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Human serum albumin binding and synergistic effects of gefitinib in combination with regorafenib on colorectal cancer cell lines
Author(s) -
Hamid Tanzadehpanah,
Hanie Mahaki,
Mohammadreza Moradi,
Saeid Afshar,
Omid Rajabi,
Rezvan Najafi,
Razieh Amini,
Massoud Saidijam
Publication year - 2018
Publication title -
colorectal cancer
Language(s) - English
Resource type - Journals
eISSN - 1758-1958
pISSN - 1758-194X
DOI - 10.2217/crc-2017-0018
Subject(s) - regorafenib , downregulation and upregulation , gefitinib , medicine , flow cytometry , colorectal cancer , population , pharmacology , cancer research , cancer , apoptosis , immunology , chemistry , biochemistry , epidermal growth factor receptor , environmental health , gene
This study aimed to evaluate the combination effect of gefitinib (GEF) and regorafenib (REG) against HCT116, CT26 and SW948 colorectal cancer cell lines. Results showed synergistic effects on HCT116 and CT26 cells, while the additive effect was observed on SW948 cells. Combination of GEF and REG induced sub-G1 peak as the apoptotic population on HCT116 cells, through flow cytometry histogram. Downregulation of AKT1 and TGFB2 and upregulation of CASP3 were observed in the combination of GEF and REG in HCT116 cells, using quantitative real-time PCR analysis. HSA binding properties exhibit that the first drug increased binding affinity between the second drug and HSA; as a result, HSA could transport both drugs. Thus, we hope this study creates a promising strategy to treat colorectal cancer.

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