Modulation of multidrug resistance by three bisbenzyl-isoquinolines in comparison with verapamil
Abstract
AIM: To compare cycleanine (Cyc), insularine (Insr), insulanoline (Insn) and
verapamil (Ver) in modulation of multidrug resistance (MDR) in vitro.
METHODS: The cytotoxic effect was determined by 3-[4, 5-dimethylthiazol-2-yl],
5-diphenyl tetarzolium bromide (MTT) assay. The intracellular doxorubincin (Dox)
accumulation was assayed by spectrofluorometer.
RESULTS: Cyc, Insr, Insn, and Ver showed significant activities in modulating Dox
and vincristine resistances in acquired resistant MCF-7/Adr and KBv200 cell lines
in a dose-dependent manner. Cyc, Insr, Insn, and Ver increased intracellular Dox
accumulation in MCF-7/Adr cells. Cyc and Insr had greater activities than Ver in
modulating MDR, while Insn had similar activity to that of Ver.
CONCLUSION: MDR was modulated by Cyc, Insr, and Insn, due to the increase of
intracellular Dox accumulation.
Keywords:
verapamil (Ver) in modulation of multidrug resistance (MDR) in vitro.
METHODS: The cytotoxic effect was determined by 3-[4, 5-dimethylthiazol-2-yl],
5-diphenyl tetarzolium bromide (MTT) assay. The intracellular doxorubincin (Dox)
accumulation was assayed by spectrofluorometer.
RESULTS: Cyc, Insr, Insn, and Ver showed significant activities in modulating Dox
and vincristine resistances in acquired resistant MCF-7/Adr and KBv200 cell lines
in a dose-dependent manner. Cyc, Insr, Insn, and Ver increased intracellular Dox
accumulation in MCF-7/Adr cells. Cyc and Insr had greater activities than Ver in
modulating MDR, while Insn had similar activity to that of Ver.
CONCLUSION: MDR was modulated by Cyc, Insr, and Insn, due to the increase of
intracellular Dox accumulation.