| 论文简介 |
In order to develop an affinity HPLC method for screening direct thrombin inhibitors from Traditional Chinese
Medicine (TCM), thrombin was immobilized on the glutaraldehyde-modified amino silica gel and was used as
thrombin stationary phase. A thrombin affinity column (TAC) was made by packing the thrombin stationary
phase into a bare column (2.0 * 1.0 mm, i.d.). The direct thrombin inhibitors could be screened through this TAC
column. For the purpose of improvement of the discovery efficiency, a TAC-HPLC-MS/MS system was used to
screen thrombin inhibitors from Radix Salviae Miltiorrhiae (RSM), a famous traditional Chinese medicine. After
optimization of all the conditions, cryptotanshinone (Cry), dihydrotanshinone I (Dih-I) and tanshinone IIA (Tan-
IIA) were screened out and identified as potential active components. The anticoagulant effects of these three
compounds were tested by anticoagulant experiments in vitro. Furthermore, the interaction of three compounds
with thrombin was studied by molecular docking. The result shows they have the potential to be used as pre-
ventive drugs. In short, this method can be used to screen anticoagulant drugs from traditional Chinese medi-
cine, which provides convenience for screening anticoagulant drugs. |
(创新港)
