Sorokina I V, Tolstikova T G, Zhukova N A, Petrenko N I, Uzenkova N V, Shul'ts E E, Popova N A
Laboratory of Pharmacological Studies, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Division of the Russian Academy of Sciences.
Bull Exp Biol Med. 2006 Jul;142(1):69-72. doi: 10.1007/s10517-006-0294-x.
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.
我们研究了四种含有氨基酸片段（d，l-α-丙氨酸、β-丙氨酸及其甲酯）的桦木酸合成酰胺对C57Bl/6小鼠移植性Lewis肺癌生长速率和转移扩散的影响。受试化合物以500 mg/kg的单次剂量灌胃给药。3-[-氧代-20(29)-羽扇豆-28-油酰胺基]-丙酸抑制原发性肿瘤生长（抑制率为26%）并减少肺转移瘤数量（减少超过2倍）。桦木酸中氨基酸片段甲基化后，三萜类化合物的抗肿瘤和抗转移活性降低。
