Conjugation, Identification and Bionomics Analysis of EGFR Targeting Drug TGF α-Saporin as a Bioactive Stent Coating Material

Abstract:

Objective: To identify and testify the cytotoxicity of the EGFR targeting drug TGFa-SAP conjugated and synthesized with N-succinimidyl-3 (2-pyridyldithio) propionate on human hepatoma cell line BEL-7404 cells and proliferating vascular smooth muscle cells. Methods: Conjugation of saporin with TGFa was accomplished after derivatization of TGFa and saporin with N-succinimidyl-3 (2-pyridyldithio) proprionate and the purification of the conjugate was achieved through Eppendorf Centrifugal Filter. Cytotoxicity assays were measured by MTS assays. The value of Thymidine incorporation in BEL-7404 cells was measured by ³H-thymidine uptake. Results: Cytotoxicity assays testified that TGFa-SAP conjugate could remarkably inhibit the proliferation of human hepatoma cell line BEL-7404 cells in vitro. The value of thymidine incorporation of BEL-7404 cells in TGFa-SAP groups significantly decreased compared with the control group (P<0.05), and it had dose-dependence on TGFa-SAP’s concentration. But Saporin could not affect BEL-7404 cells even at higher level (10^-5). TGFa-SAP conjugate had effective cytotoxicity on proliferating vascular smooth muscle cells, also. Conclusion: The results indicated that the conjugated EGFR targeting drug TGFa-SAP had effective cytotoxicity not only on BEL-7404 cells, but also on proliferating vascular smooth muscle cells, as a potential bioactive stent coating material.

• Periodical: Advanced Materials Research (Volumes 1120-1121)
• Pages: 793-797
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.1120-1121.793
• Online since: July 2015
• Authors: Jun Yang, Fang Li, Ou Zeng, Jian Luo, Zhi Xiong Wu, Ting Xiao, Chun Chu*
• Keywords: Coating Material, Cytotoxicity, Saporin, Transforming Growth Factor-A, Vascular Smooth Muscle Cells

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