G. Schumacher et P. Neuhaus, The physiological estrogen metabolite 2-methoxyestradiol reduces tumor growth and induces apoptosis in human solid tumors, J CANC RES, 127(7), 2001, pp. 405-410
2-Methoxyestradiol (2-ME) is a physiological metabolite of estrogen, which
is excreted with the urine. In contrast to most estrogens, tumor growth-inh
ibiting effects were observed. Further studies have revealed that it may be
an effective anticancer compound for many tumor types. Several different m
echanisms have been attributed to 2-ME. Besides a strong antiangiogenic eff
ect on endothelial cells and tumors, there is a tubulin-inhibiting mechanis
m, causing cells to arrest in the G2/M phase of the cell cycle. In other tu
mors, p53-dependent and p53-independent mechanisms with induction of apopto
sis have been shown. The number of different tumors examined for a growth-i
nhibiting effect is increasing, and new mechanisms are continuously describ
ed. In vivo studies in mice, rats, and dogs show no or very little toxicity
, even at high doses. Here, we discuss the antitumor activity and their mec
hanisms. 2-ME appears to be a new anti-tumor compound with strong potential
for clinical application.