There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy(HRT). The present study was designed to investigate the in vitro effects of estrogen-like activitie...There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy(HRT). The present study was designed to investigate the in vitro effects of estrogen-like activities of two widespread coumarins, osthole and imperatorin, using the MCF-7 cell proliferation assay and their alkaline phosphatase(ALP) activities in osteoblasts Saos-2 cells. The two compounds were found to strongly stimulate the proliferation of MCF-7 cells. The estrogen receptor-regulated ERα, progesterone receptor(PR) and PS2 m RNA levels were increased by treatment with osthole and imperatorin. All these effects were significantly inhibited by the specific estrogen receptor antagonist ICI182, 780. Cell cycle analysis revealed that their proliferation stimulatory effect was associated with a marked increase in the number of MCF-7 cells in S phase, which was similar to that observed with estradiol. It was also observed that they significantly increased ALP activity, which was reversed by ICI182,780. These results suggested that osthole and imperatorin could stimulate osteoblastic activity by displaying estrogenic properties or through the ER pathway. In conclusion, osthole and imperatorin may represent new pharmacological tools for the treatment of osteoporosis.展开更多
Objective:To systematically evaluate the protective effects of Humulus lupulus L.extract(HLE)on osteoporosis mice.Methods:In vivo experiment,a total of 3512-week-old female ICR mice were equally divided into 5 groups:...Objective:To systematically evaluate the protective effects of Humulus lupulus L.extract(HLE)on osteoporosis mice.Methods:In vivo experiment,a total of 3512-week-old female ICR mice were equally divided into 5 groups:the sham control group(sham);the ovariectomy with vehicle group(OVX);the OVX with estradiol valerate[EV,0.2 mg/(kg·d)];the OVX with low-or high-dose HLE groups[HLE,1 g/(kg·d)and 3 g/(kg·d)],7 in each group.Treatment began 1 week after the ovariectomized surgery and lasted for 12 weeks.Bone mass and trabecular bone mircoarchitecture were evaluated by micro computed tomography,and bone turnover markers in serum were evaluated using enzyme-linked immunosorbent assay(ELISA)kits.In vitro experiment,osteoblasts and osteoclasts were treated with HLE at doses of 0,4,20 and 100μg/mL.Biomarkers for bone formation in osteoblasts and bone resorption in osteoclasts were analyzed.Results:Compared with the OVX group,HLE exerted bone protective effects by the increase of estradiol(P<0.05),the improvement of cancellous bone structure,bone mineral density(P<0.01)and the reduction of serum alkaline phosphatase(ALP),tartrate resistant acid phosphatase(TRAP),bone gla-protein,c-terminal telopeptides of typeⅠcollagen(CTX-Ⅰ)and deoxypyridinoline levels(P<0.01 for all).In vitro experiment,compared with the control group,HLE at 20μg/mL promoted the cell proliferation(P<0.01),and increased the expression of bone morphogenetic protein-2 and osteopontin levels in osteoblasts(both P<0.05).HLE at 100μg/mL increased the osteoblastic ALP activities,and HLE at all dose enhanced the extracellular matrix mineralization(both P<0.01).Furthermore,compared with the control group,HLE at 20μg/m L and 100μg/m L inhibited osteoclastic TRAP activity(P<0.01),and reduced the expression of matrix metalloproteinase-9 and cathepsin K(both P<0.05).Conclusion:HLE may protect against bone loss,and have potentials in the treatment of osteoporosis.展开更多
Flavonoids are a large group of phenolic secondary metabolites havinga wide range of biochemical and pharmacological effects.Quantitative analysis of flavonoid profiles in the genus Actinidia,which has not been intens...Flavonoids are a large group of phenolic secondary metabolites havinga wide range of biochemical and pharmacological effects.Quantitative analysis of flavonoid profiles in the genus Actinidia,which has not been intensively conducted,is useful to a better understanding of the pattern and distribution of flavonoids.In the present work,a liquid chromatography-electrospray ionization-tandem mass spectrometry(LC-ESI-MS/MS)method was developed to profile the flavonoids,which was then used to determine the dynamic change of 17 biologically active flavonoids in the leaves of Actinidia valvata at the main growing stages,including glucuronides and acylated di-and triglycosides of flavonoids.The contents of flavonoid triglycosides were significantly higher than other flavonoids.The highest concentrations of kaemperol glycosides were observed in June,while other flavonoids showed highest concentrations in October.On the other hand,the contents of four isorhamnetin glycosides were increased sharply in September to October.The flavonoid profiles seem to be related to temperature,UV-B,and water deficit.Further studies are required to examine the functions of flavonoids in the Actinidia valvata and the underlying molecular mechanisms of actions.展开更多
基金supported by the National Natural Science Foundation of China(No.81202865)
文摘There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy(HRT). The present study was designed to investigate the in vitro effects of estrogen-like activities of two widespread coumarins, osthole and imperatorin, using the MCF-7 cell proliferation assay and their alkaline phosphatase(ALP) activities in osteoblasts Saos-2 cells. The two compounds were found to strongly stimulate the proliferation of MCF-7 cells. The estrogen receptor-regulated ERα, progesterone receptor(PR) and PS2 m RNA levels were increased by treatment with osthole and imperatorin. All these effects were significantly inhibited by the specific estrogen receptor antagonist ICI182, 780. Cell cycle analysis revealed that their proliferation stimulatory effect was associated with a marked increase in the number of MCF-7 cells in S phase, which was similar to that observed with estradiol. It was also observed that they significantly increased ALP activity, which was reversed by ICI182,780. These results suggested that osthole and imperatorin could stimulate osteoblastic activity by displaying estrogenic properties or through the ER pathway. In conclusion, osthole and imperatorin may represent new pharmacological tools for the treatment of osteoporosis.
