摘要
目的采用黄花蒿悬浮培养细胞研究二氢青蒿酸(Ⅰ)的生物转化。方法向预培养14 d的黄花蒿细胞悬浮培养体系中加入底物二氢青蒿酸,培养2 d后终止转化。通过TLC和HPLC检测转化产物,利用硅胶、Seph-adex LH-20以及ODS柱色谱分离纯化转化产物,并根据理化数据和波谱技术鉴定转化产物的化学结构,最后利用HPLC考察共培养时间对转化率的影响。结果二氢青蒿酸在黄花蒿培养体系中成功地进行了转化并分离得到两个转化产物:3-α-羟基二氢青蒿酸(Ⅱa)和3-β-羟基二氢青蒿酸(Ⅱb)。两个转化产物的最佳共培养时间均为1d,总的摩尔转化率分别为2.6%(Ⅱa)和15.7%(Ⅱb)。结论本研究首次利用黄花蒿培养细胞生物转化二氢青蒿酸,且得到一对区域特异性的羟基化转化产物。
Objective To investigate the biotransformation of dihydroartemisinc acid（Ⅰ） by cultured cells of Artemisia annua.Methods Dihydroartemisinic acid was added to the suspension cells of A.annua which had been pre-cultured for 14 d and co-cultured for another 2 d.The biotransfromed products were detected with TLC and HPLC,and isolated by various chromatographic methods.Results The chemical structures of biotransformed products were elucidated on the basis of spectroscopic data.3-α-Hydroxy-dihydroartemisinic acid（Ⅱa） and 3-β-hydroxy-dihydroartemisinic acid（Ⅱb） were obtained after 2 d administration of dihydroartemisinic acid to the suspension cells of A.annua.Ⅱa and Ⅱb yields could reach a maxium mole ratio of 2.6% and 15.7% after 1 d incubation,respectivly.Conclusion It is the first time for the biotransformation of dihydroartemisinic acid to epimeric 3-hydroxyartemisinic acid by using suspension culture cell of A.annua.The results indicate that cells of A.annua have the ability to hydroxylate dihydroartemisinic acid region selectively.
出处
《中草药》
CAS
CSCD
北大核心
2010年第8期1358-1361,共4页
Chinese Traditional and Herbal Drugs
关键词
黄花蒿
悬浮培养细胞
二氢青蒿酸
生物转化
Artemisia annua L.
suspension culture cell
dihydroartemisinic acid
biotransformation
