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Identification of the hydroxylated derivatives of bufalin: phase I metabolites in rats
- Source :
- Journal of Asian Natural Products Research. 18:239-247
- Publication Year :
- 2015
- Publisher :
- Informa UK Limited, 2015.
-
Abstract
- Bufalin was a typical bioactive bufadienolide, existed in the traditional Chinese medicine Chan Su with the high content of 1-5%. The in vivo metabolites (1-5) of bufalin were prepared by various chromatographic techniques from the bile samples of SD rats, which were administrated with bufalin orally. Their structures were determined on the basis of the widely spectroscopic data, including HRESIMS, 1D-, and 2D NMR. And 1-3, 5 were new compounds. In the in vitro cytotoxicity assay, metabolites (1-5) showed weaker cytotoxic effects than bufalin against human cancer cell lines A549 and H1299, which indicated that the metabolism was a significant pathway for the detoxification of bufalin. Structures analyses indicated that metabolites 1-5 were hydroxylated derivatives of bufalin. This study suggested that Phase I metabolism catalyzed by CYP450 enzymes was one of the metabolic ways of bufalin, which may promote the excretion of bufalin.
- Subjects :
- Male
0301 basic medicine
Pharmaceutical Science
Bufadienolide
Pharmacology
Biology
Hydroxylation
Analytical Chemistry
Rats, Sprague-Dawley
Excretion
03 medical and health sciences
chemistry.chemical_compound
Cytochrome P-450 Enzyme System
In vivo
Drug Discovery
Animals
Humans
Medicine, Chinese Traditional
Nuclear Magnetic Resonance, Biomolecular
Molecular Structure
Organic Chemistry
Bufalin
General Medicine
Metabolism
Rats
Bufanolides
030104 developmental biology
Complementary and alternative medicine
chemistry
Biochemistry
Cell culture
Molecular Medicine
Drug metabolism
Subjects
Details
- ISSN :
- 14772213 and 10286020
- Volume :
- 18
- Database :
- OpenAIRE
- Journal :
- Journal of Asian Natural Products Research
- Accession number :
- edsair.doi.dedup.....fa60abfa6f8840b23648bbc44f7103bf