Estrogenic/Antiestrogenic Activities of Quinoid Polycyclic Aromatic Hydrocarbons
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- Hayakawa Kazuichi
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Bekki Kanae
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Yoshita Morio
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Tachikawa Chihiro
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Kameda Takayuki
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Tang Ning
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Toriba Akira
- Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University
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- Hosoi Shinzo
- The Research Center for Pharmacy Education, Kyoto Pharmaceutical University
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Estrogenic and antiestrogenic activities of 19 quinoid polycyclic aromatic hydrocarbons (PAHQs) and 9 ketone PAHs were evaluated by the yeast two-hybrid assay using yeast cells expressing estrogen receptor-α (ERα). Binding affinity of PAHQs to ERα was assayed by the polarized fluorescence method using FluormoneTM ES2. Ten PAHQs having 3-5 rings showed antiestrogenic activities. The most strongly antiestrogenic PAHQs were 1,4-chrysenequinone and 5,6-chrysenequinone. On the other hand, benzo[a]pyrene-3,6-quinone showed the strongest estrogenic activity. However, the other compounds tested did not show so strong estrogenic/antiestrogenic activities. Binding affinity to ER was required but not sufficient for estrogenic/antiestrogenic activities of PAHQs. The length-to-breadth ratios of the rectangular planes surrounding the ring molecules and the distances between the oxygen atom of the carbonyl group and farthest hydrogen atom of estrogenic/antiestrogenic PAHQs were in narrow ranges, suggesting a structure-activity relationship. As interactions between active PAHQ and ER, hydrogen bonding between carbonyl groups and amino acid residues and van der Waals forces were considered.
収録刊行物
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- JOURNAL OF HEALTH SCIENCE
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JOURNAL OF HEALTH SCIENCE 57 (3), 274-280, 2011
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679473972736
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- NII論文ID
- 130000800088
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- NII書誌ID
- AA11316464
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- ISSN
- 13475207
- 13449702
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- NDL書誌ID
- 11094653
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- IRDB
- NDL
- Crossref
- CiNii Articles
- KAKEN
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- 抄録ライセンスフラグ
- 使用不可