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


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)
Number of pages1
JournalSkin Pharmacology
Issue number2
StatePublished - Dec 1 1996

ASJC Scopus subject areas

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

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