[Antitumor activity of the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one].
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.
Sergeev
P V
PV
Semeĭkin
A V
AV
Smirnova
Z S
ZS
Rzheznikov
V M
VM
Grinenko
G S
GS
Fedosov
A V
AV
Fedotcheva
T A
TA
Shimanovskiĭ
N L
NL
D019326:17-alpha-Hydroxyprogesterone / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy*; D002277:Carcinoma / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D006801:Humans; D017258:Medroxyprogesterone Acetate / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D008808:Mice, Inbred CBA; D011372:Progestins / Q000494:pharmacology / Q000627:therapeutic use; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy*
C498329:17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one; D000970:Antineoplastic Agents; D011372:Progestins; D019326:17-alpha-Hydroxyprogesterone; D017258:Medroxyprogesterone Acetate