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| 基于再生机制的淫羊藿黄酮在骨细胞微环境的药代动力学研究思路与方法 |
| Research ideas and methods for the pharmacokinetics of epimedium flavonoids with different glycosylation number, type or location in bone cell microenvironment |
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| DOI：10.3969/j.issn.1006.7108.2017.06.025 |
| 中文关键词: 骨细胞药代动力学 再生药物 糖基数量/种类/位置 淫羊藿黄酮 |
| 英文关键词:Bone cell pharmacokinetics Regenerative drugs Glycosylation Number, Type, or Location Epimedium flavonoids |
| 基金项目:江苏省妇幼健康项目（F201656);江苏省研究生培养创新工程项目（SJLX-0584);中国博士后基金（2016M590424);江苏省博士后基金（1601184C) |
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| 中文摘要: |
| 随着全球人口老龄化的加剧以及人民生活水平的提髙，越来越多的人期望并致力于让身体组织焕发新生，这致使再生药物成为了当今医学领域研究的前沿与热点。而骨骼作为人体的重要组成部分，起着支持，保护，运动等多项作用。伴随着衰老，骨密度逐渐降低，渐而演变成骨质疏松，人变得弯腰驼背且不灵活，骨骼变得易断且断后难以恢复，严重影响着人们的生活质量及生命安危。利用再生药物实现骨再生有望从根本上攻克骨质疏松这一难题。研究表明，不同糖基数量/种类/位置淫羊蕾黄嗣（Different glycosylation Number/Type/Location of epimedium flavonoids, DGEFs)具有基于再生机制的抗骨质疏松作用，但其作用强度存在显著差异。通过查阅国内外文献及研究，我们推测淫羊藿黄酮骨再生作用的强度与其药代动力学过程密切相关，糖基数量与溶解性呈正相关,与渗透性呈负相关，糖基种类/位置决定膜转运方式，透膜后的胞内处置改变了糖基结构，并转化为活性更强的黄酮。本文从药代动力学视角，深人解析糖基数量/种类/位置的不同对淫羊藿黄酮在骨细胞微环境中的药物代谢动力学过程及骨再生作用的影响。 |
| 英文摘要: |
| With the aging of the world population and the improvement of people's living standards, more and more people are looking forward to and making efforts to let the body tissue regenerate, which made regenerative medicine a frontier and hot spot in medical research. As an important part of the human body, the skeleton plays a role in supporting, protecting, movement and so on. With aging, bone density decreases gradually, and may evolve into osteoporosis. People develop kyphosis and become not flexible. Bones break easily and are hard to restore, which seriously affects individuals’ quality of life and safety. Using regenerative drugs to achieve bone regeneration is expected to overcome the problem of osteoporosis fundamentally. Studies had shown that epimedium flavonoids with different glycosylation number, type or location could exert anti-osteoporosis action, however their strength of activity were significant different. By studying Chinese and international literature and research，we hypothesize that the intensity of epimedium flavonoids’ bone regenerate mechanism is closely related to its pharmacokinetics： the number of glycosylation and membrane permeability are negatively correlated; the number of glycosylation and solubility are positively correlated; glycosylation type and position determine membrane transport mode; the intracellular disposal changes glycosylation structure, and transforms them into more active flavonoids. In this review, from the perspective of pharmacokinetics, the influences of different glycosylation number, type or location on membrane transport and osteogenic differentiation in the bone cells microenvironment were discussed in depth. |
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