Luk G D, Sharkis S J, Abeloff M D, McCann P P, Sjoerdsma A, Baylin S B
Proc Natl Acad Sci U S A. 1983 Aug;80(16):5090-3. doi: 10.1073/pnas.80.16.5090.
The specific ornithine decarboxylase inhibitor alpha-difluoromethylornithine, when given to adult rats in vivo for 5 wk, resulted in a decrease in peripheral blood cell elements in normal rats and a marked suppression of marrow recovery in rats with chemotherapy-induced marrow hypoplasia. In normal rats, alpha-difluoromethylornithine resulted in a reduction of the leukocyte count to 73% of control, erythrocyte count to 61% of control, and platelet count to 24% of control. The bleeding time was increased to twice normal and 67% of the animals had epistaxis and 42% had melena. In rats treated with the S phase-specific chemotherapeutic agent 1-beta-D-arabinofuranosylcytosine, the simultaneous administration of alpha-difluoromethylornithine prevented the recovery of the bone marrow. The peripheral blood cell counts remained low--leukocyte count was 10% of control, and erythrocyte and platelet counts were 6% of control. All the animals developed epistaxis and melena and there was a 72% mortality. The administration of putrescine (4 mmol/kg, intraperitoneally, daily), the specific polyamine product of ornithine decarboxylase, reversed these hematologic effects in both normal and recovering marrow and resulted in rapid clinical improvement. Thus, the maintenance of normal, adult rat hematologic parameters, as with the proliferation of neoplastic and transformed cells in culture, is critically dependent on continued polyamine biosynthesis.
特异性鸟氨酸脱羧酶抑制剂α-二氟甲基鸟氨酸,在成年大鼠体内连续给药5周后,导致正常大鼠外周血细胞成分减少,并且显著抑制了化疗诱导的骨髓发育不全大鼠的骨髓恢复。在正常大鼠中,α-二氟甲基鸟氨酸使白细胞计数降至对照的73%,红细胞计数降至对照的61%,血小板计数降至对照的24%。出血时间增加至正常的两倍,67%的动物出现鼻出血,42%的动物出现黑便。在用S期特异性化疗药物1-β-D-阿拉伯呋喃糖基胞嘧啶治疗的大鼠中,同时给予α-二氟甲基鸟氨酸可阻止骨髓恢复。外周血细胞计数仍然很低——白细胞计数为对照的10%,红细胞和血小板计数为对照的6%。所有动物均出现鼻出血和黑便,死亡率为72%。给予腐胺(4 mmol/kg,腹腔内注射,每日),鸟氨酸脱羧酶的特异性多胺产物,可逆转正常和恢复中的骨髓中的这些血液学效应,并导致临床快速改善。因此,与培养中的肿瘤细胞和转化细胞增殖一样,成年大鼠血液学参数的维持严重依赖于持续的多胺生物合成。