Cited 2 time in
- Title
- Antithrombotic and antiplatelet activities of new isohopane triterpene from the roots of Rubia akane
- Author(s)
- I Park; Wonhwa Lee; Hyelim Kim; K T Quan; D Y Kim; J S Bae; M Na
- Bibliographic Citation
- Natural Product Communications, vol. 14, no. 7, pp. 862914-862914
- Publication Year
- 2019
- Abstract
- A new isohopane triterpenoid (1) and two known triterpenoids (2-3) were isolated from the roots of Rubia akane (Rubiaceae). The molecular formula C30H46O4 of 1 was determined by HRESIMS. Detailed NMR spectroscopic data analysis suggested that compound 1 is a new isohopane triterpenoid with a ketone moiety at C-16. Based on the key NOE correlations of H-3/H-5 and H-21/H3-28, compound 1 was determined as 3β-hydroxy-16-oxo-21β-isohop-22(29)-en-24-oic acid. The anticoagulant activities of new isohopane 1 were evaluated by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin (Factor IIa, FIIa) and activated factor X (FXa). The effects of 1 on expression of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were evaluated in tumor necrosis factor-α activated human umbilical vein endothelial cells. Treatment with 1 (200 μM) resulted in the prolongation of aPTT and PT and the inhibition of relative thrombin (28%) and FXa (29%) activities. In addition, 1 inhibited thrombin-catalyzed fibrin polymerization (18% inhibition at 100 μM) and platelet aggregation (21.8% inhibition at 100 μM). Compound 1 also elicited anticoagulant effects in mice in a dose-dependent manner ranging from 18.8 to 94.0 μg/mouse. In addition, treatment with 1 resulted in significant reduction of the PAI-1 to t-PA ratio (25% decreased). Collectively, the new isohopane triterpenoid 1 possesses antithrombotic activities and offers a basis for the development of a new anticoagulant agent.
- Keyword
- Isohopane triterpenoidRubia akaneRubiaceaeCoagulation cascadeFibrinolysis
- ISSN
- 1934-578X
- Publisher
- Sage
- DOI
- http://dx.doi.org/10.1177/1934578X19862914
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
- Files in This Item:
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