Identification and evaluation of neutral sphingomyelinase 2 inhibitors

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• 作者：Dong Hun Lee (1)
  Sung Hyun Kim (1)
  Kyong Hoon Ahn (1)
  Seok Kyun Kim (1)
  Jong Min Choi (1)
  Jung Eun Ji (1)
  Jong Hoon Won (1)
  Yang Hui Park (1)
  Chaemin Lim (2)
  Sanghee Kim (2)
  Dae Kyong Kim (1)
  
• 关键词：Inhibitors ; Signal transduction ; Sphingolipids ; Sphingomyelinase
• 刊名：Archives of Pharmacal Research
• 出版年：2011
• 出版时间：February 2011
• 年：2011
• 卷：34
• 期：2
• 页码：229-236
• 全文大小：518KB
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• 作者单位：Dong Hun Lee (1)
  Sung Hyun Kim (1)
  Kyong Hoon Ahn (1)
  Seok Kyun Kim (1)
  Jong Min Choi (1)
  Jung Eun Ji (1)
  Jong Hoon Won (1)
  Yang Hui Park (1)
  Chaemin Lim (2)
  Sanghee Kim (2)
  Dae Kyong Kim (1)
  
  1. Department of Environmental & Health Chemistry, College of Pharmacy, Chung-Ang University, Seoul, 156-756, Korea
  2. College of Pharmacy, Seoul National University, Seoul, 151-742, Korea
  
• ISSN：1976-3786

文摘

Sphingomyelinase catalyzes the hydrolysis of sphingomyelin to generate ceramide, an important molecule involved in the regulation of various cellular responses. In this study, we partially purified the neutral sphingomyelinase2 (nSMase2) and identified the inhibitors, d-lyxophytosphingosine and d-arabino-phytosphingosine, which have an inhibitory effect on nSMase2 in a concentration-dependent manner. A Dixon plot of each phytosphingosines revealed their probable inhibitory pattern, i.e., apparent competitive inhibition. These compounds did not inhibit the Mg2+-independent neutral SMase activity, although the known nSMase2 inhibitor, GW4869, showed inhibitory effects on Mg2+-independent neutral SMase activity. Further, the two phytosphingosines specifically inhibited the ceramide generation regulated by nSMase2.