Influence of estrogen cytostatics on activity of plasma membrane enzymes 5'-nucleotidase and N+-K+-ATPase.
We studied the effect of four conjugated synthetic derivatives of estrone and ethynylestradiol and bis-beta-chloroethylamine-containing substance on activity of plasma membrane enzymes 5'-nucleotidase and N+-K+-ATPase. As differentiated from precursors, estrogen cytostatics decreased activity of plasma membrane enzymes. Reference preparations chlorophenacyl and estradiol had little effect on activity of 5'-nucleotidase and N+-K+-ATPase. These data suggest that damage to plasma membrane enzymes is related to the effect of estrogen cytostatic molecules. Test compounds produced an antiproliferative effect on estrogen-independent tumor cells, which strongly correlated with a decrease in activity of plasma membrane enzymes 5'-nucleotidase and N+-K+-ATPase. The derivative of ethynylestradiol with the cytostatic residue in the 3-position of the steroid nucleus (Po-714-11alpha) most significantly modulated enzyme activity.
Mayatskaya
E E
EE
Research Center for Endocrinology, Russian Academy of Medical Sciences, Moscow.
Semeikin
A V
AV
Rzheznikov
V M
VM
Shimanovskii
N L
NL
D015720:5'-Nucleotidase / Q000187:drug effects*; D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000737:chemistry / Q000633:toxicity*; D002455:Cell Division / Q000187:drug effects; D002462:Cell Membrane / Q000201:enzymology*; D004967:Estrogens / Q000633:toxicity*; D004970:Estrone / Q000737:chemistry / Q000633:toxicity; D004997:Ethinyl Estradiol / Q000737:chemistry / Q000633:toxicity; D005021:Ethylamines / Q000737:chemistry / Q000633:toxicity; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D009368:Neoplasm Transplantation; D051381:Rats; D012509:Sarcoma / Q000188:drug therapy; D012878:Skin Neoplasms / Q000188:drug therapy; D000254:Sodium-Potassium-Exchanging ATPase / Q000187:drug effects*
D018931:Antineoplastic Agents, Hormonal; D004967:Estrogens; D005021:Ethylamines; D004970:Estrone; D004997:Ethinyl Estradiol; D015720:5'-Nucleotidase; D000254:Sodium-Potassium-Exchanging ATPase