Effects of HZ08,a novel P-glycoprotein inhibitor, on the reversal of P-glyco-protein mediated multidrug resistance in nude mice and cytochrome P-450 ac-tivities in rat liver microsomes / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 447-452, 2008.
Article
in Chinese
| WPRIM
| ID: wpr-434114
ABSTRACT
Aim:
To evaluate the effects of HZ08, a novel P-glycoprotein inhibitor, on reversing tumor resistance of K562/ADM to adriamycin in nude mice and on the activities of cytochromes P-450 (GYP) isoforms.Methods:
Nude mice bearing K562/ADM were injected at different doses of HZ08 with adriamycin for 4 weeks. The tumor weights of HZ08 treatment groups were determined and compared to those of the control and positive groups. In addition, the effects of HZ08 were examined on GYP isoforms-mediated metabolism of specific substrates by GYP isoforms in rat liver microsomes in the presence or absence of HZ08.Results:
The tumor weights of HZ08 treatment groups were significantly decreased and HZ08 was a relatively potent inhibitor of CYP3A4, with no significant effects on other isoforms tested.Conclusion:
HZ08 has potent effects on reversing P-glycoprotein mediated tumor multidrug resistance in rive with little influence on cytoehrome P-450 activities of rat liver.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of China Pharmaceutical University
Year:
2008
Type:
Article
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