关于抗肿瘤药物的研究  Ⅷ.N-甲酰溶肉瘤素酰苯丙氨酸乙酯(FSPA)对动物肿瘤的影响

STUDIES ON ANTITUMOR DRUGS VIII. THE ANTITUMOR EFFECT OF THE ETHYL ESTER OF N-FORMYL-SARCOLYSIN-PHENYLALANINE ON EXPERIMENTAL TUMORS

摘要: N-甲酰溶肉瘤素酰苯丙氨酸乙酯(FSPA)对动物肿瘤影响的实驗,得到如下的結果:FSPA 100—200毫克/公斤/日能显著的抑制大自鼠吉田腹水肉瘤的生长.FSPA一次腹腔注射,观察二天的LD₅₀为4.5克/公斤.FSPA 100毫克/公斤/日連續14天对猴无明显毒性;200毫克/公斤/日,則对末稍血液中的白血細胞有抑制作用.

Abstract: The ethyl ester of N-formyl-sarcolycine-phenylalanine (FSPA) was synthetized in this institute. At a daily dosage of 100-200 mg/kg FSPA markedly inhibited the growth of Yoshida ascites sarcoma. The intraperitoneal LD₅₀ for mice was 4.5 gm/kg. When the drug was administered orally to normal monkeys at 100 mg/kg daily for 14 days, no change in blood picture or impairment of liver and kidney functions was noted. However, at 200 mg/kg FSPA showed definite inhibitory effect on the bone marrow. This compound has been recommended for clinical trial.