Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8327140 | International Journal of Biological Macromolecules | 2018 | 14 Pages |
Abstract
It has been reported that the antiestrogen Tamoxifen induces liver tumors in rats and genotoxic effects in vitro through DNA interaction. So, it can be proposed that its structural analogue, Clomifene, also can bind to DNA. To test this hypothesis, the DNA binding properties of Clomifene have been studied by absorption spectroscopy, fluorescence spectroscopy, cellular uptake, cell viability, cell proliferation and molecular modeling techniques. Evidences are provided that Clomifene could interact with DNA via minor groove interaction mode. The negative ÎG value implied that the interaction occurred between DNA and Clomifene spontaneously. Also, the positive ÎH and positive ÎS values indicated that the binding of Clomifene with DNA is mainly entropy driven and the enthalpy is unfavorable parameter. This also suggests that the hydrophobic interaction plays a major role in the binding with overall binding constant of KÂ =Â 5.645Â ÃÂ 107Â Mâ1 at 298Â K. From the results of docking, it can be concluded that Hydrogen bonds is also one of the most important interactions. The increase in entropy of system after binding might be due to the destruction of the DNA structure.
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Authors
Seyed Zachariah Moradi, Amin Nowroozi, Komail Sadrjavadi, Sajad Moradi, Kamran Mansouri, Leila Hosseinzadeh, Mohsen Shahlaei,