4-羟基吡唑对离体大鼠肝细胞中色氨酸和甲酸代谢的影响。

Cook J S, Pogson C I

Biochem J. 1982 Apr 15;204(1):307-12. doi: 10.1042/bj2040307.

4-Hydroxypyrazole inhibits flux through tryptophan 2.3-dioxygenase in cells. The inhibition is apparently non-competitive with Ki = 0.15 mM. 2. Hydroxypyrazole inhibits the oxidation of formate to CO2 in liver cells. 3. Glycollate, which generates H2O2, stimulates formate oxidation. This process is inhibited by 4-hydroxypyrazole. 4. Methionine stimulates formate oxidation in cells and this stimulation is insensitive to 4-hydroxypyrazole. 5. It is concluded that, in freshly isolated liver cells, formate oxidation proceeds by a pathway involving catalase. In vivo, or when methionine is added to cell incubations, the pathway of oxidation involves tetrahydrofolate, and is insensitive to catalase inhibitors. 6. Methionine at physiological concentrations inhibits the activity of tryptophan 2,3-dioxygenase in isolated liver cells.

4-羟基吡唑抑制细胞中色氨酸2,3-双加氧酶的通量。这种抑制作用明显是非竞争性的，抑制常数（Ki）为0.15 mM。2. 羟基吡唑抑制肝细胞中甲酸氧化为二氧化碳。3. 产生过氧化氢的乙醇酸刺激甲酸氧化。这一过程受到4-羟基吡唑的抑制。4. 蛋氨酸刺激细胞中的甲酸氧化，且这种刺激对4-羟基吡唑不敏感。5. 得出的结论是，在新鲜分离的肝细胞中，甲酸氧化通过一条涉及过氧化氢酶的途径进行。在体内，或者当向细胞培养液中添加蛋氨酸时，氧化途径涉及四氢叶酸，并且对过氧化氢酶抑制剂不敏感。6. 生理浓度的蛋氨酸抑制分离的肝细胞中色氨酸2,3-双加氧酶的活性。

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核心技术专利：CN118964589B侵权必究

Cook J S, Pogson C I

Biochem J. 1982 Apr 15;204(1):307-12. doi: 10.1042/bj2040307.

4-Hydroxypyrazole inhibits flux through tryptophan 2.3-dioxygenase in cells. The inhibition is apparently non-competitive with Ki = 0.15 mM. 2. Hydroxypyrazole inhibits the oxidation of formate to CO2 in liver cells. 3. Glycollate, which generates H2O2, stimulates formate oxidation. This process is inhibited by 4-hydroxypyrazole. 4. Methionine stimulates formate oxidation in cells and this stimulation is insensitive to 4-hydroxypyrazole. 5. It is concluded that, in freshly isolated liver cells, formate oxidation proceeds by a pathway involving catalase. In vivo, or when methionine is added to cell incubations, the pathway of oxidation involves tetrahydrofolate, and is insensitive to catalase inhibitors. 6. Methionine at physiological concentrations inhibits the activity of tryptophan 2,3-dioxygenase in isolated liver cells.

4-羟基吡唑抑制细胞中色氨酸2,3-双加氧酶的通量。这种抑制作用明显是非竞争性的，抑制常数（Ki）为0.15 mM。2. 羟基吡唑抑制肝细胞中甲酸氧化为二氧化碳。3. 产生过氧化氢的乙醇酸刺激甲酸氧化。这一过程受到4-羟基吡唑的抑制。4. 蛋氨酸刺激细胞中的甲酸氧化，且这种刺激对4-羟基吡唑不敏感。5. 得出的结论是，在新鲜分离的肝细胞中，甲酸氧化通过一条涉及过氧化氢酶的途径进行。在体内，或者当向细胞培养液中添加蛋氨酸时，氧化途径涉及四氢叶酸，并且对过氧化氢酶抑制剂不敏感。6. 生理浓度的蛋氨酸抑制分离的肝细胞中色氨酸2,3-双加氧酶的活性。