Synthetic analogs of daidzein, having more potent osteoblast stimulating effect.

Abstract:

:A series of didzein derivatives were synthesized and assessed for stimulation of osteoblast differentiation using primary cultures of rat calvarial osteoblasts. Data suggested that three synthetic analogs, 1c, 3a and 3c were several folds more potent than daidzein in stimulating differentiation and mineralization of osteoblasts. Further, these three compounds did not show any estrogen agonistic activity, however had mild estrogen antagonistic effect. Out of the three compounds, 3c was found to maximally increase the mineralization of bone marrow osteoprogenitor cells. Compound 3c also robustly increased the mRNA levels of osteogenic genes including bone morphogenetic protein-2 and osteocalcin in osteoblasts. Unlike daidzein, 3c did not inhibit osteoclastogenesis. Collectively, we demonstrate osteogenic activity of daidzein analogs at significantly lower concentrations than daidzein.

journal_name

Bioorg Med Chem Lett

authors

Yadav DK,Gautam AK,Kureel J,Srivastava K,Sahai M,Singh D,Chattopadhyay N,Maurya R

doi

10.1016/j.bmcl.2010.12.008

subject

Has Abstract

pub_date

2011-01-15 00:00:00

pages

677-81

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01762-2

journal_volume

21

pub_type

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