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Effects and mechanisms of 8-prenylnaringenin on osteoblast MC3T3-E1 and osteoclast-like cells RAW264.7.

Luo D, Kang L, Ma Y, Chen H, Kuang H, Huang Q, He M, Peng W - Food Sci Nutr (2014)

Bottom Line: The osteoblast MC3T3-E1 and osteoclast-like cell line RAW264.7 were treated with 17β-estradiol (10(-8) mol/L), genistein (10(-5) mol/L), daidzein (10(-5) mol/L), 8-PN (10(-5) mol/L) alone or in the presence of ERα antagonist MPP (10(-7) mol/L) and ERβ antagonist PTHPP (1.5 × 10(-7) mol/L).It has been found that 8-PN did not affect osteoblast proliferation, and that 8-PN increased alkaline phosphatase (ALP) activity, osteocalcin (OCN) concentrations, and the mineralized nodules. 8-PN inhibited RAW264.7 differentiating into osteoclasts and reduced the pit area of bone resorption. 8-PN could also inhibit the protein and mRNA expression of receptor activator of nuclear factor-κB ligand (RANKL) in osteoblasts, and conversely promote the expression of osteoprotegerin (OPG).In conclusion, the effects of 8-PN on promoting osteoblastic bone formation and inhibiting osteoclastic bone resorption were mediated by ERα instead of ERβ and the efficacy was more potent than that of the two classic phytoestrogens: genistein and daidzein.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Food Science and Technology, Medical School, Nanchang University Bayi Road 461, Nanchang, Jiangxi Province, China.

ABSTRACT
8-Prenylnaringenin (8-PN) is a phytoestrogen with the highest estrogenic activity. The objective of the present study was to confirm the superiority of 8-PN on bone metabolisms and the estrogen receptor (ER) subtype mediating effects of 8-PN. The osteoblast MC3T3-E1 and osteoclast-like cell line RAW264.7 were treated with 17β-estradiol (10(-8) mol/L), genistein (10(-5) mol/L), daidzein (10(-5) mol/L), 8-PN (10(-5) mol/L) alone or in the presence of ERα antagonist MPP (10(-7) mol/L) and ERβ antagonist PTHPP (1.5 × 10(-7) mol/L). It has been found that 8-PN did not affect osteoblast proliferation, and that 8-PN increased alkaline phosphatase (ALP) activity, osteocalcin (OCN) concentrations, and the mineralized nodules. 8-PN inhibited RAW264.7 differentiating into osteoclasts and reduced the pit area of bone resorption. 8-PN could also inhibit the protein and mRNA expression of receptor activator of nuclear factor-κB ligand (RANKL) in osteoblasts, and conversely promote the expression of osteoprotegerin (OPG). These effects of 8-PN were mainly inhibited not by PTHPP but by MPP and they were weaker than estrogen's effects but stronger than those of genistein and daidzein. In conclusion, the effects of 8-PN on promoting osteoblastic bone formation and inhibiting osteoclastic bone resorption were mediated by ERα instead of ERβ and the efficacy was more potent than that of the two classic phytoestrogens: genistein and daidzein.

No MeSH data available.


Related in: MedlinePlus

(A) Effects of 17β-estradiol (E2, 10−8 mol/L), genistein (Gen, 10−5 mol/L), daidzein (Dai, 10−5 mol/L), and 8-prenylnaringenin (8PN, 10−5 mol/L) alone or supplemented with ERα antagonist methyl-piperidino-pyrazole (MPP, 10−7 mol/L) or ERβ antagonist 4-[2-phenyl-5,7-bis (tri-fluoro- methyl) pyrazolo [1,5-a] pyrimidin-3-yl] phenol (PTHPP, 1.5 × 10−7 mol/L) on bone resorption pits on bone slice observed under optical microscope (100×). (B) Different area of bone resorption pits calculated by the IPP software among groups. **P < 0.01 versus control group (Con), #P < 0.05 and ##P < 0.01 versus 8PN group. ER, estrogen receptor.
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fig07: (A) Effects of 17β-estradiol (E2, 10−8 mol/L), genistein (Gen, 10−5 mol/L), daidzein (Dai, 10−5 mol/L), and 8-prenylnaringenin (8PN, 10−5 mol/L) alone or supplemented with ERα antagonist methyl-piperidino-pyrazole (MPP, 10−7 mol/L) or ERβ antagonist 4-[2-phenyl-5,7-bis (tri-fluoro- methyl) pyrazolo [1,5-a] pyrimidin-3-yl] phenol (PTHPP, 1.5 × 10−7 mol/L) on bone resorption pits on bone slice observed under optical microscope (100×). (B) Different area of bone resorption pits calculated by the IPP software among groups. **P < 0.01 versus control group (Con), #P < 0.05 and ##P < 0.01 versus 8PN group. ER, estrogen receptor.

Mentions: RAW264.7 cells induced osteoclastic differentiation with the stimulation of RANKL and m-CSF. On day 15, after the bone slices were added, the blue bone absorption pits appeared in the round, oval, and sausage shaped (Fig. 6). The borders of the bone pits were clear and the sizes were different. When treated with the compounds, the bone slices coculturing with RAW264.7 were shown differently decreased area of the bone pits. The effects of 8-PN were similar to those of E2 and significantly stronger than those of Gen and Dai (P < 0.05) and were inhibited not by PTHPP but by MPP(P < 0.05) (Fig. 7).


