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Báo cáo khoa học: Neuropeptide Y expression and function during osteoblast differentiation – insights from transthyretin knockout mice potx

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Moreover, the higher ami-dated neuropeptide levels in TTR KO mice were related to increased bone mineral density and trabecular volume.. In summary, this work contributes to a better und

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differentiation – insights from transthyretin knockout

mice

Ana F Nunes1,2,*, Ma´rcia A Liz1, Filipa Franquinho1, Liliana Teixeira3, Vera Sousa1, Chantal

Chenu4, Meriem Lamghari3, and Mo´nica M Sousa1,

1 Nerve Regeneration, IBMC – Instituto de Biologia Molecular e Celular, Universidade do Porto, Portugal

2 ICBAS, Universidade do Porto, Portugal

3 INEB – Instituto de Engenharia Biome´dica, Divisa˜o de Biomateriais, Universidade do Porto, Portugal

4 Department of Veterinary Basic Sciences, The Royal Veterinary College, London, UK

Introduction

The regulation of bone remodeling has been

conven-tionally linked to local factors, hormones, and

mechanical loading [1–3] However, in the last decade,

several reports have provided evidence that bone

homeostasis is also under the influence of central and peripheral neural control [4–8] This concept is sup-ported by a number of histological studies revealing the existence of neuropeptide fibers and neuropeptide

Keywords

amidated neuropeptide; bone marrow

stromal cells; bone mass; NPY; osteoblastic

differentiation

Correspondence

M M Sousa, IBMC, Rua Campo Alegre

823, 4150-180 Porto, Portugal

Fax: +351 22 6099157

Tel: +351 22 6074900

E-mail: msousa@ibmc.up.pt

Website: http://www.ibmc.up.pt/nerve

*Present address

iMed.UL, Faculty of Pharmacy, University of

Lisbon, Portugal

These authors contributed equally to this

work

(Received 12 November 2009, revised

3 November 2009, accepted 5

November 2009)

doi:10.1111/j.1742-4658.2009.07482.x

To better understand the role of neuropeptide Y (NPY) in bone homeosta-sis, as its function in the regulation of bone mass is unclear, we assessed its expression in this tissue By immunohistochemistry, we demonstrated, both at embryonic stages and in the adult, that NPY is synthesized by osteoblasts, osteocytes, and chondrocytes Moreover, peptidylglycine a-am-idating monooxygenase, the enzyme responsible for NPY activation by amidation, was also expressed in these cell types Using transthyretin (TTR) KO mice as a model of augmented NPY levels, we showed that this strain has increased NPY content in the bone, further validating the expression of this neuropeptide by bone cells Moreover, the higher ami-dated neuropeptide levels in TTR KO mice were related to increased bone mineral density and trabecular volume Additionally, RT-PCR analysis established that NPY is not only expressed in MC3T3-E1 osteoblastic cells and bone marrow stromal cells (BMSCs), but is also detectable by RIA in BMSCs undergoing osteoblastic differentiation In agreement with our

in vivoobservations, in vitro, TTR KO BMSCs differentiated in osteoblasts had increased NPY levels and exhibited enhanced competence in undergo-ing osteoblastic differentiation In summary, this work contributes to a better understanding of the role of NPY in the regulation of bone forma-tion by showing that this neuropeptide is expressed in bone cells and that increased amidated neuropeptide content is related to increased bone mass

Abbreviations

ALP, alkaline phosphatase; BMD, bone mineral density; BMSC, bone marrow stromal cell; GAPDH, glyceraldehyde-3-phosphate

dehydrogenase; HPRT, hypoxanthine-guanine phosphoribosyltransferase; KO, knockout; microCT, micro computed tomography; NF200, neurofilament 200; NPY, neuropeptide Y; PAM, peptidylglycine a-amidating monooxygenase; PGP9.5, protein gene product 9.5; RANK, receptor activator of nuclear factor-jB; T4,thyroxine; TTR, transthyretin.

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receptors in bone [9] Neuropeptide Y

(NPY)-immuno-reactive fibers have been found to be mostly

distri-buted in association with blood vessels and in the

periosteum [10–12] NPY immunoreactivity was

dra-matically reduced in sympathectomized animals,

indi-cating the sympathetic origin of these nerves [11]

Despite the fact that NPY-containing nerve fibers have

been described in the bone, no data exist concerning

the expression of this neuropeptide in bone cells

How-ever, NPY has been detected in the periosteum and

bone marrow by RIA [13], particularly in

megakaryo-cytes [14] Recently, it was additionally reported that

the NPY receptor Y1, but not Y2, Y4, Y5 or Y6, was

expressed in cultured bone marrow stromal cells

(BMSCs) and osteoblasts [15]

