Gaspar A R, Potgieter D J, Vermeulen N M
Biochem Pharmacol. 1986 Feb 1;35(3):493-7. doi: 10.1016/0006-2952(86)90225-x.
The effect of sesquiterpene lactones isolated from Geigeria was tested on three glycolytic enzymes. Phosphofructokinase was inhibited irreversibly by all of the sesquiterpene lactones, with ivalin(III) giving the highest extent of inhibition. Values for the kinetic constants Ki (1.3 mM) and kp (2.2 min-1) were established. Hexokinase and glyceraldehyde-3-phosphate dehydrogenase were also strongly inhibited at 1 mM and 3 mM concentrations of sesquiterpene lactones, respectively. Pre-incubation of ivalin with dithiothreitol decreased its inhibiting effect on phosphofructokinase, hexokinase and glyceraldehyde-3-phosphate dehydrogenase activities. Phosphofructokinase and hexokinase were protected against inhibition by ivalin by their respective substrates, adenosine-5'-triphosphate and glucose.
对从盖氏菊属植物中分离出的倍半萜内酯对三种糖酵解酶的作用进行了测试。所有倍半萜内酯均不可逆地抑制磷酸果糖激酶，其中艾瓦林（III）的抑制程度最高。确定了动力学常数Ki（1.3 mM）和kp（2.2分钟-1）的值。己糖激酶和甘油醛-3-磷酸脱氢酶在倍半萜内酯浓度分别为1 mM和3 mM时也受到强烈抑制。艾瓦林与二硫苏糖醇预孵育会降低其对磷酸果糖激酶、己糖激酶和甘油醛-3-磷酸脱氢酶活性的抑制作用。磷酸果糖激酶和己糖激酶分别被其底物三磷酸腺苷和葡萄糖保护，免受艾瓦林的抑制。
