SPECTROSCOPIC STUDY OF INTERACTION OF SODIUM DOLUTEGRAVIR WITH HUMAN SERUM ALBUMIN
Journal Title: Вісник Одеського національного університету. Хімія - Year 2017, Vol 22, Issue 4
Abstract
Drug-protein binding has become an important research field in life sciences, chemistry and clinical medicine. Under physiological conditions, in vitro interaction between the antiviral drug 2 Sodium (4R, 12aS)-9-{[(2,4-difluorophenyl)methyl]carbamoyl}-4-methyl-6,8-dioxo3,4,6,8, 12,12a-hexahydro-2H-pyrido[1’,2’:4,5]pyrazino[2, 1-b][1,3]oxazin-7 –olate (dolutegravir sodium, DN) and human serum albumin (HSA) was investigated at excitation wavelength 280 nm and at different temperatures (298 K and 313 K) by fluorescence emission spectroscopy. The emission of HSA was characterized by a broad emission band at 346 nm. The results of the experiment showed that DN quench the intrinsic fluorescence of the protein as a result of static interaction in the HSA -DN system, which is confirmed by shifts in the difference UV spectra of the HSA -DN and the reduction of the binding constant for the HSA -DN system with increasing temperature. The constant (KA =9,82· 103 L·mol-1 at 298 K) and the number of binding sites of the HSA –DN system are established. The negative values of enthalpy change (ΔHº) and entropy change (ΔSº) can be attributed in part to van der Waals forces and in part to the formation of hydrogen bonds. A value of 2,14 nm for the average distance r between DN (acceptor) and tryptophan residues of HSA (donor) was derived from the fluorescence resonance energy transfer. The overlap of the absorbance spectrum of DN with the fluorescence emission spectrum of HAS has been shown. Since, the pharmaceutical firms need standardized screens for protein binding in the first step of new drug design, this kind of study of interaction between HSA with DN would be useful in pharmaceutical industry and clinical medicine.
Authors and Affiliations
A. V. Yegorova, G. V. Maltsev, Yu. V. Scrypynets, S. N. Kashutskуy, V. P. Antonovich
Keywords
Related Articles
- EP ID EP335998
- DOI 10.18524/2304-0947.2017.4(64).115917
- Views 85
- Downloads 0
SPECTROSCOPIC STUDY OF INTERACTION OF INDOMETHACIN AND DACLATASVIR DIGIDROCHLORIDE WITH HUMAN SERUM ALBUMIN
Fluorescence spectroscopy is one of the most effective methods for studying the binding of drugs to proteins, which is important for the purposes of biochemistry and medicine. When studying the interaction in vitro, huma...
ANIONS FUNCTIONS IN TRANSITION METALS COORDINATION COMPOUNDS
The effect of anions on the structure and properties of coordination compounds of transition metals has been discussed. The examples of changes in the composition of the formed complexes by replacement of the anion are g...
REGULARITIES OF EXTRACTION OF IONIC AND NONIONIC SURFACTANTS FROM THEIR BINARY AQUEOUS SOLUTIONS
Dodecylpyridinium chloride and nonionic surfactants – Twins (Tween-20, Tween-40, Tween-80) from their binary equimolar aqueous solutions under conditions of varying the acidity of the medium from 2 to 12 have been experi...
PREPARATION AND PROPERTIES OF POLYGLYCOLMALEINATPHTALATES MODIFIED WITH BIS(CITRATE)STANATES(IV) OF 3d-METALS AND THEIR COPOLYMERS WITH EPOXY RESIN EDR-20
As activators of polycondensation of phthalic and maleic anhydride with ethyleneglycoles, binuclear Sn(IV) - Co(II) (Ni(II), Mn(II), Cu(II))complexes with citric acid were explored. Complexes were added in reaction mixtu...
IDENTIFICATION AND DETERMINATION OF GERMANIUM CHEMICAL FORMS IN THE OBJECTS OF DIFFERENT NATURE
On the basis of literary sources data the questions of identification and determination of Germanium chemical forms in various objects are considered. It is marked that this area of analytical chemistry of Germanium (in...