研究者との共同研究) [継承]
学究種別 (推奨): 博士前期課程学生による研究報告 [継承]
組織 (推奨): 1.徳島大学.大学院社会産業理工学研究部.生物資源産業学域 (2017年4月1日〜) [継承]
著者 (必須): 1. (英) Takahashi Hideaki (日) 髙橋 秀明 (読) たかはし ひであき
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学籍番号 (推奨): **** [ユーザ]
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2. (英) Nguyen Binh Cao Quan (日) (読)
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3.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座])
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4. (英) Shahinozzaman Md (日) (読)
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5. (英) Tawata Shinkichi (日) (読)
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6. (英) Maruta Hiroshi (日) (読)
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[継承]
題名 (必須): (英) 1,2,3-Triazolyl esterization of PAK1-blocking propolis ingredients, artepillin C (ARC) and caffeic acid (CA), for boosting their anti-cancer/anti-PAK1 activities along with cell-permeability.  (日)    [継承]
副題 (任意):
要約 (任意): (英) Artepillin C (ARC) and caffeic acid (CA) are among the major anti-cancer ingredients of propolis, and block the oncogenic/melanogenic/ageing kinase PAK1. However, mainly due to their COOH moiety, cell-permeability of these herbal compounds is rather limited. Thus, in this study, in an attempt to increase their cell-permeability without any significant loss of their water-solubility, we have esterized both ARC and CA with the water-soluble 1,2,3-triazolyl alcohol through Click Chemistry. We found that this esterization boosts the anti-cancer activity of ARC and CA by 100 and over 400 folds, respectively, against the PAK-dependent growth of A549 lung cells, but show no effect on the PAK1-independent growth of B16F10 melanoma cells. Confirming this "selective" toxicity, these esters are still capable of blocking the kinase PAK1 strongly in cell culture (with IC around 5 µM), and the anti-PAK1 activity of 15A (ARC ester) and 15C (CA ester) appears to be 30-fold and 140-fold higher than ARC and CA, respectively. The 15A and 15C are 8-fold and 70-fold more cell-permeable (through the multi-drug resistant cell line EMT6) than ARC and CA, respectively. These data altogether suggest that both 15A and 15C would be far more useful than propolis for the treatment of a wide variety of PAK1-dependent diseases/disorders such as cancers, Alzheimer's diseases (AD), hypertension, diabetes (type 2), and hyper-pigmentation.  (日)    [継承]
キーワード (推奨): 1. (英) PAK1 (日) (読) [継承]
2. (英) artepillin C (日) (読) [継承]
3. (英) caffeic acid (日) (読) [継承]
4. (英) click chemistry (日) (読) [継承]
5. (英) triazolyl esters (日) (読) [継承]
発行所 (推奨):
誌名 (必須): Drug Discoveries & Therapeutics (Shandong da xue zhong ri yao wu shai xuan zhongxin/International Advancement Center for Medicine & Health Research)
(pISSN: 1881-7831, eISSN: 1881-784X)

ISSN (任意): 1881-7831
ISSN: 1881-7831 (pISSN: 1881-7831, eISSN: 1881-784X)
Title: Drug discoveries & therapeutics
Title(ISO): Drug Discov Ther
Supplier: 特定非営利活動法人 バイオ&ソーシャル・サイエンス推進国際研究交流会
Publisher: International Advancement Center for Medicine & Health Research Co., Ltd. (IACMHR Co., Ltd.)
 (NLM Catalog  (医中誌Web  (J-STAGE  (Scopus  (CrossRef (Scopus information is found. [need login])
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(必須): 104 109 [継承]
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年月日 (必須): 西暦 2017年 5月 30日 (平成 29年 5月 30日) [継承]
URL (任意):
DOI (任意): 10.5582/ddt.2017.01009    (→Scopusで検索) [継承]
PMID (任意): 28442677    (→Scopusで検索) [継承]
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指導教員 (推奨): 1.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座]) [継承]
備考 (任意): 1.(英) Article.ELocationID: 10.5582/ddt.2017.01009  (日)    [継承]
2.(英) Article.PublicationTypeList.PublicationType: Journal Article  (日)    [継承]
3.(英) KeywordList.Keyword: PAK1  (日)    [継承]
4.(英) KeywordList.Keyword: artepillin C  (日)    [継承]
5.(英) KeywordList.Keyword: caffeic acid  (日)    [継承]
6.(英) KeywordList.Keyword: click chemistry  (日)    [継承]
7.(英) KeywordList.Keyword: triazolyl esters  (日)    [継承]

標準的な表示

和文冊子 ● Hideaki Takahashi, Quan Binh Cao Nguyen, Yoshihiro Uto, Md Shahinozzaman, Shinkichi Tawata and Hiroshi Maruta : 1,2,3-Triazolyl esterization of PAK1-blocking propolis ingredients, artepillin C (ARC) and caffeic acid (CA), for boosting their anti-cancer/anti-PAK1 activities along with cell-permeability., Drug Discoveries & Therapeutics, Vol.11, No.2, 104-109, 2017.
欧文冊子 ● Hideaki Takahashi, Quan Binh Cao Nguyen, Yoshihiro Uto, Md Shahinozzaman, Shinkichi Tawata and Hiroshi Maruta : 1,2,3-Triazolyl esterization of PAK1-blocking propolis ingredients, artepillin C (ARC) and caffeic acid (CA), for boosting their anti-cancer/anti-PAK1 activities along with cell-permeability., Drug Discoveries & Therapeutics, Vol.11, No.2, 104-109, 2017.

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