Phenanthrenes isolated from diocorea batatas Decne peel with anti-platelet aggregation activity via direct factor Xa inhibitory activity. (October 2020)

• Record Type: Journal Article
• Authors: Jeong, So Yeon; Lee, Mijeong; Lim, Ji Sun; Park, Eui Kyun; Baek, Moon-Chang; Kim, Jong-Sang; Hahn, Dongyup; Bae, Jong-Sup
• Is Part Of: Journal of functional foods. Volume 73(2020)
• Publication Date: 2020-10
• Subjects: Dioscorea batatas Decne peel -- Phenanthrenes -- Factor Xa -- Platelet aggregation; aPTT activated partial thromboplastin time -- BSA bovine serum albumin -- DMSO dimethyl sulfoxide -- ECL enhanced chemiluminescence -- EDTA ethylenediaminetetraacetic acid -- ET-1 Endothelin-1 -- FXa Factor Xa -- GP glycoprotein -- H&E hematoxylin and eosin -- HUVEC human umbilical vein endothelial cell -- MARCKS myristoylated alanine-rich C kinase substrate -- MTT 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide -- NO Nitrogen Monoxide -- PAC-1 procaspase-activating compound-1 -- PKC protein kinase C -- PLC phospholipase C -- PPP platelet-poor plasma -- PRP platelet rich plasma -- PT prothrombin time -- SD standard deviation -- SDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresis -- TF tissue factor -- TNF-α tumor necrosis factor-α -- tPA tissue plasminogen activator -- TXA2 thromboxane A2; Functional foods -- Analysis -- Periodicals; Food -- Biotechnology -- Periodicals; Nutrition -- Periodicals; 613.2
• DOI: 10.1016/j.jff.2020.104138
• Languages: English
• ISSNs: 1756-4646

Abstract

Graphical abstract: Highlights: Small molecules 1 –2 from Dioscorea batatas Decne peel were isolated and they prolonged coagulation time. Compounds 1 –2 inhibited the activities and productions of FXa. Compounds 1 –2 inhibited the platelet aggregation. Compounds 1 –2 showed enhanced antithrombotic effects in vivo . Abstract: Phenanthrene is a class of phenolic metabolites present in Dioscorea batatas which has bioactivities such as antifungal, anti-inflammatory and antioxidative activities. Two phenanthrenes isolated from D. batatas Decne peel, exhibited inhibition against factor Xa and platelet aggregation. They were evaluated for their anti-FXa and anti-platelet aggregation properties by monitoring clotting time, platelet aggregation, FXa activity, and thrombus formation. They exhibited inhibition of the catalysis of FXa and inhibition of adenosine diphosphate- and U46619- induced platelet aggregation. They also inhibited phosphorylation of myristoylated alanine-rich C kinase substrate induced by ADP- and U46619 and the expression of P-selectin, while activating GP IIb/IIIa 1 in platelets. Improved production of nitric oxide and inhibition of endothelin-1 oversecretion were observed. In vivo studies demonstrated the enhanced antithrombotic effects and elicited anticoagulant effects of the compounds. Their anti-thrombotic efficacy were equivalent to rivaroxaban.