目的 探讨微生物对青蒿素 (Ⅰ)的转化作用。方法 通过华根霉和雅致小克银汉霉在土豆培养基中发酵产酶,对青蒿素进行转化。结果 两株菌对底物均有转化作用,分离出去氧青蒿素 deoxyartem isinin (Ⅱ),3α-羟基去氧青蒿素 3α- hydroxydeoxyartemisinin(Ⅲ)和 9β-羟基青蒿素 9β- hydroxyartemisinin(Ⅳ)共 3个产物,其中 为一新化合物,同时振荡条件下底物在无菌培养基中也能发生微量转化得到产物 。结论 青蒿素易被实验两株真菌转化,同时过氧桥也易断裂而失去一个氧原子成为去氧青蒿素,丧失抗疟活性,起作用的可能是土豆培养基中的铁元素

Object To study the microbial transformation of antimalarial drug artemisinin (Ⅰ) Methods The enzymes secreted by fermentation of Rhizopus chinensis Saito CICC 3043 and Cunninghamella elegans Lendn AS 3 1207 in the potato medium were employed to transform artemisinin Results Three products were obtained, among which deoxyartemisinin (Ⅱ) was also found in the controls without microorganisms The other two were identified as 3α hydroxydeoxyartemisinin (Ⅲ) and 9β hydroxyartemisinin (Ⅳ) Compound (Ⅳ) was identified as a new one Conclusion Artemisinin could be transformed by the two title strains of microorganisms It is easy to release one oxygen atom by breaking of perexide bridge in potato medium and to form deoxyartemisinin, thus making it lose its antimalarial activity The iron (Fe) in the potato medium may have the above function