Endo A, Kitahara N
J Antibiot (Tokyo). 1981 Oct;34(10):1351-4. doi: 10.7164/antibiotics.34.1351.
Hydroxybenzoic and phthalic acids and their related compounds were tested for inhibitory activity to brain glutamate decarboxylase. Of mono-, di-, and trihydroxybenzoic acids, gallic acid was the most inhibitory, giving 50% inhibition at a concentration of 0.17 mM. Dihydroxybenzoic acids were less inhibitory than the trihydroxyacids but more than monohydroxybenzoic acids. Of the phthalic acid-related compounds tested, 4,5-dihydroxyisophthalic acid was the most potent inhibitor, producing 50% inhibition at 0.61 microM. The inhibition of these compounds was competitive with respect to L-glutamate. The Ki values were 0.02, 1.2 and 4.9 microM for 4,5-dihydroxyisophthalic acid, 5-hydroxyisophthalic acid and gallic acid, respectively. When administered intraventricularly to mice, 4,5-dihydroxyisophthalic acid produced a significant decrease in the gamma-aminobutyric acid content of the brain, resulting in induction of convulsions.
对羟基苯甲酸和邻苯二甲酸及其相关化合物进行了对脑谷氨酸脱羧酶抑制活性的测试。在单羟基、二羟基和三羟基苯甲酸中，没食子酸的抑制作用最强，在浓度为0.17 mM时产生50%的抑制率。二羟基苯甲酸的抑制作用比三羟基苯甲酸弱，但比单羟基苯甲酸强。在所测试的邻苯二甲酸相关化合物中，4,5-二羟基间苯二甲酸是最有效的抑制剂，在0.61 microM时产生50%的抑制率。这些化合物的抑制作用对L-谷氨酸具有竞争性。4,5-二羟基间苯二甲酸、5-羟基间苯二甲酸和没食子酸的Ki值分别为0.02、1.2和4.9 microM。当向小鼠脑室内注射4,5-二羟基间苯二甲酸时，可使脑中γ-氨基丁酸含量显著降低，从而诱发惊厥。
