Laboratory of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology, Guangzhou, China.
Eur J Med Chem. 2012 Jul;53:235-45. doi: 10.1016/j.ejmech.2012.04.005. Epub 2012 Apr 16.
Sixty-one curcumin-related compounds were synthesized and evaluated for their anticancer activity toward cultured prostate cancer PC-3 cells, pancreas cancer Panc-1 cells and colon cancer HT-29 cells. Inhibitory effects of these compounds on the growth of PC-3, Panc-1 and HT-29 cells were determined by the MTT assay. Compounds E10, F10, FN1 and FN2 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, Panc-1 and HT-29 cells. The IC(50) for these compounds was lower than 1 μM in all three cell lines. E10 was 72-, 46- and 117-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. F10 was 69-, 34- and 72-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. FN1 and FN2 had about the same inhibitory effect as E10 and F10 toward Panc-1 cells but were less active than E10 and F10 toward PC-3 and HT-29 cells. The active compounds were potent stimulators of apoptosis. The present study indicates that E10, F10, FN1 and FN2 may have useful anticancer activity.
合成了 61 种姜黄素相关化合物，并对其在培养的前列腺癌 PC-3 细胞、胰腺癌 Panc-1 细胞和结肠癌 HT-29 细胞中的抗癌活性进行了评价。采用 MTT 法测定这些化合物对 PC-3、Panc-1 和 HT-29 细胞生长的抑制作用。化合物 E10、F10、FN1 和 FN2 对培养的 PC-3、Panc-1 和 HT-29 细胞的生长表现出异常强的抑制作用。这些化合物在所有三种细胞系中的 IC50 均低于 1 μM。E10 对 PC-3、Panc-1 和 HT-29 细胞生长的抑制活性分别比姜黄素高 72 倍、46 倍和 117 倍。F10 对 PC-3、Panc-1 和 HT-29 细胞生长的抑制活性分别比姜黄素高 69 倍、34 倍和 72 倍。FN1 和 FN2 对 Panc-1 细胞的抑制作用与 E10 和 F10 相似，但对 PC-3 和 HT-29 细胞的活性低于 E10 和 F10。活性化合物是凋亡的有效刺激物。本研究表明，E10、F10、FN1 和 FN2 可能具有有用的抗癌活性。
