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目的对灯盏乙素葡萄糖醛酸羧基进行结构修饰,合成葡萄糖醛酸羧基酯类衍生物,并测定这些衍生物的体外抗凝血活性。方法通过将灯盏乙素葡萄糖醛酸羧基先成盐后酯化的方法合成6个灯盏乙素酯类衍生物,其中灯盏乙素乙酯及苄酯为已知化合物,其余4个为新化合物,目标化合物的抗凝血活性采用家兔的贫血小板血浆(PPP)进行凝血酶原时间(PT)、凝血酶时间(TT)、活化部分凝血活酶时间(APTT)及纤维蛋白原的测定(FIB),以80%EtOH作溶剂,以生理盐水作为阳性对照。结果与结论合成了6个灯盏乙素酯类衍生物Ⅱa~Ⅱf。药理实验表明,该类衍生物的抗凝血活性没有灯盏乙素强,灯盏乙素羧酸基改造后对凝血活性影响不大。
OBJECTIVE To structurally modify the carboxyl groups of scutellar glucuronate and synthesize glucuronide carboxyl ester derivatives and determine the in vitro anticoagulant activity of these derivatives. Methods Six scutellarin derivatives were synthesized by esterification of scutellar glucuronic acid carboxyl groups. The scutellarin ethyl ester and benzyl ester were known compounds, and the other four were new compounds. Anticoagulant activity of target compounds Prothrombin time (PT), thrombin time (TT), activated partial thromboplastin time (APTT), and fibrinogen assay (FIB) were measured using platelet poor plasma (PPP) ), 80% EtOH as solvent and normal saline as positive control. RESULTS AND CONCLUSION Six scutellarin derivatives Ⅱa ~ Ⅱf were synthesized. Pharmacological experiments show that the derivatives of the anticoagulant activity is not scutellarin strong, scutellar behencarboxylate modified coagulation activity little effect.