- 著者
- Keiko MORITO Toshiharu HIROSE Junei KINJO Tomoki HIRAKAWA Masafumi OKAWA Toshihiro NOHARA Sumito OGAWA Satoshi INOUE Masami MURAMATSU Yukito MASAMUNE
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Biological and Pharmaceutical Bulletin (ISSN:09186158)
- 巻号頁・発行日
- vol.24, no.4, pp.351-356, 2001 (Released:2002-04-26)
- 参考文献数
- 37
- 被引用文献数
- 391 473
The human estrogen receptor (hER) exists as two subtypes, hER α and hER β, that differ in the C-terminal ligand-binding domain and in the N-terminal transactivation domain. In this study, we investigated the estrogenic activities of soy isoflavones after digestion with enteric bacteria in competition binding assays with hER α or hER β protein, and in a gene expression assay using a yeast system. The estrogenic activities of these isoflavones were also investigated by the growth of MCF-7 breast cancer cells. Isoflavone glycoside binds weakly to both receptors and estrogen receptor-dependent transcriptional expression is poor. The aglycones bind more strongly to hER β than to hER α. The binding affinities of genistein, dihydrogenistein and equol are comparable to the binding affinity of 17 β-estradiol. Equol induces transcription most strongly with hER α and hER β. The concentration required for maximal gene expression is much higher than expected from the binding affinities of the compounds, and the maximal activity induced by these compounds is about half the activity of 17 β-estradiol. Although genistin binds more weakly to the receptors and induces transcription less than does genistein, it stimulates the growth of MCF-7 cells more strongly than does genistein.
- 著者
- Masateru Ono Chikako Masuoka Mihoko Koto Michiko Tateishi Haruki Komatsu Hiromasa Kobayashi Keiji Igoshi Yasuyuki Ito Masafumi Okawa Toshihiro Nohara
- 出版者
- 公益社団法人日本薬学会
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.50, no.10, pp.1416-1417, 2002 (Released:2002-10-01)
- 参考文献数
- 6
- 被引用文献数
- 5 10
A new ortho-benzoyloxyphenyl acetic acid ester, called vaccihein A (1), was isolated from the fruit of rabbiteye blueberry (Vaccinium ashei). The chemical structure was determined on the basis of spectroscopic data. Compound 1 had antioxidative activity using the ferric thiocyanate method. In addition, 1 showed a scavenging effect on the stable free radical 1,1-diphenyl-2-picrylhydrazyl.
- 著者
- Yu-Ming Chi Motoyuki Nakamura Toyokichi Yoshizawa Xi-Ying Zhao Wen-Mei Yan Fumio Hashimoto Junei Kinjo Toshihiro Nohara Shinobu Sakurada
- 出版者
- 公益社団法人日本薬学会
- 雑誌
- Biological and Pharmaceutical Bulletin (ISSN:09186158)
- 巻号頁・発行日
- vol.28, no.10, pp.1989-1991, 2005 (Released:2005-10-01)
- 参考文献数
- 18
- 被引用文献数
- 14 24
To determine the antinociceptive mechanism of incarvillateine (INCA), the opiate antagonists nor-binaltorphimine (nor-BNI), β-funaltrexamine (β-FNA) and naltrindole (NTI) were pretreated prior to its injection in a formalin test. The antinociceptive effect of INCA was antagonized by nor-BNI (κ-receptor antagonist) and β-FNA (μ-receptor antagonist), while NTI (δ-receptor antagonist) did not influence its effect. Furthermore, the antinociceptive effect of INCA was blocked by theophylline (THEO), an adenosine-receptor antagonist. These results suggested that the antinociceptive effect arose from the activation of μ-, κ-receptors and adenosine-receptor.