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.
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.
Siddiqui
Jawed A
JA
Division of Endocrinology, Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow, India.
Sharan
Kunal
K
Swarnkar
Gaurav
G
Rawat
Preeti
P
Kumar
Manmeet
M
Manickavasagam
Lakshmi
L
Maurya
Rakesh
R
Pierroz
Dominique
D
Chattopadhyay
Naibedya
N
D000818:Animals; D015519:Bone Density / Q000187:drug effects; D001853:Bone Marrow / Q000187:drug effects; D001842:Bone and Bones / Q000187:drug effects / Q000648:ultrastructure; D002478:Cells, Cultured; D024042:Collagen Type I / Q000652:urine; D004195:Disease Models, Animal; D005260:Female; D005960:Glucosides / Q000302:isolation & purification; D006801:Humans; D015675:Osteocalcin / Q000187:drug effects; D010010:Osteoclasts / Q000187:drug effects*; D010012:Osteogenesis / Q000187:drug effects; D015663:Osteoporosis, Postmenopausal / Q000188:drug therapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D011794:Quercetin / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology* / Q000502:physiology; D051381:Rats; D034403:Ulmus / Q000737:chemistry*; D014599:Uterus / Q000166:cytology / Q000187:drug effects
D024042:Collagen Type I; D005960:Glucosides; D010936:Plant Extracts; C558502:quercetin-6-C-beta-D-glucopyranoside; D015675:Osteocalcin; D011794:Quercetin