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 89
- Downloads 0
INTERACTION OF THE LANTHANA, YTTRIA WITH NEODYMIA AT TEMPERATURE 1600 °C
First, the phase equilibria in the ternary La2О3–Y2O3–Nd2О3 system at 1600 °C were studied by X–ray diffraction and petrography in the overall concentration range. The samples of different compositions have been prepared...
SPECTROPHOTOMETRIC DETERMINATION OF ASCORBIC ACID USING 18-MOLYBDODIPHOSPHATE IN INTENSELY COLORED JUICES
A simple, selective and highly sensitive method is proposed for spectrophotometric determination of ascorbic acid in juices, which have their own intense coloration with the use of a 18-molybdodiphosphate heteropoly comp...
SYNTHESIS OF 3,5-DIBROMO- AND 2,4,5-TRIBROMO-1,8-NAPHTHALIMIDES
3,5-Dibromo-1,8-naphthalic acid and 2,4,5-tribromo-1,8-naphthalic acid were synthesized by oxidation of 1,5,7-tribromoacenaphthylene and 3,5,6-tribromoacenaphthylene by sodium dichromate in anhydrous acetic acid. The ob...
EFFECTS OF KUYALNIK ESTUARY DEGRADATION (NORTHWEST BLACK SEA REGION, UKRAINE )
Based on the generalization of multiyear (2000-2013) comprehensive hydrological and hydrochemical research of Kuyalnik estuary aquatic and terrestrial ecosystems we identified causes and consequences of the degradation o...
THE STUDY OF CLINOPTILOLITE MODIFIED WITH3d METALS HALIDES BY IR AND DIFFUSE REFLECTANCE SPECTROSCOPY
The results of investigation of natural clinoptilolite (N-CLI) and that modified with 3d metal halides (MeCl2/N-CLI, where Me are Cu, Co, and Mn) by IR and diffuse reflectance spectroscopy are summarized. A band at 3437...