C2-Ceramide Increases Cytoplasmic Calcium Concentrations in Human Parathyroid Cells Radu Mihai, Teresa Lai, George Schofield,* and John R. Farndon Department of Surgery, Bristol Royal Infirmary, Bristol BS2 8HW, United Kingdom; and *Department of Biochemistry, School of Medical Sciences, University of Bristol, Bristol, United Kingdom Received December 29, 1999 Effects of extracellular calcium ([Ca 2 ] ext ) on para- thyroid cells are mainly due to the activation of a plasma membrane calcium receptor (CaR) coupled with release of intracellular calcium. In addition, high [Ca 2 ] ext activates the sphingomyelin pathway in bovine parathyroid cells, generating ceramides and sphingosine. This study explored the direct ef- fects of synthetic ceramides on [Ca 2 ] i in human parathyroid cells. Cells from five parathyroid adeno- mas removed from patients with primary hyperpara- thyroidism were dispersed and maintained in pri- mary culture. Intracellular calcium concentration ([Ca 2 ] i ) [Ca 2 ] i was monitored using standard quan- titative fluorescence microscopy in Fura-2/AM- loaded cells. Laser scanning microscopy was used to monitor the intracellular distribution of a fluores- cent ceramide analogue (BODIPY-C5). After addi- tion of 10 M C2-ceramide (N-acetyl-D-erythro- sphingosine), [Ca 2 ] i increased rapidly (30 – 60 s) to a peak three times above basal levels in 70% of cells (37/55 cells in four experiments). This effect ap- peared to be due to release of Ca 2 from intracellular stores rather than Ca 2 entry from the extracellular medium. C2-responsive cells had a smaller [Ca 2 ] i response to subsequent stimulation with the CaR agonist—neomycin (1 mM). These responses were specific to C2 since C6-ceramide (N-hexanoyl-D- erythro-sphingosine) did not affect basal [Ca 2 ] i nor the responses to an increase in [Ca 2 ] ext and to neo- mycin. C5-BODIPY generated intense perinuclear fluorescence, suggesting targeting of the ceramides to the Golgi apparatus. These data demonstrate that endogenous generation of ceramides has the poten- tial to modulate changes in [Ca 2 ] i and secretion in response to [Ca 2 ] ext in human parathyroid cells. © 2000 Academic Press Key Words: human parathyroid cells; hyperparathy- roidism; C2-, C6-ceramide; sphingosine; Fura-2/AM; C5-BODIPY; fluorescence microscopy; confocal microscopy. Extracellular calcium concentration ([Ca 2+ ] ext ) is the main factor controlling secretion from parathyroid cells. Changes in [Ca 2+ ] ext are sensed by a plasma mem- brane calcium receptor (CaR) (1). High [Ca 2+ ] ext and other agents (e.g. neomycin and trivalent cations La 3+ and Gd 3+ ) stimulate the CaR, which is coupled to the G-protein-phospholipase C pathway that leads to gen- eration of inositol 1,4,5-trisphosphate (IP 3 ) and release of Ca 2+ from intracellular stores (1). In this way, high [Ca 2+ ] ext is translated into high [Ca 2+ ] i and this inhibits secretion through an as yet unknown mechanism. In bovine parathyroid cells high [Ca 2+ ] ext increases the concentration of sphingosine (2), one of the intermediates in the sphingomyelin pathway. In many cell types, the sphingomyelin pathway is involved in the regulation of cell proliferation, cell-cell interaction, differentiation and oncogenesis (3). Its activation begins with hydrolysis of membrane sphingomyelin by a neutral sphingomyeli- nase, leading to increased ceramide levels in target cells. The hydrolysis of ceramide by a ceramidase produces free sphingosine, which can be further converted to sphingosine-1-phosphate (by a sphingosine-kinase) or to sphingosine-phosphorylcholine. Although very little is known about the effects of sphingolipids in the parathy- roid cells, the increase in sphingosine concentration in response to [Ca 2+ ] ext (2) raises the possibility that the sphingomyelin pathway is functionally important in parathyroid cell. The aim of this study was to explore the possibility that compounds generated through the sphingomyelin pathway modulate the response of human parathyroid cells to changes in [Ca 2+ ] ext . The effects of synthetic ceramides on [Ca 2+ ] i were investigated in human para- thyroid cells from patients with primary hyperparathy- roidism. [Ca 2+ ] i was measured in individual cells using the widely-accepted method of quantitative fluores- cence microscopy in cells loaded with the calcium- marker Fura-2/AM. Confocal microscopy was used to monitor the intracellular distribution of a fluorescent ceramide analogue (C5-BODIPY). Biochemical and Biophysical Research Communications 268, 636 – 641 (2000) doi:10.1006/bbrc.2000.2159, available online at http://www.idealibrary.com on 636 0006-291X/00 $35.00 Copyright © 2000 by Academic Press All rights of reproduction in any form reserved.