生物活性导向分离山楂炭中止血活性成分及其作用机制研究  

Bioactivity-guided isolation of hemostatic active component in hawthorn charcoal and its mechanism

作　　者：田瑞 王峥涛[1] 谢燕 TIAN Rui;WANG Zheng-tao;XIE Yan(Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;School of Public Health,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]上海中医药大学中药研究所,上海201203 [2]上海中医药大学公共健康学院,上海201203

出　　处：《中草药》2023年第3期817-824,共8页Chinese Traditional and Herbal Drugs

基　　金：上海市卫生健康学科带头人项目(2022XD026)。

摘　　要：目的研究山楂炭中发挥止血作用的活性成分及其作用机制。方法采用HPLC图谱对山楂及山楂炭中的化学成分进行比较研究;采用剪尾法、毛细管法对山楂炭体内止血及凝血效果进行考察;分离山楂炭不同极性部位,结合药效学考察,确定山楂炭药效部位;再进一步采用柱色谱分离技术结合体外凝血实验,从药效部位中分离得到发挥止血作用的化学成分,并通过体外凝血四项及血小板聚集率对其机制进行初步探究。结果山楂炮制成山楂炭的过程中化学成分发生较大变化,有新成分生成;山楂炭具有止血作用,且其醇提液药效作用比水煎液更强;从山楂炭醇提液中分离得到的醋酸乙酯部位能够显著缩短小鼠的止血及凝血时间,为山楂炭发挥止血作用的药效部位,从中分离获得药效成分松柏醛,该成分能够显著降低凝血酶时间,增加纤维蛋白原含量,提高血小板聚集率。结论首次从山楂炭中发现并分离得到具有止血作用的化学成分松柏醛,为山楂炭的临床应用提供理论依据,并为其他炭药的研究提供了参考。Objective To study the active components in hawthorn charcoal that exert the hemostatic effect and its mechanism.Methods The chemical constituents in Shanzha(Crataegi Fructus)and hawthorn charcoal were compared by HPLC chromatogram.The in vivo hemostatic and coagulation effects of hawthorn charcoal were investigated by mouse tail cutting method and capillary method.The different polar extracts of hawthorn charcoal were separated,and the effective parts of hawthorn charcoal were ensured through pharmacodynamics investigation.The chemical components with hemostatic effect in hawthorn charcoal were separated from the ethyl acetate part by column chromatography combined with in vitro coagulation experiments,and the mechanism was explored through the four items of coagulation and platelet aggregation rate in vitro.Results The chemical composition of hawthorn charcoal changed greatly during the process of hawthorn charcoal,and new components were found.Hawthorn charcoal showed hemostatic effect,and its alcohol extract had stronger hemostatic effect compared with the aqueous extract;Furthermore,the ethyl acetate part separated from the alcoholic extract of hawthorn charcoal can significantly shorten the bleeding time and coagulation time in mice,which is the effective part of hawthorn charcoal.The pharmacodynamic component coniferaldehyde was separated from the ethyl acetate part,which can significantly reduce thrombin time,increase the content of fibrinogen,and enhance the platelet aggregation rate.Conclusion The chemical component coniferaldehyde with hemostatic effect is discovered and obtained from hawthorn charcoal for the first time.The present study provided a theoretical basis for the clinical application of hawthorn charcoal,and offered a reference for the research of other charcoal medicines.

关 键 词：山楂 山楂炭 松柏醛 止血作用 生物活性导向分离 

分 类 号：R285.5[医药卫生—中药学]