[Antitumor activity of the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one].

Abstract

Antitumor activity of a new highly active promising gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one (butagest) was studied in mice with model cervical carcinoma (RShM-5). The reference drug was medroxyprogesteron acetate (MPA, Depo Provera) used in clinics. The new preparation introduced perorally in a dose of 1 mg per mice inhibited the model tumor growth by 73%, which was 18% (p < 0.01) more effective than the action of the reference drug MPA. The effect of the new gestagen was also studied in vitro with respect to human breast carcinoma of the MCF-7 line and human cervical carcinoma HeLa. The viability of the tumor cells was studied during a 6-day incubation with the drug at a concentration of 10(-7)-10(-5) M (MTT test). The reference compounds were progesterone and MPA. These drugs suppressed the growth of both MCF-7 and, in higher concentrations, of HeLa. Butagest inhibited the growth of HeLa in all concentrations. Thus, the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one is capable of suppressing the viability of human breast carcinoma and human cervical carcinoma, being comparable or even more effective than the reference drugs.

• Authors: P V Sergeev, A V Semeĭkin, Z S Smirnova, V M Rzheznikov, G S Grinenko, A V Fedosov, T A Fedotcheva, N L Shimanovskiĭ
• Journal: Eksperimental'naia i klinicheskaia farmakologiia (Eksp Klin Farmakol) 2004 Jul-Aug Vol. 67 Issue 4 Pg. 54-6 ISSN: 0869-2092 [Print] Russia (Federation)
• Vernacular Title: Izuchenie protivoopukholevoĭ aktivnosti novogo gestagena 17 al'fa-atsetoksi-3 beta-butanoiloksi-6-metil-pregna-4,6-dien-20-ona.
• PMID: 15500049 (Publication Type: English Abstract, Journal Article)

Chemical References

• 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one
• Antineoplastic Agents
• Progestins
• 17-alpha-Hydroxyprogesterone
• Medroxyprogesterone Acetate

Topics

• 17-alpha-Hydroxyprogesterone (analogs & derivatives, pharmacology, therapeutic use)
• Animals
• Antineoplastic Agents (pharmacology, therapeutic use)
• Breast Neoplasms (drug therapy)
• Carcinoma (drug therapy)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Female
• Humans
• Medroxyprogesterone Acetate (pharmacology, therapeutic use)
• Mice
• Mice, Inbred CBA
• Progestins (pharmacology, therapeutic use)
• Uterine Cervical Neoplasms (drug therapy)