Liu Dan, Song Dandan, Guo Gang, Wang Rui, Lv Jinling, Jing Yongkui, Zhao Linxiang
Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Bioorg Med Chem. 2007 Aug 15;15(16):5432-9. doi: 10.1016/j.bmc.2007.05.057. Epub 2007 May 26.
18beta-Glycyrrhetinic acid (GA), 3beta-hydroxyl-11-oxo-olean-12-ene-29-oic acid, has been found to inhibit growth and to induce apoptosis in cancer cells. Through structural modification, 16 GA derivatives (12 novel compounds) with modified structures at the C(3) and C(29) positions were synthesized. The antiproliferative effects and apoptosis induction abilities of these compounds were determined in human leukemia HL-60 cells. The replacement of the hydroxyl group of GA with a carbonyl group or an oxime group at C(3) position does not influence the antiproliferative effect. However, the antiproliferative and apoptosis induction abilities of the compounds with a replaced alkoxyimino group at position C(3) and a free C(29) carboxyl group are markedly increased.
18β-甘草次酸（GA），即3β-羟基-11-氧代-齐墩果-12-烯-29-酸，已被发现可抑制癌细胞生长并诱导其凋亡。通过结构修饰，合成了16种在C(3)和C(29)位具有结构修饰的GA衍生物（12种新化合物）。测定了这些化合物对人白血病HL-60细胞的抗增殖作用和凋亡诱导能力。在C(3)位将GA的羟基用羰基或肟基取代不影响抗增殖作用。然而，在C(3)位具有取代烷氧基亚氨基且C(29)羧基游离的化合物的抗增殖和凋亡诱导能力显著增强。
