Effect of chlorpromazine on PZ-peptidase and several other peptidase activities in cloned osteoblastic cells (MC3T3-E1).
BIOCHEMICAL PHARMACOLOGY（1987）
摘要
The effect of chlorpromazine (CPZ) on the degradation of collagen and non-collagenous peptides in clonal osteoblastic MC3T3-E1 cells was investigated by measuring the activities of PZ-peptidase, collagenase-like peptidase (CL-peptidase), dipeptidyl-aminopeptidase (DAP), leucine aminopeptidase (LAP) (EC 3.4.11.1), and post-proline cleaving enzyme (PPCE) (EC 3.4.21.26). CPZ increased PZ-peptidase and CL-peptidase activities in a dose-related fashion, but it had no effect on LAP and PPCE activities in the cells. CPZ (10 micrograms/ml) enhanced the specific activities of PZ-peptidase, CL-peptidase, and DAP for 72 hr after the start of CPZ stimulation; in particular, about a 3.3-fold increase of PZ-peptidase activity was observed at 12 hr of culture. Furthermore, other phenothiazine derivatives specifically enhanced the PZ-peptidase, CL-peptidase, and DAP activities as well as CPZ. Since PZ-peptidase, CL-peptidase, and DAP, involved in the degradation of collagen peptides, were induced significantly by CPZ (and/or other phenothiazine derivatives) in comparison with LAP and PPCE, involved in the degradation of non-collagenous peptides, these results show that CPZ specifically stimulated collagen catabolism by inducing the collagen-catabolizing enzymes. In addition, CPZ specifically inhibited collagen synthesis in clonal osteoblasts.
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关键词
pz-pro-leu,gly-pro-pro-mca,phenoxybenzamine hydrochloride,dpp iv,trifluoperazine hydrochloride,(gly-l-pro)-4-methylcoumaryl-7-amide tosylate,tfpz,ppce,4-phenylazobenzyloxycarbonyl-l-pro-l-leu,α-minimum essential medium,pnz,cl-peptidase,dap,7-amino-4-methyl coumarin,amc,leucine aminopeptidase,cpz,dl-propranolol hydrochloride,suc-gplgp-mca,(succinyl-gly-l-pro-l-leu-gly-l-pro)-4-methylcoumaryl 7-amide,l-leu-4-metnylcoumaryl-7-amide,(gly-l-pro-l-pro)-4-methylcoumaryl-7-amide,perphenazine,pba,dipeptidyl-peptidase iv,lap,post-proline cleaving enzyme,gly-pro-mca,α-mem,pz-peptide,dipeptidyl-aminopeptidase,pro,4-phenylazobenzyloxycarbonyl-l-pro-l-leu-gly-l-pro-d-arg,chlorpromazine hydrochloride,leu-mca,collagenase-like peptidase
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