Pub. Date : 2016 Dec 18
PMID : 28263536
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Effectiveness of human cytochrome P450 3A4 present in liposomal and microsomal nanoparticles in formation of covalent DNA adducts by ellipticine. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 2 | However, since its anticancer efficiency depends on the CYP3A4-mediated metabolism in cancer cells, the aim of our research is to develop nanoparticles containing this enzyme that can be transported to tumor cells, thereby potentiating ellipticine cytotoxicity. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 3 | METHODS: The CYP3A4 enzyme encapsulated into two nanoparticle forms, liposomes and microsomes, was tested to activate ellipticine to its reactive species forming covalent DNA adducts. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 4 | RESULTS: The CYP3A4 enzyme both in the liposome and microsome nanoparticle forms was efficient to activate ellipticine to species forming DNA adducts. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 5 | Two DNA adducts, which are formed from ellipticine metabolites 12-hydroxy- and 13-hydroxyellipticine generated by its oxidation by CYP3A4, were formed by both CYP3A4 nanoparticle systems. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 6 | Two DNA adducts, which are formed from ellipticine metabolites 12-hydroxy- and 13-hydroxyellipticine generated by its oxidation by CYP3A4, were formed by both CYP3A4 nanoparticle systems. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 7 | A higher effectiveness of CYP3A4 in microsomal than in liposomal nanoparticles to form ellipticine-DNA adducts was found. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 8 | CONCLUSION: Further testing in a suitable cancer cell model is encouraged to investigate whether the DNA-damaging effects of ellipticine after its activation by CYP3A4 nanoparticle forms are appropriate for active targeting of this enzyme to specific cancer cells. | ellipticine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |