植物精提复合酶转化防风中升麻素苷的研究

目的: 研究利用酶法在体外条件下,将防风中含量较高的色原酮类成分升麻素苷,转化为体内高吸收主要入血性成分升麻素,并优化其转化条件。 方法: 首先从防风中分离制备升麻素苷,然后利用植物精提复合酶SPE-007转化升麻素苷为其苷元升麻素,并采用HPLC法,以升麻素苷的转化率为评价指标,在单因素分析的基础上对酶解反应条件(酶解时间、酶解温度和酶浓度)进行优化。 结果: 酶浓度、酶解温度、酶解时间对酶法转化升麻素苷具有显著影响,其最佳酶反应条件为:酶浓度1.1 mg·mL^-1,酶解温度48℃,酶解时间48 h。在此条件下,升麻素苷较完全地酶解转化为升麻素。 结论: 利用酶法转化传统中药有效成分已成为开发中药高活性成分的重要手段,酶法转化中草药中有效成分因其反应特异性强、高效、条件温和、易于控制等优点而具有广阔的应用前景。本实验应用植物精提符合酶SPE-007转化升麻素苷来制备升麻素,此酶法转化率可达到98%以上,如此简便、经济的方法可为升麻素的工业化生产提供重要参考。

Objective: To study conversion of chromones composition prim-O-glucosylcimifugin with high content in Saposhnikovia divaricata into cimifugin which can be highly absorbed in blood in vivo by use of enzymatic method in vitro,and optimize the conversion condition. Methods: Firstly,prim-O-glucosylcimifugin from Saposhnikovia divaricata was separated and prepared,and then the plant extraction complex enzyme SPE-007 was used to transform prim-O-glucosylcimifugin to its aglycone cimifugin,and the HPLC method was adopted and the conversion rate of prim-O-glucosylcimifugin was taken as the assessment index to optimize enzymolysis reaction conditions(enzymolysis time,enzymolysis temperature and enzyme concentration) on the basis of single factor analysis. Results: The enzyme concentration,enzymolysis temperature and enzymolysis time had significant effects on conversion of prim-O-glucosylcimifugin via enzymatic method,and the optimal enzyme reaction condition was:enzyme concentration of 1.1 mg·mL^-1,enzymolysis temperature of 48℃ and enzymolysis time of 48 h,under which prim-O-glucosylcimifugin was relatively completely conversed into cimifugin. Conclusion: The conversion of active ingredients of traditional Chinese medicine via enzymatic method has become an important means to develop high-activity component.Due to strong specificity,high efficiency,moderate condition,easy control and other advantages,this method has wide application prospect.This test prepares cimifugin by the plant extraction complex enzyme SPE-007 to converse prim-O-glucosylcimifugin,and the conversion rate can be above 98% by this method; such a convenient,economical and green method will provide important reference for industrialized production of cimifugin.