基金Supported by the National Natural Science Foundation of China(No.U1603283)。
文摘Objective:To systematically evaluate the protective effects of Humulus lupulus L.extract(HLE)on osteoporosis mice.Methods:In vivo experiment,a total of 3512-week-old female ICR mice were equally divided into 5 groups:the sham control group(sham);the ovariectomy with vehicle group(OVX);the OVX with estradiol valerate[EV,0.2 mg/(kg·d)];the OVX with low-or high-dose HLE groups[HLE,1 g/(kg·d)and 3 g/(kg·d)],7 in each group.Treatment began 1 week after the ovariectomized surgery and lasted for 12 weeks.Bone mass and trabecular bone mircoarchitecture were evaluated by micro computed tomography,and bone turnover markers in serum were evaluated using enzyme-linked immunosorbent assay(ELISA)kits.In vitro experiment,osteoblasts and osteoclasts were treated with HLE at doses of 0,4,20 and 100μg/mL.Biomarkers for bone formation in osteoblasts and bone resorption in osteoclasts were analyzed.Results:Compared with the OVX group,HLE exerted bone protective effects by the increase of estradiol(P<0.05),the improvement of cancellous bone structure,bone mineral density(P<0.01)and the reduction of serum alkaline phosphatase(ALP),tartrate resistant acid phosphatase(TRAP),bone gla-protein,c-terminal telopeptides of typeⅠcollagen(CTX-Ⅰ)and deoxypyridinoline levels(P<0.01 for all).In vitro experiment,compared with the control group,HLE at 20μg/mL promoted the cell proliferation(P<0.01),and increased the expression of bone morphogenetic protein-2 and osteopontin levels in osteoblasts(both P<0.05).HLE at 100μg/mL increased the osteoblastic ALP activities,and HLE at all dose enhanced the extracellular matrix mineralization(both P<0.01).Furthermore,compared with the control group,HLE at 20μg/m L and 100μg/m L inhibited osteoclastic TRAP activity(P<0.01),and reduced the expression of matrix metalloproteinase-9 and cathepsin K(both P<0.05).Conclusion:HLE may protect against bone loss,and have potentials in the treatment of osteoporosis.
基金financially supported by National Natural Science Foundation of China(Nos.81102336 and U1203104)Special Project of Biological Medicine of Science and Technology Commission of Shanghai Municipality(No.10431900500)
文摘Flavonoids are a large group of phenolic secondary metabolites havinga wide range of biochemical and pharmacological effects.Quantitative analysis of flavonoid profiles in the genus Actinidia,which has not been intensively conducted,is useful to a better understanding of the pattern and distribution of flavonoids.In the present work,a liquid chromatography-electrospray ionization-tandem mass spectrometry(LC-ESI-MS/MS)method was developed to profile the flavonoids,which was then used to determine the dynamic change of 17 biologically active flavonoids in the leaves of Actinidia valvata at the main growing stages,including glucuronides and acylated di-and triglycosides of flavonoids.The contents of flavonoid triglycosides were significantly higher than other flavonoids.The highest concentrations of kaemperol glycosides were observed in June,while other flavonoids showed highest concentrations in October.On the other hand,the contents of four isorhamnetin glycosides were increased sharply in September to October.The flavonoid profiles seem to be related to temperature,UV-B,and water deficit.Further studies are required to examine the functions of flavonoids in the Actinidia valvata and the underlying molecular mechanisms of actions.
