Li Jing, Yu Guoyong, Fan Junfeng
Department of Food Science and Engineering, College of Bioscience and Biotechnology, Beijing Forestry University, P.O.112, 35 Qinghua East Road, Haidian District, Beijing 100083, China.
Department of Food Science and Engineering, College of Bioscience and Biotechnology, Beijing Forestry University, P.O.112, 35 Qinghua East Road, Haidian District, Beijing 100083, China.
J Ethnopharmacol. 2014 Aug 8;155(1):285-92. doi: 10.1016/j.jep.2014.05.018. Epub 2014 May 28.
Vinegar has been used as both a common seasoning and a traditional Chinese medicine. Sorghum vinegar is an excellent source of physiological substances with multiple health benefits.
To evaluate the antiplatelet aggregation activity of alditols and monosaccharides extracted from sorghum vinegar and analysis its mechanism.
Alditol and monosaccharide extract (AME) from sorghum vinegar was first evaluated for antiplatelet activity using the turbidimetric method. Blood was collected from healthy volunteer donors. The platelet aggregation was induced by arachidonic acid (AA), collagen, adenosine diphosphate (ADP) and thrombin in vitro. AME was divided into three experimental groups with the concentration were 0.10, 0.25 and 0.50 mg/mL. In order to determine the inhibitory activity of AME on COX1, TXS and TXA2 production experiments were conducted using the COX1, TXS and TXB2 EIA kit. Computational docking was used to find the docking pose of monosaccharides and alditols with COX1.
AME showed significant induction of antiplatelet activity by arachidonic acid (AA), collagen, adenosine diphosphate (ADP) and thrombin in a concentration-dependent manner (p<0.05). AME (0.50 mg/mL) reduced the AA-induced aggregation rate to 10.35%±0.46%, which was comparable to acetylsalicylic acid (aspirin, ASA) (0.50 mg/mL, 6.35%±0.58%), a medical standard. Furthermore, AME strongly inhibited cyclooxygenase-1 (COX1) and thromboxane-A2 synthase (TXS), and subsequently attenuated thromboxane-A2 (TXA2) production. These findings indicated that AME attenuates platelet aggregation through the AA metabolism pathway. Computational docking showed that alditols (L-erythritol, L-arabitol, xylitol and D-sorbitol), monosaccharides (D-glucopyranose, D-fructofuranonse, D-xylopyranose, D-galactopyranose and D-ribose), ethyl glucoside and 3,4-(methylenedioxy) mandelic acid could dock directly into the active site of COX1.
Alditols and monosaccharides from sorghum vinegar inhibit multiple steps in the platelet aggregation pathway, and may be beneficial for the treatment of cardiovascular diseases.
醋一直被用作常见的调味品和传统中药。高粱醋是多种具有生理活性物质的优质来源，对健康有益。
评估从高粱醋中提取的糖醇和单糖的抗血小板聚集活性并分析其作用机制。
首先采用比浊法评估高粱醋中的糖醇和单糖提取物（AME）的抗血小板活性。从健康志愿者捐献者采集血液。在体外通过花生四烯酸（AA）、胶原蛋白、二磷酸腺苷（ADP）和凝血酶诱导血小板聚集。AME分为三个实验组，浓度分别为0.10、0.25和0.50mg/mL。为了确定AME对COX1、TXS和TXA2生成的抑制活性，使用COX1、TXS和TXB2酶联免疫吸附测定试剂盒进行实验。采用计算对接方法寻找单糖和糖醇与COX1的对接构象。
AME对花生四烯酸（AA）、胶原蛋白、二磷酸腺苷（ADP）和凝血酶诱导的血小板聚集具有显著的抑制作用，且呈浓度依赖性（p<0.05）。AME（0.50mg/mL）将AA诱导的聚集率降低至10.35%±0.46%，与医学标准药物乙酰水杨酸（阿司匹林，ASA）（0.50mg/mL，6.35%±0.58%）相当。此外，AME强烈抑制环氧合酶-1（COX1）和血栓素-A2合酶（TXS），进而减少血栓素-A2（TXA2）的生成。这些结果表明，AME通过AA代谢途径减弱血小板聚集。计算对接显示，糖醇（L-赤藓醇、L-阿拉伯糖醇、木糖醇和D-山梨醇）、单糖（D-吡喃葡萄糖、D-呋喃果糖、D-吡喃木糖、D-吡喃半乳糖和D-核糖）、葡萄糖苷乙酯和3,4-（亚甲二氧基）扁桃酸可直接对接至COX1的活性位点。
高粱醋中的糖醇和单糖可抑制血小板聚集途径中的多个步骤，可能对心血管疾病的治疗有益。
