Quercetin-6-C-β-D-glucopyranoside isolated from Ulmus wallichiana planchon is more potent than quercetin in inhibiting osteoclastogenesis and mitigating ovariectomy-induced bone loss in rats

Menopause. 2011 Feb;18(2):198-207. doi: 10.1097/gme.0b013e3181e84e67.

Abstract

Objective: The aim of this study was to determine the skeletal effect of quercetin-6-C-β-D-glucopyranoside (QCG) isolated from the extract of Ulmus wallichiana and compare this effect with quercetin (Q) in a rat model of postmenopausal bone loss.

Methods: Murine bone marrow cells were used to study the effect of QCG or Q on osteoclast differentiation. QCG or Q (1.0 and 5.0 mg kg(-1) d(-1) doses) was administered orally to ovarietomized (OVx) rats for 12 weeks. Sham-operated + vehicle and OVx + vehicle groups served as positive and negative controls, respectively. Bone mineral density, bone microarchitecture, biomechanical strength, bone turnover markers, and uterotrophic effect were studied. One-way analysis of variance was used to test significance of effects.

Results: QCG at 1.0 nM significantly inhibited differentiation of multinucleated osteoclasts and expression of osteoclastogenic genes from bone marrow cells, whereas Q at 10.0 μM had comparable results. OVx rats treated with QCG exhibited significantly higher bone mass and better microarchitecture in trabecular and cortical bones compared with OVx + vehicle. QCG treatment of OVx rats had better functional impact than did Q-treated OVx rats, evident from increased bone biomechanical strength. Serum osteocalcin and urinary fragments of type 1 collagen were significantly lower in QCG-treated OVx rats compared with OVx + vehicle group. The protective effect of QCG under ovariectomy-induced bone loss setting was found to be significantly better than Q. Uterine histomorphometry parameters of OVx rats did not change with QCG treatment.

Conclusions: QCG improves bone biomechanical quality more effectively than Q through positive modifications of bone mineral density and bone microarchitecture without a hyperplastic effect on the uterus.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bone Density / drug effects
  • Bone Marrow / drug effects
  • Bone and Bones / drug effects
  • Bone and Bones / ultrastructure
  • Cells, Cultured
  • Collagen Type I / urine
  • Disease Models, Animal
  • Female
  • Glucosides / isolation & purification
  • Humans
  • Osteocalcin / drug effects
  • Osteoclasts / drug effects*
  • Osteogenesis / drug effects
  • Osteoporosis, Postmenopausal / drug therapy
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Quercetin / analogs & derivatives*
  • Quercetin / isolation & purification
  • Quercetin / pharmacology*
  • Quercetin / physiology
  • Rats
  • Ulmus / chemistry*
  • Uterus / cytology
  • Uterus / drug effects

Substances

  • Collagen Type I
  • Glucosides
  • Plant Extracts
  • quercetin-6-C-beta-D-glucopyranoside
  • Osteocalcin
  • Quercetin