Anticancer Vitamin K3 Analogs: A Review

2016 ◽  
Vol 16 (8) ◽  
pp. 1017-1030 ◽  
Author(s):  
Kirti D. Badave ◽  
Ayesha A. Khan ◽  
Sandhya Y. Rane
Keyword(s):  
1968 ◽  
Vol 19 (03/04) ◽  
pp. 383-388 ◽  
Author(s):  
R Losito ◽  
C. A Owen ◽  
E. V Flock ◽  

SummaryThe metabolism of vitamin K1- 14C and menadione-14C (vitamin K3-14C) was studied in normal and hepateetomized rats. After the administration of menadione, about 70% of the 14C was excreted in the urine in 24 hrs in both types of rats. Two urinary metabolites were identified by enzymatic hydrolysis: one a glucuronide and the other a sulfate of reduced menadione. Thus, the liver is not necessary for the metabolism of menadione. In the vitamin K1 studies, the intact rats excreted only 10% of the 14C and the hepatectomized rats excreted less than 0.5%. The retention of vitamin K1 may explain its superiority over menadione as an antidote for overdosages of oral anticoagulants.


Animals ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 1140
Author(s):  
Huakai Wang ◽  
Pan Yang ◽  
Longxian Li ◽  
Nan Zhang ◽  
Yongxi Ma ◽  
...  

Six types of vitamin K3 (VK3); two sources (menadione sodium bisulfite, MSB; menadione nicotinamide bisulfite, MNB), and three different forms (crystal, micro-capsule, and micro-sphere) were used to determine the retention of VK3 in vitamin premixes (Experiment 1) or vitamin trace mineral (VTM) premixes (Experiment 2) after 1, 2, 3, and 6 months of storage. The retention of VK3 in vitamin premixes was evaluated at 25 °C/60% relative humidity or 40 °C/75% relative humidity in an incubator in Experiment 1 and in VTM premixes (choline chloride: 0 vs. 16,000 mg/kg) stored at room temperature in Experiment 2. The VK3 retention in vitamin premix or VTM premix decreased significantly with the extension of storage time (p < 0.05). In Experiment 1, the VK3 retention was higher in the 25 °C/60% incubator (56%) than in the 40 °C/75% incubator (28%). The MNB retention (52%) was higher than MSB retention (32%). The retention of VK3 in micro-capsules (43%) or micro-spheres (48%) was higher than the crystal form (35%) after six months of storage. In Experiment 2, there was no difference between the retention of MSB (49%) or MNB (47%). The retention of VK3 of micro-capsule (51%) or micro-sphere (54%) was higher than that of crystal form (40%). The VK3 retention was higher in the choline-free group (51%) than in the choline group (47%) after six months of storage. Finally, the predicted equations of VK3 retention with storage time in vitamin premixes or VTM premixes were established. The R2 of the prediction equations was ≥0.9005, indicating that time is an important factor in predicting VK3 retention. In conclusion, the higher temperature-relative humidity, choline had negative effects on VK3 retention during premix storage. MNB retention was higher than MSB during storage of vitamin premix. The encapsulated forms of VK3, micro-capsules and micro-spheres, could improve VK3 storage stability in vitamin premix and VTM premix.


2021 ◽  
Vol 330 ◽  
pp. 115707
Author(s):  
Xiangli Liu ◽  
Michael H. Abraham ◽  
William E. Acree

1990 ◽  
Vol 55 (23) ◽  
pp. 5862-5866 ◽  
Author(s):  
S. Colonna ◽  
A. Manfredi ◽  
R. Annunziata ◽  
N. Gaggero ◽  
L. Casella

1995 ◽  
Vol 33 (2324) ◽  
pp. 2475-2477 ◽  
Author(s):  
Waldemar Adam ◽  
Jianhua Lin ◽  
Chantu R. Saha-Möller ◽  
Wolfgang A. Herrmann ◽  
Richard W. Fischer ◽  
...  

2009 ◽  
Vol 297 (6) ◽  
pp. C1358-C1367 ◽  
Author(s):  
Gerald J. Atkins ◽  
Katie J. Welldon ◽  
Asiri R. Wijenayaka ◽  
Lynda F. Bonewald ◽  
David M. Findlay

The vitamin K family members phylloquinone (vitamin K1) and the menaquinones (vitamin K2) are under study for their roles in bone metabolism and as potential therapeutic agents for skeletal diseases. We have investigated the effects of two naturally occurring homologs, phytonadione (vitamin K1) and menatetrenone (vitamin K2), and those of the synthetic vitamin K, menadione (vitamin K3), on human primary osteoblasts. All homologs promoted in vitro mineralization by these cells. Vitamin K1-induced mineralization was highly sensitive to warfarin, whereas that induced by vitamins K2 and K3 was less sensitive, implying that γ-carboxylation and other mechanisms, possibly genomic actions through activation of the steroid xenobiotic receptor, are involved in the effect. The positive effect on mineralization was associated with decreased matrix synthesis, evidenced by a decrease from control in expression of type I collagen mRNA, implying a maturational effect. Incubation in the presence of vitamin K2 or K3 in a three-dimensional type I collagen gel culture system resulted in increased numbers of cells with elongated cytoplasmic processes resembling osteocytes. This effect was not warfarin sensitive. Addition of calcein to vitamin K-treated cells revealed vitamin K-dependent deposition of mineral associated with cell processes. These effects are consistent with vitamin K promoting the osteoblast-to-osteocyte transition in humans. To test whether vitamin K may also act on mature osteocytes, we tested the effects of vitamin K on MLO-Y4 cells. Vitamin K reduced receptor activator of NF-κB ligand expression relative to osteoprotegerin by MLO-Y4 cells, an effect also seen in human cultures. Together, our findings suggest that vitamin K promotes the osteoblast-to-osteocyte transition, at the same time decreasing the osteoclastogenic potential of these cells. These may be mechanisms by which vitamin K optimizes bone formation and integrity in vivo and may help explain the net positive effect of vitamin K on bone formation.


Gels ◽  
2018 ◽  
Vol 4 (4) ◽  
pp. 86 ◽  
Author(s):  
Brenda Molina ◽  
Eva Domínguez ◽  
Elaine Armelin ◽  
Carlos Alemán

In this work, we report the design and fabrication of a dual-function integrated system to monitor, in real time, the release of previously loaded 2-methyl-1,4-naphthoquinone (MeNQ), also named vitamin K3. The newly developed system consists of poly(3,4-ethylenedioxythiophene) (PEDOT) nanoparticles, which were embedded into a poly-γ-glutamic acid (γ-PGA) biohydrogel during the gelling reaction between the biopolymer chains and the cross-linker, cystamine. After this, agglomerates of PEDOT nanoparticles homogeneously dispersed inside the biohydrogel were used as polymerization nuclei for the in situ anodic synthesis of poly(hydroxymethyl-3,4-ethylenedioxythiophene) in aqueous solution. After characterization of the resulting flexible electrode composites, their ability to load and release MeNQ was proven and monitored. Specifically, loaded MeNQ molecules, which organized in shells around PEDOT nanoparticles agglomerates when the drug was simply added to the initial gelling solution, were progressively released to a physiological medium. The latter process was successfully monitored using an electrode composite through differential pulse voltammetry. The fabrication of electroactive flexible biohydrogels for real-time release monitoring opens new opportunities for theranostic therapeutic approaches.


Sign in / Sign up

Export Citation Format

Share Document