杨晶,包斌,钱士云,等.海洋纤溶活性化合物FGFC1和FGFC2影响血小板聚集特性的研究[J].中国海洋药物,2019,38(3):33-39. |
海洋纤溶活性化合物FGFC1和FGFC2影响血小板聚集特性的研究 |
Effects of marine bisindole fibrinolytic active compounds on platelet aggregation |
投稿时间:2019-01-14 修订日期:2019-02-22 |
DOI: |
中文关键词: 海洋天然产物 吲哚纤溶活性化合物 血小板聚集 环磷酸腺苷 TXA2 |
English Keywords:Marine natural product indole fibrinolytic active compound platelet aggregation cAMP TXA2 |
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中文摘要: |
目的:研究新型海洋双吲哚纤溶活性化合物FGFC1对血小板聚集的影响,发现纤溶活性化合物FGFC1与血小板相关因子变化的关系,同时比较双吲哚化合物FGFC1和单吲哚化合物FGFC2作用于血小板的异同。方法:从新鲜兔血收集血小板,调整反应体系血小板密度,以乙酰水杨酸为阳性对照,采用微量比浊法分析FGFC1和FGFC2对血小板聚集率的影响,用酶联免疫法测定FGFC1和FGFC2对血小板生理因子含量的变化。结果:FGFC1对ADP和AA诱导的血小板聚集具有抑制作用,最大抑制率分别达到42.58%±1.7%和47.82%±2.18%;FGFC2对ADP、AA和胶原诱导的血小板聚集均具有抑制作用,最大抑制率分别为50.12%±1.02%、45.28%±1.09%和50.28%±2.12%。FGFC1与FGFC2均能提升血小板内环磷酸腺苷含量,且FGFC2能明显降低血小板内血栓素A2含量。结论:海洋双吲哚纤溶活性化合物显著抑制血小板聚集,FGFC1通过影响血小板环磷酸腺苷的含量实现抑制血小板聚集,FGFC2可能通过不止一种途径抑制血小板聚集。吲哚化合物抑制血小板聚集与分子结构密切相关。 |
English Summary: |
OBJECTIVE: To investigate the effect of novel marine bisindole fibrinolytic active compound (FGFC1) on platelet aggregation. The relationship between the FGFC1 and changes in the platelet physiological factors was studied. At the same time, the similarities and differences in the action of the bisindole compound FGFC1 and the indole compound FGFC2 on platelets were compared. METHODS: Platelets were collected from fresh rabbit blood to adjust the platelet density of the reaction system. Acetylsalicylic acid was used as a positive control. The effect of FGFC1 and FGFC2 on platelet aggregation rate was analyzed by micro-turbidimetry. The changes of platelet physiological factors by FGFC1 and FGFC2 were determined by ELISA. RESULTS: FGFC1 inhibited ADP and AA-induced platelet aggregation and the maximum inhibition rates were 42.58%±1.7% and 47.82%±2.18%, respectively. FGFC2 also inhibited ADP, AA and collagen-induced platelet aggregation and the maximum inhibition rate of 50.12% ± 1.02%, 45.28% ± 1.09% and 50.28% ± 2.12%, respectively. Both FGFC1 and FGFC2 can increase the cAMP in platelets, and FGFC2 is significantly reduced the content of thromboxane A2 in platelets. CONCLUSION: The marine bisindole fibrinolytic active compound significantly inhibits platelet aggregation. FGFC1 inhibits platelet aggregation by affecting the content of platelet cAMP. FGFC2 may inhibit platelet aggregation through more than one pathway. Therefore, this study clearly depicted that the inhibition of platelet aggregation by guanidine compounds is closely related to their molecular structure. |
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