Stimulation of TNF-alpha production by 2-(1-adamantylamino)-6-methylpyridine (AdAMP) - a novel immunomodulator with potential application in tumour immunotherapy

Cancer Chemother Pharmacol. 2002 Sep;50(3):213-22. doi: 10.1007/s00280-002-0496-5. Epub 2002 Jul 31.

Abstract

The immunomodulatory effects of a recently synthesized adamantane derivative of aminopyridine - 2-(1-adamantylamino)-6-methylpyridine (AdAMP) - were tested on normal and neoplastic cells in vitro. When incubated with TNF-alpha gene-transduced mouse melanoma cells (B78/TNF), AdAMP significantly enhanced basal production of TNF-alpha by these cells, both by "high" and "moderate" TNF-alpha-producer cells. A similar TNF-alpha production-enhancing effect was observed in cultures of human ovarian carcinoma cells (CAOV1) which spontaneously produce TNF-alpha but not in cultures of tumour cells incapable of TNF-alpha secretion. RT-PCR analysis showed that the enhancement of TNF-alpha production by AdAMP was associated with an increase in TNF-alpha mRNA expression in the treated cells. The results of an electrophoretic mobility shift assay (EMSA) showed that AdAMP significantly activated nuclear factor kappaB (NF-kappaB) in both CAOV1 and B78/TNF cells. The role of NF-kappaB in enhancement of TNF-alpha production was confirmed in experiments in which MG132, an inhibitor of NF-kappaB activation, reversed the effect of AdAMP. Unexpectedly, dexamethasone, a potent antiinflammatory agent and a strong inhibitor of TNF-alpha production in vivo, increased both spontaneous and AdAMP-augmented production of TNF-alpha in in vitro cultures of ovarian carcinoma cells and B78/TNF cells. AdAMP also enhanced TNF-alpha secretion by LPS-induced monocytes. AdAMP-induced augmentation of TNF-alpha production by B78/TNF cells was accompanied by morphological changes in the treated cells and a decrease in their adherence to fibrinogen and collagen IV. In view of these properties, AdAMP seems to be a therapeutically promising compound with potential application as an adjuvant augmenting the efficacy of cancer vaccine-based therapies or in the local treatment of certain tumours.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adamantane / analogs & derivatives
  • Adamantane / pharmacology*
  • Aminopyridines / pharmacology*
  • Animals
  • Female
  • Humans
  • Melanoma / pathology*
  • Mice
  • NF-kappa B / biosynthesis
  • Ovarian Neoplasms / pathology
  • RNA, Messenger / analysis
  • Tumor Cells, Cultured
  • Tumor Necrosis Factor-alpha / biosynthesis*

Substances

  • 2-(1-adamantylamino)-6-methylpyridine
  • Aminopyridines
  • NF-kappa B
  • RNA, Messenger
  • Tumor Necrosis Factor-alpha
  • Adamantane