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Kobayashi, J. et al.

Kobayashi, Shigemori, Hosoyama, Chen, Akiyama, Naito, Tsuruo,

Multidrug resistance reversal activity of taxoids from Taxus cuspidata in KB-C2 and 2780AD cells.

Some non-taxol-type taxoids having neither an oxetane ring at C-4 and C-5 nor an N-acylphenyl-isoserine group at C-13, such as taxuspine C, 2'-desacetoxyaustrospicatine, and 2-desacetoxytaxinine J, which were isolated from the Japanese yew Taxus cuspidata, increased cellular accu-mulation of vincristine (VCR) in multidrug-resistant 2780AD cells as potently as verapamil, and efficiently inhibited [(3)H]azidopine photolabeling of P-glycoprotein (P-gp). Taxuspine C, 2'-desacetoxyaustrospicatine, and 2-desacetoxytaxinine J at 10 microM completely reversed the resistance to colchicine, VCR, and taxol in KB-C2 cells, which overexpress P-gp, while taxinine and taxinine M showed no effect. Taxuspine C, 2'-desacetoxyaustrospicatine, and 2-desacetoxytaxinine J may be candidate pharmaceuticals for reversing multidrug resistance ( MDR) and also may be good modifiers of MDR in cancer chemotherapy.[1]

References

Multidrug resistance reversal activity of taxoids from Taxus cuspidata in KB-C2 and 2780AD cells. Kobayashi, J., Shigemori, H., Hosoyama, H., Chen, Z., Akiyama, S., Naito, M., Tsuruo, T. Jpn. J. Cancer Res. (2000) [Pubmed]

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