摘要
目的 :探讨放、化疗细胞保护剂WR - 2 72 1对生理性激活剂ADP、胶原和血小板激活因子(PAF)引起的血小板激活的影响。方法 :取 2 0～ 35岁健康人血液 ,分别给予生理性激活剂ADP 1μmol·L- 1、胶原 2mg·L- 1和PAF 0 .1mg·L- 1后 ,再用终浓度为 10 - 7～ 10 - 5mol·L- 1的WR 2 72 1处理 ,观察对血小板聚集的影响 ,然后观察血栓素B2 (TXB2 )和NO的水平。结果 :WR 2 72 1抑制ADP、胶原和PAF诱导的血小板聚集和TXB2 产生 ,并存在剂量依赖关系。在终浓度为 5 μmol·L- 1时 ,WR 2 72 1明显增加用ADP、胶原和PAF诱导的NO的产生 ,表明活化血小板释放的NO参与WR 2 72 1的抑制效应。结论 :WR 2 72 1体外可有效地抑制生理性激活剂引起的血小板活化。除了细胞保护作用外 ,WR 2 72
AIM: To explore in vitro the effects of WR 2721, a cytoprotector of chemotherapy and radiation, on platelet activation induced by physiologic agonists ADP, collagen and PAF. METHODS: Blood, obtained from Chinese healthy volunteers aged 20-35 years, was treated with physiologic agonists at the given concentrations: ADP 1 μmol·L -1 , collagen 2 mg·L -1 , and PAF 0.1 mg·L -1 . Then WR 2721 was added to the experimental system at final concentrations range of 10 -7 -10 -5 mol·L -1 . The effect of WR 2721 on platelet aggregation induced by the agonists was studied. Thromboxane B 2 (TXB 2) levels and nitric oxide (NO) production were determined. RESULTS: WR 2721 inhibited both platelet aggregation and TXB 2 production induced by ADP, collagen and PAF, in a dose dependent manner. When WR 2721 was added at the final concentration of 5 μmol·L -1 , it significantly increased ADP, collagen and PAF induced NO production, which suggested that NO release by activated platelets was involved in the inhibitory effect of WR 2721. CONCLUSION: WR 2721 can effectively inhibit platelet activation induced in vitro by physiologic agonists. It may be not only a cytoprotectant, but also a therapeutic agent.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2002年第6期518-521,共4页
Chinese Journal of Clinical Pharmacology and Therapeutics
