کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
11020268 | 1717599 | 2018 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Screening bioactive compounds with multi-targets from Rhodiola crenulata by a single column containing co-immobilized beta2-adrenergic receptor and voltage dependent anion channel isoform 1
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The pursuit of drugs having improved therapeutic efficacy necessitates increasing research on new assays for screening bioactive compounds with multi-targets. This work synthesized a chromatographic stationary phase containing co-immobilized beta2-adrenergic receptor (β2-AR) and voltage dependent anion channel isoform 1 (VDAC-1) to achieve such purpose. Specific ligands of the two receptors (e.g. salbutamol, methoxyphenamine, ATP and NADH) were utilized to characterize the specificity and bioactivity of the column. Validated application of the stationary phase was performed by screening multi-target compounds of Rhodiola crenulata using high performance affinity chromatography coupled with ESI-Q-TOF-MS. By zonal elution, we identified salidroside as a bioactive compound simultaneously binding to β2-AR and VDAC-1. The compound exhibited the binding sites of 1.0â¯Ãâ¯10â7 and 4.0â¯Ãâ¯10â7â¯M on the β2-AR and VDAC-1. On these sites, the association constants were calculated to be 3.3â¯Ãâ¯104 and 1.0â¯Ãâ¯104â¯Mâ1. Molecular docking indicated that the binding of salidroside to the two receptors occurred on Ser169 and Phe255of β2-AR, and the channel wall of VDAC-1. Taking together, we concluded that the column containing co-immobilized receptors has potential for screening bioactive compounds with multi-targets from complex matrices including traditional Chinese medicines.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Chromatography B - Volumes 1100â1101, 15 November 2018, Pages 76-82
Journal: Journal of Chromatography B - Volumes 1100â1101, 15 November 2018, Pages 76-82
نویسندگان
Ting Liu, Yani Hou, Jiajun Liu, Qian Li, Jing Wang, Yuan Liang, Liujiao Bian, Xinfeng Zhao,