中华抱茎蓼中(+)-Afzelechin和(-)-Afzelechin的分离鉴定及抗凝活性测定

Isolation,Identification and Anticoagulant Activity Identification of(+)-Afzelechin and(-)-Afzelechin in Zhonghua Baojingliao(Polygonum Amplexicaule)

目的:分离中华抱茎蓼抗凝活性部位单体,研究单体化合物抗凝血作用及对血小板聚集的影响。方法:通过正相硅胶柱、正相滴柱、高效液相色谱法等对中华抱茎蓼乙酸乙酯部位浸膏分离,首次从该药中得到—(-)-Afzelechin(1)即(-)-阿夫儿茶精,(+)-Afzelechin(2)即(+)-阿夫儿茶精、urticol(3)即2,3-顺式-2-羟基-甲基-3[双(4-羟基-3-甲氧基苯基)甲基]丁内酯。以二磷酸腺苷(ADP)诱导血小板聚集,采用比浊法测定血小板聚集率,基于凝固法原理测定凝血酶原时间(PT)、凝血酶时间(TT)、活化部分凝血活酶时间(APTT)。结果:化合物1、化合物2能显著延长兔血浆APTT、TT,能显著抑制由ADP诱导的兔血小板聚集。结论:(-)-Afzelechin(1)、(+)-Afzelechin(2)具有一定抗凝活性、抑制血小板聚集作用,抗凝活性主要影响内源性凝血系统,对外源性凝血系统影响较弱。

Objective:To isolate the anticoagulant active monomers of Zhonghua Baojingliao(Polygonum Amplexicaule),and to study the anticoagulant effect of monomer compounds and its effect on platelet aggregation.Methods:The ethyl acetate extracts of Zhonghua Baojingliao were separated by normal-phase silica gel column,normal-phase drip column,and high performance liquid chromatography.(-)-Afzelechin(1),(+)-Afzelechin(2)and urticol(3)——2,3-cis-2-hydroxy-methyl-3[bisl(4-hydroxy-3-methoxyphenyl)methl]butanolactone were first obtained from this medicine.Platelet aggregation was induced by adenosine diphosphate(ADP),and platelet aggregation rate was measured by turbidimetry. Prothrombin time(PT),thrombin time(TT),activated partial thromboplastin time(APTT) were determined based on the principle of coagulation method. Results:Compound 1 and compound2 significantly prolonged rabbit plasma APTT,TT,and significantly inhibited rabbit platelet aggregation induced by ADP. Conclusions:(-)-Afzelechin(1) and (+)-Afzelechin(2) have certain anticoagulant activity and inhibit platelet aggregation. The anticoagulant activity mainly affects the endogenous coagulation system,but has little effect on the exogenous coagulation system.