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| 荧光示踪法原位观察大黄蒽醌的骨靶向-抗骨质疏松作用 |
| The observation of bone targeted anti-osteoporosis effect of free rhubarb anthraquinone using fluorescent traceing method. |
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| DOI：10.3969/j.issn.1006-7108.2014.10.004 |
| 中文关键词: 大黄蒽醌 骨靶向-抗骨质疏松 荧光示踪 大鼠 |
| 英文关键词:Free rhubarb anthraquinone Bone targeted anti-osteoporosis Fluorescent trace Rat |
| 基金项目:东莞市科技计划资助项目 (DK200911) |
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| 中文摘要: |
| 目的 探讨游离大黄蒽醌类化合物对糖皮质激素诱导性骨质疏松大鼠的骨靶向抗骨质疏松作用。方法 采用荧光示踪法观察游离大黄蒽醌类化合物在糖皮质激素诱导的大鼠骨质疏松模型股骨远端骨骺部位对称剖面的荧光,并将其与同位的骨密度(BMD)和骨矿量(BMC)进行关联分析，4月龄♀SD大鼠126只随机分成泼尼松组(Pred)、泼尼松加大黄蒽醌组(Pred+FAQ) 和正常对照组(CON)，每个组设7个时间点，灌服给药时间最长13周。以pQCT骨密度仪分别测定各组各时间点大鼠股骨远心端(2mm)的骨密度和骨矿量，再以荧光显微镜采集Pred+FAQ组各时间点骨标本骨骺部位对称剖面的荧光图像。结果 Pred+FAQ组股骨远心端的骨密度相对Pred组均显著增加(P<0.05)，但Pred+FAQ组各时间点骨标本骨骺部位对称剖面的荧光强度随骨骺“生长-闭合”周期而“上升-消除”，与骨标本的骨密度无显著相关，骨矿量(BMC) 也与骨标本的骨密度无显著相关。结论 游离大黄蒽醌可以预防糖皮质激素性骨质疏松，具有荧光的游离大黄蒽醌类原型化合物在大鼠股骨中无显著的蓄积现象和骨靶向作用。该实验为从骨组织原位药效动力学与药代动力学相关联（pD-pK link）角度探索骨靶向抗骨质疏松成分作了有益的尝试。 |
| 英文摘要: |
| Objective To investigate the bone targeted anti-osteoporosis effect of free rhubarb anthraquinone compounds in rats with glucocorticoid-induced osteoporosis. Methods Using fluorescent tracing method, the fluorescence in the epiphysis of the distal femurs was observed in rats with glucocorticoid-induced osteoporosis in situ. It was correlated with bone mineral density (BMD) and bone mineral content (BMC) at the same location. One hundred and twenty-six 4-month-old female SD rats were randomly divided into prednisone group (Pred), prednisone + free anthraquinones group (Pred+FAQ), and normal control group (CON). Each group was further subdivided into 7 subgroups. The administration period was 13 weeks at the last. BMD and BMC in distal part (2mm) of the femurs were scanned using pQCT. The photofluorogram of the coronary symmetrical section of the bone samples in Pred+FAQ group was obtained using epifluorescence microscope. Results BMD of the distal part of the femur was significantly increased in Pred+FAQ group (P<0.05) compared to those in Pred group. The fluorescence of the epiphysis of bone samples at all time points elevated or eliminated following the epiphyseal “growth-closed” cycle in Pred+FAQ group. It was not significantly correlated with BMD of the bone samples. BMC was not significantly correlated with BMD of the bone samples. Conclusion Free rhubarb anthraquinone compounds can prevent bone loss due to glucocorticoid-induced osteoporosis. There is no significant accumulation of fluorescence combined free anthraquinone compounds and bone targeting property. This experiment explores a beneficial research model for investigate bone targeted anti-osteoporosis effective components in bone tissue through pharmacodynamics/pharmacokinetics link perspective. |
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