Despite the existence of NPY fibers and one of its

receptors in the bone, NPY knockouts (KOs) have

normal bone mass, questioning a role for NPY control

in bone activity [8] On the other hand, different

mouse models that have in common the fact that they

present increased NPY levels, the Y2 receptor-KO and

the leptin-deficient and leptin receptor-deficient mouse

(ob⁄ ob and db ⁄ db mice, respectively), display a high

cancellous bone mass phenotype associated with

increased osteoblast activity [5,7,16], supporting a role

for NPY in bone biology In the case of ob⁄ ob mice

and db⁄ db mice, there is increased NPY activity in the

hypothalamus, owing to the lack of leptin-induced

inhibition of NPY expression [16] Y2 receptor KO

and leptin-deficient mice share key characteristics, with

similar increases in cancellous bone mass and NPY

levels in the hypothalamus, suggesting a commonality

of mechanism However, it was recently shown that

leptin and Y2 receptor pathways independently

modu-late cancellous bone homeostasis [17] With regard to

Y2 receptor-deficient mice, both germline and

condi-tional hypothalamic Y2 receptor KO mice share the

same high bone mass phenotype [5], demonstrating

that central hypothalamic Y2 receptors are crucial for

this process Interestingly, although germline Y1

recep-tor KO mice also display increased bone formation,

conditional deletion of hypothalamic Y1 receptors did

not alter bone homeostasis, suggesting a

nonhypotha-lamic control of bone mass [6] The Y1 receptor being

the only NPY receptor identified in the bone, these

results suggest that absence of NPY signaling in the

bone (as occurs in Y1 receptor-deficient mice) results

in increased bone mass

NPY effects in bone mass have been further

inves-tigated by exogenous administration Whereas

intra-cerebroventricular infusion of NPY decreased bone

mass [7], vector-mediated overexpression of NPY in

the hypothalamus of wild-type mice resulted in no

alteration in cancellous bone volume, although osteo-blast activity, estimated using osteoid width, was markedly reduced following adeno-associated virus NPY injection [17,18] These results are not in accor-dance with the cancellous bone phenotype of the above-mentioned mouse models of elevated NPY lev-els All of these opposing results make necessary a closer look at the role of NPY in the regulation of bone mass

Transthyretin (TTR) KO mice show increased levels

of amidated neuropeptides, owing to overexpression of peptidylglycine a-amidating monooxygenase (PAM) [19], the only enzyme that a-amidates peptides, and which is rate-limiting in the process of neuropeptide maturation, as its substrates exist in excess [20,21] Among the neuropeptides that are amidated by PAM, NPY is the most abundant in both the central and the peripheral nervous systems As NPY requires PAM-mediated a-amidation for biological activity [22], PAM overexpression in TTR KO mice results in increased levels of processed amidated NPY, without an increase

in NPY expression [19] As a consequence of the increased amidated NPY levels, TTR KO mice show a significant NPY overexpressor phenotype

Given the lack of information on the expression of NPY in the bone, together with the controversy con-cerning its function in bone homeostasis, we aimed at gaining a better understanding of the role of this neu-ropeptide in the control of bone mass by making use

of TTR KO mice, a model of increased NPY

Results

In bone, NPY is detected in chondrocytes, osteoblasts, and osteocytes

NPY expression was investigated in wild-type (WT) and TTR KO bone tissue by immunohistochemistry, using an antibody specific for the amidated form of NPY NPY immunolabeling was observed in bone marrow cells, including megakaryocytes (Fig 1Aa), as already described in the literature [14] The periosteum (Fig 1Ab) also showed NPY immunoreactivity, as already reported for mice and rats [10–12] However,

we observed NPY immunostaining in chondrocytes, osteoblasts, and osteocytes (Fig 1Ac–f, respectively, arrows) No NPY immunoreactivity was found in osteoclasts (data not shown) Similar to our observa-tions in the adult bone, NPY immunoreactivity was detected starting at embryonic day 16 in megakaryo-cytes, osteoblasts, and chondrocytes; this NPY detec-tion pattern was maintained at embryonic day 18 (Fig 1B) No immunoreactivity was detected when the

