• Biomolecules & Therapeutics
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• v.16 no.2
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• pp.87-94
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• 2008

In view of obtaining potential anticancer compounds, we studied the inhibitory activity and the cytotoxic effects of a candidate compound in cancer cells. The cytotoxic effects of cannabidiol (CBD) in vitro were evaluated in NIH3T3 fibroblasts, B16 melanoma cells, A549 lung cancer cells, MDA-MB-231 breast cancer cells, Lenca kidney cells and SNU-C4 colon cancer cells. The cells were cultured in various concentrations of CBD for 48 h and 25 ${\mu}$M of CBD for 6-36 h. The cells were observed to exhibit inhibitory effects of the cell viability in their growth, and then cytotoxicity was estimated. The inhibitory activity of CBD was increased in all cancer cells and showed especially strong increment in breast cancer cells. The cytotoxicity of CBD increased in a dose- and time-dependent manner with growth inhibition in all cancer cell lines. Also, to assess the membrane toxicity induced by CBD, we investigated lactate dehydrogenase (LDH) release. After treatment with various concentrations of CBD, LDH release rate of cancer cells was accelerated. On the other hand, in the induction of cell death, caspase-3, -8 and -9 activations were detected in cancer cells after treatment with various concentrations of CBD, and CBD effectively induced activity of caspase-3, -8 and -9 in A549 lung cancer cells, MDAMB-231 breast cancer cells and Renca kidney cells. Therefore these results suggest that CBD has a possibility of anticancer agents and anticancer effects against cancer cells by modulation of apoptotic pathway in the range of 5-80 ${\mu}$M concentration.

• Journal of Gynecologic Oncology
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• v.29 no.6
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• pp.99.1-99.11
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• 2018

Objective: The present study is to evaluate the biological functions of long non-coding RNA (lncRNA), X-inactive specific transcript, X-inactive specific transcript (XIST) in human epithelial ovarian cancer (EOC). Methods: XIST was upregulated in EOC cell lines, CAOV3 and OVCAR3 cells by lentiviral transduction. The effects of XIST overexpression on cancer cell proliferation, invasion, chemosensitivity and in vivo tumor growth were investigated, respectively. Possible sponging interaction between XIST and human microRNA hsa-miR-214-3p was further evaluated. Furthermore, hsa-miR-214-3p was overexpressed in XIST-upregulated CAOV3 and OVCAR3 cells to evaluate its effect on XIST-mediated EOC regulation. Results: Lentivirus-mediated XIST upregulation had significant anticancer effects in CAOV3 and OVCAR3 cells by suppressing cancer cell proliferation, invasion, increasing cisplatin chemosensitivity and inhibiting in vivo tumor growth. Hsa-miR-214-3p was confirmed to directly bind XIST, and inversely downregulated in XIST-upregulated EOC cells. In EOC cells with XIST upregulation, secondary lentiviral transduction successfully upregulated hsa-miR-214-3p expression. Subsequently, hsa-miR-214-3p upregulation functionally reversed the anticancer effects of XIST-upregulation in EOC. Conclusion: Upregulation of lncRNA XIST may suppress EOC development, possibly through sponging effect to induce hsa-miR-214-3p downregulation

• Journal of Ginseng Research
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• v.43 no.4
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• pp.692-698
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• 2019

Background: Breast cancer is a severe disease and the second leading cause of cancer death in women worldwide. To surmount this, various diagnosis and treatment options for breast cancer have been developed. One of the most effective strategies for cancer treatment is to induce apoptosis using naturally occurring compounds. Compound K (CK) is a ginseng saponin metabolite generated by human intestinal bacteria. CK has been studied for its cardioprotective, antiinflammatory, and liver-protective effects; however, the role of CK in breast cancer is not fully understood. Methods: To investigate the anticancer effects of CK in SKBR3 and MDA-MB-231 cells, cell viability assays and flow cytometry analysis were used. In addition, the direct targets of CK anticancer activity were identified using immunoblotting analysis and overexpression experiments. Invasion, migration, and clonogenic assays were carried out to determine the effects of CK on cancer metastasis. Results: CK-induced cell apoptosis in SKBR3 cells as determined through 3-(4-5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide assays, propidium iodide (PI) and annexin V staining, and morphological changes. CK increased the cleaved forms of caspase-7, caspase-8, and caspase-9, whereas the expression of Bcl-2 was reduced by CK. In assays probing the cell survival pathway, CK activated only AKT1 and not AKT2. Moreover, CK inhibited breast cancer cell invasion, migration, and colony formation. Through regulation of AKT1 activity, CK exerts anticancer effects by inducing apoptosis. Conclusion: Our results suggest that CK could be used as a therapeutic compound for breast cancer.

• Preventive Nutrition and Food Science
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• v.4 no.1
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• pp.33-37
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• 1999

The antimutagenic effects of buchu kimchi and Chinese cabbage kimchi and theri cytotoxic effects against human cancer cell line were investigated in the Salmonella typhimurium system and MTT assay, respectively. Leek and Chinese cabbage were aslo evaluated in the same system. Buchu kimchi was fermented at 15 $^{\circ}C$ for 4 days . Buchu kimchi samples showed somewhat higher antimutagenic effects against aflatoxin B1(AFB1) than CHinese cabbage kimchi in Salmonella typhimurium TA100 strain. There was no difference onthe antimutagenic activity according to the length of fermentation . Leek exerted stronger antimutagenicity against AFB1 than Chinese cabbage in the Ames assay. In MTT assay, 6-day fermented buchu kimchin revealed the highest cytotoxicity against AGS human gastric adenocarcinoma cells in which 62% and 82% of the inhibition were observed wiht the addition of 100ug, 400ug/well, respectively. Buchu kimchi samples caused 60~70% inhibition on the proliferation of HT-29 at 400ug/well. Leek exhibited higher antiproliferative effect against both AGS cells and HT-29 cells than Chinese cabbage in MTT assay. From these results, it is considered that buchu kimchi has stronger antimutagenic and in vitro anticancer effects than Chinese cabbage kimchi and the high inhibition rate of buchu kimchi probably results from leek, the major ingredient of buchu kimchi .

