Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla. Ciudad Universitaria, 72570 Puebla, Pue, México.
Eur J Med Chem. 2011 Sep;46(9):3877-86. doi: 10.1016/j.ejmech.2011.05.058. Epub 2011 May 30.
The synthesis and biological evaluation of the new cholestane glycoside (25R)-3β,16β-diacetoxy-22-oxocholest-5-en-26-yl β-d-glucopyranoside starting from diosgenin is described. This compound showed selective antiproliferative activity against CaSki, ViBo, and HeLa cervicouterine cancer cells. Its effect on the cell-cycle was determined. The cytotoxic effects of the title compound on cervicouterine cancer cell lines and human lymphocytes indicate that the main cell death process is not necrosis; hence it is not cytotoxic. The title compound induced apoptosis in cervicouterine cancer cells. Importantly, the antiproliferative activity on tumor cells did not affect the proliferative potential of peripheral blood lymphocytes. The title compound showed selective antitumor activity and greater antiproliferative activity than its aglycon, and therefore serves as a promising lead candidate for further optimization.
从薯蓣皂素出发，合成并对新型甾体糖苷（25R）-3β，16β-二乙酰氧基-22-氧代胆甾-5-烯-26-β-D-吡喃葡萄糖苷进行了生物评价。该化合物对 CaSki、ViBo 和 HeLa 宫颈癌细胞表现出选择性增殖抑制活性。测定了其对细胞周期的影响。标题化合物对宫颈癌细胞系和人淋巴细胞的细胞毒性作用表明，主要的细胞死亡过程不是坏死，因此它不是细胞毒性的。标题化合物诱导宫颈癌细胞凋亡。重要的是，该化合物对肿瘤细胞的增殖抑制活性不会影响外周血淋巴细胞的增殖潜力。该化合物表现出选择性抗肿瘤活性和比其糖苷配基更强的增殖抑制活性，因此是进一步优化的有前途的先导候选物。
