Antitumor and antimetastatic effects of betulonic acid amides in mice with transplantable lewis carcinoma.
We studied the effects of four synthetic amides of betulonic acid containing amino acid fragments (d,l-alpha-alanine, beta-alanine, and their methyl esters) on the rate of growth and metastatic dissemination of transplantable Lewis lung carcinoma in C57Bl/6 mice. The test compounds were administered intragastrically in a single dose of 500 mg/kg. 3-[-oxo-20(29)-lupen-28-oilamino]-propionic acid suppressed primary tumor growth (by 26%) and decreased the number of lung metastases (by more than 2 times). Antitumor and antimetastatic activity of triterpenoids decreased after methylation of the amino acid fragment in betulonic acid.
Sorokina
I V
IV
Laboratory of Pharmacological Studies, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Division of the Russian Academy of Sciences. sorokina@nioch.nsc.ru
Tolstikova
T G
TG
Zhukova
N A
NA
Petrenko
N I
NI
Uzenkova
N V
NV
Shul'ts
E E
EE
Popova
N A
NA
D000409:Alanine / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D009362:Neoplasm Metastasis / Q000473:pathology / Q000517:prevention & control*; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use; D000094062:Betulinic Acid
D000409:Alanine; D000970:Antineoplastic Agents; D009828:Oleanolic Acid; C508784:(3-oxo-20(29)-lupene-28-oyl)-3-aminopropionamide; D000094062:Betulinic Acid