ISSN: 2155-9600
+32 25889658
Jia-Lin Guo, Yin-Bo Chen, Hui-Yun Tsai, Shiming Li, Chi-Tang Ho and Yu-Kuo Chen
National Pingtung University of Science and Technology, Taiwan
Rutgers University, USA
Posters & Accepted Abstracts: J Nutr Food Sci
Tangeretin (TAN), a kind of polymethoxyflavones (PMFs) is found in citrus peels and has been proved to have many kinds of bioactivities including anti-inflammatory, anti-atherosclerosis and antitumor activities. Prostate cancer is universal malignant in male genital system. According to studies, 5-demethyltangeretin has hydroxyl group at the C5 position, and higher cytotoxicity than TAN for cancer cells, but the low solubility of 5-DTAN limits their availability in biological system. For the reason that we prepared 5-DTAN derivative (with acetyl group at the C5 position, 5-acetyltangeretin derivative; 5-ATAN), and hope to increase its solubility and bioavailability. The objective of this study is to investigate the anti-proliferation and cellular uptake of 5-ATAN in PC-3 human prostate cancer cells. Esterase present in the cells, therefor, 5-ATAN will be converted to 5-DTAN when 5-ATAN was uptaken into cells. We could use high-performance liquid chromatography lined electrochemical detector (ECD) to detect concentration of 5-DTAN within PC-3 cell. In MTT assay, it demonstrated that 5-ATAN significantly inhibit growth of PC-3 cells in dose- and time-depend manners. In condition of HPLC-ECD showed that 300 mV is the best volt, and retention time of 5-DTAN is 11.6 minutes, and linear regression is 0.1-10 �¼M. Moreover, the quantification and detection limits (LOQ and LOQ) of 5-DTAN were 7.16 and 1.79 �¼g/ml, respectively. In bioavailability test, intracellular concentration of 5-DTAN of 5-ATAN-treated group was significantly higher than those of 5-DTAN-treated group, which showed dose- and time-depend responses. Overall, the results indicate that 5-ATAN showed highest anti-proliferation activity than TAN & 5-DTAN in PC-3 cancer cells, and had greater bioavailability than 5-DTAN. 5-ATAN will be expected to have better oral bioavailability in vivo.
Jia Lin Guo is currently pursuing his Master’s degree in Food Science from National Pingtung University of Science and Technology and has expertise in HPLC analysis of natural compounds.
Email: lazypapaman@gmail.com