Mammalian folylpoly-.gamma.-glutamate synthetase. 4. In vitro and in vivo metabolism of folates and analogues and regulation of folate homeostasis

Biochemistry ◽  
1987 ◽  
Vol 26 (2) ◽  
pp. 530-539 ◽  
Author(s):  
Janine D. Cook ◽  
David J. Cichowicz ◽  
Sabu George ◽  
Ann Lawler ◽  
Barry Shane
Keyword(s):  
In Vivo Metabolism ◽  
Glutamate Synthetase ◽  
Folate Homeostasis

scholarly journals Boosting GSH Using the Co-Drug Approach: I-152, a Conjugate of N-acetyl-cysteine and β-mercaptoethylamine

Nutrients ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 1291 ◽  
Author(s):  
Rita Crinelli ◽  
Carolina Zara ◽  
Michaël Smietana ◽  
Michele Retini ◽  
Mauro Magnani ◽  
...  
Keyword(s):  
Cell Cultures ◽  
In Vivo Studies ◽  
In Vivo Metabolism ◽  
Pharmacokinetic Properties ◽  
Immunomodulatory Properties ◽  
Acetyl Cysteine ◽  
High Doses ◽  
The Brain

Glutathione (GSH) has poor pharmacokinetic properties; thus, several derivatives and biosynthetic precursors have been proposed as GSH-boosting drugs. I-152 is a conjugate of N-acetyl-cysteine (NAC) and S-acetyl-β-mercaptoethylamine (SMEA) designed to release the parent drugs (i.e., NAC and β-mercaptoethylamine or cysteamine, MEA). NAC is a precursor of L-cysteine, while MEA is an aminothiol able to increase GSH content; thus, I-152 represents the very first attempt to combine two pro-GSH molecules. In this review, the in-vitro and in-vivo metabolism, pro-GSH activity and antiviral and immunomodulatory properties of I-152 are discussed. Under physiological GSH conditions, low I-152 doses increase cellular GSH content; by contrast, high doses cause GSH depletion but yield a high content of NAC, MEA and I-152, which can be used to resynthesize GSH. Preliminary in-vivo studies suggest that the molecule reaches mouse organs, including the brain, where its metabolites, NAC and MEA, are detected. In cell cultures, I-152 replenishes experimentally depleted GSH levels. Moreover, administration of I-152 to C57BL/6 mice infected with the retroviral complex LP-BM5 is effective in contrasting virus-induced GSH depletion, exerting at the same time antiviral and immunomodulatory functions. I-152 acts as a pro-GSH agent; however, GSH derivatives and NAC cannot completely replicate its effects. The co-delivery of different thiol species may lead to unpredictable outcomes, which warrant further investigation.

Determination of S-containing drug metabolites from in vitro and in vivo metabolism studies by using LC-ICP/MS

2012 ◽  
Vol 404 (2) ◽  
pp. 539-551 ◽  
Author(s):  
Cristina Losada ◽  
Joan J. Albertí ◽  
Javier Saurina ◽  
Sonia Sentellas
Keyword(s):  
In Vivo Metabolism ◽  
Drug Metabolites ◽  
Icp Ms

Synthesis and Characterization of Urofuranoic Acids: In Vivo Metabolism of 2-(2-Carboxyethyl)-4-methyl-5-propylfuran-3-carboxylic Acid (CMPF) and Effects on in Vitro Insulin Secretion

2017 ◽  
Vol 60 (5) ◽  
pp. 1860-1875 ◽  
Author(s):  
Edith Nagy ◽  
Ying Liu ◽  
Kacey J. Prentice ◽  
Kyle W. Sloop ◽  
Phillip E. Sanders ◽  
...  
Keyword(s):  
Insulin Secretion ◽  
Carboxylic Acid ◽  
Synthesis And Characterization ◽  
In Vivo Metabolism ◽  
In Vitro Insulin Secretion

scholarly journals Chemical synthesis, characterisation and in vitro and in vivo metabolism of the synthetic opioid MT-45 and its newly identified fluorinated analogue 2F-MT-45 with metabolite confirmation in urine samples from known drug users

2018 ◽  
Vol 36 (2) ◽  
pp. 359-374 ◽  
Author(s):  
Craig McKenzie ◽  
Oliver B. Sutcliffe ◽  
Kevin D. Read ◽  
Paul Scullion ◽  
Ola Epemolu ◽  
...  
Keyword(s):  
Chemical Synthesis ◽  
Drug Users ◽  
Urine Samples ◽  
In Vivo Metabolism
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