Tsutsumi N, Kawashima K, Nagata H, Ujiie A, Endo H
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan.
Jpn J Pharmacol. 1995 Feb;67(2):169-71. doi: 10.1254/jjp.67.169.
3,9-Dihydroxy-5H-benzofuro[3,2-c]quinoline-6-one (KCA-012), the chemical structure of which is closely similar to that of the phytoestrogen coumestrol, inhibited parathyroid hormone-, 1 alpha,25-dihydroxyvitamin D3- and prostaglandin E2-induced bone resorption of cultured fetal rat bones. KCA-012 also increased the calcium content of 9-day chick embryonic femur cultured in vitro. KCA-012 did not show any estrogenic activity as determined by an increase in the uterine weight of ovariectomized rats, whereas coumestrol did. These results indicate that KCA-012 has no estrogenic activity and has unique effects of inhibiting bone resorption and stimulating bone mineralization.
3,9 - 二羟基 - 5H - 苯并呋喃[3,2 - c]喹啉 - 6 - 酮（KCA - 012），其化学结构与植物雌激素香豆雌酚极为相似，它能抑制甲状旁腺激素、1α,25 - 二羟基维生素D3以及前列腺素E2诱导的培养胎鼠骨骼的骨吸收。KCA - 012还能增加体外培养的9日龄鸡胚股骨的钙含量。通过去卵巢大鼠子宫重量增加来判断，KCA - 012未表现出任何雌激素活性，而香豆雌酚则有。这些结果表明，KCA - 012不具有雌激素活性，且具有抑制骨吸收和刺激骨矿化的独特作用。
