scholarly journals HDAC inhibitor valproic acid upregulates CAR in vitro and in vivo

2007 ◽  
Vol 5 (1) ◽  
pp. 10 ◽  
Author(s):  
Blanca Segura-Pacheco ◽  
Berenice Avalos ◽  
Edgar Rangel ◽  
Dora Velazquez ◽  
Gustavo Cabrera
Keyword(s):  
2006 ◽  
Vol 175 (4S) ◽  
pp. 257-257
Author(s):  
Jennifer Sung ◽  
Qinghua Xia ◽  
Wasim Chowdhury ◽  
Shabana Shabbeer ◽  
Michael Carducci ◽  
...  

PLoS ONE ◽  
2013 ◽  
Vol 8 (1) ◽  
pp. e53100 ◽  
Author(s):  
Eva Juengel ◽  
Jasmina Makarević ◽  
Igor Tsaur ◽  
Georg Bartsch ◽  
Karen Nelson ◽  
...  

2019 ◽  
Vol 12 (4) ◽  
pp. 180 ◽  
Author(s):  
Changde Zhang ◽  
Shanchun Guo ◽  
Qiu Zhong ◽  
Qiang Zhang ◽  
Ahamed Hossain ◽  
...  

ZL277 is a prodrug of belinostat with enhanced bioavailability and efficacy as a pan histone deacetylase (HDAC) inhibitor. In this study, we investigated the metabolism and pharmacokinetics of ZL277 in liver S9 fractions, liver microsomes, liver cytosol, and in mice. Metabolic products were identified and quantified by a combination of liquid chromatography and tandem mass spectrometry. The in vitro metabolic profile of ZL277 includes ZL277-B(OH)2-452, the major oxidative metabolite ZL277-OH-424, the active ingredient belinostat, belinostat amide, belinostat acid, and methylated belinostat in liver S9 fractions. Both ZL277-OH-424 and belinostat underwent further glucuronidation in liver microsome, whereas only ZL277-OH-424, but not belinostat, underwent some level of sulfation in rat liver cytosols. These metabolites were examined in plasma and in a breast tumor model in vivo. They were also examined in urine and feces from mice treated with ZL277. The pharmacokinetic study of ZL277 showed the parameters of active drug belinostat with a half-life (t1/2) of 10.7 h, an area under curve value (AUC) of 1506.9 ng/mL*h, and a maximum plasma concentration (Cmax) of 172 ng/mL, reached 3 h after a single dose of 10 mg/kg. The hydrolysis product of the prodrug, ZL277-B(OH)2-452 showed an AUC of 8306 ng/mL*h and Cmax of 931 ng/mL 3 h after drug administration.


2019 ◽  
Vol 5 (2) ◽  
pp. 89-99
Author(s):  
Polina A. Golubinskaya ◽  
Marina V. Sarycheva ◽  
Svetlana Y. Burda ◽  
Maksim V. Puzanov ◽  
Natalya A. Nadezhdina ◽  
...  

Introduction: Valproic acid (VA) is carboxylic acid with a branched chain, which is used as an antiepileptic drug. Valproic acid influence on cells in vivo: VA, which is an antiepileptic drug, is also a teratogen, which causes defects of a neural tube and an axial skeleton, although the mechanisms are not yet fully clear. Valproic acid influence on mesenchymal stem cells (MSC) in vitro: It is shown that valproic acid reduces the intracellular level of oxygen active forms. Valproic acid effect on tumor cells: VA inhibits tumor growth through several mechanisms, including the cell cycle stop, differentiation induction and inhibition of growth of tumor vessels. Valproic acid influence on enzymes: It affects mainly GSK-3. Valproic acid influence on animals’ cells: It is shown that VA can significantly improve an ability to develop in vitro and improve nuclear reprogramming of embryos. Erythropoietin (EPO): Is an hypoxia-induced hormone and a cytokine, which is necessary for normal erythropoiesis. EPO is widely used in in vitro experiments. Conclusion: Thus, the influence of VA and EPO on cells can be used in cell technologies.


2014 ◽  
Vol 20 (5) ◽  
pp. 1274-1287 ◽  
Author(s):  
Chun-Han Chen ◽  
Mei-Chuan Chen ◽  
Jing-Chi Wang ◽  
An-Chi Tsai ◽  
Ching-Shih Chen ◽  
...  

2008 ◽  
Vol 144 (3) ◽  
pp. 357-362 ◽  
Author(s):  
S. Sami ◽  
N. Hoti ◽  
H.-M. Xu ◽  
Z. Shen ◽  
X. Huang

2009 ◽  
Vol 8 (4) ◽  
pp. 802-808 ◽  
Author(s):  
Madeleine S.Q. Kortenhorst ◽  
Sumit Isharwal ◽  
Paul J. van Diest ◽  
Wasim H. Chowdhury ◽  
Cameron Marlow ◽  
...  

2018 ◽  
Vol 295 ◽  
pp. S246
Author(s):  
C.P. Fisher ◽  
O. Hatley ◽  
B. van Vugt ◽  
F. Bois ◽  
S. Escher ◽  
...  

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