Sergeev A V
Vopr Med Khim. 1977 Sep-Oct;23(5):601-6.
Inhibition of serine-hydroxymethyl transferase activity by dimer of cycloserine--diketopiperazin (DP) was studied in vivo in mice liver tissue. DP (2500 mg and 4000 mg per kg of body weight) caused a decrease in the enzyme activity by 14% and 30%, respectively, within 2 hrs after intraperitoneal administration into the animals. Complete reactivation of the enzyme was observed in presence of pyridoxal phosphate added into the experimental samples. DP inhibited the rate of mice liver regeneration after partial hepatectomy, if it was administered separately or in combination with methotrexate within 8 days before and 4 days after the operation. The decreased rate of the tissue regeneration occurred simultaneously with a distinct decrease in the serine-hydroxymethyl transferase activity in vivo. Methotrexate did not affect the liver tissue regeneration after hepatectomy. A method is described for estimation of the serine-hydroxymethyl transferase activity in tissue extracts in presence of partially purified preparation of 5,10-methylene-H4-folate-dehydrogenase.
在小鼠肝脏组织中对环丝氨酸-二酮哌嗪（DP）二聚体对丝氨酸羟甲基转移酶活性的抑制作用进行了体内研究。给动物腹腔注射DP（每千克体重2500毫克和4000毫克）后2小时内，酶活性分别降低了14%和30%。在实验样品中添加磷酸吡哆醛后观察到酶完全重新激活。如果在手术前8天和手术后4天单独给予DP或与甲氨蝶呤联合给予，DP会抑制部分肝切除术后小鼠肝脏的再生率。组织再生率降低与体内丝氨酸羟甲基转移酶活性明显降低同时发生。甲氨蝶呤不影响肝切除术后的肝脏组织再生。描述了一种在存在部分纯化的5,10-亚甲基-H4-叶酸脱氢酶制剂的情况下估计组织提取物中丝氨酸羟甲基转移酶活性的方法。
