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Synthesis and Preliminary Study on the DNA-binding Property of Tranexamic Acid Derivatives

Author(s): D. X. Zhao* and K. Lu1
School of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450 001, 1School of Material and Chemical Engineering, Henan Institute of Engineering, Zhengzhou 450 007, China.

Correspondence Address:
School of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450 001, China

Tranexamic acid derivatives modified by amino acids, i.e., tranexamic acid-His, tranexamic acid-Leu-His, tranexamic acid-Glu-Phe, tranexamic acid-Glu-Lys, tranexamic acid-Ser-Tyrand, tranexamic acid-Ser-Phe, were synthesized by Fmoc solid-phase peptide synthesis, purified by reversed-phase high performance liquid chromatography and characterized by 1H and electrospray ionisation mass spectrometry. The interactions of tranexamic acid and derivatives with ctDNA were preliminarily investigated by ultraviolet-visible absorption spectroscopy. The adsorption spectra of ctDNA show a hypochromic effect, indicating that tranexamic acid and derivative scan interact with ctDNA through a mixture mode of groove-binding and electrostatic interaction. The higher affinity of tranexamic acid derivatives for ctDNA compared with free tranexamic acid indicates that the side chains of amino acid residues helped form a special surrounding and spatial structure to interact with ctDNA. The stronger interaction of tranexamic acid derivatives with ctDNA suggested that the modified tranexamic acid probably had significant practical value and should be further studied.

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