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Fig 1 NPY immunohistochemistry in the bone tissue BM, bone marrow; C, chondrocytes; O, osteoblasts; AC, articular chondrocytes; Os, osteocytes; M, megakaryocytes; P, periosteum Scale bar: 50 lm (A) NPY immunoreactivity in bone cells, namely bone marrow cells and megakaryocytes (a), periosteum (b), articular cartilage chondrocytes (c), late proliferating chondrocytes (d), osteoblasts (e), and osteocytes (f) Arrows indicate labeled cells, and fibers in the case of the periosteum (B) NPY immunoreactivity in the bone at embryonic day 18, show-ing NPY stainshow-ing in megakaryocytes (a), chondrocytes (b), and osteoblasts (c) (C) Immunohistochemistry in bone sections where the anti-body against NPY was replaced by mouse IgG (D) NPY immunohistochemistry in NPY KO bone sections (E) Comparison between NPY (right) and osteocalcin (left) immunolabeling in the bone tissue Arrows indicate labeled osteoblasts (F) Nerve fiber (NF200 and PGP9.5) immunohistochemistry: articular cartilage chondrocytes (a), proliferating chondrocytes (b), osteoblasts (c), bone marrow cells (d), and perios-teum (e).

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NPY antibody was replaced by mouse IgGs (Fig 1C).

Moreover, in NPY KO mouse bone sections, none of

the different bone cells showed NPY immunostaining

(Fig 1D), suggesting that the immunoreactivity

observed in WT and TTR KO bone tissue was

NPY-specific To further demonstrate NPY synthesis in

os-teoblasts, osteoblast-specific staining was performed

with an antibody against osteocalcin (Fig 1E, left

panel, arrow) The results obtained revealed that the

pattern of staining was comparable to that obtained

for NPY, as shown in the right panel of Fig 1E, thus

confirming NPY expression in osteoblasts To further

demonstrate that NPY is synthesized in these bone

cells, additional negative controls were performed

Using antibody against neurofilament 200 (NF200) or

antibody against protein gene product 9.5 (PGP9.5),

two nerve fiber markers, no staining was observed in

chondrocytes, osteoblasts, or bone marrow cells

(Fig 1Fa–d, respectively), whereas in the periosteum

typical nerve fiber labeling was detected (Fig 1Fe)

TTR KO bone tissue has increased amidated NPY levels

From the comparison between WT and TTR KO NPY immunoreactivity in bone sections, we observed that TTR KO bone tissue displayed increased amidated NPY levels when compared to the wild type (Fig 2A, arrows), further demonstrating the expression of this neuropep-tide by bone cells NPY immunostaining was increased

in chondrocytes, osteoblasts, osteocytes, bone marrow cells and megakaryocytes (Fig 2a–e, respectively) from TTR KO mice when compared to the same WT cells This result is in accordance with the increased NPY lev-els reported in the nervous system of TTR KOs [19], sug-gesting that the increased NPY levels in this strain are not nervous system-restricted Given the increased NPY levels in TTR KO bones, PAM expression was subse-quently evaluated in this tissue by immunohistochemis-try; PAM was detected in bone marrow cells, including megakaryocytes (Fig 2Ba, arrows), osteoblasts, and

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Fig 2 Analysis of NPY and PAM in WT and TTR KO bone sections Scale bar: 50 lm (A) Comparison of NPY immunostaining in

WT and TTR KO bone sections Arrows indicate the different cell types in evidence

in each panel, namely articular cartilage chondrocytes (a), proliferating chondrocytes (b), osteoblasts (c), osteocytes (d), bone marrow cells (BM) and megakaryocytes (M) (e) (B) PAM immunostaining in the bone marrow (a; arrows indicate megakaryo-cytes), osteocytes (b; arrows), osteoblasts (b;p arrowheads), and chondrocytes (c) (C) Quantification of the density of PAM immunostaining in the bone marrow of WT and TTR KO mice a P < 0.05.

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osteocytes (Fig 2Bb, arrowheads and arrows,

respec-tively), as well as in chondrocytes (Fig 2Bc) The major

difference in PAM expression among WT and TTR KO

bones was found in the bone marrow, where PAM

immunostaining was approximately two-fold higher in

TTR KO mice (Fig 2C) Despite the fact that NPY and

PAM expression were not observed in osteoclasts, the

hypothesis that increased NPY levels in the bone of

TTR KO mice may have an indirect effect on osteoclasts

existed To address this hypothesis, preosteoclasts and

mature osteoclasts in WT and TTR KO bones were

detected by OSCAR staining Following quantification,

no differences in osteoclast number were detected

between strains (data not shown)

TTR KO mice have increased bone mineral

density (BMD) and trabecular volume

To address whether the increased NPY levels observed

in TTR KO femurs have physiological consequences in

the bone, we started by comparing bone histology in

WT and TTR KO mice The femur length did not

dif-fer significantly between strains (wild type,

15.6 ± 1.4 mm; TTR KO, 15.9 ± 1.0 mm) To

fur-ther analyze in detail the bone phenotype, micro

com-puted tomography (microCT) scanning analysis of

femurs, including measurement of BMD, was

per-formed As shown in Fig 3A (left and middle panels),

two-dimensional trabecular number and thickness were

increased in TTR KO femurs when compared with

WT femurs Furthermore, three-dimensional trabecular

bone volume in the proximal metaphysis was also

higher in TTR KO animals (Fig 3A, right panel)

