Benvenuti S, Petilli M, Frediani U, Tanini A, Fiorelli G, Bianchi S, Bernabei P A, Albanese C, Brandi M L
Department of Clinical Physiopathology, University of Florence, School of Medicine, Italy.
Biochem Biophys Res Commun. 1994 Jun 30;201(3):1084-9. doi: 10.1006/bbrc.1994.1816.
Ipriflavone, a synthetic isoflavone derivative, reduces bone resorption by inhibiting osteoclasts activity. In order to evaluate the role of Ipriflavone on osteoclast growth and differentiation, we tested Ipriflavone and its four "in vivo" main metabolites (Metabolites I, II, III, and V) on a clonal population of human osteoclast precursor cells (FLG 29.1). Pharmacological doses of Ipriflavone and Metabolite III were able to inhibit cell proliferation and interleukin 6 release. In co-cultures of FLG 29.1 cells and osteoblastic (Saos-2) cells Ipriflavone at 1 microM dose inhibited the adhesion of FLG 29.1 cells to the osteoblastic monolayer and reduced the immunocytochemical reaction of the vitronectin receptor. Binding studies with tritiated Ipriflavone showed the presence of a single specific binding site, wtih a Kd of about 70 nM and a binding capacity of 8 fmol/10(6) cells. These results demonstrate a direct effect of Ipriflavone and of Metabolite III on the human osteoclast precursor cell line FLG 29.1.
依普黄酮是一种合成异黄酮衍生物，通过抑制破骨细胞活性来减少骨吸收。为了评估依普黄酮在破骨细胞生长和分化中的作用，我们在人破骨细胞前体细胞（FLG 29.1）的克隆群体上测试了依普黄酮及其四种“体内”主要代谢物（代谢物I、II、III和V）。药理剂量的依普黄酮和代谢物III能够抑制细胞增殖和白细胞介素6的释放。在FLG 29.1细胞与成骨细胞（Saos-2）的共培养中，1 microM剂量的依普黄酮抑制了FLG 29.1细胞与成骨细胞单层的粘附，并降低了玻连蛋白受体的免疫细胞化学反应。用氚标记的依普黄酮进行的结合研究表明存在一个单一的特异性结合位点，解离常数（Kd）约为70 nM，结合容量为8 fmol/10(6)个细胞。这些结果证明了依普黄酮和代谢物III对人破骨细胞前体细胞系FLG 29.1有直接作用。
