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研究巴戟天根中的菊糖,探讨其作为抗骨质疏松症药物的潜在治疗应用。

Investigation of inulins from the roots of Morinda officinalis for potential therapeutic application as anti-osteoporosis agent.

机构信息

School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China.

Department of Pharmacology, Guangdong Medical University, Dongguan, Guangdong 523808, China.

出版信息

Int J Biol Macromol. 2018 Dec;120(Pt A):170-179. doi: 10.1016/j.ijbiomac.2018.08.082. Epub 2018 Aug 18.

DOI:10.1016/j.ijbiomac.2018.08.082
PMID:30125630
Abstract

SCOPE

In China, the root of M. officinalis has been widely used over thousands of years against a wide range of bone disease such as lumbago, limb-ache, sciatica and rheumatic arthralgia, and has tremendous medicinal value. But the bioactive constituents responsible for the osteoprotective effects in M. officinalis remain unknown.

METHODS AND RESULTS

M. officinalis polysaccharides were extracted, isolated and purified via DEAE-cellulose 52 and Sephacryl S-100HR column to obtain two saccharides (MOP70-1 and MOP70-2). The results of osteogenic activity assays revealed that MOP70-1 and MOP70-2 significantly promoted the proliferation, differentiation and mineralization of MC3T3-E1 cells. Furthermore, MOP70-2 also upregulated gene expression of runt-related transcription factor 2, osterix, osteocalcin, osteopontin, bone sialoprotein and osteoprotegerin, which implied that MOP70-2 stimulated osteoblastic differentiation by up-regulating osteogenic differentiation-related marker genes. In addition, structural analysis indicated that MOP70-2 contained (2 → 1)-linked-β-D-Fruf residues and terminated with a glucose residue. Morphological and conformational analyses indicated that MOP70-2 exhibited spherical structure of conglomeration and had no triple helix structure.

CONCLUSION

Our studies reported the osteogenic inulins obtained from root of M. officinalis for the first time. The systematical investigation including extraction, purification, biological activities and structural characterization provide a strong evidence for future therapeutic applications as anti-osteoporosis agent.

摘要

范围

在中国,数千年以来,麦冬的根部被广泛用于治疗多种骨骼疾病,如腰痛、四肢疼痛、坐骨神经痛和风湿性关节炎等,具有巨大的药用价值。但是,麦冬中负责骨保护作用的生物活性成分仍不清楚。

方法和结果

通过 DEAE-纤维素 52 和 Sephacryl S-100HR 柱对麦冬多糖进行提取、分离和纯化,得到两种多糖(MOP70-1 和 MOP70-2)。成骨活性测定结果表明,MOP70-1 和 MOP70-2 能显著促进 MC3T3-E1 细胞的增殖、分化和矿化。此外,MOP70-2 还上调了 runt 相关转录因子 2、osterix、骨钙素、骨桥蛋白、骨唾液蛋白和骨保护素的基因表达,表明 MOP70-2 通过上调成骨分化相关标记基因来刺激成骨细胞分化。此外,结构分析表明,MOP70-2 含有(2→1)-连接的-β-D-Fruf 残基,并以葡萄糖残基结尾。形态和构象分析表明,MOP70-2 表现出团聚的球形结构,没有三螺旋结构。

结论

我们的研究首次报道了从麦冬根部获得的具有成骨作用的菊糖。包括提取、纯化、生物活性和结构特征在内的系统研究为将来作为抗骨质疏松药物的治疗应用提供了有力的证据。

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