From the statistical analysis of WT (n = 9) and TTR

KO (n = 10) femurs, the results obtained demonstrate

an increased trabecular volume (bone volume⁄

trabecu-lar volume) and BMD in TTR KO mice when

com-pared with WT littermates (Fig 3B) These results

suggest that increased amidated neuropeptide levels are

related to increased bone density and volume The

increase in bone volume was, however, detected only

in trabeculae, whereas the bone cortex was unaffected

This result suggested that the process of endochondral

ossification might be specifically affected To assess

this hypothesis, the growth plates of WT and TTR

KO mice were analyzed As can be seen in Fig 3C, no

differences were detectable by histological analysis of

growth plates from WT and TTR KO mice

NPY is expressed in osteoblasts

To further address NPY expression in bone cells,

namely in the osteoblastic cell line MC3T3-E1, and in

primary cultures of BMSCs throughout osteoblastic differentiation, we performed RT-PCR analysis of NPY expression Using brain as the positive control of NPY expression, we detected NPY in MC3T3-E1 cells and in both WT and TTR KO BMSCs (Fig 4A) Fur-thermore, both WT and TTR KO BMSCs on days 3,

7 and 14 of culture in osteogenic differentiation media showed NPY expression; no statistical differences were observed between WT and TTR KO BMSC cultures throughout the differentiation period (data not shown) To determine whether TTR KO mice BMSCs undergoing osteoblastic differentiation recapitulate our findings in the nervous system, i.e show increased PAM transcription and increased levels of amidated NPY, without increased NPY mRNA expression, we quantified PAM expression and the levels of the bio-logically active neuropeptide in differentiating WT and TTR KO BMSC cultures As expected, TTR KO mice BMSCs displayed increased amidated NPY levels (approximately 2.4-fold at day 3) when compared to

WT cells (Fig 4B) Despite the fact that the NPY con-tent decreased over the 14 days of differentiation, indi-cating that undifferentiated BMSCs have higher levels

of NPY than differentiated osteoblasts, these still expressed amidated neuropeptide One should, how-ever, note that in WT BMSCs, NPY levels were not altered throughout the course of BMSC differentiation (days 3–14; Fig 4B) Therefore, NPY should not be regarded as either a marker of osteoblast differentia-tion or a marker of mature osteoblasts In agreement with the increased NPY levels, PAM expression in TTR KO BMSCs was increased, with a similar fold change as that observed for the levels of amidated NPY (Fig 4C) Y1 expression was detected by RT-PCR in differentiating WT and TTR KO BMSCs, with no Y2 or Y5 receptor amplification (data not shown), in accordance with recently published results [15] However, no statistical difference was observed between the two strains regarding Y1 expression (data not shown)

TTR KO BMSCs show increased osteoblast differentiation

To examine whether WT and TTR KO BMSCs differ

in their capability to undergo osteoblast differentia-tion, as a possible consequence of their differential am-idated NPY content, isolated BMSCs from WT and TTR KO mice were cultured under osteoblast differen-tiation conditions Osteoblast phenotype markers such

as alkaline phosphatase (ALP) activity and osteocalcin expression were determined In both cultures, ALP activity increased in a time-dependent manner and

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Fig 3 MicroCT in WT and TTR KO mouse femurs (A) Bone microarchitecture in WT and TTR KO mice Left and middle panels: 2D microCT images of metaphyseal bone, showing reconstructed longitudinal sections (left panel) and transverse sections taken

 1 mm from the growth plate (middle panel) The line crossing the transversal sections indicates the orientation of the longitudinal sections Right panel: 3D mi-croCT images of metaphyseal trabecular bone in WT and TTR KO mice (B) Quantifi-cation of trabecular volume [bone vol-ume ⁄ trabecular volume (BV ⁄ TV)] and BMD

in WT and TTR KO mice Results are pre-sented as average ± standard error of the mean a P < 0.05 (C) Hematoxylin ⁄ eosin staining of the growth plate (femur) of WT and TTR KO mice (3 months old) Scale bars: 50 lm.

