Anti-inflammatory and antiproliferating properties of allylamines

U. E. Berry, T. S. Choi, S. C. Geen, N. B. Silverberg, W. L. Lee, A. R. Shalita

Research output: Contribution to journalArticlepeer-review

Abstract

Terbinafme (TB, SF86-327), a synthetic allylamine, is a broad-spectrum, orally active antifungal. Cytospin data showed that TB-treated (10-50 ug/ml for 30 min at 37 °C) human polymorphonuclear leukocytes (PMNs) displayed nuclear rounding with loss of lobulations and a reduction in the cytoplasmic to nuclear ratio. Similar cytoplasmic to nuclear ratio reductions were also demonstrated in TB-treated peripheral blood lymphocytes (PBLs). TB-treated PMNs (at > 25 ng/ml) exhibited normal respiratory burst activity measured by Superoxide anion production and chemiluminescence (CL), but showed reduced chemotaxis (CT). TB significantly (p < 0.01-0.05) inhibited PMN and PBL adhesion to human microvascular endothelium (HMEC-1). The TB-treated leukocytes were stimulated by chemotactic factors or mitogens, and cell adhesion was measured by uptake of rose bengal stain using an ELISA reader. TB analogues (85-190 or naftifine) produced similar dose-dependent inhibitory effects on CT and cell adhesion to HMEC-1, the latter also inhibited CL. Cell cycle flow cytometric analysis showed doseand time-dependent alterations in Gl and/or G2+M phase(s) consistent with cell cycle and mitotic blockade in mitogen-activated PBLs and a promyelocytic cell line (HL60). Our data collectively demonstrates morphological and functional differences among allylaminetreated cells, which may explain many of the antiinflammatory and antiproliferation effects.

Original languageEnglish (US)
Pages (from-to)143
Number of pages1
JournalSkin Pharmacology
Volume9
Issue number2
StatePublished - 1996

ASJC Scopus subject areas

  • Dermatology
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)

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