Baek N I, Choi S Y, Park J K, Cho S W, Ahn E M, Jeon S G, Lee B R, Bahn J H, Kim Y K, Shon I H
Department of Life Sciences, Kyunghee University, Suwon, Korea.
Arch Pharm Res. 1999 Apr;22(2):219-24. doi: 10.1007/BF02976550.
In our search for the anticonvulsant constituent of Gastrodia elata repeated column chromatographies guided by activity assay led to isolation of an active compound, which was identified as gastrodin on the basis of spectral data. Brain succinic semialdehyde dehydrogenase (SSADH) was inactivated by preincubation with gastrodin in a time-dependent manner and the reaction was monitored by absorption and fluorescence spectroscopic methods. The inactivation followed pseudo-first-order kinetics with the second-rate order constant of 1.2 x 10(3) M-1min-1. The time course of the reaction was significantly affected by the coenzyme NAD+, which affected complete protection against the loss of the catalytic activity, whereas substrate succinic semialdehyde failed to prevent the inactivation of the enzyme. It is postulated that the gastrodin is able to elevate the neurotransmitter GABA levels in central nervous system by inhibitory action on one of the GABA degradative enzymes, SSADH.
在我们对天麻抗惊厥成分的研究中,以活性测定为导向的反复柱色谱法分离出了一种活性化合物,根据光谱数据鉴定其为天麻素。脑琥珀酸半醛脱氢酶(SSADH)与天麻素预孵育后会以时间依赖性方式失活,该反应通过吸收光谱法和荧光光谱法进行监测。失活遵循假一级动力学,二级速率常数为1.2×10³ M⁻¹min⁻¹。反应进程受到辅酶NAD⁺的显著影响,NAD⁺能完全保护酶的催化活性不丧失,而底物琥珀酸半醛无法阻止酶的失活。据推测,天麻素能够通过抑制γ-氨基丁酸(GABA)降解酶之一SSADH的活性,提高中枢神经系统中神经递质GABA的水平。