Tetramethylpyrazine inhibition on binding of radiolabeled ligand to VEGFR
- VernacularTitle:川芎嗪对VEGF受体与其放射性配体结合的抑制
- Author:
Jundong FENG
;
Xiaoyu XU
;
Yiyong HU
;
Gang CHEN
;
Weihai CHEN
;
Lirong YANG
- Publication Type:Journal Article
- Keywords:
tetramethylpyrazine(TMP);
reversed-phase high performance liquid chromatography(RP-HPLC);
radioligand binding assay(RBA);
maximum binding capacity(B_(max));
dissociation constant(K_d);
serological pharmacology
- From:
Chinese Pharmacological Bulletin
2003;0(08):-
- CountryChina
- Language:Chinese
-
Abstract:
Aim To study the effect of tetramethylpyrazine(TMP) on binding of 125I-VEGF to VEGF receptor. Methods The mice sera were collected after peritoneal injection with big-dose TMP,low-dose TMP,protamine and NS. A reversed-phase high performance liquid chromatography(RP-HPLC) method was used to determine the TMP in mice serum. The culture medium of ECV304 was treated with the mice sera in different groups. Radioligand binding assay(RBA) of receptor and Scatchard pot were performed to observe the changes of the maximum binding capacity(B_ max) and dissociation constant(K_d).Results The sera of big-dose TMP inhibited 125I-VEGF binding to its receptor, K_d=343.30?36.64 pmol?L-1,B_ max=46.26?5.85 fmol/2?10~5 cells(P0.05),but B_ max decreased(P