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锶-桑色素配合物的合成及其体外反应:抑制破骨细胞分化而维持成骨细胞矿化能力。

Synthesis of Sr-morin complex and its in vitro response: decrease in osteoclast differentiation while sustaining osteoblast mineralization ability.

机构信息

Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto - Universidade de São Paulo - Departamento de Química, Brazil.

出版信息

J Mater Chem B. 2019 Feb 7;7(5):823-829. doi: 10.1039/c8tb02045k. Epub 2019 Jan 11.

DOI:10.1039/c8tb02045k
PMID:32254857
Abstract

Strontium ranelate (SrR) has been used as the ultimate choice for osteoporosis treatment. However, the development of more tolerable and bioactive Sr carriers is still a need. The design of Sr-based platforms has moved towards the obtention of anion carriers that can also exhibit a positive effect on bone metabolism. In this sense, we used morin, a natural flavonoid, as a new arrangement for Sr carriage in the synthesis of an Sr complex. It has been claimed that phenolic compounds promote bone health. Therefore, we hypothesized that the association of Sr with morin could improve its anabolic effects. Complexes with the general formula [(CHO)Sr(HO)]Cl·3HO were synthesized and characterized by elemental analysis, thermogravimetry, UV-Vis and infrared absorption spectroscopies and H-nuclear magnetic resonance. We showed that the complexation between morin and Sr occurred among the 3-OH and 4C[double bond, length as m-dash]O groups of morin. Preosteoclasts cultures with the Sr-morin complex exhibited a reduced osteoclast differentiation rate and sustained osteoblast mineralization ability. The response of Sr-morin was higher than that observed for SrR at the same concentration range. Considering the above-mentioned observations, the Sr-morin complex could be an interesting approach to be further exploited not only as an alternative treatment for osteoporosis but also in the design of materials for faster osteointegration.

摘要

雷奈酸锶(SrR)一直被用作骨质疏松症治疗的首选药物。然而,开发更耐受和更具生物活性的 Sr 载体仍然是一种需求。基于 Sr 的平台的设计已经朝着获得可以对骨代谢产生积极影响的阴离子载体的方向发展。在这方面,我们使用了一种天然黄酮类化合物——桑色素,作为在 Sr 配合物合成中携带 Sr 的新方法。据称,酚类化合物有益于骨骼健康。因此,我们假设 Sr 与桑色素的结合可以提高其合成代谢作用。我们合成并通过元素分析、热重分析、紫外-可见和红外吸收光谱以及 H-核磁共振对通式为[(CHO)Sr(HO)]Cl·3HO 的配合物进行了表征。我们表明,Sr 与桑色素之间的络合发生在桑色素的 3-OH 和 4C[双键,长度为 m-dash]O 基团之间。Sr-桑色素配合物的破骨细胞前体细胞培养物显示出降低的破骨细胞分化率和持续的成骨细胞矿化能力。在相同的浓度范围内,Sr-桑色素配合物的反应高于 SrR。考虑到上述观察结果,Sr-桑色素配合物不仅可以作为骨质疏松症的替代治疗方法,而且可以作为更快骨整合设计材料的方法进行进一步探索。

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Synthesis of Sr-morin complex and its in vitro response: decrease in osteoclast differentiation while sustaining osteoblast mineralization ability.锶-桑色素配合物的合成及其体外反应:抑制破骨细胞分化而维持成骨细胞矿化能力。
J Mater Chem B. 2019 Feb 7;7(5):823-829. doi: 10.1039/c8tb02045k. Epub 2019 Jan 11.
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Horm Metab Res. 2010 Aug;42(9):627-31. doi: 10.1055/s-0030-1255091. Epub 2010 Jun 17.

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