The reversal effect of TTD (a Chinese medicine) on human multidrug- resista
nt KBV200 cell line was studied and compared with verapamil (VPL). The chem
osensitivity of KBV200 was detected by MTT assay in vitro and the level of
MDR1 mRNA of KBV200 was investigated by RT-PCR. The cytotoxicity of TTD to
KBV200 and the parent sensitive cell line KB is very low and nearly same wi
th a concentration of 10(-6) mol.L-1. With the concentration TTD increased
VCR cytotoxicity on KBV200, 50% inhibitory concentration (IC50) decreased f
rom 1122.5+/-72.36 mol.L-1 to 31.76+/-5.4 nmol.L-1 (p<0.001). It was more e
ffective than VPL was (p<0.01). The combination of low concentration of TTD
(10(-8)mol.L-1) and VCR (100 nmol.L-1) has significantly increased VCR cyto
toxicity on KBV200, cell Surviving Fraction decreased from 0.91+/-0.056 to
0.74+/-0.07 (p<0.02). TTD did not inhibit the expression of MDR1 mRNA of KB
V200 with the concentration of 10(-6) mol.L-1. These data indicated that TT
D could reverse VCR resistance of KBV200 and may be useful in enhancing the
clinical effectiveness of VCR.