【摘要】 目的:探讨血小板膜糖蛋白(GP)Ⅱb/Ⅲa受体拮抗剂替罗非班在体外对血浆炎症因子的影响,为合理应用血小板GPⅡb/Ⅲa受体拮抗剂提供理论依据。方法:以二磷酸腺苷(ADP)或凝血酶为诱聚剂在体外激活血小板,同时加入20%、50%和80%抑制浓度的替罗非班,37℃共同孵育30min,标本离心,取上清液用ELISA法检测P-选择素和IL-6、IL-1β等炎症因子的改变。结果:ADP(终浓度为10μmol/L)可诱导P-选择素增多;此效应能被31.25μmol/L(IC20)以上浓度的替罗非班抑制;ADP对IL-6、IL-1β的产生无影响。凝血酶(终浓度0.03U/L)可诱导P-选择素、IL-6、IL-1β产生增多;此效应能被156.25μmol/L(IC50)以上浓度的替罗非班抑制。各浓度替罗非班单独应用对P-选择素、IL-6、IL-1β均无影响。结论:替罗非班浓度在IC50以上时可抑制凝血酶诱导的P-选择素和炎症因子增多。充足剂量的替罗非班在体外有抑制血小板活化和炎症反应的双重效应。更多还原

【Abstract】 AIM:To explore the anti-inflammatory effects of tirofiban in vitro, and to provide the theoretical basis for properly using the GP Ⅱb/Ⅲa receptor antagonists. METHODS: The platelets in the blood samples were activated in vitro with adenosine diphosphate (ADP) or thrombin respectively. Tirofiban was added to each sample in 20%, 50% or 80% inhibiting concentrations. Then the mixed liquor was incubated in 37 ℃ for 30 minutes. After centrifugation, the samples were divided to supernatants and sediments. The P-selectin, interleukin-6 (IL-6) and interleukin-1β (IL-1β) of were detected by enzyme linked immunosorbent assay (ELISA). RESULTS:ADP (final concentration: 10 μmol/L) could induce the production of P-selectin, that could be inhibited by tirofiban in concentrations higher than 31.25 μmol/L (IC20). ADP had no effect on the production of IL-6 or IL-1β. Thrombin (final concentration: 0.03 U/L) could induce the production of P-selectin, IL-6 and IL-1β, those could be inhibited by tirofiban in concentrations higher than 156.25 μmol/L (IC50). Tirofiban without ADP or thrombin had no effect on the production of P-selectin, IL-6 or IL-1β. CONCLUSION: Tirofiban in concentration higher than IC50 could inhibit the production of P-selectin and inflammatory factors induced by thrombin. Tirofiban in full dosage could inhibit the activation of platelet and decrease the production of inflammatory factors at the same time in vitro.更多还原