Dunzendorfer U
Urol Int. 1982;37(5):349-57. doi: 10.1159/000280839.
The therapeutic concept of irreversible inhibition of both ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase (SAMDC) by alpha-difluoromethylornithine (DFMO) and methylglyoxal bis-guanylhydrazone (MGBG) is based on pathologic activities of these enzymes in tumor tissue. The polyamines putrescine, spermidine and spermine are measured in highest concentration in the prostate of both men and animals, with a significant increase of spermine in benign hyperplasia of the prostate. Patients with metastatic cancer of the prostate have elevated putrescine levels in the 24-hour urine. Treatment with 3 or 1% DFMO or 11 mg/kg MGBG in transplantable human and experimental cancer of the prostate demonstrated a significant anti-growth effect. A combination of DFMO and MGBG is tumor-destructive. The combination of 1% DFMO and 11 mg/kg MGBG distinctly reduces the activity of ODC and SAMDC and significantly lowers the levels of putrescine, spermidine and spermine in the tumor.
α-二氟甲基鸟氨酸（DFMO）和甲基乙二醛双脒腙（MGBG）对鸟氨酸脱羧酶（ODC）和S-腺苷甲硫氨酸脱羧酶（SAMDC）进行不可逆抑制的治疗理念，是基于这些酶在肿瘤组织中的病理活性。多胺腐胺、亚精胺和精胺在男性和动物前列腺中的浓度最高，前列腺良性增生时精胺显著增加。前列腺转移性癌患者24小时尿液中的腐胺水平升高。在可移植的人类前列腺癌和实验性前列腺癌中，用3%或1%的DFMO或11mg/kg的MGBG进行治疗显示出显著的抗生长作用。DFMO和MGBG联合使用具有肿瘤破坏作用。1%的DFMO和11mg/kg的MGBG联合使用可明显降低ODC和SAMDC的活性，并显著降低肿瘤中腐胺、亚精胺和精胺的水平。
