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钙拮抗剂维拉帕米和硝苯地平对兔多形核白细胞溶酶体酶释放的干扰。

Interference of the calcium antagonists verapamil and nifedipine with lysosomal enzyme release from rabbit polymorphonuclear leukocytes.

作者信息

Elferink J G

出版信息

Arzneimittelforschung. 1982;32(11):1417-20.

PMID:6891245
Abstract

Lysosomal enzyme release by exocytosis in rabbit polymorphonuclear leukocytes, induced by chemotactic peptide ionophore A 23187 or fluoride, is inhibited by high concentrations (0.2-1 mmol/l) of the calcium antagonists verapamil and nifedipine. Inhibition of enzyme release could be reversed by increasing the extracellular Ca2+-concentration. Verapamil and nifedipine also inhibited phagocytosis of opsonized zymosan and concomitant release of lysosomal enzymes. Inhibition of phagocytosis occurred at lower concentrations as compared with inhibition of enzyme release induced by non-particulate agents. Nifedipine is a stronger inhibitor than verapamil as regards phagocytosis and enzyme release induced by A 23187 as well as chemotactic peptide, but with respect to fluoride-induced enzyme release verapamil was stronger inhibitor. It is concluded that verapamil and nifedipine interfere with Ca2+-transport across the membrane, or with an intracellular Ca2+-requiring process that can be modulated by extracellular Ca2+.

摘要

趋化肽、离子载体A 23187或氟化物诱导兔多形核白细胞通过胞吐作用释放溶酶体酶,可被高浓度(0.2 - 1 mmol/l)的钙拮抗剂维拉帕米和硝苯地平抑制。增加细胞外Ca2+浓度可逆转酶释放的抑制作用。维拉帕米和硝苯地平还抑制调理酵母聚糖的吞噬作用以及溶酶体酶的伴随释放。与抑制非颗粒剂诱导的酶释放相比,较低浓度时即可发生吞噬作用的抑制。就A 23187以及趋化肽诱导的吞噬作用和酶释放而言,硝苯地平是比维拉帕米更强的抑制剂,但就氟化物诱导的酶释放而言,维拉帕米是更强的抑制剂。得出的结论是,维拉帕米和硝苯地平干扰Ca2+跨膜转运,或干扰可被细胞外Ca2+调节的细胞内需要Ca2+的过程。

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