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摘要：姜黄素(Curcumin)是从姜科姜黄属植物中提取的有效成分, 在姜黄中的含量约为3%～6%。大量研究发现姜黄素具有广泛的药理活性, 尤其是它的抗肿瘤效果好、价格低廉、无毒副作用，逐渐成为研究的热点。但是，由于姜黄素溶解性差、生物利用度低、代谢快等缺点极大的限制了其应用。因此人们试图通过各种方法来克服姜黄素的诸多缺点，如进行结构改造和修饰、改变剂型，与其他物质形成包合物等等。31601
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磷是生命的中心元素，所有的生命活动都直接或间接有磷的参与。它不仅在生命代谢和遗传过程中起着重要的作用，而且在抗癌药物的设计中扮演着重要的角色。五配位磷化合物是60年代发展起来的一类新型有机磷化合物，以其丰富的化学内涵开拓了生物有机磷化学新的研究领域。
本文从磷化学的角度出发，设计并合成五配位双氨基酸磷烷化合物并以Atherton-Todd反应为模型，对具有抗癌活性的天然产物姜黄素进行结构上的含磷修饰，并且得到了姜黄素的含磷衍生物。这种对姜黄素的结构修饰可以在很大程度上改善此类化合物的溶解性和透膜性，是一种很好的药物改造方法。而且文献表明所得到的姜黄素含磷衍生物较母体姜黄素而言对多种不同的人肿瘤细胞具有更好的增殖抑制作用。
毕业论文关键词：姜黄素；五配位磷；Atherton-Todd反应
The design and synthesis of derivatives of curcumin containing Pentacoordinate phosphorus
Abstract：Curcumin about 3%～6% from the rhizome of the herb Curcuma longa L could be isolated. Numerous studies have shown that curcumin with low price and less toxicity possesses multifunctional pharmacological properties, especially its excellent anticancer effects. However, because of its poor solubility, bioavailability and instability under physiological conditions, its application is limited. Therefore, the studies on the curcumin by different approaches, such as, reforming its structure; changing the dosage form; mixing it with other drugs to get new mixture were invertigated previously.
Phosphorus is a central element of life, all life activities are directly or indirectly the involvement of phosphorus.It not only lives in metabolism and heredity plays an important role in the process, and plays an important role in anti-cancer drug design.pentacoordinate phosphorous compounds were developed in the 60’s and it was a new type of organic phosphorus compounds , with its rich connotation of chemistry opens up new Bioorganic phosphorus chemistry research areas.
From the chemical point of view, design and synthesis of Penta-coordinate pair of amino acid and phosphorus compound and Atherton-Todd reactions as a model, the natural product anticancer activity Curcumin is structure of phosphorus-modified,And got a phosphorus-containing derivatives of Curcumin.This structural modification of Curcumin can improve the solubility of these compounds and membrane in a large extent , so it is a good way to drug reform.literature suggests that Derivatives of Curcumin containing phosphorus have more better inhibitory for many different human tumor cells than the curcumin.
Keyword : curcumin ；pentacoordinated phosphorus ；Atherton-Todd reactions
目录
第一章 绪论
1.1姜黄素的介绍1
1.2姜黄素的抗肿瘤作用1
1.3五配位磷化合物的介绍2
1.3.1 五配位磷化合物2
1.3.2 五配位氨基酸氢膦烷2
1.3.3 五配位双氨基酸氢磷烷的结构和命名3
1.3.4 氢磷烷的化学反应活性4
1.4 Atherton-Todd反应研究发展.5
1.5 论文的主要内容和研究意义5
第二章 实验部分
2.1实验仪器与试剂6
2.2双氨基酸五配位氢磷烷的合成6
2.3姜黄素含五配位磷衍生物的合成初探索8
2.3.1苯丙氨酸五配位氢磷烷与姜黄素的反应8