一种新型天然脲酶抑制剂曲霉素的结构与抑酶效应

Studies on characteristics, Crystal Structure and Effectiveness of Urease Inhibitor From Aspergillus Ochraccus Wilh

从赭曲霉（Aspergillusochraoeus）代谢产物中获得一种新型的脲酶抑制剂曲霉素，经核磁共振，质谱仪等分析，推导出该化学结构为3－（1′，2′-环氧（丙基）－5，6-双氢-5-羟基-吡喃-正酮。通过X-射线衍射测定进一步肯定了上述结论。它是一种白色晶体，易溶于水和乙酸乙酯，对热较稳定，对刀豆脲酶和土壤脉酶有抑制作用，其抑制作用随抑制剂浓度增加而增强。抑制类型为非竞争抑制，Ki为1.3×10-3mol/L其抑制机理与该物质结构中的-C=O，-OH，-COOH基团有关。

A new urease inhibitor was purified from the metablic product of Aspergillus. Spp producingurease inhibitor. The molecular structure of C9H12O4 has been determined by NMR, IR, MS andelement analysis methods. The results have further been checded by X-ray diffraction method.The Mr= 184. 21 which was white and dissolved easily in the water and ethl acetate. The activity of -Sword usease and soil urease was retarded by the inhibtor. The rate of inhibition of ureaseactivity increase with an increase in concentrion of C9H122O4, which was found to be noncompetitive inhibitor, Ki was 4 ×10-3 mol/L. The crystal was orthorhombic. Its mechanism of inhibiting urease could be considered in connection with - C = O, - OH and - COOH group in itsmolecular structure