Objective:Gut-derived serotonin strongly inhibits bone formation by inhibiting osteoblast proliferation.Our previous study demonstrated that the lignan-rich fraction prepared from Sambucus willimasii Hance,a folk herb...Objective:Gut-derived serotonin strongly inhibits bone formation by inhibiting osteoblast proliferation.Our previous study demonstrated that the lignan-rich fraction prepared from Sambucus willimasii Hance,a folk herbal medicine used to treat bone fractures and joint diseases in China,exerted bone-protective effects,and its actions were modulated by suppressing the synthesis of gut-derived serotonin via the inhibition of intestinal tryptophan hydroxylase 1(TPH-1).However,there is no direct evidence for the action of lignans on TPH-1.This study aimed to verify the direct action of lignans on the TPH-1 and its influence on serotonin synthesis and bone properties.Methods:Molecular docking and surface plasmon resonance were performed to determine the affinities of lignans to TPH-1.The cell viability and the protein activity and expression of TPH-1 were measured in RBL2H3 cells.The serum serotonin level and bone mineral density upon lignan treatment in ovariectomized mice were determined.Result:The lignans showed high binding scores and binding affinities to TPH-1,inhibited the activity and protein expression of TPH-1,suppressed the serum serotonin levels in ovariectomized mice as well as promoted bone mineral density.Conclusion:This is the first study to report that lignans are novel TPH-1 inhibitors and that these lignans could be potential agents for the management of serotonin-related diseases,including osteoporosis.展开更多
[Objectives] To explore the antioxidant activity of Sambucus williamsii seed oil. [Methods]DPPH scavenging method and Prussian blue method( total reducing power) were used. S. williamsii seed oil has antioxidant activ...[Objectives] To explore the antioxidant activity of Sambucus williamsii seed oil. [Methods]DPPH scavenging method and Prussian blue method( total reducing power) were used. S. williamsii seed oil has antioxidant activity. In the DPPH scavenging free radical experiment,S. williamsii oil showed the ability to scavenge free radicals,and its scavenging ability had linear relationship with oil concentration( R =0. 999 6). Besides,the IC_(50) value of S. williamsii seed oil scavenging DPPH free radicals was 61. 30 ± 0. 88 mg/mL. In the total reducing power measurement experiment,the S. williamsii seed oil has a reducing ability,and its reducing ability is proportional to the oil concentration,and has the concentration dependence. Through studying the inhibitory effect of S. williamsii seed oil on α-glucosidase,the hypoglycemic activity of S. williamsii seed oil was determined. The ability of samples to inhibit α-glucosidase was judged through measuring the absorbance at 400 nm of the reaction system. [Results]In the concentration range of 1. 56-25. 00 mg/mL,the S. williamsii seed oil can effectively inhibit α-glucosidase,and the inhibition rate was 62. 66%-85. 22%. The animal in vivo experiment was used to determine the hypolipidemic activity of the S. williamsii seed oil. First,a high fat modelwas established,S. williamsii seed oil was given through intragastric administration. Then,total cholesterol( TC),triglyceride( TG),high-density lipoprotein cholesterol( HDL-C),and low density lipoprotein cholesterol( LDL-C) were measured. Through comparison of high,medium and low dose groups of S. williamsii seed oil with the high fat modelcontrol group,it was found that the TC,TG,LDL-C levels were significantly decreased( P < 0. 01) and the HDL-C levels were significantly increased( P < 0. 05),indicating that S. williamsii seed oil can effectively reduce the levels of TC,TG,LDL-C in the serum of hyperlipidemic mice,and effectively inhibit the decrease of HDL-C level,thus S. williamsii seed oil can reduce blood lipids in mice,namely,has hypolipidemic effects. In addition,the greater the dose of S. williamsii seed oil,the more obvious the effect of blood lipid levels in mice,indicating that the hypolipidemic effect of S. williamsii seed oil was dose dependent. [Conclusions] S. williamsii seed oil has reducing ability,and there is a significant dose-effect relationship in the concentration range of 2-10 mg/mL. As natural plant oil,S. williamsii seed oil has the advantages of good stability,small toxic and side effects,and strong effect,and has high value of developing new antioxidants.展开更多
目的综述接骨木治疗骨质疏松症的活性成分及作用机制的研究进展,为其进一步研究和开发利用提供参考。方法利用中国知网、万方、维普、Web of Science和PubMed数据库,对1992-2022年发表的有关接骨木治疗骨质疏松症的国内外文献进行检索...目的综述接骨木治疗骨质疏松症的活性成分及作用机制的研究进展,为其进一步研究和开发利用提供参考。方法利用中国知网、万方、维普、Web of Science和PubMed数据库,对1992-2022年发表的有关接骨木治疗骨质疏松症的国内外文献进行检索阅读并归纳总结。结果接骨木中多种化学成分具有抗骨质疏松作用,主要为木脂素类化合物。研究发现接骨木活性成分具有调节成骨细胞和破骨细胞的形成和分化,调控ERK MAPK信号传导通路,参与氨基酸及脂质代谢和抑制骨质疏松发生的作用。结论接骨木在治疗骨质疏松症方面潜力巨大,值得进一步研究。展开更多
基金supported by the Natural Science Foundation of Guangdong Province(2021A1515010648)the National Natural Science Foundation of China(81903616)+1 种基金The Hong Kong Polytechnic University Start-up Funding(A0038607)The Mainland-Hong Kong Joint Funding Scheme(ITFMOST:MHX/002/20).
