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KMID : 0606920030110030169
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Biomolecules & Therapeutics
2003 Volume.11 No. 3 p.169 ~ p.173
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Inhibition of a Neutral Form of Sphingomyelinase by Alkylthioureido-l,3-propandiols, KY353X Series
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Jung SM
Jeong EM/Jo DH/Chin MR/Jun HJ/Kim YH/Jeon HJ/Lee DH/Park MJ
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Abstract
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Alkylthioureido-1,3-propandiols (KY353X series) were synthesized and evaluated as inhibitors for neutral sphingomyelinase (N-SMase). To examine whether KY353X series inhibit N-SMase, we purified the N-SMase from bovine brain. The N-SMase was partially purified by sequential chromatographies of DEAE-Cellulose anionic exchange and phenyl-5PW hydrophobic HPLC. These seqeuntial procedures for N-SMase resulted in a 67-fold purification and excluded other isoforms of SMase. Based on in vitro assay, KY353X series inhibited N-SMase activity in time, concentration-dependent manners and completely inactivated N-SMase at 50 μM. In particular, KY3535 and KY3536 inhibited more effectively than the others. To further determine the .inhibitory pattern, a Dixon plot was constructed, to showing that the inhibition by KY3535 and KY3536 were competitive. The inhibition constant (Ki) of KY3535 and KY3536 was 1.7 μM and 2.5μM in 100 mM Tris-HCl buffer, pH 7.0, respectively.
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