کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
7839803 | 1505859 | 2018 | 24 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Spectroscopic and molecular docking studies of the binding of the angiotensin II receptor blockers (ARBs) azilsartan, eprosartan and olmesartan to bovine serum albumin
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی تئوریک و عملی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Angiotensin receptor blockers (ARBs) represent a group of widely used therapeutic agents for the effective control of hypertension and other cardiovascular problems. Herein, the interactions of three important members of the ARBs (azilsartan, eprosartan and olmesartan) with bovine serum albumin (BSA) have been explored employing a set of simple spectroscopic approaches complemented with molecular docking studies. Steady state fluorescence emission results demonstrated the ARBs-induced quenching of the intrinsic fluorescence of BSA, which turned out to be a result of the formation of non-fluorescent complexes. The determined Stern-Volmer and binding constants were in the 104 magnitude, which were declined with the increase in temperature that primarily indicated static type of quenching. Subsequent analysis of the fluorescence data to explore the thermodynamic characteristics of these interactions showed spontaneous reactions with negative ÎH⦠values and positive ÎS⦠values, which suggest the involvement of electrostatic binding forces along with hydrogen bonding. Competitive binding studies were conducted with the aid of known BSA site markers to find the binding region of BSA for the investigated ligands. This was further supported by molecular docking simulations that ascertained the efficient binding of the three ligands to Sudlow site I (subdomain IIA) in the BSA structure.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Luminescence - Volume 203, November 2018, Pages 616-628
Journal: Journal of Luminescence - Volume 203, November 2018, Pages 616-628
نویسندگان
Amer M. Alanazi, Ali S. Abdelhameed, Ahmed H. Bakheit, Eman S.G. Hassan, Maha S. Almutairi, Hany W. Darwish, Mohamed I. Attia,