Bygbjerg I C
Eur J Clin Pharmacol. 1985;28(3):287-90. doi: 10.1007/BF00543325.
The in vitro effect of proguanil and its active metabolite cycloguanil on proliferating human blood mononuclear cells was studied. Proguanil had no effect on 14C-thymidine incorporation or on the number of cells. Cycloguanil, in concentrations corresponding to the plasma levels found in clinical practice, blocked the endogenous synthesis of thymidine and decreased the number of mitogen- and antigen-stimulated cells. The effect on phytohaemagglutinin-stimulated cells was transient. Higher concentrations of cycloguanil, corresponding to intralymphocytic levels in clinical practice, permanently suppressed the growth of lymphocytes. The effect of cycloguanil could be reversed by low doses of folinic acid and high doses of folic acid.
研究了氯胍及其活性代谢产物环氯胍对人血单核细胞增殖的体外作用。氯胍对14C-胸腺嘧啶核苷掺入或细胞数量均无影响。环氯胍在临床实际中发现的血浆浓度下,可阻断胸腺嘧啶核苷的内源性合成,并减少有丝分裂原和抗原刺激细胞的数量。对植物血凝素刺激细胞的作用是短暂的。在临床实际中相当于淋巴细胞内浓度的较高剂量环氯胍可永久性抑制淋巴细胞生长。低剂量亚叶酸和高剂量叶酸可逆转环氯胍的作用。