Effect of melatonin on bone metabolism in ovariectomized rats

Ladizesky, M.; Cutrera, Rodolfo A.; Boggio, Verónica; Somoza, J.; Centrella, José M.; Mautalén, C.; Cardinali, Daniel P.

doi:10.1016/s0024-3205(01)01431-x

Cited by 59 publications

(65 citation statements)

References 28 publications

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“…20,31,37 Other studies have also determined that MEL supports bone and mineral metabolism. 19,20,31,38 MEL has no depressive effect on the cardiovascular system, and minimal other side effects including slight sedation and disturbance of circadian rhythmicity and sleep-wake cycle, which are negligible symptoms in trauma patients. 23 In recent studies MEL has been suggested to be an anti-ageing hormone, with ageing believed to be a syndrome of pineal inefficiency or MEL reduction.…”

Section: Discussionmentioning

confidence: 98%

The effect of exogenous melatonin administration on trabecular width, ligament thickness and TGF-β1 expression in degenerated intervertebral disk tissue in the rat

Turğut

Öktem

Uslu

et al. 2006

Journal of Clinical Neuroscience

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Section: Discussionmentioning

confidence: 98%

The effect of exogenous melatonin administration on trabecular width, ligament thickness and TGF-β1 expression in degenerated intervertebral disk tissue in the rat

Turğut

Öktem

Uslu

et al. 2006

Journal of Clinical Neuroscience

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“…It is synthesized in the pineal gland during the dark period [1]. Melatonin has been described as functioning in many physio-pathological processes including sleep disorders, mild depression [2], obesity [3], cancer [4] and bone formation [5]. The synthesis of melatonin from serotonin is directed by a series of enzymes, of which arylalkylamine (serotonin) N-acetyltransferase (AANAT; EC 2.3.1.87) catalyses the penultimate and rate-limiting step.…”

mentioning

confidence: 99%

New substrate analogues of human serotonin N‐acetyltransferase produce in situ specific and potent inhibitors

Ferry

Ubeaud

Mozo

et al. 2003

European Journal of Biochemistry

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Melatonin is synthesized by an enzymatic pathway, in which arylalkylamine (serotonin) N‐acetyltransferase catalyzes the rate‐limiting step. A previous study [Khalil, E.M., De Angelis, J., Ishii, M. & Cole, P.A. (1999) Proc. Natl Acad. Sci. USA96, 12418–12423] reported the discovery of bromoacetyltryptamine (BAT), a new type of inhibitor of this enzyme. This compound is the precursor of a potent bifunctional inhibitor (analogue of the transition state), capable of interfering with both the substrate and the cosubstrate binding sites. This inhibitor is biosynthesized by the enzyme itself in the presence of free coenzyme A. In the present report, we describe the potency of new N‐halogenoacetyl derivatives leading to a strong in situ inhibition of serotonin N‐acetyltransferase. The new concept behind the mechanism of action of these precursors was studied by following the biosynthesis of the inhibitor from tritiated‐BAT in a living cell. The fate of tritiated‐phenylethylamine (PEA), a natural substrate of the enzyme, in the presence or absence of [3H]BAT was also followed, leading to their incorporation into the reaction product or the inhibitor (N‐acetyl[3H]PEA and coenzyme A‐S[3H]acetyltryptamine, respectively). The biosynthesis of this bifunctional inhibitor derived from BAT was also followed by nuclear magnetic resonance during its catalytic production by the pure enzyme. In a similar manner we studied the production of another inhibitor generated from N‐[2‐(7‐hydroxynaphth‐1‐yl)ethyl]bromoacetamide. New derivatives were also screened for their capacity to inhibit a purified enzyme, in addition to enzyme overexpressed in a cellular model. Some of these compounds proved to be extremely potent, with IC50s of ≈ 30 nm. As these compounds, by definition, closely resemble the natural substrates of arylalkylamine N‐acetyltransferase, we also show that they are potent ligands at the melatonin receptors. Nevertheless, these inhibitors form a series of pharmacological tools that could be used to understand more closely the inhibition of pineal melatonin production in vivo.

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“…Although, the variable changes according to the time of blood collection, types of study and used animals were reported, and some augments were existed in interpret base on bone turnover and bone formation, serum osteocalcin levels were generally accepted as a marker of bone turnover. 31,32) GR extracts showed dramatical and dose-dependent inhibition on the increase of serum osteocalcin induced by OVX osteoporosis, thus it is considered as indirect evidence that GR extracts has an anti-resorption of bone. Although, somewhat another reason of increase of serum Ca and P levels were exist, it is generally accepted that the increase of serum Ca and P levels were marker of bone formations in osteoporotic animal models.…”

Section: Discussionmentioning

confidence: 99%

The Anti-osteoporotic Effect of Aqueous Extracts of Gastrodiae Rhizoma In Vitro and In Vivo

Seo

Joo

Park

et al. 2010

JOURNAL OF HEALTH SCIENCE

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The anti-osteoporotic effects of aqueous extracts of Gastrodiae Rhizoma (GR) were observed in vitro and in vivo. The effects on proliferation and alkaline phosphatase activity of primary osteoblasts, bone nodule formation, pit formation of osteoclasts and osteoclastogenesis were observed in vitro, and to observe the in vivo efficacy GR were orally administered once a day for 28 days to bilateral ovariectomy-induced osteoporosis mice at 125, 250 and 500 mg/kg. GR extracts enhanced the proliferation, differentiation, and bone nodule formation of primary cultured osteoblasts, but they inhibited the pit formation and the number of multinucleated osteoclast-like cells, osteoclastogenesis in vitro. As results of ovariectomy-induced osteoporotic process, dramatical decreases of bone weights and thickness of bone at epiphyseal regions, bone Ca and P contents, bone mineral density and failure load, serum Ca and P levels with increase of serum osteocalcin level. At histopathology-histomorphometry, dramatical decreases of trabecular and cortical bone masses were detected with classic histomorphometrical changes of bones including decrease of trabecular bone volume, thickness, length and number and cortical bone thickness and increase of osteoclast/bone perimeter. Hoevere, these estrogen-deficient osteoporotic changes were also dramatically and dose-dependently inhibited by treatment of all three different dosages of GR extracts. It was concluded that GR extracts has relatively good favorable effect to prevention and/or treatment of ovariectomy (OVX)-induced osteoporosis through osteoblast activation and inhibition of osteoclastogenesis and osteoclast activity.

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Effect of melatonin on bone metabolism in ovariectomized rats

Cited by 59 publications

References 28 publications

The effect of exogenous melatonin administration on trabecular width, ligament thickness and TGF-β1 expression in degenerated intervertebral disk tissue in the rat

The effect of exogenous melatonin administration on trabecular width, ligament thickness and TGF-β1 expression in degenerated intervertebral disk tissue in the rat

New substrate analogues of human serotonin N‐acetyltransferase produce in situ specific and potent inhibitors

The Anti-osteoporotic Effect of Aqueous Extracts of Gastrodiae Rhizoma In Vitro and In Vivo

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