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. 2012 Winter;11(1):325-30.

Fluoxetine competes with cortisol for binding to human serum albumin

Mostafa Rezaei-Tavirani  1 , Roya Tadayon, Seyyed Alireza Mortazavi, Arvin Medhet, Said Namaki, Shiva Kalantari, Ellaheh Noshinfar
Affiliations

Fluoxetine competes with cortisol for binding to human serum albumin

Mostafa Rezaei-Tavirani et al. Iran J Pharm Res. 2012 Winter.

Abstract

Human serum albumin (HSA) is an important protein that carries variety of substances like some hormones and drugs in blood. Pharmacological studies of the interaction of many drugs and HSA are reported during several decades, specially recently years. Interaction of cortisol and fluoxetine hydrochloride (FLX) (as a common anti-stress drug) with HSA (as their carrier in blood) has been studied separately by using different spectroscopic techniques. Here, considering the increment of anti-stress drugs consumption, conformational change of HSA in presence of cortisol and FLX in 50 mM tris buffer, at pH = 7.5 and 37°C, is investigated via pH meter, UV absorption and fluorescence spectroscopy and circular dichroism methods. pH meter findings indicate that the acid denaturation of HSA in the presence of drug and cortisol occurs in the similar manner and this pattern is different relative to the denaturation of HSA in the absence of two reagents. The results of the other techniques consistent with the pH meter findings show that FLX effects on the physiochemical properties of HSA are as that of Cortisol. In-vivo study in Rats confirms in-vitro findings which means blood cortisol level increased in the presence of FLX. Experimental results indicate that FLX and cortisol alter the structural aspects of HSA in similar manner, so, this findings lead to the following reasonable conclusion: "FLX is a competitive ligand for the binding of cortisol to HSA. Binding of FLX to HSA interferes to the interaction of cortisol-HSA."

Keywords: Cortisol; Fluoxetine; Human serum albumin; Spectroscopic methods; pH meter.

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Figures

Figure 1
Figure 1
The pH meter curves of HSA (solid line), HSA-Fluoxetine (dotted line) and HSA-cortisol (dashed line) in 50 mM Tris buffer, pH of 7.5 and at 37°C, that 50 μL of HCl 0.1 M is added to them step by step and the sample is incubated for 5 min at 37°C for each of the steps
Figure 2
Figure 2
The UV spectra of HSA (solid line), HSA-Fluoxetine (dotted line) and HSA-cortisol (dashed line) in Tris buffer 50 mM and with pH of 7.5 at 37°C
Figure 3
Figure 3
The fluorescence spectra of HSA (solid line), HSA-Fluoxetine (dotted line) and HSA-cortisol (dashed line) in Tris buffer 50 mM, pH = 7.5 at 37°C
Figure 4
Figure 4
Far-UV CD spectra of HSA (solid line), HSA-Fluoxetine (dotted line) and HSA-cortisol (dashed line) in Tris buffer 50 mM, pH = 7.5 at 37°C
Figure 5
Figure 5
Mean value of blood cortisol level in Rats. Group 1: control group include 10 Rats that are treated by tail injection of isotonic saline (100 μL). Group 2: sample group include 9 Rats; (one of them was died) and there are treated by 100 μL FLX (0.5 mg/Kg) contain isotonic saline and powders of FLX (p-value ≤ 0.01).
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