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.

以齐墩果酸和熊果酸为先导化合物，合成了一系列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（人非小细胞肺癌细胞）、MCF-7（人乳腺癌细胞）和 HeLa（人宫颈癌细胞）细胞中检查了这些化合物的潜在抗增殖活性。 3β- O- [4-(2-氨基乙基氨基)-4-氧代丁酰]齐墩果-12-烯-28-oate (DABO-Me) 被认为是一种有前途的体外和体内抗增殖剂。 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上调促凋亡蛋白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 和流式细胞术检测表明 DABO-Me 抑制 MCF-7 细胞增殖、迁移和侵袭，并诱导细胞凋亡和 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 可以开发为一种有效的抗肿瘤药物。