2018年11月
Inhibitor for Fc epsilon RI expression on mast cell from Verbasucum thapsus L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- ,
- ,
- ,
- 巻
- 28
- 号
- 20
- 開始ページ
- 3342
- 終了ページ
- 3345
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmcl.2018.09.007
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
We found out 2',3'-dihydroxypuberulin from South American medicinal plant, V. thapsus L., as a candidate of an anti-allergic lead which inhibits the expression of high-affinity receptor of IgE (Fc epsilon RI) on the surface of mast cells. Furthermore, the analysis of structure-activity relationship by using synthesized 2',3'-dihydroxypuberulin analogs revealed that both hydroxy groups in the side chain and both of methyl moieties on phenolic hydroxy groups were crucial for potent activity, but absolute configuration of C-3' position wasn't. The active principle, 2',3'-dihydroxypuberulin, was disclosed to down-regulate the mRNA level of beta-chain of Fc epsilon RI, different from previous reported active natural product reducing.-chain level.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bmcl.2018.09.007
- ISSN : 0960-894X
- eISSN : 1464-3405
- PubMed ID : 30217416
- Web of Science ID : WOS:000447383900012