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Fig 4 NPY and PAM expression in bone cells from WT and TTR KO mice (A) NPY RT-PCR analysis in brain, MC3T3-E1 cells, and BMSCs (B) NPY quantification in BMSCs from WT and TTR KO mice at days 1, 3, 7 and 14 of differentiation into osteoblasts (C) Semiquantitative RT-PCR analysis of PAM expression normalized for b-actin (left) or HPRT (right) expression in BMSCs from WT and TTR KO mice at days 3 and 14 of osteoblast differentiation Results are presented as average ± stan-dard error of the mean; a P < 0.05.

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peaked on day 7, with significantly increased levels (ranging from two-fold to three-fold) being seen in TTR KO osteogenic cultures at days 3 and 7 when compared to WT cultures (Fig 5A) Regarding osteo-calcin expression, WT cultures displayed a time-depen-dent increase in osteocalcin levels, with a peak of expression on day 14 (Fig 5B), which is characteristic

of the osteoblastic differentiation process in vitro In the case of TTR KO BMSCs, no increase in osteocal-cin expression was observed from day 3 to day 7 of differentiation, probably because those cells already showed high osteocalcin levels at day 3 of differentia-tion (Fig 5B) Nonetheless, at day 14, TTR KO cul-tures showed a significant increase in osteocalcin expression when compared with the WT cultures (Fig 5B) To further confirm these data, RT-PCR was performed using additional housekeeping genes [those encoding glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and hypoxanthine-guanine phosphoribosyl-transferase (HPRT)] as well as osteopontin, an extra marker of osteoblastic differentiation Day 3 of BMSC differentiation was chosen for performance of the con-firmation because, at this time point, not only ALP activity but also osteocalcin expression are increased in TTR KO BMSCs The expression levels of both osteo-calcin (Fig 5C) and osteopontin (Fig 5D) were always increased in TTR KO BMSCs, irrespective of the housekeeping gene used to perform the normalization Taken together, these data suggest that TTR KO BMSCs show enhanced competence in undergoing osteoblast differentiation in vitro

Discussion The data presented in this study demonstrate that NPY is expressed in several types of bone cell, with both in vitro and in vivo evidence Moreover, we show that increased NPY levels are related to increased bone density, as well as to augmented competence in BMSC differentiation into osteoblasts In agreement with our findings, a recent report further supports the contribution

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Fig 5 Osteoblast differentiation of WT and TTR KO BMSCs as assessed by ALP, osteocalcin and osteopontin levels (A) ALP activ-ity of WT and TTR KO BMSCs under osteoblast differentiation con-ditions at days 3, 7 and 14 (B–D) Semiquantitative RT-PCR analysis

in WT and TTR KO BMSCs of (B) osteocalcin expression, normal-ized for the expression of b-actin, at days 3, 7 and 14, (C) osteocal-cin expression normalized for the expression of GAPDH and HPRT

at day 3, and (D) osteopontin expression, normalized for the expression of b-actin, GAPDH and HPRT at day 3 under osteoblast differentiation conditions Results are presented as average ± stan-dard error of the mean; a P < 0.05; b P < 0.005; c P < 0.0005.

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of the NPY pathway in bone homeostasis via a direct

action on osteoblasts [23] In that report, it was shown

that chronically elevated NPY levels modulate the

lev-els of Y2 receptor expression (according to the stage

of osteoblast differentiation) and that NPY is a

nega-tive regulator of Y1 receptor expression Moreover,

functional analysis revealed the osteogenic potential of

NPY, with osteoblast phenotype markers being

signifi-cantly enhanced in osteoprogenitor cells stimulated by

NPY, probably owing to downregulation of the Y1

receptor

Until now, NPY expression has only been detected

in bone marrow cells, including megakaryocytes [14]

