Keum Young Sam, Kim Jin, Lee Keun Hyung, Park Kwang Kyun, Surh Young Joon, Lee Jong Min, Lee Sang Sup, Yoon Jung Hoon, Joo So Yeon, Cha In Ho, Yook Jong In
Oral Cancer Research Institute, Department of Oral Pathology and Oral Biology, College of Dentistry, Yonsei University, Seoul 120-752, South Korea.
Cancer Lett. 2002 Mar 8;177(1):41-7. doi: 10.1016/s0304-3835(01)00781-9.
[6]-paradol, a pungent phenolic substance found in ginger and other Zingiberaceae plants, has been demonstrated to be an effective inhibitor of tumor promotion in mouse skin carcinogenesis. In the present study, we found that [6]-paradol and other structurally related derivatives, [10]-paradol, [3]-dehydroparadol, [6]-dehydroparadol, and [10]-dehydroparadol, with the exception of [3]-paradol induce apoptosis in an oral squamous carcinoma cell line, KB, in a dose-dependent manner. [10]-paradol and [10]-dehydroparadol exhibited a similar extent of cytotoxicity to that of [6]-paradol. [6]-Dehydroparadol and [3]-dehydroparadol appeared to be more potent, with an IC50 less than 40 microM. Treatment of KB cells with an apoptosis-inducing concentration of [6]-dehydroparadol caused induction of proteolytic cleavage of pro-caspase-3. These results suggest that [6]-paradol and structurally related derivatives induce apoptosis through a caspase-3-dependent mechanism.
[6]-姜辣素是一种在生姜及其他姜科植物中发现的辛辣酚类物质，已被证明是小鼠皮肤癌发生过程中肿瘤促进的有效抑制剂。在本研究中，我们发现[6]-姜辣素及其他结构相关衍生物，[10]-姜辣素、[3]-脱氢姜辣素、[6]-脱氢姜辣素和[10]-脱氢姜辣素，除[3]-姜辣素外，均能以剂量依赖的方式诱导口腔鳞状癌细胞系KB凋亡。[10]-姜辣素和[10]-脱氢姜辣素表现出与[6]-姜辣素相似程度的细胞毒性。[6]-脱氢姜辣素和[3]-脱氢姜辣素似乎更具效力，IC50小于40微摩尔。用诱导凋亡浓度的[6]-脱氢姜辣素处理KB细胞会导致前半胱天冬酶-3的蛋白水解切割。这些结果表明，[6]-姜辣素及结构相关衍生物通过半胱天冬酶-3依赖性机制诱导凋亡。
