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Published on: September 29, 2011
Direct evidences for the groove binding of the Clomifene to double stranded DNA
Seyed Zachariah Moradi1, Amin Nowroozi2, Komail Sadrjavadi2
1Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.
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 ΔG value implied that the interaction occurred between DNA and Clomifene spontaneously. Also, the positive ΔH and positive ΔS 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 K=5.645×107M-1 at 298K. 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.
Insights
Clomifene, a structural analogue of Tamoxifen, binds to DNA through minor groove interactions. This binding is spontaneous, primarily driven by entropy, with hydrophobic and hydrogen bonds playing key roles.
Area of Science:
- Molecular Biology
- Pharmacology
- Biophysics
Background:
- Tamoxifen, an antiestrogen, is known to induce liver tumors in rats and exhibit genotoxic effects via DNA interaction.
- Clomifene, a structural analogue of Tamoxifen, was hypothesized to possess similar DNA-binding properties.
Purpose of the Study:
- To investigate the DNA binding properties of Clomifene.
- To elucidate the mode and thermodynamics of Clomifene-DNA interaction.
Main Methods:
- Absorption and fluorescence spectroscopy
- Cellular uptake, cell viability, and cell proliferation assays
- Molecular modeling, including docking studies
Main Results:
- Clomifene interacts with DNA primarily through minor groove binding.
- The binding is spontaneous (negative ΔG), entropy-driven (positive ΔH and ΔS), with hydrophobic and hydrogen bonds being significant interaction forces.
- A high binding constant (K=5.645×10^7 M^-1 at 298K) was determined.
Conclusions:
- Clomifene exhibits significant DNA binding capabilities, suggesting potential genotoxic mechanisms.
- The binding thermodynamics indicate a complex interplay of hydrophobic and entropic factors, possibly involving DNA structural changes.
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