Here, we show for the first time that BMSCs also

con-tribute to NPY in the bone marrow, as NPY is

expressed both in BMSCs and in BMSCs undergoing

osteoblastic differentiation Moreover, this article is

the first to report NPY expression in chondrocytes,

osteoblasts, osteocytes and the osteoblastic cell line

MC3T3-E1 In relation to chondrocytes, no studies

were performed regarding the role of NPY in the

dif-ferentiation of this cell type This could probably be

the aim of a subsequent study, where possible

differ-ences in articular cartilage or growth plate between

WT and TTR KO bones should be addressed In the

case of osteoclasts, although NPY expression was not

detected in this cell type, the elevated NPY levels in

TTR KO bones might have some indirect effect on

osteoclasts In fact, we recently reported that NPY

modulates receptor activator of nuclear factor-jB

(RANK) ligand and osteoprotegerin, two key factors

regulating bone remodeling [23] The inhibitory effect

of NPY on RANK ligand production by BMSCs was

also investigated by Amano et al [24], who suggested

that the inhibitory effect of NPY on osteoclastogenesis

was caused by suppression of isoprenaline-induced

RANK ligand production by stromal cells, upstream

of RANK ligand mRNA expression

It is known that central NPY regulates bone mass, as

conditional ablation of hypothalamic Y2 receptors

results in increased bone formation [5] Moreover,

lep-tin-deficient mice, in which NPY is increased in the

hypothalamus, show high cancellous bone mass, but

reduced cortical production [25] Central NPY can also

influence peripheral tissues through alterations in

auto-nomic neuronal activity This is probably mediated by

NPY projections from the hypothalamus to the

brain-stem areas where sympathetic neuronal activity is

mod-ulated [26] Thus, to achieve its functions, NPY may act

centrally on hypothalamic receptors and⁄ or

peripher-ally on its osteoblastic receptor Y1 after being released

from sympathetic nerve terminals supplying the skeletal

tissue With this work, we have opened a new window

in which NPY may additionally function as an auto-crine factor, as it is expressed by osteoblasts as well

We further demonstrate that TTR KO bone tissue displays increased amidated NPY levels, when com-pared to WT tissue, further demonstrating the expres-sion of this neuropeptide in bone cells In theoretical terms, the major TTR ligands, thyroxine (T4) and reti-nol, could be responsible, at least in part, for the bone phenotype observed in TTR KO mice Retinol defi-ciency is known to increase BMD [27]; additionally, reti-noic acid inhibits osteogenic differentiation of BMSCs [28,29] Despite the fact that TTR KO mice have retinol plasma levels below the level of detection [30], symp-toms of vitamin A deficiency are absent in these ani-mals In agreement with this, their total retinol tissue levels are not significantly different from those of WT mice [31] Moreover, retinoic acid plasma levels are two-fold to three-two-fold higher in TTR KO mice, probably compensating for their low retinol levels [31] Taking the above into account, it is highly unlikely that, with normal retinol levels in tissues and increased retinoic acid levels in the plasma, an impairment in retinol homeostasis would be responsible for the increased BMD in TTR KO mice Regarding thyroid hormones,

it is well known that hyperthyroidism in adult patients leads to decreased BMD [32] As expected, both total T4 and tri-iodothyronine serum levels are decreased in TTR KO mice [32,33] However, similar to what is described above for retinol, this decrease is unrelated to symptoms of hypothyroidism or thyroid gland abnor-malities [34] Again, in terms of tissue content, TTR KO mice show no differences in T4 levels from WT mice [35,36] This euthyroid status probably arises as a conse-quence of the high free T4 serum pool in the TTR KO mice [34] Such a euthyroid status is essential for normal skeletal development and maintenance, and therefore it

is hard to see how the bone phenotype of TTR KO mice could be related to thyroid hormones

It is additionally possible that in TTR KO mice, as

a consequence of PAM overexpression, increased levels

of other amidated neuropeptides may produce some complexity In this respect, although contradictory results have been reported for the action in bone of some amidated neuropeptides, such as substance P, others, such as pancreatic polypeptide and calcitonin gene-related peptide, have been described as stimulat-ing the differentiation of MC3T3-E1 cells [37] or increasing the number of bone colonies formed from bone marrow stromal cells (MSC) in vitro [38], simi-larly to what is reported here in the absence of TTR However, although not discarding the possible influ-ence of the putative increases in the levels of other amidated neuropeptides in this model, which should be

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addressed in future experiments, TTR KO mice not

only show increased NPY levels when compared with

other NPY overexpression models, but also present

an accompanying NPY overexpression phenotype This

phenotype includes decreased energy expenditure,

decreased depressive-like behavior, and increased

car-bohydrate consumption and preference, and most of

these features are not commonly observed in other

NPY overexpression models [19] It is noteworthy that

the increased NPY levels in TTR KO mice are

unre-lated to increased NPY mRNA expression, and result

from increased processing and amidation by PAM,

which is upregulated in TTR KO animals In fact,

although TTR is not expressed in BMSCs, PAM

expression is increased in TTR KO BMSCs, suggesting

that TTR KO osteoblasts have intrinsically augmented

PAM expression in relation to WT cells, as a

conse-quence of their physiological TTR-free environment

A similar finding was reported for TTR KO neurons

(like BMSCs, neurons lack TTR expression), as these

cells were also shown to display intrinsically decreased

neurite outgrowth, as a consequence of their

physio-logical TTR-free environment [39]

