PhD Degree Program in Environmental Science, Environmental Science Research Center, Faculty of Science, Chiang Mai University, Chiang Mai, Thailand.
Department of Pharmaceutical Chemistry and Pharmacognosy, Naresuan University, Phitsanulok, Thailand.
Artif Cells Nanomed Biotechnol. 2021 Dec;49(1):166-172. doi: 10.1080/21691401.2021.1883044.
Biotransformations of stemofoline (), (2')-hydroxystemofoline (), (11)-1',2'-didehydrostemofoline () and stemocurtisine () were studied through fermentation with TISTR 3370. Three new stemofoline derivatives; 6 -hydroxystemofoline (), (2', 6 )-dihydroxystemofoline () and (11,6)-1',2'-didehydro-6-hydroxystemofoline (), together with the known compound 1',2'-didehydrostemofoline--oxide (), were produced by C-hydroxylation and N-oxidation reactions. Stemocurtisine was not biotransformed under these conditions. The transformed product was four times more potent (IC = 11.01 ± 1.49 µM) than its precursor (IC = 45.1 ± 5.46 µM) as an inhibitor against acetylcholinesterase.
通过利用 TISTR 3370 进行发酵，研究了蛇根叶碱（）、（2′）-羟基蛇根叶碱（）、（11）-1′，2′-去氢蛇根叶碱（）和斯蒂莫考灵（）的生物转化。通过 C-羟化和 N-氧化反应，生成了三种新的蛇根叶碱衍生物；6-羟基蛇根叶碱（）、（2′，6′）-二羟基蛇根叶碱（）和（11，6）-1′，2′-去氢-6-羟基蛇根叶碱（），以及已知化合物 1′，2′-去氢蛇根叶碱--氧化物（）。在这些条件下，斯蒂莫考灵没有发生生物转化。转化产物（）作为乙酰胆碱酯酶抑制剂的活性比其前体（）强四倍（IC = 11.01 ± 1.49 μM）（IC = 45.1 ± 5.46 μM）。
