Phenanthrenes isolated from diocorea batatas Decne peel with anti-platelet aggregation activity via direct factor Xa inhibitory activity

[Display omitted] •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. 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.