• Journal of Pharmacopuncture
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• v.15 no.2
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• pp.15-19
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• 2012

The purpose of this study was to investigate the anti-cancer effects of Sophorae Radix (SR) and doxorubicin (DOX) in human gastric and colorectal adenocarcinoma cells. We used the human gastric and colorectal adenocarcinoma cell lines (MKN-45 and WIDR cells, respectively). We examined cell death by using the MTT(3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide) assay and the caspase 3 assay with SR. To examine the inhibitory effects of SR, we performed a cell cycle (sub G1) analysis for the MKN-45 and WIDR cells after three days with SR. The reversibility of SR was examined for one-day to five-day treatments with SR. SR inhibited the growth of MKN-45 and WIDR cells in a dosedependent manner. Also, we showed that SR induced apoptosis in MKN-45 and WIDR cells by using the MTT assay, the caspase 3 assay and the sub-G1 analysis. SR combined with DOX markedly inhibited the growth of MKN-45 and WIDR cells compared to SR or DOX alone. After 3 days of treating MKN-45 and WIDR cells with SR, the fraction of cells in the sub-G1 phase was much higher than that of the control group. Our findings provide insights into unraveling the effects of SR on human gastric and colorectal adenocarcinoma cells and into developing therapeutic agents for use against gastric and colorectal adenocarcinomas.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.6
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• pp.784-789
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• 2005

The inhibitory effects of hot water extracts of Rhus verniciflua Stokes pith and peel roasted at 170, 200 and $220^{\circ}C$ on lipid peroxidation, formation of DPPH free radicals and growth of four human cancer cells such as HepG2 (liver cancer), SNU-1 (stomach cancer), MCF-7 (breast cancer) and Widr (colon cancer) were examined. The antioxidant activities and growth inhibitory effects on cancer cells of hot water extracts of peel were higher than those of pith, and the activities were dose-dependent. The roasting temperature showing the highest antioxidant activities and growth inhibitory effects on cancer cells was in the range of $170\~200^{\circ}C$ The lipid peroxidation and formation of DPPH free radicals of hot water extracts of roasted pith and peel were inhibited to 50.9, $56.5\%\;and\;79.0,\;78.4\%$ at the concentration of $500\mu g/mL$, respectively. The growth inhibitory effects of roasted pith and peel on cancer cells were in the order of Widr (41.5, $36.0\%$) > HepG2 (61.5, $44.0\%$) > MCF-7 (92.0, $69.2\%$)> SNU-1 (100, $100\%$) cells at the concentration of $1,000\mu g/mL$ as compared with the control, respectively. These results suggest that roasted Rhus verniciflua Stokes could be an useful natural medicinal plant for colon cancer.

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.581-590
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• 1998

We developed a novel water-soluble camptothecin analobue, CKD602, and evaluated the inhibition of topoisomerase I and the antitumor activities against mammalian tumor cells and human tumor xenografts. CKD602 was a nanomolar inhibitor of the topoisomerase I enzyme in the cleavable complex assay. CKD602 was found to be 3 times and slightly more potent than topotecan and camptothecin as inhibitors of topoisomerase, respecitively. In tumor cell cytotoxicity, CKD602 was more potent than topotecan in 14 out of 26 human cancer cell lines tested, while it was comparable to camptothecin. CKD602 was tested for the in vivo antitumor activity against the human tumor xenograft models. CKD602 was able to imduce regression of established HT-29, WIDR and CX-1 colon tumors, LX-1 lung tumor, MX-1 breast tumor and SKOV-3 ovarian tumor as much as 80, 94, 76, 67, 87% and 88%, respectively, with comparable body weight changes to those of topotecan. Also the therapeutic margin (R/Emax: maximum tolerance dose/$ED-{58}$) of CKD602 was significantly higher than that of topotecan by 4 times. Efficacy was determined at the maximal tolerated dose levels using schedule dependent i.p. administration in mice bearing L1210 leukemia. On a Q4dx4 (every 4 day for 4 doses) schedule, the maximum tolerated dose (MTD) was 25 mg/kg per administration, which caused great weight loss and lethality in <5% tumor bearing mouse. this schedule brought significant increase in life span (ILS), 212%, with 33% of long-term survivals. The ex vivo antitumor activity of CKD602 was compared with that of topotecan and the mean antitumor index (ATI) values recorded for CKD602 were significantly higher than that noted for topotecan. From these results, CKD602 warrants further clinical investigations as a potent inhibitor of topoisomerase I.