Re: calci-chewA collection of abstracts that suggest
rutin, quercetin, and other flavonoids help
preserve bone.
Here in the States it is possible to buy both
bulk quercetin and rutin powders as well as
tablets. Quercetin powder is very light
and is a little hard to mix into water.
Some foods are pretty good sources.
The USDA has some downloads on
food sources for flavonoids and related
substances.
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Zhong Yao Cai. 2006 May;29(5):467-70.
[Comparative study on effects of rutin and quercetin
on metabolism in osteoblast
cells]
[Article in Chinese]
Yang YJ, Yang ZL, Wang DC, Xiao XC, Li P.
Department of Traditional Chinese Medicine,
China Pharmaceutical University,
Nanjing 210038, China.
yangyajunl@163 . com
OBJECTIVE:
To investigate the mechanism of rutin and its aglycone
(quercetin) in preventing and treating osteoporosis and
their effects on stimulating bone
formation were studied comparatively in osteoblast cells.
METHODS:
The effects of rutin and quercetin on the proliferation,
differentiation and mineralization were studied respectively
by using tetrazolium (MTT), alkaline phosphatase (ALP) and
mineralized nodules assays in newborn rat calvarial
osteoblast (ROB) cells.
RESULTS:
Quercetin showed significant stimulatory effects on
proliferation and mineralization in ROB cells, so it could
promote bone formation. However, rutin could not improve
stimulation of bone formation because it increased
proliferation and inhibited differentation and had
no remarkable influence on ROB cells in vitro.
CONCLUSION:
Rutin showed less activity than quercetin on bone
formation in ROB cells in vitro. Therefore the
mechanism that some foods and traditional Chinese medicine
containing rutin can prevent and treat osteoporosis
is that its metaboite in vivo can promote bone formation
in ROB cells.
PMID: 16981462
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Eur J Pharmacol. 2004 Feb 6;485(1-3):89-96.
Quercetin, a flavonoid, inhibits the proliferation,
differentiation, and mineralization of osteoblasts in vitro.
Notoya M, Tsukamoto Y, Nishimura H, Woo JT, Nagai K,
Lee IS, Hagiwara H.
Department of Biological Sciences,
Tokyo Institute of Technology, 4259
Nagatsuta-cho, Midori-ku,
Yokohama 226-8501, Japan.
It is possible that the flavonoids that are found in
many foods might have a protective effect against osteoclastic
activity. However, little information is available about
the effects of flavonoids on osteoblastogenesis.
Therefore, we investigated the effects of quercetin,
a flavonoid, on the metabolism of rat
calvarial osteoblast-like cells (ROB cells) in culture.
The proliferation of cells was markedly inhibited upon
exposure of cells to quercetin at 5 x 10(-6) to
1 x 10(-5) M. Quercetin at 1 x 10(-5) M did not
induce apoptosis in ROB cells but arrested cells
at the G1 phase of the cell cycle. In addition,
quercetin stimulated the expression of mRNA for
p21(waf1/cip1), which inhibits the activity
of cyclin-dependent kinases, and inhibited the
phosphorylation of histone H1. Furthermore, after
cells had ceased to proliferate, quercetin reduced the
activity of alkaline phosphatase, the level of
expression of mRNA for osteocalcin, the rate of
deposition of Ca(2+), and the formation of mineralized
nodules, all of which are markers of osteoblast
differentiation. These findings indicate that
quercetin inhibits the proliferation, differentiation, and
mineralization of osteoblastic cells.
PMID: 14757127
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J Bone Miner Res. 2000 Nov;15(11):2251-8.
Comment in:
J Bone Miner Res. 2001 May;16(5):970-1.
Rutin inhibits ovariectomy-induced osteopenia in rats.
Horcajada-Molteni MN, Crespy V, Coxam V, Davicco MJ,
Rémésy C, Barlet JP.
Unité Maladies Métaboliques et Micronutriments,
Institut National de la Recherche
Agronomique, Clermont-Theix, France.
Several studies suggest that polyphenols might exert a protective
effect against osteopenia. The present experiment was
conducted to observe the effects of rutin
(quercetin-3-O-glucose rhamnose) on bone metabolism
in ovariectomized (OVX) rats. Thirty 3-month-old Wistar
rats were used. Twenty were OVX while the 10 controls
were sham-operated (SH). Among the 20 OVX, for 90 days
after surgery 10 were fed the same synthetic diet as the
SH or OVX ones, but 0. 25% rutin (OVX + R) was
added. At necropsy, the decrease in uterine weight was
not different in OVX and OVX + R rats. Ovariectomy also
induced a significant decrease in both total and
distal metaphyseal femoral mineral density, which was
prevented by rutin consumption. Moreover, femoral
failure load, which was not different in OVX and
SH rats, was even higher in OVX + R rats than in
OVX or SH rats. In the same way, on day 90,
both urinary deoxypyridinoline (DPD) excretion
(a marker for bone resorption) and calciuria were
higher in OVX rats than in OVX + R or SH rats.
