scholarly journals Inhibitory effect of ciprofloxacin on β-glucuronidase-mediated deconjugation of mycophenolic acid glucuronide

2014 ◽  
Vol 35 (5) ◽  
pp. 275-283 ◽  
Author(s):  
Takaaki Kodawara ◽  
Satohiro Masuda ◽  
Yoshitaka Yano ◽  
Kazuo Matsubara ◽  
Toshiaki Nakamura ◽  
...  
Keyword(s):  
Mycophenolic Acid ◽  
Inhibitory Effect ◽  
Mycophenolic Acid Glucuronide

Investigation of the Crossreactivity of Mycophenolic Acid Glucuronide Metabolites and of Mycophenolate Mofetil in the Cedia MPA Assay

2010 ◽  
Vol 32 (1) ◽  
pp. 79-85 ◽  
Author(s):  
Maria Shipkova ◽  
Ekkehard Schütz ◽  
Ingo Besenthal ◽  
Peter Fraunberger ◽  
Eberhard Wieland
Keyword(s):  
Mycophenolate Mofetil ◽  
Mycophenolic Acid ◽  
Mycophenolic Acid Glucuronide

HPLC determination of mycophenolic acid and mycophenolic acid glucuronide in human plasma with hybrid material

2004 ◽  
Vol 36 (3) ◽  
pp. 649-651 ◽  
Author(s):  
Magali Bolon ◽  
Laetitia Jeanpierre ◽  
Mirna El Barkil ◽  
Karim Chelbi ◽  
Martine Sauviat ◽  
...  
Keyword(s):  
Human Plasma ◽  
Mycophenolic Acid ◽  
Hybrid Material ◽  
Hplc Determination ◽  
Mycophenolic Acid Glucuronide

scholarly journals Synthesis and Evaluation of Mycophenolic Acid Derivatives as Potential Anti-Toxoplasma Gondii Agents

2021 ◽  
Author(s):  
Fan-Fan Shang ◽  
Mei-Yuan Wang ◽  
Jiang-Ping Ai ◽  
Qing-Kun Shen ◽  
Hong-Yan Guo ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Mycophenolic Acid ◽  
Alanine Aminotransferase ◽  
Abdominal Cavity ◽  
Inhibitory Effect ◽  
Protective Effects ◽  
Appetite Loss ◽  
Human Foreskin Fibroblasts ◽  
First Time

Abstract Nineteen mycophenolic acid (MPA) derivatives were designed and synthesized, and their anti-Toxoplasma activity evaluated for the first time. Among them, N-propylimidazole-modified compound E5 demonstrated the strongest activity, and the IC50 against HFF-1 (Human Foreskin Fibroblasts-1) cells following infection with T. gondii is 80.9 μM (MPA-211.5 μM) and its selectivity value is 2.2 (MPA-1.2). In vivo experiments, E5 significantly inhibited the proliferation of tachyzoites in the abdominal cavity of mice acutely infected with T. gondii (inhibition rates 46.7%), and this inhibitory effect was greater than that of spiramycin (inhibition rates 31.3%) and MPA (inhibition rates 15.9%), this indicated that E5 had significant protective effects on the host during acute Toxoplasma infection. In addition E5 significantly reduced the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum of infected mice, significantly increased the level of glutathione (GSH) in the liver, and significantly reduced the level of malondialdehyde (MDA), indicating that it has a significant hepatoprotective effect against T. gondii infection. Similarly, E5 can relieve hepatomegaly and splenomegaly induced by acute Toxoplasma infection. Spiramycin aggravated appetite loss in infected mice, while E5 did not. In summary, the results indicated that E5 has potential as a candidate anti-T. gondii drug.

scholarly journals IMP-dehydrogenase inhibition in human lymphocytes and lymphoblasts by mycophenolic acid and mycophenolic acid glucuronide

1997 ◽  
Vol 43 (12) ◽  
pp. 2312-2317 ◽  
Author(s):  
Andrea Griesmacher ◽  
Günter Weigel ◽  
Gernot Seebacher ◽  
Mathias M Müller
Keyword(s):  
Human Plasma ◽  
Mycophenolic Acid ◽  
Human Lymphocytes ◽  
Cell Types ◽  
Type I ◽  
Type Ii ◽  
Inhibitory Effects ◽  
Mediated Effects ◽  
Transplant Patients ◽  
Mycophenolic Acid Glucuronide

Abstract Inosine 5′-monophosphate dehydrogenase (IMP-DH) activities were measured in human lymphocytes (exhibiting type I IMP-DH activity) and human lymphoblasts (exhibiting type II IMP-DH activity) in the presence of various amounts of mycophenolic acid (MPA) (0–20 μmol/L) and MPA glucuronide (MPAG) (0–200 μmol/L). Moreover, the influences of human serum albumin (HSA) and human plasma on the MPA- and MPAG-mediated effects were investigated. In the presence of water, 2.5 μmol/L MPA decreased the IMP-DH activity measured in lymphocytes by 60%, whereas in lymphoblasts a 80% inhibition was detectable. In the presence of ≥10 μmol/L MPA, lymphocytic as well as lymphoblastic IMP-DH activities were reduced in a similar manner. The concentration of MPAG required for 50% inhibition was for both cell types >25 μmol/L and <50 μmol/L, respectively. MPAG (200 μmol/L) reduced lymphocytic as well as lymphoblastic IMP-DH activity by ∼80%. With 100 g/L HSA or human plasma as diluent, the inhibitory effects of MPA and MPAG were significantly (P <0.05) diminished, whereas HSA concentrations ≤25 g/L only slightly influenced the inhibition of IMP-DH activity by MPA and MPAG. In summary, it can be clearly demonstrated that not only MPA but also MPAG contributes to the inhibition of both IMP-DH isoenzymes, which might be relevant for the immunosuppressive properties of mycophenolate mofetil in transplant patients.

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