Twist Form of Teleocidin Derivatives is Active in in Vivo Tumor Promotion by (-)-Benzolactam-V8-310
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概要
- 論文の詳細を見る
Teleocidin derivatives and the core structure, (-)-indolactam-V ((-)-IL-V), adopt two conformations in solution, the "twist" and he "sofa" forms. (-)-Benzolactam-V8-310 ((-)-BL-V8-310), which specifically adopts the twist form in solution, has been reported to have a significant effect on HL-60 cells and protein kinase C affinity. In this paper, we describe the biological activity with regard to tumor promotion on mouse skin and the wide variety of biological activity of (-)-BL-V8-310 and its derivatives. In both twist and sofa forms (-)-BL-V8-310 inhibited specific ^3H-12-O-tetradecanoylphorbol-13-acetate (TPA) binding to a particulate fraction of mouse skin more strongly than (-)-IL-V. The doses for 50% inhibition (IC_<50>) of (-)-IL-V, (-)-BL-V8-310,and teleocidin B-4 were 1000,400 and 12nM, respectively. As for the induction of tumor necrosis factor-α(TNF-α) release into the medium from HL-60 cells, the EC_<200> values, which are the concentrations of the compound required to achieve 200 pg/ml TNF-α in the medium, were 1700,500 and 19 nM for (-)-IL-V, (-)-BL-V8-310 and telecidin B-4,respectively. The same amounts (5.5 nmol per application) of (-)-BL-V8-310 and teleocidin B-4,induced tumors on mouse skin initiated with 7,12-dimethylbenz(a)anthracene (DMBA) in 13.3% abd 86.7% of tumor-bearing mice, respectively, in week 20. These results confirmed that the twist form of teleocidin derivatives is the active form as far as the induction of biological activity is concerned. Also (-)-BL-V8-310 is a new synthetic tumor promoter designed from data obtained using the receptor cavity model of TPA-type tumor promoters.
- 公益社団法人日本薬学会の論文
- 1998-05-15
著者
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遠藤 泰之
東北薬科大学薬学部
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ENDO Yasuyuki
Faculty of Pharmaceutical Sciences, The University of Tokyo
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SHUDO Koichi
Faculty of Pharmaceutical Sciences, The University of Tokyo
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FUJIKI Hirota
Saitama Cancer Center Research Institute
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Shudo Koichi
Graduate School Of Pharmaceutical Sciences The University Of Tokyo
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Shudo Koichi
Faculty Of Pharmaceutical Science Kyushu University
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SUEOKA Naoko
Saitama Cancer Center Research Institute
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Shudo K
Research Foundation Itsuu Laboratory
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SUGANUMA Masami
Saitama Cancer Center, Research Institute for Clinical Oncology
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Komori Atsumasa
Saitama Cancer Center Research Institute
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OKABE Sachiko
Saitama Cancer Center Research Institute
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Okabe S
Kyoto Pharmaceutical Univ. Kyoto Jpn
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Sueoka Naoko
Saitama Cancer Center
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Fujiki H
Saitama Cancer Center
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Fujiki Hirota
Laboratory Of Biochemistry Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Fujiki Hirota
Saitama Cancer Center
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Sugihara M
Saitama Cancer Center Saitama Jpn
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Endo Yasuyuki
Faculty Of Pharmaceutical Sciences Tohoku Pharmaceutical University
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Suganuma Masami
Research Institute For Clinical Oncology Saitama Cancer Center
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Okabe Sachiko
Saitama Cancer Center
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SUGANUMA Masami
Saitama Cancer Center
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