文摘Objective:Gut-derived serotonin strongly inhibits bone formation by inhibiting osteoblast proliferation.Our previous study demonstrated that the lignan-rich fraction prepared from Sambucus willimasii Hance,a folk herbal medicine used to treat bone fractures and joint diseases in China,exerted bone-protective effects,and its actions were modulated by suppressing the synthesis of gut-derived serotonin via the inhibition of intestinal tryptophan hydroxylase 1(TPH-1).However,there is no direct evidence for the action of lignans on TPH-1.This study aimed to verify the direct action of lignans on the TPH-1 and its influence on serotonin synthesis and bone properties.Methods:Molecular docking and surface plasmon resonance were performed to determine the affinities of lignans to TPH-1.The cell viability and the protein activity and expression of TPH-1 were measured in RBL2H3 cells.The serum serotonin level and bone mineral density upon lignan treatment in ovariectomized mice were determined.Result:The lignans showed high binding scores and binding affinities to TPH-1,inhibited the activity and protein expression of TPH-1,suppressed the serum serotonin levels in ovariectomized mice as well as promoted bone mineral density.Conclusion:This is the first study to report that lignans are novel TPH-1 inhibitors and that these lignans could be potential agents for the management of serotonin-related diseases,including osteoporosis.
基金Supported by Fundamental Research Funds for Research Institutes of Heilongjiang Province(2014-02)Key Project of Longjiang Forest Industry(sgzj Y2014021)
文摘[Objectives] To explore the antioxidant activity of Sambucus williamsii seed oil. [Methods]DPPH scavenging method and Prussian blue method( total reducing power) were used. S. williamsii seed oil has antioxidant activity. In the DPPH scavenging free radical experiment,S. williamsii oil showed the ability to scavenge free radicals,and its scavenging ability had linear relationship with oil concentration( R =0. 999 6). Besides,the IC_(50) value of S. williamsii seed oil scavenging DPPH free radicals was 61. 30 ± 0. 88 mg/mL. In the total reducing power measurement experiment,the S. williamsii seed oil has a reducing ability,and its reducing ability is proportional to the oil concentration,and has the concentration dependence. Through studying the inhibitory effect of S. williamsii seed oil on α-glucosidase,the hypoglycemic activity of S. williamsii seed oil was determined. The ability of samples to inhibit α-glucosidase was judged through measuring the absorbance at 400 nm of the reaction system. [Results]In the concentration range of 1. 56-25. 00 mg/mL,the S. williamsii seed oil can effectively inhibit α-glucosidase,and the inhibition rate was 62. 66%-85. 22%. The animal in vivo experiment was used to determine the hypolipidemic activity of the S. williamsii seed oil. First,a high fat modelwas established,S. williamsii seed oil was given through intragastric administration. Then,total cholesterol( TC),triglyceride( TG),high-density lipoprotein cholesterol( HDL-C),and low density lipoprotein cholesterol( LDL-C) were measured. Through comparison of high,medium and low dose groups of S. williamsii seed oil with the high fat modelcontrol group,it was found that the TC,TG,LDL-C levels were significantly decreased( P < 0. 01) and the HDL-C levels were significantly increased( P < 0. 05),indicating that S. williamsii seed oil can effectively reduce the levels of TC,TG,LDL-C in the serum of hyperlipidemic mice,and effectively inhibit the decrease of HDL-C level,thus S. williamsii seed oil can reduce blood lipids in mice,namely,has hypolipidemic effects. In addition,the greater the dose of S. williamsii seed oil,the more obvious the effect of blood lipid levels in mice,indicating that the hypolipidemic effect of S. williamsii seed oil was dose dependent. [Conclusions] S. williamsii seed oil has reducing ability,and there is a significant dose-effect relationship in the concentration range of 2-10 mg/mL. As natural plant oil,S. williamsii seed oil has the advantages of good stability,small toxic and side effects,and strong effect,and has high value of developing new antioxidants.
文摘目的综述接骨木治疗骨质疏松症的活性成分及作用机制的研究进展,为其进一步研究和开发利用提供参考。方法利用中国知网、万方、维普、Web of Science和PubMed数据库,对1992-2022年发表的有关接骨木治疗骨质疏松症的国内外文献进行检索阅读并归纳总结。结果接骨木中多种化学成分具有抗骨质疏松作用,主要为木脂素类化合物。研究发现接骨木活性成分具有调节成骨细胞和破骨细胞的形成和分化,调控ERK MAPK信号传导通路,参与氨基酸及脂质代谢和抑制骨质疏松发生的作用。结论接骨木在治疗骨质疏松症方面潜力巨大,值得进一步研究。