NPY control of bone mass is still controversial On

the one hand, there are two different mouse models

with increased NPY expression that show high

cancel-lous bone mass, the Y2 receptor KO mice [5] and mice

lacking leptin (ob⁄ ob mice) [7,16] Although sharing a

similar high cancellous bone phenotype, both models

differ in cortical bone regulation, with increased

corti-cal bone mass in Y2 receptor KO mice and decreased

cortical density in ob⁄ ob mice [23] On the other hand,

no NPY signaling in the bone, as is the case in Y1

receptor KO mice, leads to high bone mass [6], and

central NPY overexpression yields decreased osteoblast

activity [18] and bone mass [7], with no alteration in

cancellous bone volume [17,18] With regard to this

central NPY overexpression, the consequential increase

in leptin levels [40,41] cannot be excluded as the cause

of the effects observed Furthermore, the apparent

dis-crepancy between Y1 and Y2 receptor KO models

regarding NPY signaling and bone phenotype was

recently clarified by the hypothesis that the increased

central NPY levels observed in the Y2

receptor-defi-cient mice lead to Y1 receptor downregulation on bone

cells, which would explain their increased bone mass

phenotype [15] The fact that deletion of both Y1 and

Y2 receptors did not produce additive effects on

increased bone mass further supports this hypothesis,

as it suggests a common pathway from the

hypothala-mus to the bone involving both Y2 and Y1 signaling

[6], with probable central Y2 and peripheral Y1 effects

on bone tissue The NPY KO mouse is not very

help-ful in this matter, as its bone mass is normal [8] Here

we show that in TTR KO mice, an additional model showing increased NPY levels, an increased cancellous bone mass phenotype is observed, in agreement with the Y2 receptor KO and ob⁄ ob mouse phenotypes, fur-ther suggesting that increased NPY content might be related to increased cancellous bone mass Despite all the concerns discussed above regarding the use of TTR KO mice as a model of increased NPY levels, the main advantage of these animals over other NPY over-expression models is that, in addition to the increase in NPY levels, the leptin level is not altered [42], exclud-ing its interference in the bone phenotype observed

In summary, we provide evidence that NPY is expressed in bone cells, namely in osteoblasts Further-more, we report that in a model of increased amidated neuropeptide levels, showing an NPY overexpression phenotype, an increased bone mass phenotype is pres-ent Finally, on the basis of these findings, further work is needed to determine the localization of NPY and NPY receptors during bone injury, disease, and aging, and thereby elucidate the possible role of NPY

in the bone regeneration process

Experimental procedures Animals

Mice were handled according to the European Communi-ties Council Directive (86⁄ 609 ⁄ EEC) and national rules, and all studies performed were approved by the Portuguese General Veterinarian Board Male WT and TTR KO [33] littermate offspring of heterozygous breeding pairs, in the

129⁄ Sv background, were maintained at 24 ± 1 C under a

12 h light⁄ dark cycle and fed regular chow and tap water

ad libitum Prior to all experimental procedures, animals were anesthetized with ketamine (1 mgÆg)1body weight)⁄ mede-tomidine (0.02 lgÆg)1 body weight) Animals were killed with an overdose of anesthetic

Immunohistochemistry

Femurs from 3 month old male WT (n = 6) and TTR KO (n = 5) littermates were fixed in 4% paraformaldehyde

in NaCl⁄ Pi, decalcified in TBD-1 commercial solution (Thermo Electron Corporation), and embedded in paraffin; serial 4 lm thick longitudinal sections were then cut For studies during embryonic development, 16 day or 18 day

WT pregnant females were killed by cervical dislocation, and the fetuses were collected by cesarian section Sections were then deparaffinized, dehydrated in a modified alcohol series, and blocked for the endogenous peroxidase activity NPY immunohistochemistry was performed with the MOM Kit (Vector, Peterborough, UK), following the manufacturer’s

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instructions Briefly, bone sections from WT and TTR KO

