Prostate Cell Membrane Chromatography–LC/MS Method for Screening a1A-Adrenoceptor Antagonists from Lotus Plumule
Title of Paper:
Prostate Cell Membrane Chromatography–LC/MS Method for Screening a1A-Adrenoceptor Antagonists from Lotus Plumule
Summary:
The a1A-adrenoceptor (a1A-AR) plays an
important role in drug discovery and development. An
online analytical method coupling prostate cell membrane
chromatography (CMC) with high-performance liquid
chromatography/mass spectrometry (LC/MS) was established
to screen a1A-AR antagonists in traditional Chinese
medicines (TCMs). The prostate cell membrane stationary
phase (CMSP) was prepared by immobilizing the prostate
cell membrane onto the surface of the silica carrier. The
surface and chromatographic characteristics of the prostate
CMSP were studied using tamsulosin as a model molecule.
The retained fractions from the prostate CMC were analyzed
by transferring them to an LC/MS system through a
10-port switch valve. The active component, which could
act on the prostate cell membrane and receptor on it (such
as a1A-AR), was determined using a displacement experiment.
The results indicated that liensinine, isoliensine, and
neferine from Lotus Plumule exhibited similar retention
characteristics to the control drug tamsulosin when utilizing
the prostate CMC model. This new prostate CMC–LC/
MS method is applicable for screening a1A-AR antagonists
from TCMs such as Lotus Plumule and could be employed
as a drug discovery tool for natural medicinal herbs
Co-author:
J Ren, D Dai, H Du, M Sun, SC Wang*
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