五环三萜类化合物促进骨形成研究

发布时间：2018-06-29 22:20

本文选题：五环三萜类化合物 + 血清素　；参考：《中国骨质疏松杂志》2017年03期

【摘要】：目的探讨五环三萜类化合物对血清素合成的抑制活性以及促骨形成活性。方法采用高效液相色谱、ELISA试剂盒和荧光实时定量PCR测试五环三萜类化合物对RBL-2H3细胞中血清素合成的关键酶色氨酸羟化酶-1(TPH-1)的抑制率、含量及mRNA的表达。构建去势大鼠骨质疏松症模型(OVX)25只,并将骨质疏松大鼠随机分为3组不同浓度灌胃给药组[10mg/(kg·d)组、20 mg/(kg·d)组、30 mg/(kg·d)组]、一组空白对照组(OVX组)和一组假手术组(Sham组),给药35 d后采用高效液相色谱测试血清和小肠中血清素水平。采用MTT法测试五环三萜类化合物对成骨细胞促进活性。结果在RBL-2H3细胞中,五环三萜类化合物对于TPH-1的抑制呈剂量依赖性,抑制率为3.6%~76.5%,其中18β-甘草次酸(GA)在30μM浓度下展现出了最高抑制率(76.5%),并能较空白组(219 ng/m L)显著地降低TPH-1含量(34 ng/m L)及mRNA的表达。与Sham组相比,大鼠摘除卵巢(OVX组)后血清和小肠中血清素的水平明显增高,而经过GA给药后的大鼠血清和小肠中血清素的水平却明显降低,在30μM浓度下血清(426 ng/m L)和小肠(304 ng/m L)中血清素的浓度较OVX组(含量分别为1050ng/m L和723 ng/m L)降低了至少2倍;此外,GA能够促进乳小鼠成骨细胞增殖。结论 18β-甘草次酸能够作为促进骨形成的先导化合物,值得深入研究。
[Abstract]:Objective to investigate the inhibitory and osteogenic activity of pentacyclic triterpenoids on serotonin synthesis. Methods the inhibition rate, content and mRNA expression of pentacyclic triterpenoids on tryptophan hydroxylase 1 (TPH-1), a key enzyme of serotonin synthesis in RBL-2H3 cells, were measured by HPLC Elisa kit and real-time quantitative PCR. OVX model was established in 25 ovariectomized rats. The osteoporosis rats were randomly divided into three groups: the 10mg/ (kg d) group, the control group (OVX group) and the sham-operated group (sham group). After 35 days of administration, the serum and serum were measured by high performance liquid chromatography (HPLC), and the control group (OVX group) and the sham-operated group (Sham group) were divided into three groups: 10mg/ (kg d) group, 20 mg/ (kg d) group and 30 mg/ (kg d) group, respectively. Serotonin levels in the small intestine. MTT assay was used to test the activity of pentacyclic triterpenoids on osteoblasts. Results in RBL-2H3 cells, pentacyclic triterpenoids inhibited TPH-1 in a dose-dependent manner. The inhibitory rate was 3.6% and 76.5%, in which 18 尾 -glycyrrhetinic acid (GA) showed the highest inhibitory rate (76.5%) at 30 渭 M concentration, and could significantly lower the TPH-1 content (34 ng/m L) and the expression of TPH-1 (34 ng/m L) compared with the control group (219 ng/m L). Compared with the sham group, the serum and small intestine serotonin levels in the ovariectomized rats (OVX group) were significantly increased, but the serum and small intestine serotonin levels in the rats treated with GA were significantly lower than those in the sham group. The concentration of serotonin in serum (426 ng/m L) and small intestine (304 ng/m L) at 30 渭 M was at least 2 times lower than that in OVX group (1050ng/m L and 723 ng/m L, respectively). Conclusion 18 尾-glycyrrhetinic acid can be used as a leading compound to promote bone formation.
【作者单位】：仙桃市第一人民医院骨外二科;
【分类号】：R580

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