中国中药杂志

2021, v.46(19) 4907-4921

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血小板功能检测方法及中药抗血小板研究进展
Platelet function tests and Chinese medicines with antiplatelet function:a review

肖顺丽;丁世兰;孙正霄;廖福龙;游云;
XIAO Shun-li;DING Shi-lan;SUN Zheng-xiao;LIAO Fu-long;YOU Yun;Institute of Chinese Materia Media, China Academy of Chinese Medical Sciences;

摘要(Abstract):

血小板功能检测已越来越多地用于辅助诊断血小板疾病、血栓前状态及抗血小板治疗的疗效监测和个性化治疗。在光学比浊法测定的基础上,新的血小板功能检测方法也陆续被研究和开发。目前我国在血小板功能快检仪器研发方面仍是空白。抗血小板中药有效成分大体上可以分为萜类、黄酮类、皂苷类、有机酸类、木脂素类、二酮类、挥发油、二苯乙烯类等。中药及其化合物抗血小板作用的量效关系结果显示,大部分的中药提取物或单体成分抗血小板的起效多在微摩尔浓度级(μmol·L~(-1)),其中丹酚酸B和银杏内酯K、银杏内酯B、银杏内酯A的抗血小板效应强度最强。这提示中药抗血小板的作用强度可能低于化药及生物制品,有必要对现有中药化合物开展构效研究,通过结构改造进一步提高其药效强度。中药及其化合物抗血小板作用机制具有多途径、多靶点特点,这些研究成果为临床应用提供了参考;然而目前尚缺乏大规模多中心临床试验明确其临床应用的有效性及安全性。各类成分结构与相应功能的关系之间的规律性尚待明朗,今后仍需在相关信号转导通路和构效关系分析等方面深入研究。
Platelet function tests have been increasingly used to assist in the diagnosis of platelet disorders and prethrombotic state, monitoring of the efficacy of antiplatelet therapies, and personalized treatment. On the basis of light transmission aggregometry, new methods for platelet function test have been developed successively. At present, the research and development of platelet function detector is in its infancy in China. The active constituents of antiplatelet Chinese medicines can be classified into terpenoids, flavonoids, saponins, organic acids, lignans, diketones, volatile oils, and stilbenes. The results of dose-antiplatelet effect relationship of Chinese medicines and the active constituents showed that the effective concentration of the extracts or monomers of Chinese medicines was at micromolar level(μmol·L~(-1)), among which salvianolic acid B and ginkgolide K, ginkgolide B, and ginkgolide A had the strongest antiplatelet effect. These results suggest that the antiplatelet effect of Chinese medicine may be weaker than that of chemical drugs and biological products. Therefore, it is necessary to explore the structure-activity relationship of the active constituents in existing Chinese medicines and further improve their efficacy through structure modification. The antiplatelet effect of Chinese medicines and the constituents involves multiple pathways and multiple targets. These research results provide a reference for clinical application of them. However, there is still a lack of large-scale multi-center clinical trials to confirm the efficacy and safety of them. The regularity of the relationship between the structures of various constituents and their corresponding functions is still unknown and the relevant signal transduction pathways and structure-activity relationship need to be further studied. This paper summarized and analyzed the determination methods of platelet functions and the research results of antiplatelet Chinese medicines, which is of reference value for the research of effective and safe antiplatelet Chinese medicines.

关键词(KeyWords): 中药;血小板功能检测;抗血小板;作用机制
Chinese medicine;platelet function tests;antiplatelet;mechanisms

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基金项目(Foundation): 国家“重大新药创制”科技重大专项(2018ZX09721004-006-003)

作者(Author): 肖顺丽;丁世兰;孙正霄;廖福龙;游云;
XIAO Shun-li;DING Shi-lan;SUN Zheng-xiao;LIAO Fu-long;YOU Yun;Institute of Chinese Materia Media, China Academy of Chinese Medical Sciences;

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