Structural Modification of Tyroservatide and the  Prelimary Evaluation of Their Stability and Safety

CHEN Peng; WU Long; GUO Cuiping; CAI Shaohui; CHEN Heru

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Structural Modification of Tyroservatide and the Prelimary Evaluation of Their Stability and Safety

更新时间：2023-12-11

- Structural Modification of Tyroservatide and the Prelimary Evaluation of Their Stability and Safety
- Acta Scientiarum Naturalium Universitatis SunYatseni Vol. 52, Issue 2, Pages: 101-105(2013)
- 作者机构：
  
  1. 暨南大学药学院中药及天然药物研究所,广东,广州,510632
  2. 暨南大学药学院药理教研室,广东,广州,510632
  3. 广东省中药药效物质基础及创新药物研究重点实验室,广东,广州,510632
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Published：2013，
  
  Published Online：25 March 2013，
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CHEN Peng, WU Long, GUO Cuiping, et al. Structural Modification of Tyroservatide and the Prelimary Evaluation of Their Stability and Safety. [J]. Acta Scientiarum Naturalium Universitatis SunYatseni 52(2):101-105(2013)
DOI：

CHEN Peng, WU Long, GUO Cuiping, et al. Structural Modification of Tyroservatide and the Prelimary Evaluation of Their Stability and Safety. [J]. Acta Scientiarum Naturalium Universitatis SunYatseni 52(2):101-105(2013) DOI：

摘要

通过固相多肽法成功合成了酪丝缬肽（YSV）以及其结构修饰物（Z-GP-YSV-NH

），总收率分别为45.3%和52.3%.分别研究了YSV和Z-GP-YSV-NH

在PBS缓冲液、DMEM培养基和大鼠血浆中的稳定性，发现两者在PBS和DMEM中都很稳定，但YSV在大鼠血浆中温浴2 h后基本降解完全；而Z-GP-YSV-NH

温浴12 h后只降解67%。还评价了YSV和Z-GP-YSV-NH

对人胚肾细胞293的细胞毒性，发现两者的细胞毒性都很低。当剂量为200 μg/mL时，其增殖抑制率分别为20%和10.3%。

Abstract

Tyroservatide (YSV) and its structural modification (Z-GP-YSV-NH

) were successfully synthesized by solidphase peptide synthesis. The overall yields were 45.3% and 52.3% respectively. The stabilities of YSY and Z-GP-YSV-NH

in PBS buffer

DMEM culture and rat blood plasma were also investigated in this study. It was found that both YSV and Z-GP-YSV-NH

were stable in either PBS or DMEM medium. However

YSV was completely degraded after bathing in rat blood plasma for 2 h; while only 67% of Z-GP-YSV-NH

was degraded after 12-hours bath. In current paper

the cytotoxicities of YSV and Z-GP-YSV-NH

to human renal cell 293 were also evaluated. It was displayed that the cytotoxicities of both compounds were very low

in which the growth inhibition rate were 20% and 10.3% respectively when the dosages were 200 μg/mL.

关键词

酪丝缬肽结构修饰抗肿瘤肽

Keywords

tyroservatidestructural modificationantitumor peptides

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