In vitro cytotoxicity and DNA/HSA interaction study of triamterene using molecular modelling and multi-spectroscopic methods

Abstract

The anticancer activity of triamterene on HCT116 and CT26 colon cancer cells lines was investigated. Furthermore, the mechanism of interaction between triamterene and calf thymus DNA (ct-DNA) and also human serum albumin (HSA) was conducted using spectroscopic and molecular docking techniques. In vitro cytotoxicity of triamterene against HCT116 and CT26 cells showed promising anticancer effects with IC50 values of 31.30 and 24.45 μM, respectively. Competitive studies of the triamterene with NR (neutral red) and MB (methylene blue) as intercalator probes showed that triamterene can be replaced by these probes. The viscosity data also confirmed that triamterene binds to calf–thymus DNA through intercalation binding mode. Binding properties of triamterene with HSA in the presence of warfarin and ibuprofen showed that triamterene competes with warfarin for the site I of human serum albumin (HSA). In addition, the binding modes of triamterene with DNA and HSA were verified by molecular docking technique.

Abbreviations
ct-DNA	=	calf thymus DNA
CV	=	cyclic voltammetry
DNA	=	deoxyribonucleic acid
DPV	=	differential pulse voltammetry
FBS	=	fetal bovine serum
HSA	=	human serum albumin
NR	=	neutral red
MB	=	methylene blue
MTT	=	3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazoliumbromide

Communicated by Ramaswamy H. Sarma

Keywords:

• triamterene
• calf thymus DNA
• human serum albumin
• neutral red
• methylene blue

Acknowledgments

The financial support from Bu-Ali Sina University Research Center is gratefully acknowledged.

Disclosure statement

No potential conflict of interest was reported by the authors.