β-蜕皮激素对去卵巢大鼠具有骨保护作用而无雌激素样作用。
Beta-ecdysone has bone protective but no estrogenic effects in ovariectomized rats.
机构信息
Department of Endocrinology, University Medical Center Goettingen, Goettingen, Germany.
出版信息
Phytomedicine. 2010 Sep;17(11):884-9. doi: 10.1016/j.phymed.2010.03.021.
Estrogens exert beneficial effects in the bone. Their chronic use however bares several risks. Therefore intensive search for non-estrogenic, bone protective compounds is going on. We observed that an extract of Tinospora cordifolia has antiosteoporotic effects and identified 20-OH-Ecdysone (beta-Ecdysone=Ecd) as a possible candidate for this action. Ovariectomized (ovx) rats were treated orally over 3 months with no Ecd (control) or 18, 57 or 121 mg Ecd/day/animal. Estradiol-17beta benzoate (E2) 159 microg/day/animal) fed animals served as positive controls. Bone mineral density (BMD) of tibia was measured by quantitative computer tomography, serum Osteocalcin and CrossLaps were measured in a ligand binding assay. Utilizing an estrogen receptor (ER) containing cytosolic extract of porcine uteri the capability of Ecd to bind to ER was tested. Ecd did not bind to ER. BMD was reduced by more than 50% in the control. In the Ecd animals BMD was dose dependently higher. Serum CrossLaps was lower in the Ecd and E2 group while serum Osteocalcin levels were decreased in the E2 but increased in the Ecd fed animals. Ecd has an antiosteoporotic effect which does not involve activation of ER.
雌激素对骨骼有有益的影响。然而，其长期使用存在多种风险。因此，人们正在积极寻找非雌激素、具有保护骨骼作用的化合物。我们发现，三叶鬼针草提取物具有抗骨质疏松作用，并鉴定出 20-羟基蜕皮甾酮（β-蜕皮甾酮=Ecd）可能是其作用的候选物质之一。去卵巢（ovx）大鼠在 3 个月内经口给予无 Ecd（对照组）或 18、57 或 121mg Ecd/天/只。以每天 159μg 苯甲酸雌二醇（E2）喂养的动物作为阳性对照。通过定量计算机断层扫描测量胫骨的骨矿物质密度（BMD），用配体结合法测量血清骨钙素和交联 C 端肽。利用含有猪子宫的雌激素受体（ER）的细胞质提取物，测试 Ecd 与 ER 结合的能力。Ecd 不能与 ER 结合。对照组 BMD 降低超过 50%。在 Ecd 处理的动物中，BMD 呈剂量依赖性升高。Ecd 和 E2 组的血清交联 C 端肽降低，而 E2 组的血清骨钙素水平降低，Ecd 组的血清骨钙素水平升高。Ecd 具有抗骨质疏松作用，不涉及 ER 的激活。
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