Ovejera A A, Houchens D P, Catane R, Sheridan M A, Muggia F M
Cancer Res. 1979 Aug;39(8):3220-4.
The chemotherapeutic effects of 6-diazo-5-oxo-L-norleucine (DON) and N-[N-gamma-glutamyl-6-diazo-5-oxo-norleucinyl]6-diazo-5-oxo-norleucine (azotomycin) were evaluated in a spectrum of transplantable experimental tumor systems including xenografts of human tumors in athymic mice. Both drugs displayed remarkable activity against the murine leukemia L1210 and P388, the Colon Tumors C26 and C38 and the CD8F1 mammary tumor. No significant activity was observed against Lewis lung carcinoma, B16 carcinoma, B16 melanoma, and intracranial ependymoblastoma. DON and azotomycin also exhibited striking inhibitory effects on the growth of s.c. human tumor (MX-1 mammary, LX-1 lung and CX-1 and CX-2 colon) xenografts in athymic mice. With the exception of one colon xenograft (CX-1), all tumor lines were markedly responsive to both drugs. Tumor regressions below the initial tumor sizes of 100 to 300 mg, albeit temporary, were brought about by one course of treatment every 4 days for 3 doses (at optimal dose) with either drug. Although these drugs have been tested previously in the clinic and have shown only limited therapeutic effectiveness, they seem to worthy of a second and closer look in light of the recent laboratory results.
在一系列可移植的实验肿瘤系统中，包括无胸腺小鼠体内的人肿瘤异种移植模型，评估了6-重氮-5-氧代-L-正亮氨酸（DON）和N-[N-γ-谷氨酰-6-重氮-5-氧代正亮氨酰基]6-重氮-5-氧代正亮氨酸（偶氮丝氨酸）的化疗效果。这两种药物对小鼠白血病L1210和P388、结肠癌C26和C38以及CD8F1乳腺肿瘤均表现出显著活性。对Lewis肺癌、B16癌、B16黑色素瘤和颅内室管膜母细胞瘤未观察到明显活性。DON和偶氮丝氨酸对无胸腺小鼠体内皮下接种的人肿瘤（MX-1乳腺、LX-1肺以及CX-1和CX-2结肠）异种移植瘤的生长也表现出显著抑制作用。除一种结肠异种移植瘤（CX-1）外，所有肿瘤细胞系对这两种药物均有明显反应。两种药物每4天给药1个疗程，共3剂（最佳剂量），可使肿瘤缩小至初始肿瘤大小100至300 mg以下，尽管这种缩小是暂时的。尽管这些药物此前已在临床上进行过测试，且仅显示出有限的治疗效果，但鉴于最近的实验室结果，它们似乎值得再次进行更深入的研究。
