scholarly journals Antagonists of Vitamin K—Popular Coumarin Drugs and New Synthetic and Natural Coumarin Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1465 ◽  
Author(s):  
Kinga Kasperkiewicz ◽  
Michał B. Ponczek ◽  
Jacek Owczarek ◽  
Piotr Guga ◽  
Elżbieta Budzisz
Keyword(s):  
Vitamin K ◽  
Chemical Methods ◽  
Structures And Properties ◽  
Anticoagulant Drugs ◽  
Epoxide Reductase ◽  
Methods Of Synthesis ◽  
Long Time ◽  
Natural Coumarin ◽  
Coumarin Drugs ◽  
Natural Coumarins

Many natural coumarins and their chemically synthesized analogs and derivatives exert diverse properties, such as anticancer, antioxidant, anti-inflammatory, or anticoagulant, with the latter being of the utmost importance. The widely used warfarin, acenocoumarol, and phenprocoumon exert anticoagulant properties by inhibiting the vitamin K epoxide reductase complex. In this interdisciplinary review, we present biochemical principles of the coagulation processes and possible methods for their tuning based on the use of coumarins. We also summarize chemical methods of synthesis of coumarins and discuss structures and properties of those that have been used for a long time, as well as newly synthesized compounds. Brief information on the clinical use of coumarins and other anticoagulant drugs is given, including the severe effects of overdosing and methods for reversing their action.

Comparison of vitamin K1 and K2 kinetics of vitamin K epoxide reductase C1

2008 ◽  
Vol 28 (S 01) ◽  
pp. S106-S106
Author(s):  
P. Westhofen ◽  
M. Watzka ◽  
M. Hass ◽  
C. Müller-Reible ◽  
D. Lütjohann ◽  
...  
Keyword(s):  
Vitamin K ◽  
Vitamin K1 ◽  
Vitamin K Epoxide Reductase ◽  
Epoxide Reductase ◽  
Kinetics Of

Unusual case of soft palate and uvula haematoma in a patient on anticoagulant drugs

2020 ◽  
Vol 13 (12) ◽  
pp. e236513
Author(s):  
Stephanie Farrugia ◽  
Karl Sapiano ◽  
Robert Sciberras
Keyword(s):  
Atrial Fibrillation ◽  
Vitamin K ◽  
Soft Palate ◽  
Unusual Case ◽  
Sudden Onset ◽  
Anticoagulant Drugs ◽  
International Normalised Ratio ◽  
Oral Steroids

A 91-year-old Caucasian man on warfarin for atrial fibrillation presented in view of sudden-onset haemoptysis with fresh bleeding with clots immediately after having eaten a piping-hot traditional cheesecake (pastizz) and burning the soft-palate of his mouth. The haemoptysis had resolved by the time that the patient had arrived to hospital. On examination, a 2 cm by 2 cm dark red, solitary mass could be seen just anterior to the uvula. This was not causing any pain or discomfort to the patient. Blood results were mostly unremarkable except for a raised international normalised ratio (INR) of 3.53. The patient was administered 5 mg vitamin K orally in attempt to lower the INR level and warfarin was subsequently omitted for 7 days. He was also prescribed oral steroids on discharge. The lesion resolved in 7 days and warfarin was restarted then with no further consequences.

Vitamin K epoxide reductase significantly improves carboxylation in a cell line overexpressing factor X

Blood ◽  
2005 ◽  
Vol 106 (12) ◽  
pp. 3811-3815 ◽  
Author(s):  
Yan-Mei Sun ◽  
Da-Yun Jin ◽  
Rodney M. Camire ◽  
Darrel W. Stafford
Keyword(s):  
Binding Site ◽  
Cell Line ◽  
Vitamin K ◽  
Turnover Rate ◽  
Factor X ◽  
Vitamin K Epoxide Reductase ◽  
Transfected Cells ◽  
Epoxide Reductase ◽  
A Cell ◽  
Practical Implications

Previously we reported that we could increase the fraction of carboxylated factor X by reducing the affinity of the propeptide for its binding site on human gamma glutamyl carboxylase. We attributed this to an increased turnover rate. However, even with the reduced affinity propeptide, when sufficient overproduction of factor X is achieved, there is still a significant fraction of uncarboxylated recombinant factor X. We report here that the factor X of such a cell line was only 52% carboxylated but that the fraction of carboxylated factor X could be increased to 92% by coexpressing the recently identified gene for vitamin K epoxide reductase. Because vitamin K is in excess in both the untransfected and vitamin K epoxide reductase (VKOR)–transfected cells, the simplest explanation for this result is that VKOR catalyzes both the reduction of vitamin K epoxide to vitamin K and the conversion of vitamin K to vitamin K hydroquinone. In addition to its mechanistic relevance, this observation has practical implications for overproducing recombinant vitamin K–dependent proteins for therapeutic use.

Identification of the gene for vitamin K epoxide reductase

Nature ◽  
2004 ◽  
Vol 427 (6974) ◽  
pp. 541-544 ◽  
Author(s):  
Tao Li ◽  
Chun-Yun Chang ◽  
Da-Yun Jin ◽  
Pen-Jen Lin ◽  
Anastasia Khvorova ◽  
...  
Keyword(s):  
Vitamin K ◽  
Vitamin K Epoxide Reductase ◽  
Epoxide Reductase
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