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| 天花粉蛋白结构改造对引产活性的影响 | |
| 引用本文： | 何贤辉,孙荭,曾耀英,徐丽慧,邵鹏柱,谭兆祥.天花粉蛋白结构改造对引产活性的影响[J].暨南大学学报,2000,21(4):11-15. |
| 作者姓名： | 何贤辉 孙荭 曾耀英 徐丽慧 邵鹏柱 谭兆祥 |
| 作者单位： | 1. 暨南大学组织移植与免疫实验中心,广东,广州,510632 2. 香港中文大学生物化学系 3. 香港中文大学生理学系,香港 |
| 基金项目： | 国家自然科学基金(39570822)及香港研究基金委员会基金(CUHK374/95M)资助项目 |
| 摘 要： | 目的：研究结构改造对天花粉蛋白（ＴＣＳ）引产活性的影响。方法：利用定点突变将ＴＣＳ第２１９位的天冬酰胺残基改变为半胱氨酸残基（Ｑ２１９Ｃ）以供定点聚乙二醇（ＰＥＧ）修饰，测定修饰产物的致本失活活性及小鼠中期引产活性。结果：ＰＥＧ修饰使的致核糖体失活活性约降低９０％；相对分子质量为５０００的ＰＥＧ修饰对引产活性无明显影响，而相对分子质量为２００００的ＰＥＧ修饰却明显增强引产活性；此外，ＰＥＧ修饰使Ｔ |
| 关 键 词： | 天花粉蛋白 修饰 引产活性 结构改造 引产药物 |
| 文章编号： | 1000-9965(2000)04-0011-05 |
| 修稿时间： | 1999-11-15 |
Effect of structural modification of trichosanthin on its abortifacient activity |
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| HE Xian-hui,SUN Hong,ZENG Yao-ying,XU Li-hui,SHAW Pang-zhui,TAM Siu-cheung.Effect of structural modification of trichosanthin on its abortifacient activity[J].Journal of Jinan University(Natural Science & Medicine Edition),2000,21(4):11-15. | |
| Authors: | HE Xian-hui SUN Hong ZENG Yao-ying XU Li-hui SHAW Pang-zhui TAM Siu-cheung |
| Institution: | HE Xian-hui ,SUN Hong ,ZENG Yao-ying ,XU Li-hui ;(Institute of Tissue Transplantation and Immunology,Jinan University,Guangzhou 510632,China);SHAW Pang-zhui ;(Dept.of Biochemistry);TAM Siu-cheung ;(Dept.of Physiology,The Chinese University of Hong Kong,Hong Kong,China) |
| Abstract: | Aim: To study the effect of structural modification on the abortifacient activity of trichosanthin. Methods: Glutamine residue in 219 of trichosanthin was mutated into cysteine residue (Q219C) by site-directed mutagenesis. The mutein was then modified by polyethylene glycol (PEG). Ribosome-inactivating activity and abortifacient activity of the modified products were determined. Results: Ribosome-inactivating activity was decreased by 90% after PEG modification. There was no significant change in abortifacient activity by 5 000 PEG modification, whereas the activity was significantly enhanced when TCS was modified by 20 000 PEG. Besides, biological half-life of TCS was greatly prolonged by PEG modification. Conclusion: Site-directed PEG modification can enhance the abortifacient activity of TCS, probably due to that prolonged half-life in vivo increases the acting time of the drug. |
| Keywords: | trichosanthin site-directed mutagenesis PEG modification abortifacient activity |
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