Oleanolic and ursolic acids were used as lead compounds to synthesize a series of pentacyclic triterpenoid derivatives bearing ethylenediamine, butanediamine, or hexanediamine groups at the C-3 position. The potential antiproliferative activity of these compounds was examined in A549 (human non-small cell lung cancer cells), MCF-7 (human breast cancer cells), and HeLa (human cervical carcinoma cells) cells. Methyl 3β-O-[4-(2-aminoethylamino)-4-oxo-butyryl]olean-12-ene-28-oate (DABO-Me) was identified as a promising antiproliferative agent in vitro and in vivo. DABO-Me strongly suppressed the proliferation of A549, MCF-7, and HeLa cells (IC₅₀ = 4–7 µM). In MCF-7 cells, DABO-Me upregulated the pro-apoptotic protein Bax, downregulated the anti-apoptotic protein Bcl-2, promoted the release of cytochrome c, and activated caspase-3/9. Transwell and flow cytometry assays showed that DABO-Me inhibited MCF-7 cell proliferation, migration, and invasion, and induced apoptosis and S phase arrest. In vitro and in vivo experiments indicated that DABO-Me inhibited MCF-7 cell proliferation and suppressed tumor growth. Taken together, these results indicate that DABO-Me could be developed as an effective antitumor drug.

齐墩果酸和熊果酸被用作先导化合物，以合成一系列在C-3位带有乙二胺，丁二胺或己二胺基团的五环三萜衍生物。在A549（人类非小细胞肺癌细胞），MCF-7（人类乳腺癌细胞）和HeLa（人类宫颈癌细胞）细胞中检查了这些化合物的潜在抗增殖活性。甲基3β- ö - [4-（2-氨基乙基氨基）-4-氧代-丁酰基]齐墩果-12-烯-28 -酸酯（DABO-Me）中被鉴定为有希望的抗增殖剂在体外和体内。DABO-Me强烈抑制A549，MCF-7和HeLa细胞的增殖（IC ₅₀ = 4–7 µM）。在MCF-7细胞中，DABO-Me上调凋亡原蛋白Bax，下调抗凋亡蛋白Bcl-2，促进细胞色素c的释放，并激活caspase-3 / 9。Transwell和流式细胞仪检测表明DABO-Me抑制MCF-7细胞的增殖，迁移和侵袭，并诱导凋亡和S期阻滞。体外和体内实验表明，DABO-Me抑制MCF-7细胞增殖并抑制肿瘤生长。综上所述，这些结果表明DABO-Me可以被开发为有效的抗肿瘤药。