A method for the sensitive determination of dechloroethylcylclophosphamide (3-DCl) in microsomal incubation mixtures was developed. 3-DCl, a side-chain oxidation product of cyclophosphamide (CP), was isolated by extraction with acetic acid ethyl ester following solid-phase extraction on C8 cartridges. Quantification of the metabolite was performed by direct capillary gas chromatography with a nitrogen-phosphorus detector without prior derivatization. The method showed good sensitivity and reproducibility with a detection limit of 1 ng/ml and a limit of quantification of 5 ng/ml. The suitability of the method is shown for the quantification of 3-DCl following incubation of CP with human liver microsomes.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0378-4347(95)00236-c | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
[Comparative study on metabolites in rat liver microsomes, urine, feces and bile between Shuganning Injection and Scutellariae Radix extract].
Zhongguo Zhong Yao Za Zhi
December 2024
School of Pharmaceutical Sciences, Guizhou Medical University Guiyang 550004, China Engineering Research Center for Development and Application of Ethnic Medicine and Traditional Chinese Medicine, Guizhou Medical University Guiyang 550004, China.
This study aims to compare the metabolic differences of baicalin and its analogues between Shuganning Injection and Scutellariae Radix extract. Twelve SD rats were randomly divided into a Shuganning Injection group and a Scutellariae Radix extract group, with 6 rats in each group. Their liver microsomes were incubated with the drugs, and then the samples were collected.
View Article and Find Full Text PDFResearch on the metabolites and key metabolic enzymes of allocryptopine in chicken liver microsomes via stable isotope tracing technology.
J Pharm Biomed Anal
January 2025
Shanxi Key Lab. for modernization of TCVM, College of Veterinary Medicine, Shanxi Agricultural University, Jinzhong 030801, China; College of Veterinary Medicine, Hunan Agricultural University, Changsha 410128, China. Electronic address:
Allocryptopine (ALL), a principal active component of the novel veterinary medicine Bopu Powder®, has gained widespread application in the poultry farming sector for the effective management of Escherichia coli (E. coli) diarrhea. In order to explore the metabolites and the pivotal enzymes associated with ALL, this study was conducted employing an in vitro chicken liver microsomal incubation.
View Article and Find Full Text PDFPreclinical evaluation of the potential PARP-imaging probe [carbonyl-C]DPQ.
EJNMMI Radiopharm Chem
January 2025
Division of Nuclear Medicine, Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, Vienna, Austria.
Background: Poly (ADP-ribose) polymerase (PARP) enzymes are crucial for the repair of DNA single-strand breaks and have become key therapeutic targets in homologous recombination-deficient cancers, including prostate cancer. To enable non-invasive monitoring of PARP-1 expression, several PARP-1-targeting positron emission tomography (PET) tracers have been developed. Here, we aimed to preclinically investigate [carbonyl-C]DPQ as an alternative PARP-1 PET tracer as it features a strongly distinct chemotype compared to the frontrunners [F]FluorThanatrace and [F]PARPi.
View Article and Find Full Text PDFHeterotropic Activation of Cytochrome P450 3A4 by Perillyl Alcohol.
Pharmaceutics
December 2024
College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
: Perillyl alcohol (POH), a monoterpene natural product derived from the essential oils of plants such as perilla (), is currently in phase I and II clinical trials as a chemotherapeutic agent. In this study, we investigated the effect of POH on cytochrome P450 (CYP) activity for evaluating POH-drug interaction potential. : The investigation was conducted using pooled human liver microsomes (HLMs), recombinant CYP3A4 (rCYP3A4) enzymes, and human pluripotent stem cell-derived hepatic organoids (hHOs) employing liquid chromatography-tandem mass spectrometry.
View Article and Find Full Text PDFDifferences in metabolite genotoxicity test results of rat liver S9 microsomes treated with various microsomal enzyme inducers.
Toxicol Mech Methods
January 2025
Drug Safety Research and Evaluation, Research, Takeda Pharmaceutical Company Limited, Fujisawa, Japan.
The rat S9 microsome fraction is commonly used to assess compound metabolite formation during genotoxicity assessments. However, methods using S9 have not been standardized for genotoxicity studies, and different experimental methods are used at various facilities. Therefore, this study investigated whether the differences between the two experimental conditions (1) S9 inducers, phenobarbital + beta-naphthoflavones vs.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!