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KMID : 0043320110340020229
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Archives of Pharmacal Research
2011 Volume.34 No. 2 p.229 ~ p.236
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Identification and evaluation of neutral sphingomyelinase 2 inhibitors
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Lee Dong-Hun
Kim Sung-Hyun
Ahn Kyong-Hoon
Kim Seok-Kyun
Choi Jong-Min
Ji Jung-Eun
Won Jong-Hoon
Park Yang-Hui
Lim Chae-Min
Kim Sang-Hee
Kim Dae-Kyong
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Abstract
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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.
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KEYWORD
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Inhibitors, Signal transduction, Sphingolipids, Sphingomyelinase
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