Kobayashi J, Hosoyama H, Wang X X, Shigemori H, Sudo Y, Tsuruo T
Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.
Bioorg Med Chem Lett. 1998 Jun 16;8(12):1555-8. doi: 10.1016/s0960-894x(98)00262-5.
Taxuspine C (1), a new taxoid from the Japanese yew Taxus cuspidata, increasing the cellular accumulation of vincristine (VCR) in multidrug-resistant tumor cells as potent as verapamil enhanced the chemotherapeutic effect of VCR in P388/VCR-bearing mice. When taxuspine C (1) was given i.p. daily at 200 mg/kg with 0.2 mg/kg VCR for 5 days, a treated/control (T/C) value of 138% was obtained. The other new taxoids, taxezopidines G (8) and H (9), from the yew also increased the VCR accumulation as potent as verapamil. These results suggest that some taxoids may be useful for overcoming multidrug resistance in tumor cells.
紫杉刺碱C（1）是从日本红豆杉（Taxus cuspidata）中分离得到的一种新型紫杉烷类化合物，它能像维拉帕米一样有效地增加多药耐药肿瘤细胞中长春新碱（VCR）的细胞内蓄积，增强VCR对携带P388/VCR小鼠的化疗效果。当以200 mg/kg的剂量每日腹腔注射紫杉刺碱C（1）并联合0.2 mg/kg的VCR给药5天时，治疗组与对照组（T/C）的值为138%。从红豆杉中分离得到的其他新型紫杉烷类化合物，紫杉氮杂环丁烷G（8）和H（9），也能像维拉帕米一样有效地增加VCR的蓄积。这些结果表明，某些紫杉烷类化合物可能有助于克服肿瘤细胞中的多药耐药性。