Effects and mechanisms of 8-prenylnaringenin on osteoblast MC3T3-E1 and osteoclast-like cells RAW264.7.

Luo D, Kang L, Ma Y, Chen H, Kuang H, Huang Q, He M, Peng W - Food Sci Nutr (2014)

(A) Effects of 17β-estradiol (E2, 10−8 mol/L), genistein (Gen, 10−5 mol/L), daidzein (Dai, 10−5 mol/L), and 8-prenylnaringenin (8PN, 10−5 mol/L) alone or supplemented with ERα antagonist methyl-piperidino-pyrazole (MPP, 10−7 mol/L) or ERβ antagonist 4-[2-phenyl-5,7-bis (tri-fluoro- methyl) pyrazolo [1,5-a] pyrimidin-3-yl] phenol (PTHPP, 1.5 × 10−7 mol/L) on bone resorption pits on bone slice observed under optical microscope (100×). (B) Different area of bone resorption pits calculated by the IPP software among groups. **P < 0.01 versus control group (Con), #P < 0.05 and ##P < 0.01 versus 8PN group. ER, estrogen receptor.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4221832&req=5

fig07: (A) Effects of 17β-estradiol (E2, 10−8 mol/L), genistein (Gen, 10−5 mol/L), daidzein (Dai, 10−5 mol/L), and 8-prenylnaringenin (8PN, 10−5 mol/L) alone or supplemented with ERα antagonist methyl-piperidino-pyrazole (MPP, 10−7 mol/L) or ERβ antagonist 4-[2-phenyl-5,7-bis (tri-fluoro- methyl) pyrazolo [1,5-a] pyrimidin-3-yl] phenol (PTHPP, 1.5 × 10−7 mol/L) on bone resorption pits on bone slice observed under optical microscope (100×). (B) Different area of bone resorption pits calculated by the IPP software among groups. **P < 0.01 versus control group (Con), #P < 0.05 and ##P < 0.01 versus 8PN group. ER, estrogen receptor.
Mentions: RAW264.7 cells induced osteoclastic differentiation with the stimulation of RANKL and m-CSF. On day 15, after the bone slices were added, the blue bone absorption pits appeared in the round, oval, and sausage shaped (Fig. 6). The borders of the bone pits were clear and the sizes were different. When treated with the compounds, the bone slices coculturing with RAW264.7 were shown differently decreased area of the bone pits. The effects of 8-PN were similar to those of E2 and significantly stronger than those of Gen and Dai (P < 0.05) and were inhibited not by PTHPP but by MPP(P < 0.05) (Fig. 7).

Bottom Line: The osteoblast MC3T3-E1 and osteoclast-like cell line RAW264.7 were treated with 17β-estradiol (10(-8) mol/L), genistein (10(-5) mol/L), daidzein (10(-5) mol/L), 8-PN (10(-5) mol/L) alone or in the presence of ERα antagonist MPP (10(-7) mol/L) and ERβ antagonist PTHPP (1.5 × 10(-7) mol/L).It has been found that 8-PN did not affect osteoblast proliferation, and that 8-PN increased alkaline phosphatase (ALP) activity, osteocalcin (OCN) concentrations, and the mineralized nodules. 8-PN inhibited RAW264.7 differentiating into osteoclasts and reduced the pit area of bone resorption. 8-PN could also inhibit the protein and mRNA expression of receptor activator of nuclear factor-κB ligand (RANKL) in osteoblasts, and conversely promote the expression of osteoprotegerin (OPG).In conclusion, the effects of 8-PN on promoting osteoblastic bone formation and inhibiting osteoclastic bone resorption were mediated by ERα instead of ERβ and the efficacy was more potent than that of the two classic phytoestrogens: genistein and daidzein.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Food Science and Technology, Medical School, Nanchang University Bayi Road 461, Nanchang, Jiangxi Province, China.

ABSTRACT
8-Prenylnaringenin (8-PN) is a phytoestrogen with the highest estrogenic activity. The objective of the present study was to confirm the superiority of 8-PN on bone metabolisms and the estrogen receptor (ER) subtype mediating effects of 8-PN. The osteoblast MC3T3-E1 and osteoclast-like cell line RAW264.7 were treated with 17β-estradiol (10(-8) mol/L), genistein (10(-5) mol/L), daidzein (10(-5) mol/L), 8-PN (10(-5) mol/L) alone or in the presence of ERα antagonist MPP (10(-7) mol/L) and ERβ antagonist PTHPP (1.5 × 10(-7) mol/L). It has been found that 8-PN did not affect osteoblast proliferation, and that 8-PN increased alkaline phosphatase (ALP) activity, osteocalcin (OCN) concentrations, and the mineralized nodules. 8-PN inhibited RAW264.7 differentiating into osteoclasts and reduced the pit area of bone resorption. 8-PN could also inhibit the protein and mRNA expression of receptor activator of nuclear factor-κB ligand (RANKL) in osteoblasts, and conversely promote the expression of osteoprotegerin (OPG). These effects of 8-PN were mainly inhibited not by PTHPP but by MPP and they were weaker than estrogen's effects but stronger than those of genistein and daidzein. In conclusion, the effects of 8-PN on promoting osteoblastic bone formation and inhibiting osteoclastic bone resorption were mediated by ERα instead of ERβ and the efficacy was more potent than that of the two classic phytoestrogens: genistein and daidzein.

No MeSH data available.


Related in: MedlinePlus