mice, as well as sections from NPY KO mice (prepared

simi-larly to WT and TTR KO mouse samples; a kind gift from

H Herzog, Garvan Institute, Australia) were incubated in

the MOM kit blocking reagent for 1 h at room temperature,

prior to incubation with the monoclonal NPY antibody

NPY05 (generously provided by E Grouzmann, University

Hospital, Lausanne, Switzerland; diluted 1 : 2000 in MOM

diluent) for 1 h at room temperature NPY05 is specific for

the amidated form of NPY [30] Antigen visualization was

performed with the MOM avidin–biotinylated peroxidase

complex reagent (Vector), using 3-amino-9-ethyl carbazole

(Sigma, Lisbon, Portugal) as substrate On parallel control

sections, the primary antibody was replaced by mouse IgG

(Sigma) Immunohistochemical investigations for NF200

and PGP9.5, both markers of nerve fibers, osteocalcin (a

positive control for osteoblast staining), PAM and OSCAR

(a marker of preosteoclasts and mature osteoclasts) were

also performed Briefly, sections were incubated in blocking

buffer (1% BSA and 4% bovine serum in NaCl⁄ Pi) for

30 min at 37C in a moist chamber, and then incubated with

primary antibodies at the appropriate dilution in blocking

buffer, overnight at 4C The dilutions used were 1 : 2500

for rabbit NF200 IgG (Sigma), 1 : 4000 for rabbit

PGP9.5 IgG (Serotec, Kidlington, UK), 1 : 500 for goat

anti-osteocalcin IgG (Biomedical Technologies Inc., Stoughton,

MA, USA), 1 : 500 for rabbit anti-PAM IgG (a kind gift

from R Mains, University of Connecticut Health Center),

and 1 : 100 for mouse anti-OSCAR IgG (Santa Cruz

Bio-technology, Heidelberg, Germany) Antigen visualization

was performed with the biotin–extravidin–peroxidase kit

(Sigma), using 3-amino-9-ethylcarbazole (Sigma) as

sub-strate On parallel control sections, the primary antibody was

replaced with blocking buffer Immunohistochemical

analy-sis was performed independently by two observers For

quantification of PAM immunohistochemistry, the number

of labeled cellsÆmm)2 was scored in three nonoverlapping

micrographs with a magnification of· 40

Bone histology

Femurs were harvested from 3 month old male WT

(n = 6) and TTR KO (n = 5) mice After their length had

been measured, bones were fixed in 4% paraformaldehyde

in NaCl⁄ Pi, decalcified as described above, and embedded

in paraffin Serial 10 lm thick longitudinal sections were

cut Sections were then deparaffinized, dehydrated in a

modified alcohol series, and stained for hematoxylin⁄ eosin

MicroCT analysis

Dissected hindlimbs (femur plus tibia from WT and TTR

KO littermates, n = 9 and n = 10, respectively) were

scanned with high resolution (5 lm pixel size) microCT

(Skyscan 1172; Skyscan, Kontich, Belgium) The whole

mouse femur and tibia were reconstructed, and the trabecu-lar bone in the proximal metaphysis, comprising a region starting 0.25 mm from the growth plate and extending 1.5 mm (or 300 tomograms) distally, was analyzed Histo-morphometric analysis in two and three dimensions was performed with Skyscan software (ct-analyser v 1.5.1.3, Skyscan) For analysis of trabecular bone, cortical bone including the trabecular compartment was excluded by operator-drawn regions of interest, and 3D algorithms were used to determine the bone volume percentage (bone volume⁄ trabecular volume)

BMD measurement by microCT

Volumetric BMD values of the trabecular bone compart-ment within the femural and tibial metaphysis were mea-sured from the same regions of interest used to derive the microarchitectural parameters, using the manufacturer’s instructions Briefly, two calibration phantoms (Skyscan) with densities of 0.25 and 0.75 gÆcm)3and a sample of water were scanned and reconstructed using the same settings used for the femurs and tibiae The gray scale density values were converted into Hounsfield units, which were then used to compute the mean volumetric BMD of each femur and tibia

Cell cultures MC3T3-E1 mouse osteoblastic cell line culture

MC3T3-E1 cells, established as an osteoblastic cell line from normal mouse calvaria, were grown in alpha-MEM (Invitro-gen, Carlsbad, CA, USA) supplemented with 10% (v⁄ v) fetal bovine serum (Invitrogen), 0.5% (v⁄ v) gentamicin (Invitro-gen), 1% (v⁄ v) fungizone (Invitrogen), 50 lgÆmL)1vitamin C (Sigma) and 10 mm b-glycerophosphate (Sigma) in a humidi-fied 5% CO2incubator at 37C The medium was changed twice weekly At confluence, the cells were trypsinized and seeded in 24-well plates at a cell seeding density of

4· 104cells per well

BMSC culture

Primary BMSCs were obtained according to the method developed by Maniatopoulos et al [43] Briefly, femurs and tibias from 1 month old male WT and TTR KO littermates were aseptically excised from the hindlimbs, the epiphyses were cut off, and the marrow was flushed with standard culture medium, which consisted of alpha-MEM supple-mented with 10% fetal bovine serum, 50 lgÆmL)1 gentami-cin sulfate, and 2.5 lgÆmL)1 amphotericin B (Invitrogen) Cells were seeded in 75 cm2plastic culture flasks, and incu-bated in a humidified incubator (37C and 5% CO2) The medium was changed after the first 24 h to remove nonad-herent cells Subsequently, the adnonad-herent cells were cultured for 10 days, the medium being renewed every 3 days

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