Kui Hongqian, Lei Yan, Jia Chunxue, Xin Quancheng, Tursun Rustam, Zhong Miao, Liu Chuanxin, Yuan Ruijuan
School of Chinese Materia Medica, Beijing University of Chinese Medicine, China.
Department of Metabolism and Endocrinology, Endocrine, and Metabolic Disease Center, The First Affiliated Hospital, and College of Clinical Medicine of Henan, University of Science and Technology, Medical Key Laboratory of Hereditary Rare Diseases of Henan, Luoyang Sub-center of National Clinical Research Center for Metabolic Diseases, Luoyang, China.
Heliyon. 2024 Mar 19;10(7):e27828. doi: 10.1016/j.heliyon.2024.e27828. eCollection 2024 Apr 15.
As a traditional Chinese medicine, leech has obvious pharmacological activities in anticoagulantion and antithrombosis. Whitman (WP) is the most commonly used leech in the Chinese market. It is often used in clinical applications after high-temperature processing by talcum powder to remove the fishy taste and facilitate crushing. The anticoagulant and thrombolytic active ingredients are protein and polypeptide, which may denaturate and lose activity after high-temperature processing. The rationality of its processing has been questioned in recent years. This study aims to investigate the effect of talcum powder scalding on the antithrombotic activity of WP and to discuss its pharmacodynamic mechanism .
Raw and talcum-powdered processed WP were administered intragastrically for 14 days, and carrageenan was injected intraperitoneally to prepare a mouse model of tail vein thrombosis. The incidence rate of tail vein thrombosis and the thrombus area under pathological tissue sections were calculated to evaluate the antithrombotic effect between raw and processed WP. Non-targeted metabolomics was conducted using UPLC-Q-TOF/MS technology to analyze the changes of small molecule metabolites in the body after administration of WP.
After intragastric administration, both the raw product and the processed product of WP could inhibit the thrombosis induced by carrageenan, and the processed product had a more apparent antithrombotic effect than the raw product. The administration of WP could regulate the changes of some small molecular metabolites, such as amino acids, lipids, and steroids, in Sphingolipid metabolism and Glycerophospholipid metabolism.
Based on the results of pharmacodynamics and metabolomics, processed WP will not reduce the antithrombotic activity of WP. This study provided a scientific basis for the rational use of leeches.
水蛭作为一味传统中药，在抗凝和抗血栓形成方面具有明显的药理活性。宽体金线蛭（WP）是中国市场上最常用的水蛭品种。它通常经过滑石粉高温处理以去除腥味并便于粉碎后用于临床应用。其抗凝和溶栓活性成分是蛋白质和多肽，高温处理后可能会变性并失去活性。近年来，其炮制的合理性受到质疑。本研究旨在探讨滑石粉烫炙对宽体金线蛭抗血栓活性的影响，并探讨其药效学机制。
将生品和滑石粉烫炙品宽体金线蛭灌胃给药14天，腹腔注射角叉菜胶制备小鼠尾静脉血栓模型。计算尾静脉血栓发生率及病理组织切片下的血栓面积，以评价生品和烫炙品宽体金线蛭之间的抗血栓作用。采用超高效液相色谱-四极杆飞行时间质谱（UPLC-Q-TOF/MS）技术进行非靶向代谢组学分析，以分析宽体金线蛭给药后体内小分子代谢物的变化。
灌胃给药后，宽体金线蛭生品和烫炙品均能抑制角叉菜胶诱导的血栓形成，且烫炙品的抗血栓作用比生品更明显。宽体金线蛭给药可调节鞘脂代谢和甘油磷脂代谢中一些小分子代谢物如氨基酸、脂质和类固醇的变化。
基于药效学和代谢组学结果，烫炙后的宽体金线蛭不会降低其抗血栓活性。本研究为水蛭的合理应用提供了科学依据。
