Novel effect of N-palmitoyl-l-serine phosphoric acid on cytosolic Ca 2+ levels in human osteoblasts

Chung Ren Jan, Yih Chau Lu, Bang Ping Jiann, Hong Tai Chang, Jue Long Wang, Wei Chung Chen, Jong Khing Huang*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

3 Scopus citations

Abstract

The effect of N-palmitoyl-L-serine phosphoric acid (L-NASPA), which has been used as an inhibitor of lysophosphatidic acid receptors, on intracellular Ca2+ concentration ([Ca2+]i) in human osteosarcoma MG63 cells was measured by using fura-2. L-NASPA (0.1-10 μM) caused a rapid and transient plateau [Ca2+]i rise in a concentration-dependent marmer (EC50=0.5 μM). The L-NASPA-induced [Ca2+]i rise was partly reduced by removal of extracellular Ca2+ but was not altered by L-type voltage-gated Ca2+ channel blockers. In Ca2+-free medium, thapsigargin, an inhibitor of the endoplasmic reticulum Ca2+-ATPase, induced a [Ca2+]i rise, after which the increasing effect of L-NASPA on [Ca2+]i was completely inhibited; also, pretreatment with L-NASPA partly reduced thapsigargin-induced [Ca 2+]i rise. U73122, an inhibitor of phospholipase C, abolished histamine (but not L-NASPA)-induced [Ca2+]i rise. Overnight incubation with 1 μM L-NASPA did not affect cell proliferation, but 10-20 μM L-NASPA exerted 4% and 15% inhibition, respectively. Collectively, L-NASPA rapidly increased [Ca2+] i in MG63 cells by evoking both extracellular Ca2+ influx and intracellular Ca2+ release, and is cytotoxic at higher concentrations.

Original languageEnglish
Pages (from-to)71-76
Number of pages6
JournalPharmacology and Toxicology
Volume93
Issue number2
DOIs
StatePublished - 01 08 2003
Externally publishedYes

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