【摘要】 目的 为对抗骨质疏松症化合物进行初步药理活性筛选寻找快捷、方便、经济的工具。 方法 取16天胎龄的胎鼠尺骨，置于含BGJ培养基的培养瓶中，分别加入待测雌酚酮、骨靶向新化合物四环素-哌嗪雌酚酮（XW630）及其衍生物四环素-（2-羧酸酯）-哌嗪雌酚酮（ZWI-1），通入CO2、N2和O2混合气体，密闭后在旋转装置上培养48 h，测量骨干长和骨 总长，石蜡包埋切片后进行HE染色，光镜下计数破骨细胞和肥大软骨细胞。 结果 待测化合物浓度为10-7mol/L时，与对照组骨干长〔(1.22±0.08)mm〕、骨总长〔 (3.54±0.07)mm〕、破骨细胞〔(12.3±1.5)个〕及肥大软骨细胞〔(10.0±1.0)个〕 相比，雌酚酮组、XW630组和ZWI-1组骨干长依次分别增至(1.39±0.09)mm、(1.46±0. 08)mm和(1.49±0.06)mm(均为P＜0.01)。骨总长分别增至(3.76±0.13)mm(P ＜0.05)、(3.77±0.22)mm(P＜0.05)和(3.90±0.12)mm(P＜0.01) 。破 骨细胞分别减至(5.3±0.6)个、(6.0±1.6)个和(5.7±0.6)个(均为P＜0.01) 。肥大软骨细胞分别增至(15.3±1.5)个(P＜0.01)、(14.2±1.3)个(P＜0 .05)和(15.6±1.3)个(P＜0.01)。 结论 用该模型可同时观察到化合物对骨吸收和骨形成的作用，可用于雌激素类化合物抗骨质疏松药理活性的快速初筛。The use of cultured long bones from fetal mice for the primary screening of anti-osteoporosis with estrogen derivatives
LI Lingzhi ZHANG Yongliang MA Liying, et al.
（Dep artment of Pharmaceutical Chemistry, West China University of Medical Sciences, Chengdu 610041,China）
【Abstract】 Objective To influences estrone, XW630 and ZWI-1 to the growth of cultured long bones of fetal mice were examined in order to find out a proper mo del used for primary quick screening of anti-osteoporosis with estrogen. Methods Long bones from 16-day-old female mouse fetus were cultured in GBJ medium wit h mixing N2,O2 and CO2 in a rotating device for 48 h, estrone, XW630 and ZWI -1 were added to the culture medium separately. The bones were harvested and then the l ength of bones and their diaphyses were measured. The histomorphormetric analyse s on midlongtigitudinal sections of bones were performed and the number of osteo clasts and hypertrophic chondrocytes were determined. Results When the concentra tion of estrone, XW630 and ZWI-I was at 10-7 mol/L, the length of diaphys eal and bone, and the number of hypertrophic chondrocytes significantly increased compar ed with that of the controls, while the number of osteoclasts significantly decr
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