Relationship between the structure of taxol and other taxanes on induction of tumor necrosis factor-alpha gene expression and cytotoxicity

Cancer Res. 1994 Nov 15;54(22):5779-82.

Abstract

Taxol is an antitumor drug with cytotoxic properties that correlate with its microtubule-stabilizing activities. It has been reported that taxol parallels lipopolysaccharide in its effects on the induction of tumor necrosis factor-alpha (TNF-alpha) gene expression in macrophages (C. Bogdan and A. Ding, J. Leukocyte Biol., 52: 119-121, 1992; C. L. Manthey, M. E. Brandes, P. Y. Perera, and S. Vogel, J. Immunol., 149: 2459-2465, 1992; J. M. Carboni, C. Singh, and M. A. Tepper, Natl. Cancer Inst. Monogr., 15: 95-101, 1993). Structure-activity studies using taxol and related taxanes have been done to determine the relationship between the effects of taxol on TNF-alpha gene expression and its cytotoxic and microtubule-stabilizing activities. Using Northern blot analysis, it was found that changes in the structure of taxol that did not alter cytotoxicity did prevent the induction of TNF-alpha gene expression. The data presented in this paper demonstrate that the effects of taxol on TNF-alpha gene expression are distinct from its known cytotoxic properties.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Fibrosarcoma / metabolism
  • Gene Expression Regulation, Neoplastic / drug effects
  • Mice
  • Paclitaxel / analogs & derivatives
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacology*
  • RNA, Messenger / biosynthesis
  • RNA, Neoplasm / biosynthesis
  • Structure-Activity Relationship
  • Tumor Cells, Cultured
  • Tumor Necrosis Factor-alpha / biosynthesis*
  • Tumor Necrosis Factor-alpha / genetics

Substances

  • Antineoplastic Agents, Phytogenic
  • RNA, Messenger
  • RNA, Neoplasm
  • Tumor Necrosis Factor-alpha
  • Paclitaxel