Molecular and cellular pharmacologyMitochondrial protein targets of radiosensitisation by 1,8-dihydroxy-3-acetyl-6-methyl-9,10 anthraquinone on nasopharyngeal carcinoma cells

In our preliminary study, 1,8-dihydroxy-3-acetyl-6-methyl-9,10 anthraquinone (GXHSWAQ-1), synthesised according to the basic structure of emodin, exhibited a 1.58-fold radiosensitisation on nasopharyngeal carcinoma CNE-1 cells. This study demonstrated that its radiosensitisation activity was achieved by altering the mitochondrial structure: swollen volume, fragmented crista, and decreasing transmembrane potential (P<0.01). Using isobaric tag for relative and absolute quantitation (iTRAQ) technology, 1396 proteins were identified, and the differentially expressed proteins were involved in metabolism, cell proliferation, angiogenesis, DNA repair process according to the biological process clustering results. Bioinformatic analysis showed that CDH1, RAC1, CDC42 proteins might be mostly mitochondrial targets in the radiosensitisation process. Western blotting analyses verified the differential expression of these proteins.

Bioinformatics analysis indicated protein CDC42, RAC1, CDH1 might be the promising targets in the radiosensitization process of GXHSWAQ-1. Their expressions have been verified by western blot.178