• 대한약침학회지
• /
• 제15권2호
• /
• pp.15-19
• /
• 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.

• 한국식품영양과학회지
• /
• 제34권6호
• /
• pp.784-789
• /
• 2005

옻나무의 속과 껍질부분을 분리해 $170,200,220^{\circ}C$로 온도를 달리하여 볶은 후 $100^{\circ}C$에서 열수 추출하여 얻은 추출물의 과산화지질생성 억제능, DPPH 유리라디칼 소거능 및 4종류의 인체유래의 암세포 즉 간암세포 HepG2, 위암세포 SNU-1, 유방암세포 MCF-7 및 대장암세포 WiDr에 대한 성장저지효과를 알아보았다. 저농도보다 고농도에서, 속보다 껍질부분이, $170\~200^{\circ}C$범위로 볶음처리를 한 시료의 과산화지질생성 억제능, 유리라디칼 소거능 및 암세포의 성장 저지효과가 높았다 가장 높은 과산화지질생성 억제능은 $200^{\circ}C$에서 볶은 속과 껍질추출물을 $500\mu g/mL$의 농도로 첨가 시 50.9, $56.5\%$였고, 유리라디칼 소거능은 각각 200, $170^{\circ}C$에서 볶은 속과 껍질추출물을 $500\mu g/mL$의 농도로 첨가 시 79.0, $8.4\%$였다. 또한 암세포 생존율은 $1,000\mu g/mL$의 농도로 첨가 시 가장 낮았는데 속과 껍질추출물 첨가군의 생존율은 WiDr세포가 $170^{\circ}C$에서 볶음처리 시 41.5, $36.0\%$로 가장 낮았고 ,다음은 HepG2세포로 $200^{\circ}C$에서 볶음처리 시 61.5, $44.3\%$, 이어서 MCF-7세포가 $170^{\circ}C$에서 닥음처리 시 92.0, $69.2\%$였으며, SNU-1세포는 볶음처리와 상관없이 100, $100\%$의 순으로 높아 특히 WiDr세포에 대한 성장저지효과가 현저하게 높음을 알 수 있었다. 또한 WiDr세포에 대해서는 $1,000\mu g/mL$의 농도에서 볶음처리를 하지 않은 속과 껍질추출물에서도 63.9, $6.8\%$의 낮은 생존율을 보여 옻나무는 사용한 암세포 중 대장암세포에서 강한 암세포성장 저지활성을 나타내었다.

• Archives of Pharmacal Research
• /
• 제21권5호
• /
• pp.581-590
• /
• 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.