Simultaneously, plasma osteocalcin (OC) concentration
(a marker for osteoblastic activity) was higher in
OVX + R rats than in SH rats. High-performance liquid
chromatography (HPLC) profiles of plasma samples from
OVX + R rats revealed that mean plasma concentration of
active metabolites (quercetin and isorhamnetin) from
rutin was 9.46+/-1 microM, whereas it was undetectable
in SH and OVX rats. These results indicate that rutin
(and/or its metabolites), which appeared devoid of
any uterotrophic activity, inhibits ovariectomy-induced
trabecular bone loss in rats, both by slowing down
resorption and increasing osteoblastic activity.
PMID: 11092407
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Flavonoid quercetin decreases osteoclastic differentiation
induced by RANKL via a mechanism involving NF kappa B and AP-1.
Wattel A, Kamel S, Prouillet C, Petit JP, Lorget F,
Offord E, Brazier M.
Unité de Recherche sur les Mécanismes de la Résorption Osseuse,
Laboratoire de Pharmacie Clinique,
Université de Picardie Jules Verne,
1 rue des Louvels, 80037
Amiens, France.
alice.wattel@sa.u-picardie . fr
Flavonoids are micronutrients widely present in food of
plant origin. They have been attributed pharmacological
properties such as anticancer and prevention of
age-related pathologies. It has been recently
hypothesized that flavonoids increase bone mass
and prevent osteoporosis. However, little is
known about the in vitro effects of flavonoids on
osteoclast activities. We investigated the
effects of quercetin, one of the most commonly
occurring flavonoids, on osteoclast differentiation
which is a critical determinant step of in vivo bone
resorption. Two in vitro models of osteoclast
differentiation were used in this study: a murine one,
involving the culture of RAW 264.7 cells in presence of
receptor activator of NF kappa B ligand (RANKL),
and a human model consisting of differentiating
peripheral blood monocytic cells (PBMC) isolated
from peripheral blood in presence of RANKL and
macrophage-colony stimulating factor (M-CSF).
Osteoclastogenesis was assessed by osteoclast-like
number, tartrate resistant acid phosphatase (TRAP)
activity, and bone resorbing activity. We showed that
quercetin (0.1-10 microM) decreased osteoclastogenesis
in a dose dependent manner in both models with
significant effects observed at low concentrations,
from 1 to 5 microM. The IC(50) value was about
1 microM. Analysis of protein-DNA
interaction by electrophoretic mobility shift assay
(EMSA) performed on RAW cells showed that a pre-treatment
with quercetin inhibited RANKL-induced nuclear factor
kB (NF kappa B) and activator protein 1 (AP-1) activation.
NF kappa B and AP-1 are transcription factors highly
involved in osteoclastic differentiation and
their inhibition could play an important role in
the decrease of osteoclastogenesis observed in
the presence of quercetin. In conclusion, the
present results demonstrate for the first time
that quercetin, a flavonoid characterized by
antioxidant activities, is a potent inhibitor
of in vitro osteoclastic differentiation, via a
mechanism involving NF kappa B and AP-1.
Copyright 2004 Wiley-Liss, Inc.
PMID: 15108355
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Biochem Pharmacol. 2004 Apr 1;67(7):1307-13.
Stimulatory effect of naturally occurring flavonols
quercetin and kaempferol on alkaline phosphatase
activity in MG-63 human osteoblasts through ERK and estrogen
receptor pathway.
Prouillet C, Mazière JC, Mazière C, Wattel A,
Brazier M, Kamel S.
Laboratoire de Biochimie,
JE 23 29, CHRU d'Amiens,
Hôpital Nord, 80054 Amiens
Cedex 01, France.
Many plant-derived substances have estrogenic activities.
Due to their ability to bind the estrogen receptor (ER),
these compounds have the potential to counteract
the deleterious effects of estrogen deficiency
on bone. In this study, we investigated the
in vitro effect of two widespread flavonols,
quercetin and kaempferol, on alkaline phosphatase (ALP)
activity in MG-63 cultured human osteoblasts.
We found that both flavonols significantly
increased ALP activity. This effect was markedly
reduced by PD 98059, an inhibitor of the extracellular
regulated kinase (ERK) pathway, and by ICI 182780, an
antagonist of ERs. Western blot studies confirmed that
ERK is rapidly activated in cells treated by both
flavonols. Finally, ICI 182780 markedly inhibits
the flavonol-induced ERK activation. The data presented
in this study support the conclusion that, in
MG-63 osteoblasts (i) the increase in ALP activity
by flavonols involves a rapid stimulation of ERK
activation but also involves the ER, and that (ii) the
activation of ERK by flavonols occurs most likely
downstream of the ERs activation. Taken together,
these results suggest that flavonols derivatives as
quercetin and kaempferol can stimulate osteoblastic
activity. Such compounds may represent
new pharmacological tools for the treatment of osteoporosis.
PMID: 15013846