Epoxidation is the preferred pathway of first-stage metabolism of abiraterone acetate in brown bullhead (Ameiurus nebulosus)

Mach, Samuel; Jegorov, Alexandr; Kuzma, Marek; Zápal, Jakub; Šimek, Zdeněk; Čejka, Jan; Eigner, Václav

doi:10.1007/s11356-019-06568-y

Cited by 1 publication

(3 citation statements)

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“…Therefore, the phase II metabolism of ABR in vivo needs further study in the future. Interestingly, epoxidation is a recognized pathway for ABR, and epoxidation of steroids has also been described (24). The [M+H] + of M4 is 366.2597, and the secondary fragment ions are 334.2191, 316.2325, 262.2264.…”

Section: Discussionmentioning

confidence: 98%

“…A total of 5 major metabolites were found in this study, among which 4 hydroxylated metabolites were mainly produced in the metabolism of liver microsomes in vitro. The cleavage of ABR and each potential degradation product are calculated by combining the information obtained from the analysis of LC/MS n -IT-TOF with relevant literature reports (22)(23)(24). The [M+H] + of metabolites M1, M2, M3 and M4 is 366.2573, which are isomers.…”

Section: Discussionmentioning

confidence: 99%

“…It is reported that ABR-sulfate and ABR-sulfate-N-Oxide are the two main circulating metabolites of ABR, accounting for about 43% of the exposure (11,24,25). Several methods for bioanalysis of ABR in human plasma have been reported (25,26).…”

Section: Discussionmentioning

confidence: 99%

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Biotransformation of Abiraterone Into Five Characteristic Metabolites by the Rat Gut Microbiota and Liver Microsomes

Keranmu

Yang²,

Wahafu³

et al. 2022

Front. Oncol.

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It is well known that the role of gut microbiota in drug metabolism, especially in oral difficult absorbable drugs. Understanding the gut microbiota could enable us to understand drugs in new ways. The purpose of the study was to investigate explore the metabolites of the anti-prostate cancer drug Abiraterone by examining gut microbiota metabolism and hepatic metabolism in vitro. In this study, five metabolites (M1, M2, M3, M4 and M5) of Abiraterone were discovered using LC/MSn-IT-TOF. Four isomeric metabolites M1-M4 were found in liver microsome. M5 was found in the intestinal contents of Sprague-Dawley rats with a molecular weight of 388.31. Among them, M4 was found to be Abiraterone N-Oxide by comparison with the standard sample. After further comparing the metabolic behavior of Abiraterone in rat gut microbiota and liver microsomes, we delineated the possible metabolic pathways of Abiraterone. In conclusion, Abiraterone is metabolized specifically in liver microsomes and gut microbiota. This study can provide a theoretical basis for elucidating the metabolic mechanism of Abiraterone and guide its rational application in clinic.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%