To overcome multidrug resistance (MDR) in cancer chemotherapy, we prepared various plant extracts and searched for a component which is effective for inhibition of MDR. MDR inhibition activity was determined by measuring cytotoxicity to MDR cells using multidrug resistant human fibrocarcinoma KB V20C, which is resistant to 20 nM vincristine and expresses high level ofmdr1 gene. Of various plant extracts, the MeOH extract of the root ofAconitum pseudo-laeve var.erectum was found to have potent inhibitory activity on MDR. The bioassay-guided fractionation of the MeOH extract of the plant led to the isolation of an alkaloid, lycaconitine, as an active principle. And the IC50 of lycaconitne for KB V20C cells was 74 μg/ml.
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Kim, D.K., Kwon, H.Y., Lee, K.R. et al. Isolation of a multidrug resistance inhibitor fromAconitum pseudo-laeve var.erectum . Arch. Pharm. Res. 21, 344–347 (1998). https://doi.org/10.1007/BF02975299
- Multidrug Resistance (MDR)
- Aconitum pseudo-laeve var.erectum