title: Alditols and monosaccharides from sorghum vinegar can attenuate platelet aggregation by inhibiting cyclooxygenase-1 and thromboxane-A2 synthase.
abstract: BACKGROUND
  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.
  
  
  OBJECTIVE
  To evaluate the antiplatelet aggregation activity of alditols and monosaccharides extracted from sorghum vinegar and analysis its mechanism.
  
  
  METHODS
  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.
  
  
  RESULTS
  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.
  
  
  CONCLUSIONS
  Alditols and monosaccharides from sorghum vinegar inhibit multiple steps in the platelet aggregation pathway, and may be beneficial for the treatment of cardiovascular diseases.
authors.affiliation: 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.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.affiliation: 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.
authors.forename: Guoyong
authors.initials: G
authors.lastname: Yu
authors.affiliation: 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. Electronic address: fanjunfeng@bjfu.edu.cn.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Fan
mesh_terms: D019342:Acetic Acid / Q000737:chemistry* / Q000302:isolation & purification; D000328:Adult; D016718:Arachidonic Acid / Q000378:metabolism; D001241:Aspirin / Q000494:pharmacology; D051545:Cyclooxygenase 1 / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D062105:Molecular Docking Simulation; D009005:Monosaccharides / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D045868:Sorghum / Q000737:chemistry; D013402:Sugar Alcohols / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D013928:Thromboxane A2 / Q000378:metabolism; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors; D055815:Young Adult
chemical_list: D004791:Enzyme Inhibitors; D009005:Monosaccharides; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; D013402:Sugar Alcohols; D016718:Arachidonic Acid; D013928:Thromboxane A2; D051545:Cyclooxygenase 1; D013930:Thromboxane-A Synthase; D019342:Acetic Acid; D001241:Aspirin
keywords: Adenosine diphosphate (PubChem CID: 6022); Antiplatelet; Arachidonic acid; Arachidonic acid (PubChem CID: 444899); Aspirin; Aspirin (PubChem CID: 2244); Cardiovascular diseases; Collagen (PubChem CID: 6913668); Computational docking; Ethyl glucoside (PubChem CID: 11127487); Ribitol (PubChem CID: 827); Thrombus; Xylitol (PubChem CID: 6912); d-Fructofuranose (PubChem CID: 439163); d-Galactopyranose (PubChem CID: 6036); d-Glucopyranose (PubChem CID: 5793)