微生物来源中性鞘磷脂酶抑制剂N-1530 A的研究

 目的从微生物代谢物中筛选中性鞘磷脂酶抑制剂。方法使用ODS柱层析、制备HPLC等方法进行化合物的分离纯化,利用紫外、质谱等理化分析以及核磁共振等分析方法进行结构解析,使用酸性和中性SMase的活性测定方法进行活性评价。结果从微生物代谢产物的菌种中,筛选得到一个活性化合物N-1530A,其对中性SMase的IC₅₀为7.2μmol·L^-1。对酸性SMase的活性测定的结果表明,此物质在95.5μmol·L^-1。的浓度下未见抑制作用。此化合物的化学结构与PI6621相同。结论N-1530A为一个活性较强的微生物来源中性SMase特异性的抑制剂。

N-1530A, a neutral sphinogominase inhibitor from metabolites of microorganisms

OBJECTIVE To screen neutral sphingomyelinase inhibitors from the metabolites of microorganism. METHODS The compound was isolated by ODS column chromatography and preparative HPLC system. The structure was identified by its physicochemical properties,¹³C-NMR and ¹H-NMR analysis. The activity was evaluated by acid and neutral sphingomyelinase assay. RESULTS N-1530A, an active compound, was isolated from the fungi N-1530. The compound was identified to be PI6621. The compound showed strong inhibitory activity against human neutral sphingomyelinase with IC₅₀ of 7.2μmol·L^-1, but no inhibitory against acid sphingomyelinase at the concentration of 95.5 μmol·L^-1. CONCLUSION N-1530A is a strong specific neutral sphingomyelinase inhibitor from the metabolites of microorganisms which is firstly reported in this study.