NPC-14686, a novel anti-inflammatory agent, increased intracellular Ca2+ concentrations in MDCK renal tubular cells

NPC-14686 (Fmoc-l-homophenylalanine)-induced Ca2+ increases and death in human prostate cancer cells

“…How NPC-14686 releases Ca 2+ from the endoplasmic reticulum needs further investigation. Previous studies have reported that NPC-14686 can increase [Ca 2+ ] i in other cell types (Jan et al, 2000(Jan et al, , 2003; however, possible toxicity of NPC-14686 on cell proliferation has not been studied. Our data show that overnight treatment with 1 AM NPC-14686 could cause a significant decrease in cell proliferation.…”

“…However, the cellular mechanism(s) of these drugs' action is unclear. Among them, NPC-14686 (Fmoc-l-homophenylalanine) has been commercialized and has been shown to prevent gastric mucosal lesions after compound 48 / 80 injection into rats (Ohta et al, 1999), and to increase intracellular free Ca 2+ levels ([Ca 2+ ] i ) in human hepatoma cells (Jan et al, 2003) and canine renal tubular cells (Jan et al, 2000). However, the underlying mechanisms of NPC-14686's effects are unclear.…”

Structure‐Based Rationale Design and Synthesis of Aurantiamide Acetate Analogues – Towards a New Class of Potent Analgesic and Anti‐inflammatory Agents

“…This revealed the importance of Boc group or N-substitution in exerting better pharmacological properties. On the other hand, when Fmoc of Val (14) was replaced by Bpoc (15), there was an increase in the activity which may be due to the presence of biphenyl system in the latter.…”

“…In addition, these compounds also increased intracellular Ca 2+ concentrations in Madin-Darby canine kidney (MDCK) renal tubular cells (15). These agents do not act by inhibiting lipid metabolic enzymes.…”

Design and synthesis of new N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides as anti-inflammatory agents

“…Other research has shown that several N-Fmoc amino acids exert anti-inflammatory activity by recruitment of neutrophils into the inflammatory site [14,15]. In addition, these compounds also increased intracellular Ca 2þ concentrations in Madin Darby canine kidney (MDCK) renal tubular cells [16].…”