Tsutsumi N, Kawashima K, Arai N, Nagata H, Kojima M, Ujiie A, Endo H
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan.
Bone Miner. 1994 Mar;24(3):201-9. doi: 10.1016/s0169-6009(08)80137-7.
The effects of 3,9-bis(N,N-dimethylcarbamoyloxy)-5H-benzofuro[3,2-c]quinoli ne-6-one (KCA-098), a derivative of coumestrol, on bone resorption was studied in organ cultures of 20-day fetal rat femora. KCA-098 increased the length, dry weight, and calcium and phosphorus contents of parathyroid hormone (PTH)-treated fetal rat femur. As PTH significantly reduced the calcium and phosphorus contents of the femora, probably by stimulating bone resorption, KCA-098 seems to inhibit bone resorption. In fact, KCA-098 inhibited the PTH-induced release of 45Ca from pre-labeled fetal rat femora into the medium in organ culture. Coumestrol also inhibited the release of 45Ca from bone into the medium. However, KCA-098 did not increase the uterine weight of ovariectomized rats, whereas coumestrol did so. Thus KCA-098 is a unique, new inhibitor of bone resorption that has no estrogenic activity.
研究了香豆雌酚衍生物3,9-双（N,N-二甲基氨甲酰氧基）-5H-苯并呋喃[3,2-c]喹啉-6-酮（KCA-098）对20日龄胎鼠股骨器官培养物中骨吸收的影响。KCA-098增加了甲状旁腺激素（PTH）处理的胎鼠股骨的长度、干重以及钙和磷含量。由于PTH可能通过刺激骨吸收显著降低了股骨的钙和磷含量，KCA-098似乎抑制了骨吸收。实际上，KCA-098在器官培养中抑制了PTH诱导的预标记胎鼠股骨中45Ca释放到培养基中。香豆雌酚也抑制了骨中45Ca释放到培养基中。然而，KCA-098并未增加去卵巢大鼠的子宫重量，而香豆雌酚则有此作用。因此，KCA-098是一种独特的新型骨吸收抑制剂，无雌激素活性。
