Synthesis, characterization of strontium-bile acid salts and their bioactivity vs. the anti-osteoporosis drug strontium ranelate.
The strontium salts Sr(cholate)2, (Compound 1), Sr(dehydrocholate)2, (Compound 2) and Sr3(3-dehydrocholanoyliden-L-tartrate)2, (Compound 3) have been prepared and characterized. The potential anti-osteoporotic activity of these compounds was tested on human primary osteoblasts (hOBs) and human primary osteoclasts (hOCs) in comparison with the bioactivity of strontium ranelate, previously registered as drug in the treatment of post-menopausal osteoporosis. Our results led to the hypothesis that the tested compounds, particularly Compound 2, may have requirements for modulating skeletal tissue regeneration or at least down regulating the loss of bone mass. In fact, all tested compounds have been shown to induce maturation in human primary osteoblasts (hOBs) and apoptosis of human primary osteoclasts (hOCs) at the same time.
Bergamini
Paola
P
Dipartimento di Chimica, Università degli Studi di Ferrara, Via Luigi Borsari 46, 44100 Ferrara, Italy.
Marchesi
Elena
E
Pagnoni
Antonella
A
Lambertini
Elisabetta
E
Franceschetti
Tiziana
T
Penolazzi
Letizia
L
Piva
Roberta
R
D001647:Bile Acids and Salts / Q000737:chemistry / Q000494:pharmacology*; D002454:Cell Differentiation / Q000187:drug effects; D002478:Cells, Cultured; D006801:Humans; D009942:Organometallic Compounds / Q000494:pharmacology*; D010010:Osteoclasts / Q000187:drug effects*; D010024:Osteoporosis / Q000188:drug therapy*; D013324:Strontium / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000494:pharmacology*
D001647:Bile Acids and Salts; D009942:Organometallic Compounds; D013876:Thiophenes; C081587:strontium ranelate; D013324:Strontium