Kwon B M, Lee S H, Choi S U, Park S H, Lee C O, Cho Y K, Sung N D, Bok S H
Korea Research Institute of Bioscience & Biotechnology, Taejon, Korea.
Arch Pharm Res. 1998 Apr;21(2):147-52. doi: 10.1007/BF02974019.
Cinnamaldehydes and related compounds were synthesized from various cinnamic acids based on the 2'-hydroxycinnamaldehyde isolated from the bark of Cinnamomum cassia Blume. The cytotoxicity to human solid tumor cells such as A549, SK-OV-3, SK-MEL-2, XF498 and HCT15 were measured. Cinnamic acid, cinnamates and cinnamyl alcohols did not show any cytotoxicity against the human tumor cells. Cinnamaldehydes and related compounds were resistant to A549 cell line up to 15 micrograms/ml. In contrast, HCT15 and SK-MEL-2 cells were much sensitive to these cinnamaldehyde analogues which showed ED50 values 0.63-8.1 micrograms/ml. Cytotoxicity of the saturated aldehydes was much weak compared to their unsaturated aldehydes. From these studies, it was found that the key functional group of the cinnamaldehyde-related compounds in the antitumor activity is the propenal group.
基于从肉桂树皮中分离出的2'-羟基肉桂醛，由各种肉桂酸合成了肉桂醛及其相关化合物。测定了它们对人实体瘤细胞如A549、SK-OV-3、SK-MEL-2、XF498和HCT15的细胞毒性。肉桂酸、肉桂酸酯和肉桂醇对人肿瘤细胞没有显示出任何细胞毒性。肉桂醛及其相关化合物对A549细胞系的抗性高达15微克/毫升。相比之下，HCT15和SK-MEL-2细胞对这些肉桂醛类似物更为敏感，其半数有效剂量（ED50）值为0.63 - 8.1微克/毫升。与不饱和醛相比，饱和醛的细胞毒性要弱得多。从这些研究中发现，肉桂醛相关化合物在抗肿瘤活性中的关键官能团是丙烯醛基团。
