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- 자료유형
- 학술저널
- 저자정보
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- 한국응용약물학회 The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology 제11권 제3호
- 발행연도
- 2003.1
- 수록면
- 169 - 173 (5page)
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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 $\mu$M. 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 $\mu$M and 2.5$\mu$M in 100 mM Tris-HCl buffer, pH 7.0, respectively.
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