Abstract | ETHNOPHARMACOLOGICAL RELEVANCE: AIM OF THIS STUDY: 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 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. CONCLUSION:
|
Authors | Jing Li, Guoyong Yu, Junfeng Fan |
Journal | Journal of ethnopharmacology
(J Ethnopharmacol)
Vol. 155
Issue 1
Pg. 285-92
(Aug 08 2014)
ISSN: 1872-7573 [Electronic] Ireland |
PMID | 24877847
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
|
Copyright | Copyright © 2014 Elsevier Ireland Ltd. All rights reserved. |
Chemical References |
- Enzyme Inhibitors
- Monosaccharides
- Plant Extracts
- Platelet Aggregation Inhibitors
- Sugar Alcohols
- Arachidonic Acid
- Thromboxane A2
- Cyclooxygenase 1
- Thromboxane-A Synthase
- Acetic Acid
- Aspirin
|
Topics |
- Acetic Acid
(chemistry, isolation & purification)
- Adult
- Arachidonic Acid
(metabolism)
- Aspirin
(pharmacology)
- Cyclooxygenase 1
(drug effects, metabolism)
- Dose-Response Relationship, Drug
- Enzyme Inhibitors
(administration & dosage, isolation & purification, pharmacology)
- Humans
- In Vitro Techniques
- Molecular Docking Simulation
- Monosaccharides
(administration & dosage, isolation & purification, pharmacology)
- Plant Extracts
(administration & dosage, pharmacology)
- Platelet Aggregation Inhibitors
(administration & dosage, isolation & purification, pharmacology)
- Sorghum
(chemistry)
- Sugar Alcohols
(administration & dosage, isolation & purification, pharmacology)
- Thromboxane A2
(metabolism)
- Thromboxane-A Synthase
(antagonists & inhibitors)
- Young Adult
|