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基于4-噻唑烷酮的化疗药物与含聚乙二醇的聚合物纳米载体的水分散复合物的增强促凋亡作用。

Enhanced Proapoptotic Effects of Water Dispersed Complexes of 4-Thiazolidinone-Based Chemotherapeutics with a PEG-Containing Polymeric Nanocarrier.

作者信息

Kobylinska L, Ivasechko I, Skorokhyd N, Panchuk R, Riabtseva A, Mitina N, Zaichenko A, Lesyk R, Zimenkovsky B, Stoika R, Vari S G

机构信息

Department of Biochemistry, Danylo Halytsky Lviv National Medical University, Pekarska St., 69a, Lviv, 79010, Ukraine.

Department of Regulation of Cell Proliferation and Apoptosis, Institute of Cell Biology, Drahomanov St., 14/16, Lviv, 79005, Ukraine.

出版信息

Nanoscale Res Lett. 2019 Apr 23;14(1):140. doi: 10.1186/s11671-019-2945-7.

DOI:10.1186/s11671-019-2945-7
PMID:31016407
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6478785/
Abstract

AIM

To study whether water formulation of the complex of 4-thiazolidinone derivatives with a PEG-containing polymeric nanocarrier enhances their pro-apoptotic action towards rat glioma C6 cells.

METHODS

Mechanisms of antineoplastic effects of 4-thiazolidinone derivatives were investigated in vitro with rat glioma C6 cells. Cell nativity, cell cycling pattern, and Annexin V expression were evaluated and DNA damage was estimated by DNA comet analysis. A novel water-based formulation of 4-thiazolidinone derivatives complexed with a polymeric nanocarrier was utilized for enhancing pro-apoptotic action towards C6 cells.

RESULTS

The studied 4-thiazolidinone derivatives use apoptosis mechanisms for killing rat glioma C6 cells, as confirmed by FACS analysis of these cells in pre-G1 stage, the appearance of Annexin V positive C6 cells, and an increased number of DNA comets of higher classes. Complexation of the studied compounds with a PEG-containing polymeric nanocarrier significantly increased pro-apoptotic effects in rat glioma C6 cells measured by all methods mentioned above.

CONCLUSION

Complexation of 4-thiazolidinone derivatives with a PEG-containing polymeric nanocarrier provided them with water solubility and enhanced pro-apoptotic effects in rat glioma C6 cells.

摘要

目的

研究4-噻唑烷酮衍生物与含聚乙二醇的聚合物纳米载体复合物的水性制剂是否能增强其对大鼠胶质瘤C6细胞的促凋亡作用。

方法

在体外以大鼠胶质瘤C6细胞研究4-噻唑烷酮衍生物的抗肿瘤作用机制。评估细胞活性、细胞周期模式和膜联蛋白V表达，并通过DNA彗星分析估计DNA损伤。一种与聚合物纳米载体复合的新型4-噻唑烷酮衍生物水性制剂用于增强对C6细胞的促凋亡作用。

结果

通过对处于G1期前的这些细胞进行流式细胞术分析、膜联蛋白V阳性C6细胞的出现以及更高等级DNA彗星数量的增加证实，所研究的4-噻唑烷酮衍生物利用凋亡机制杀死大鼠胶质瘤C6细胞。所研究的化合物与含聚乙二醇的聚合物纳米载体复合，通过上述所有方法测量，显著增强了大鼠胶质瘤C6细胞中的促凋亡作用。

结论

4-噻唑烷酮衍生物与含聚乙二醇的聚合物纳米载体复合赋予它们水溶性，并增强了对大鼠胶质瘤C6细胞的促凋亡作用。

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