Effects of KCA-098 on Bone Metabolism: Comparison with Those of Ipriflavone.
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概要
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We previously found that 3, 9-bis(<I>N</I>, <I>N</I>-dimethylcarbamoyloxy)-5<I>H</I>-benzofuro[3, 2-<I>c</I>]quinoline-6-one (KCA-098) inhibited bone resorption in organ culture. In this study, to determine if KCA-098 is therapeutically applicable for the treatment of osteoporosis, we compared the effect of KCA-098 on bone tissues with that of ipriflavone, a drug that is clinically used for the treatment of osteoporosis. Both KCA-098 and ipriflavone inhibited parathyroid hormone-, prostaglandin E<SUB>2</SUB>-, 1α, 25-dihydroxyvitamin D<SUB>3</SUB>- and interleukin 1β-induced bone resorption of fetal rat bones, but the inhibitory activity of KCA-098 was more potent than that of ipriflavone. In fact, the effective concentrations of KCA-098 were 10 to 100 times lower than those of ipriflavone. Oral administration of KCA-098 (1 and 3 mg/kg) or ipriflavone (100 mg/kg) to ovariectomized rats on a low-calcium diet increased the breaking force and bone density of the femora, indicating that KCA-098 is as effective on the whole animal as ipriflavone. Furthermore, KCA-098 increased the length and calcium content of 9-day chick embryonic femora cultured in vitro, whereas ipriflavone did not, suggesting that KCA-098 had a direct stimulatory effect on bone mineralization. Therefore, KCA-098 seems to be more potent than ipriflavone in stimulating bone tissue formation and may thus be expected to become a useful agent for the treatment of osteoporosis.
- 公益社団法人 日本薬理学会の論文
著者
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Arai Nobuhiko
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Kojima Masami
Central Research Laboratory Kissei Pharmaceutical
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Endo Hiroyoshi
Department Of Physiological Chemistry Faculty Of Pharmaceutical Sciences Teikyo University
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Nagata Hideo
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Itoh Fumiaki
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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UJIIE Arao
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
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Ujiie Arao
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Tsutsumi Naoyuki
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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Kawashima Kohtaro
Department of Physiological Chemistry, Faculty of Pharmaceutical Sciences, Teikyo University
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Tsuyuki Junko
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
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Arai Nobuhiko
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.
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