中国骨质疏松杂志
中國骨質疏鬆雜誌
중국골질소송잡지
CHINESE JOURNAL OF OSTEOPOROSIS
2014年
5期
500-503
,共4页
侯进%李萍%曾菊绒%胥晓丽%魏明%熊晓云%弥曼
侯進%李萍%曾菊絨%胥曉麗%魏明%熊曉雲%瀰曼
후진%리평%증국융%서효려%위명%웅효운%미만
骨质疏松%雌激素受体(ER)
骨質疏鬆%雌激素受體(ER)
골질소송%자격소수체(ER)
Osteoporosis%Estrogen receptor (ER)
目的：研究苯并二氢吡喃衍生物xy2004对去势雌鼠骨质疏松的治疗作用，并初步探讨其机制。方法将50只SD大鼠随机分为5组，假手术组、模型组、genistein组、xy2004高、低剂量组。假手术组、模型组均给予蒸馏水10 mL· kg-1，给药组分别给予小剂量xy20043 mg· kg-1和大剂量xy20047 mg· kg-1，genistein组给genistein 6 mg· kg-1，灌胃给药。观察xy2004对去势雌鼠骨密度的影响；检测大鼠体内血清钙、血清磷及碱性磷酸酶、白细胞介素-6等生化指标；用放射性配体结合法考察化合物与雌激素受体（ estrogenic receptor ，ER）的亲和力。结果去势后大鼠骨密度下降，使用xy2004灌胃3个月后，能明显抑制去势雌鼠骨密度的下降，降低血中ALP含量，抑制IL-6分泌。 Xy2004与ER有亲和力，对ERα和ERβ的IC50分别为4.12×10-7 M和7.38×10-5 M。结论化合物xy2004通过与去势雌鼠体内雌激素受体结合，影响去势大鼠骨代谢，增强去势雌鼠骨密度，抗去势雌鼠骨质疏松。
目的：研究苯併二氫吡喃衍生物xy2004對去勢雌鼠骨質疏鬆的治療作用，併初步探討其機製。方法將50隻SD大鼠隨機分為5組，假手術組、模型組、genistein組、xy2004高、低劑量組。假手術組、模型組均給予蒸餾水10 mL· kg-1，給藥組分彆給予小劑量xy20043 mg· kg-1和大劑量xy20047 mg· kg-1，genistein組給genistein 6 mg· kg-1，灌胃給藥。觀察xy2004對去勢雌鼠骨密度的影響；檢測大鼠體內血清鈣、血清燐及堿性燐痠酶、白細胞介素-6等生化指標；用放射性配體結閤法攷察化閤物與雌激素受體（ estrogenic receptor ，ER）的親和力。結果去勢後大鼠骨密度下降，使用xy2004灌胃3箇月後，能明顯抑製去勢雌鼠骨密度的下降，降低血中ALP含量，抑製IL-6分泌。 Xy2004與ER有親和力，對ERα和ERβ的IC50分彆為4.12×10-7 M和7.38×10-5 M。結論化閤物xy2004通過與去勢雌鼠體內雌激素受體結閤，影響去勢大鼠骨代謝，增彊去勢雌鼠骨密度，抗去勢雌鼠骨質疏鬆。
목적：연구분병이경필남연생물xy2004대거세자서골질소송적치료작용，병초보탐토기궤제。방법장50지SD대서수궤분위5조，가수술조、모형조、genistein조、xy2004고、저제량조。가수술조、모형조균급여증류수10 mL· kg-1，급약조분별급여소제량xy20043 mg· kg-1화대제량xy20047 mg· kg-1，genistein조급genistein 6 mg· kg-1，관위급약。관찰xy2004대거세자서골밀도적영향；검측대서체내혈청개、혈청린급감성린산매、백세포개소-6등생화지표；용방사성배체결합법고찰화합물여자격소수체（ estrogenic receptor ，ER）적친화력。결과거세후대서골밀도하강，사용xy2004관위3개월후，능명현억제거세자서골밀도적하강，강저혈중ALP함량，억제IL-6분비。 Xy2004여ER유친화력，대ERα화ERβ적IC50분별위4.12×10-7 M화7.38×10-5 M。결론화합물xy2004통과여거세자서체내자격소수체결합，영향거세대서골대사，증강거세자서골밀도，항거세자서골질소송。
Objective To investigate the therapeutic effect of xy2004, a kind of benzene and dihydropyran derivatives, on postmenopausal osteoporosis in ovariectomized rats, and to preliminarily explore its mechanism.Methods Fifty female SD rats were divided into 5 groups:sham operation group, ovariectomized group ( OVX) , genistein group, xy2004 high dose group, and xy2004 low dose group.Forty SD rats were ovariectomized except 10 rats in sham operated group.Rats in sham operated group and OVX group were treated with 10 ml/kg distilled water.Rats in xy2004 high and low dose group were treated with 7 mg/kg and 3 mg/kg xy2004, respectively.And rats in genistein group were treated with 6 mg/kg genistein.All the drugs or distilled water were given through gavage administration.The effect of xy2004 on bone mineral density ( BMD) in OVX rats was observed.The serum levels of calcium, phosphorous, and IL-6 were detected.The affinity of xy2004 to estrogenic receptor ( ER) was detected using radio-ligand binding assay.Results BMD in OVX rats decreased.After 3-month gavage, xy2004 could significantly inhibit the decrease of BMD in OVX female rats, reduce serum ALP level, and inhibit the secretion of IL-6.The affinity of xy2004 to ER was detected, and the IC50 to ERαand ERβwas of 4.12 ×10 -7 M and 7.38 ×10 -5 M, respectively.Conclusion By binding with ER in female OVX rats, xy2004 can affect bone metabolism in rats , improve BMD in female OVX rats, and prevent postmenopausal osteoporosis in OVX rats .
