2012 Fiscal Year Final Research Report
Synthetic approaches toward the identification of target proteins of physalins
| Project/Area Number |
22603014
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
ケミカルバイオロジー
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| Research Institution | The Institute of Physical and Chemical Research |
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Principal Investigator |
HIRAI Go 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 専任研究員 (50359551)
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| Co-Investigator(Renkei-kenkyūsha) |
TSUCHIYA Ayako 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 客員研究員 (80442987)
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| Research Collaborator |
OZAWA Masaaki 独立行政法人理化学研究所, 袖岡有機合成化学研究室, 特別研究員 (30617262)
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| Project Period (FY) |
2010 – 2012
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| Keywords | ホオズキ / ステロイド / 有機合成 / NF-kB / physalin / ワンポット反応 / ドミノ反応 / 構造活性相関 |
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| Research Abstract |
In this research grant, we intended to clarify the mode of action of oxygenated steroids, physalins, by means of organic synthesis and chemical biology. First, the constructions of E- and C-ring moieties from cage-shaped DFGH-ring compound of physalin B, whose synthetic strategy has been already established, were investigated. The synthesis of DEFGH-ring compounds were realized by adopting our original strategy to construct the unique cage-shaped skeleton as a key reaction for the precursor, which possessed an appropriate functionality at C17 on F-ring. For C-ring moiety, the establishing the strategy to form the C-C bonds at C13 or C14 of the precursor of DEFHG-ring compounds was also successful. Furthermore, structure-activity relationship study of synthetic DEFGH-ring compounds and natural products of oxygenated steroids isolated from physalis plants was carried out. As a result, we found that physalin B showed potent inhibitory activity for NF-κB activation stimulated by TNF-α and have different mode of action with other oxygenated steroids.
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[Journal Article]2013
Author(s)
Masaaki Ozawa, Masaki Morita, Go Hirai, Satoru Tamura, Masao Kawai, Ayako Tsuchiya, Kana Oonuma, Keiji Maruoka, and Mikiko Sodeoka
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Journal Title
ACS. Med. Chem. Lett.
Volume: (in press)
Peer Reviewed
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[Journal Article]2012
Author(s)
Masaki Morita, Go Hirai, Meguni Ohkubo Hiroyuki Koshino, Daisuke Hashizume, Keiji Maruoka, and Mikiko Sodeoka
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Journal Title
Org. Latt.
Volume: 14
Pages: 3434-3437
Peer Reviewed
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