Alditols and monosaccharides from sorghum vinegar can attenuate platelet aggregation by inhibiting cyclooxygenase-1 and thromboxane-A(2) synthase

作者：Li, Jing; Yu, Guoyong; Fan, Junfeng^*

来源：Journal of Ethnopharmacology, 2014, 155(1): 285-292.

DOI：10.1016/j.jep.2014.05.018

• Antiplatelet
• Arachidonic acid
• Aspirin
• Cardiovascular diseases
• Computational docking
• Thrombus

Ethnopharmacological relevance: 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.
Aim of this study: To evaluate the antiplatelet aggregation activity of alditols and monosaccharides extracted from sorghum vinegar and analysis its mechanism.
Materials and 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 TXA(2) 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 COX.
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 1035% +/- 0.46%, which was comparable to acetylsalicylic acid (aspirin, ASA) (0.50 mg/mL, 635% +/- 0.58%), a medical standard. Furthermore, AME strongly inhibited cyclooxygenase-1 (COX1) and thromboxane-A(2) 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.
Conclusion: Alditols and monosaccharides from sorghum vinegar inhibit multiple steps in the platelet aggregation pathway, and may be beneficial for the treatment of cardiovascular diseases.

• 出版日期2014-8-8
• 单位北京林业大学