猪牙皂皂苷的抗肿瘤活性及其构效关系的研究

猪牙皂皂苷的抗肿瘤活性及其构效关系的研究(论文9000字)
摘要
皂苷是一类结构复杂多样的化合物, 许多皂苷都具有良好的抗肿瘤活性。其中猪牙皂皂苷尤为引人关注。猪牙皂系豆科苏木亚科皂荚属植物皂荚(G leditsia)的干燥、不育果实，被2005版5中国药典收载为常用中药之一, 主要含有多种三萜皂苷, 具有抗炎、抗过敏、抗肿瘤、抗病毒、改善心肌缺血等药理作用, 其显著的抗炎、抗癌活性成为当前研究的热点。
目前, 肿瘤治疗所面临的主要问题为药物的多药耐药和靶向性差。而部分皂苷与经典抗癌药物的联合使用时能够协同增加后者的抗肿瘤活性,提高肿瘤细胞对药物的敏感性, 因此猪牙皂皂苷皂苷类化合物的抗肿瘤活性引起了人们的广泛关注。但降低毒副反作用、提高药物的治疗效果一直是人们需要做的努力。
本课题选用几种典型的猪牙皂皂苷，观察它们对癌细胞的杀伤作用，得出相对的抗肿瘤活性，再结合各皂苷的结构探讨它们的构效关系，总结一些构效关系的规律，从而对皂苷类药物的筛选开发和临床应用提供指导。
关键词： 猪牙皂；皂苷; 抗肿瘤; 构效关系
 
The study of anti-tumor activity and the relationship between structure and effect of fructus gleditsiae saponin
Abstract
Saponin is a category of compounds with different complex structures and many of them have anti-tumor activities, especially fructus gleditsiae saponin. Fructus gleditsiae is dry and barren fruit of G leditsia, and was recorded by the national pharmacopeia (2005 edition ) as a common Chinese medicine. It mainly contains triterpene saponin and has anti-tumor, anti-inflammatory, antiallergic, anti-virus effects and so on.
Nowadays, one of the main problems anti-tumor treatment is facing is the multidrug resistance and bad targeting of these drugs. Drug combination of some classic drugs with part of soponins can synergistically enhance the anti-tumor activities of these drugs and improve the sensitivity of cells to them. Therefore, compounds belonging to fructus gleditsiae saponin have attracted people’s attention. But reducing the toxicity and side effects of drugs and improving the treatment must be taken effort to. So, study aimed at structure-activity relationship of soponin needs to be continued in order to select ideal soponin and better the treatment.
Our project chooses some kinds of classic fructus gleditsiae saponins,then obtain their relative anti-tumor activities by observing their toxicity to some human tumor cells. Then we probe into their structure-activity relationships according to their structures and conclude some rules for leading the development of drugs belonging to saponin.
Key words: fructus gleditsiae, saponin, anti-tumor, structure-activity
 

目录
摘要……………………………………………………………………………….......................Ⅰ
ABSTRACT    Ⅱ
第一章  文献综述    1
1.1  猪牙皂皂苷的种类    1
1.2  猪牙皂皂苷抗肿瘤的主要机理    1
1.2.1  抑制血管增生    2
1.2.2  降低细胞侵害，抑制肿瘤转移    2
1.2.3  诱导解毒酶和抗氧化蛋白、抗突变    2 
        1.2.4  诱导大分子的自嗜......................................2                                      
       1.2.5  诱导分化..............................................3
1.3  猪牙皂皂苷的构效关系    3
1.4  本课题的研究目的及意义    5
1.6.1  研究目的    5
1.6.2  研究意义    5
1.6.3  研究方案    6
第二章  药物活性实验………………………………………………...11
2.1实验材料    11
2.1.1 细胞    11
2.1.2 实验器材    11
2.1.3 试剂    11
   2.2细胞复苏和培养………………………………………………………….…12
   2.3药物活性实验………………………………………………………………................12
   2.4 实验结果与讨论……………………………………………………………13
   2.5 本章小结 ….................................................................................................................15
第三章 构效关系的研究.........................................17
   3.1   细胞毒实验结果总结…………………………………………………...............17
3.2  构效关系探讨    17
3.3  本章小结    22
第四章  结论与展望    24
4.1  本研究的主要结论    24
4.2  展望    25
参考文献....................................................................................................................................26