腺苷系统与细胞钙转运：钙通道阻滞剂的干扰作用

Adenosine system and cell calcium translocation: interference of calcium channel blockers.

作者信息

Laghi Pasini F, Capecchi P L, Pasqui A L, Ceccatelli L, Mazza S, Gistri A, Di Perri T

机构信息

Istituto di Patologia Medica, University of Siena, Italy.

出版信息

Exp Gerontol. 1990;25(3-4):383-91. doi: 10.1016/0531-5565(90)90076-e.

DOI:10.1016/0531-5565(90)90076-e

PMID:2226674

Abstract

Adenosine is able to inhibit in vitro neutrophil functions induced by formyl-methionyl-leucyl-phenylalanine (FMLP) and A23187, but not phorbol 12-myristate 13-acetate (PMA). The inhibiting activity on A23187 is reversed by increasing extracellular Ca2++ concentration. The calcium entry blocker flunarizine shows an activity very similar to that of adenosine. Both adenosine and flunarizine prevent Ca++ influx into activated neutrophils as detected by the fluorescent Ca++ chelator Quin-2. Finally, flunarizine binds to the neutrophil membrane and adenosine competitively inhibits flunarizine binding as assessed by 1H-Nuclear Magnetic Resonance (1H-NMR) technique, thus indicating that the two agents share a common binding site on the cell membrane.

摘要

腺苷能够在体外抑制由甲酰甲硫氨酰亮氨酰苯丙氨酸（FMLP）和A23187诱导的中性粒细胞功能，但不能抑制佛波醇12 - 肉豆蔻酸酯13 - 乙酸酯（PMA）诱导的中性粒细胞功能。增加细胞外Ca2+浓度可逆转其对A23187的抑制活性。钙通道阻滞剂氟桂利嗪表现出与腺苷非常相似的活性。通过荧光Ca2+螯合剂喹啉-2检测发现，腺苷和氟桂利嗪均能阻止Ca2+流入活化的中性粒细胞。最后，通过1H-核磁共振（1H-NMR）技术评估，氟桂利嗪与中性粒细胞膜结合，且腺苷能竞争性抑制氟桂利嗪的结合，这表明这两种药物在细胞膜上有共同的结合位点。