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01.12.2011 | Original Article

A naturally occurring rare analog of quercetin promotes peak bone mass achievement and exerts anabolic effect on osteoporotic bone

verfasst von: J. A. Siddiqui, G. Swarnkar, K. Sharan, B. Chakravarti, A. K. Gautam, P. Rawat, M. Kumar, V. Gupta, L. Manickavasagam, A. K. Dwivedi, R. Maurya, N. Chattopadhyay

Erschienen in: Osteoporosis International | Ausgabe 12/2011

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Abstract

Summary

The effect of quercetin C-glucoside (QCG) on osteoblast function in vitro and bone formation in vivo was investigated. QCG supplementation promoted peak bone mass achievement in growing rats and new bone formation in osteopenic rats. QCG has substantial oral bioavailability. Findings suggest a significant bone anabolic effect of QCG.

Introduction

Recently, we showed that extracts of Ulmus wallichiana promoted peak bone mass achievement in growing rats and preserved trabecular bone mass and cortical bone strength in ovariectomized (OVx) rats. 3,3′,4′,5,7-Pentahydroxyflavone-6-C-β-d-glucopyranoside, a QCG, is the most abundant bioactive compound of U. wallichiana extract. We hypothesize that QCG exerts bone anabolic effects by stimulating osteoblast function.

Methods

Osteoblast cultures were harvested from rat calvaria and bone marrow (BM) to study differentiation and mineralization. In vivo, growing female Sprague Dawley rats and OVx rats with osteopenia were administered QCG (5.0 or 10.0 mg kg⁻¹ day⁻¹) orally for 12 weeks. Efficacy was evaluated by examining changes in bone microarchitecture using histomorphometric and microcomputed tomographic analyses and by determination of new bone formation by fluorescent labeling of bone. Plasma and BM levels of QCG were determined by high-performance liquid chromatography.

Results

QCG was much more potent than quercetin (Q) in stimulating osteoblast differentiation, and the effect of QCG was not mediated by estrogen receptors. In growing rats, QCG increased BM osteoprogenitors, bone mineral density, bone formation rate, and cortical deposition. In osteopenic rats, QCG treatment increased bone formation rate and improved trabecular microarchitecture. Comparison with the sham group (ovary intact) revealed significant restoration of trabecular bone in osteopenic rats treated with QCG. QCG levels in the BM were ~50% of that of the plasma levels.

Conclusion

QCG stimulated modeling-directed bone accrual and exerted anabolic effects on osteopenic rats by direct stimulatory effect on osteoprogenitors likely due to substantial QCG delivery at tissue level following oral administration.

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Titel: A naturally occurring rare analog of quercetin promotes peak bone mass achievement and exerts anabolic effect on osteoporotic bone
verfasst von: J. A. Siddiqui
G. Swarnkar
K. Sharan
B. Chakravarti
A. K. Gautam
P. Rawat
M. Kumar
V. Gupta
L. Manickavasagam
A. K. Dwivedi
R. Maurya
N. Chattopadhyay
Publikationsdatum: 01.12.2011
Verlag: Springer-Verlag
Erschienen in: Osteoporosis International / Ausgabe 12/2011
Print ISSN: 0937-941X
Elektronische ISSN: 1433-2965
DOI: https://doi.org/10.1007/s00198-010-1519-4

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