Screening Bioactive Compounds of Siraitia grosvenorii by Immobilized β2-Adrenergic Receptor Chromatography and Druggability Evaluation
As the first and key step of traditional Chinese medicine (TCM)-guided drug development, lead discovery necessitates continuous exploration of new methodology for screening bioactive compounds from TCM. This work intends to establish a strategy for rapidly recognizing β2-adrenergic receptor (β2-AR)...
Saved in:
| Main Authors: | , , , , , , , , , , |
|---|---|
| Format: | Book |
| Published: |
Frontiers Media S.A.,
2019-08-01T00:00:00Z.
|
| Subjects: | |
| Online Access: | Connect to this object online. |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
MARC
| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_8f13bbd68e634e5f8c1c5e369ff7d224 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Xiaoni Jia |e author |
| 700 | 1 | 0 | |a Xiaoni Jia |e author |
| 700 | 1 | 0 | |a Jiajun Liu |e author |
| 700 | 1 | 0 | |a Baimei Shi |e author |
| 700 | 1 | 0 | |a Qi Liang |e author |
| 700 | 1 | 0 | |a Qi Liang |e author |
| 700 | 1 | 0 | |a Juan Gao |e author |
| 700 | 1 | 0 | |a Gangjun Feng |e author |
| 700 | 1 | 0 | |a Zhongman Chang |e author |
| 700 | 1 | 0 | |a Qian Li |e author |
| 700 | 1 | 0 | |a Xiaohong Zhang |e author |
| 700 | 1 | 0 | |a Jianbo Chen |e author |
| 700 | 1 | 0 | |a Xinfeng Zhao |e author |
| 245 | 0 | 0 | |a Screening Bioactive Compounds of Siraitia grosvenorii by Immobilized β2-Adrenergic Receptor Chromatography and Druggability Evaluation |
| 260 | |b Frontiers Media S.A., |c 2019-08-01T00:00:00Z. | ||
| 500 | |a 1663-9812 | ||
| 500 | |a 10.3389/fphar.2019.00915 | ||
| 520 | |a As the first and key step of traditional Chinese medicine (TCM)-guided drug development, lead discovery necessitates continuous exploration of new methodology for screening bioactive compounds from TCM. This work intends to establish a strategy for rapidly recognizing β2-adrenergic receptor (β2-AR) target compounds from the fruit of Siraitia grosvenorii (LHG). The method involved immobilization of β2-AR onto amino-microsphere to synthesize the receptor column, the combination of the column to high-performance liquid chromatography (HPLC) to screen bioactive compounds of LHG, the identification of the compounds by HPLC coupled with mass spectrometry (MS), and the evaluation of druggability through pharmacokinetic examination by HPLC-MS/MS. Mogroside V was screened and identified as the β2-AR-targeted bioactive compounds in LHG. This compound exhibited desired pharmacokinetic behavior including the time to reach peak plasma concentrations of 45 min, the relatively low elimination of 138.5 min, and the high bioavailability. These parameters indicated that mogroside V has a good druggability for the development of new drugs fighting β2-AR-mediated respiratory ailments like asthma. The combination of the methods in this work is probably becoming a powerful strategy for screening and early evaluating the bioactive compounds specifically binding to G-protein-coupled receptor target from complex matrices including TCM. | ||
| 546 | |a EN | ||
| 690 | |a high-throughput screening | ||
| 690 | |a pharmacokinetics | ||
| 690 | |a receptor chromatography | ||
| 690 | |a β2-adrenergic receptor | ||
| 690 | |a Siraitia grosvenorii | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Frontiers in Pharmacology, Vol 10 (2019) | |
| 787 | 0 | |n https://www.frontiersin.org/article/10.3389/fphar.2019.00915/full | |
| 787 | 0 | |n https://doaj.org/toc/1663-9812 | |
| 856 | 4 | 1 | |u https://doaj.org/article/8f13bbd68e634e5f8c1c5e369ff7d224 |z Connect to this object online. |