Amity Institute of Biotechnology, Amity University, Sector 125, Noida 201303, UP, India.
Eur J Med Chem. 2013 Feb;60:490-6. doi: 10.1016/j.ejmech.2012.12.017. Epub 2012 Dec 17.
Chemical investigation of stem bark of Crataeva nurvala afforded 5,7-dimethoxy-3-phenyl-1-ethyl-1,4-dihydro-4-quinolone and a steroidal glycoside with unprecedented pentacyclic ring system named crataemine (1a) and crataenoside (2) respectively. The structures of the compounds were determined by spectroscopic analysis. A series of compounds with modification at position 1 of 1a (1a-1c) were prepared. All compounds were screened for cytotoxic activity against HeLa, PC-3 and MCF-7 cells. Only 1a and 2 showed potency against all three cells. Mechanism based study for activity of the compounds demonstrated that it could block the migration of more aggressive HeLa and PC-3 cells and prevent their colony formation ability as well. The compounds potentiated apoptosis in HeLa and PC-3 cells in a significant manner.
对 Crataeva nurvala 的茎皮进行化学研究，得到了 5,7-二甲氧基-3-苯基-1-乙基-1,4-二氢-4-喹啉酮和一种甾体糖苷，分别命名为 crataemine (1a) 和 crataenoside (2)。通过光谱分析确定了化合物的结构。还制备了一系列在 1a 的 1 位修饰的化合物 (1a-1c)。所有化合物均针对 HeLa、PC-3 和 MCF-7 细胞进行了细胞毒性筛选。只有 1a 和 2 对所有三种细胞均具有活性。基于机制的研究表明，化合物可以阻止侵袭性更强的 HeLa 和 PC-3 细胞的迁移，并防止它们的集落形成能力。该化合物能显著促进 HeLa 和 PC-3 细胞的凋亡。
