title: [Antitumor and antiproliferative action of the steroidal cytostatic antiestrogen cytestrol acetate on hormone-dependent tumor models].
abstract: Cytestrole acetate (CA), in the structure of which the steroidal antiestrogen component is associated with bis-β-cloroethylamino group, exhibits a strong cytotoxic activity against hormone-dependent cancer cell lines (CaOV, HeLa, MCF-7). In doxorubicin-resistant MCF-7 cells, CA potentiates the cytotoxic effect of etoposide and doxorubicin, and the IC50 for CA in these cells is 40 times lower than that for tamoxifen (TAM). In transplantable mice breast adenocarcinoma Ca-755, the therapeutic CA dose is 25 mg/kg when administered subcutaneously in oil solution for 5 days. On the DMBA-induced mammary tumors in rats, CA injected subcutaneously led to partial regressions 4 weeks after treatment in 75% of test rats, whereas TAM produced this effect in 43% of rats. Among various drug forms of CA, the most active were oil solution of CA in gelatin capsules for oral use and liposomal emulsion for intravenous administration, since these forms exhibited the highest values of Ca-755 tumor growth inhibition index (TGI = 97 - 98%).
authors.forename: z S
authors.initials: zS
authors.lastname: Smirnova
authors.forename: V M
authors.initials: VM
authors.lastname: Rzheznikov
authors.forename: V N
authors.initials: VN
authors.lastname: Tolkachev
authors.forename: L M
authors.initials: LM
authors.lastname: Borisova
authors.forename: M P
authors.initials: MP
authors.lastname: Kiseleva
authors.forename: A V
authors.initials: AV
authors.lastname: Semeĭkin
authors.forename: T A
authors.initials: TA
authors.lastname: Fedotcheva
authors.forename: K E
authors.initials: KE
authors.lastname: Shirokikh
authors.forename: V V
authors.initials: VV
authors.lastname: Banin
authors.forename: N L
authors.initials: NL
authors.lastname: Shimanovskiĭ
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000473:pathology; D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D054697:Cytostatic Agents / Q000494:pharmacology*; D004317:Doxorubicin / Q000494:pharmacology; D004334:Drug Administration Schedule; D004357:Drug Synergism; D004965:Estrogen Antagonists / Q000494:pharmacology*; D004997:Ethinyl Estradiol / Q000031:analogs & derivatives* / Q000494:pharmacology; D005047:Etoposide / Q000494:pharmacology; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D007279:Injections, Subcutaneous; D051379:Mice; D051381:Rats; D013629:Tamoxifen / Q000494:pharmacology; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D018931:Antineoplastic Agents, Hormonal; D054697:Cytostatic Agents; D004965:Estrogen Antagonists; C000600958:cytestrol acetate; D013629:Tamoxifen; D004997:Ethinyl Estradiol; D005047:Etoposide; D004317:Doxorubicin