Messalli Enrico M, Mainini Giampaolo, Scaffa Cono, Cafiero Angela, Salzillo Pier Luigi, Ragucci Angelo, Cobellis Luigi
Department of Gynaecology, Obstetrics and Reproductive Medicine, Second University of Naples, Largo Madonna delle Grazie 1, 80138 Naples, Italy.
Maturitas. 2007 Jan 20;56(1):38-44. doi: 10.1016/j.maturitas.2006.05.007. Epub 2006 Jun 19.
Osteoprotegerin (OPG) is a protein expressed by osteoblasts that, linking the receptor activator of nuclear factor kappaB (RANK) ligand (RANKL), produced by osteoblasts, blocks the process of osteoclastic differentiation and modulates osteoclastic apoptosis. Raloxifene (RAL) stimulates the production of OPG from osteoblasts, as demonstrated in vitro, carring out their antiresorption activity, at least in part, as means of the OPG/RANK/RANKL system. The aim of this study was to evaluate in vivo if the RAL treatment of postmenopausal women was associated to changes in serum OPG; moreover, to evaluate the serum changes of bone turnover modulators interleukin-6 (IL-6) and C-telopeptides of type-1 collagen (CrossLaps).
A prospective, randomized, placebo-controlled study was designed. A group of consecutive healthy postmenopausal women (n=40) referred to II Menopause Centre of the Department of Gynaecology of Second University of Naples for climacteric syndrome was enrolled and divided in two groups: (n=20) postmenopausal women received for 6 months oral raloxifene (60 mg/day) versus (n=20) postmenopausal women received placebo tablets.
Serum OPG levels in postmenopausal women after RAL treatment are statistically significant increased (P<0.001) versus baseline (P=0.007) versus placebo.
These in vivo data demonstrate that RAL could improve osteoporosis, also through an increase of OPG production by osteoblasts.
骨保护素(OPG)是一种由成骨细胞表达的蛋白质,它与成骨细胞产生的核因子κB受体激活剂(RANK)配体(RANKL)结合,阻断破骨细胞分化过程并调节破骨细胞凋亡。雷洛昔芬(RAL)可刺激成骨细胞产生OPG,体外实验已证实这一点,其抗吸收活性至少部分是通过OPG/RANK/RANKL系统实现的。本研究的目的是在体内评估RAL治疗绝经后女性是否与血清OPG的变化有关;此外,评估骨转换调节剂白细胞介素-6(IL-6)和I型胶原C端肽(CrossLaps)的血清变化。
设计了一项前瞻性、随机、安慰剂对照研究。一组连续的健康绝经后女性(n = 40)因更年期综合征转诊至那不勒斯第二大学妇科第二更年期中心,将其纳入并分为两组:(n = 20)绝经后女性接受为期6个月的口服雷洛昔芬(60 mg/天),与(n = 20)绝经后女性接受安慰剂片。
与基线相比(P = 0.007)以及与安慰剂相比,RAL治疗后的绝经后女性血清OPG水平在统计学上显著升高(P < 0.001)。
这些体内数据表明,RAL还可通过增加成骨细胞产生OPG来改善骨质疏松症。