• Journal of the Korean Society of Food Science and Nutrition
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• v.42 no.5
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• pp.655-662
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• 2013

The antioxidant and anticancer effects of the edible mushrooms Lentinus edodes (LE, Pyogo mushroom) and Agaricus blazei (AB, Agaricus mushroom), and the medicinal mushrooms Cordyceps militaris (CM, Dong chunghacho), Ganoderma lucidum (GL, Youngji mushroom), Inonotus obliquus (IO, Chaga mushroom), and Phellinus linteus (PL, Sangwhang mushroom) were studied in vitro. The bioactive components were extracted by methanol. The antioxidant effects were evaluated using the DPPH and hydroxyl radical scavenging assays. The antioxidant activities of medicinal mushrooms (35~90%) were higher than edible mushrooms (4~23%). The in vitro anticancer effects of the mushrooms were evaluated using the MTT assay in AGS gastric adenocarcinoma cells, HCT-116 colon carcinoma cells, and HepG2 hepatoma cells. The medicinal mushrooms CM, GL, IO, and PL showed 28~91% inhibition, while the edible mushrooms LE and AB exhibited 5~40% inhibition. The medicinal mushrooms, compared to edible mushrooms, effectively down-regulated the gene expression of the anti-apoptosis related gene Bcl-2 and inflammation-related genes iNOS and COX-2, and up-regulated the pro-apoptosis gene Bax (p<0.05). Total polyphenol and flavonoids contents of the medicinal mushrooms were 9.1~35.7 mg/g, while the edible mushrooms showed 0~13.3 mg/g. This study showed that antioxidant activities and anticancer activities in vitro increased in the order LE, AB, GL, CM, IO and PL. LE and AB showed the lowest effects among the samples, GL and CM had medium effects, and IO and PL exhibited the highest effects in the antioxidant and anticancer effect for three different human cancer cells. Taken together, PL resulted in the highest and LE the lowest effects in this study.

• Journal of Life Science
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• v.28 no.1
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• pp.50-57
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• 2018

Millettia erythrocalyx, a species of plant in the Fabaceae family, is widely distributed in the tropical and subtropical regions of the world, such as the Indies, China, and Thailand. The antiviral activity of flavonoids from M. erythrocalyx has been reported; however, the antioxidative and anticancer activities of M. erythrocalyx remain unclear. In this study, we evaluated the antioxidative and anticancer effects of ethanol extract of M. erythrocalyx (EEME) and the molecular mechanism of its anticancer activity in human hepatocellular carcinoma HepG2 cells. EEME exhibited significant antioxidative effects, with a concentration at 50% inhibition ($IC_{50}$) value of $2.74{\mu}g/ml$, as measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay; moreover, it inhibited cell proliferation in a dose-dependent manner in HepG2 cells. Cell cycle analyses showed that EEME induced HepG2 cell accumulation in the subG1 phase in a dose-dependent manner. EEME also induced apoptosis of HepG2 cells, with increases in apoptotic cells and apoptotic bodies, as detected by Annexin V and 4,6-diamidino-2-phenylindole (DAPI) staining, respectively. Treatment with EEME resulted in increased expression of First apoptosis signal (Fas), a death receptor, and Bcl-2-associated X protein (Bax), a proapoptotic protein, and the activation of caspase-3, 8, and 9, resulting in the cleavage of poly (Adenosine diphosphate-ribose) polymerase (PARP). Collectively, these results suggest that EEME may exert an anticancer effect in HepG2 cells by inducing apoptosis via both the intrinsic and extrinsic pathways.

• Journal of Life Science
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• v.27 no.5
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• pp.545-552
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• 2017

Julbernardia globiflora, a tropical African tree widespread in Miombo woodland, has been used in folk medicine for the treatment of depression and stomach problems. However, the antioxidative and anticancer activities of J. globiflora remain unclear. The objective of this study is to evaluate the antioxidative and anticancer effects of methanol extract of J. globiflora (MEJG) and the molecular mechanism of its anticancer activity in human colon carcinoma HT29 cells. MEJG exhibited significant antioxidative effect with an $IC_{50}$ (concentration at 50% inhibition) value of $1.23{\mu}g/ml$ measuring by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and inhibited cell proliferation in a dose-dependent manner in HT29 cells. We found that MEJG induced apoptosis of HT29 cells with the increase of apoptotic cells and apoptotic bodies using Annexin V staining and 4,6-diamidino-2-phenylindole (DAPI) staining, respectively. The MEJG treatment showed the increase of Fas, a death receptor, and Bax, a pro-apoptotic protein, and the decrease of Bcl-2, an anti-apoptotic protein, resulting in the release of cytochrome c from the mitochondria into the cytosol and activation of caspase-3, -8 and -9. The apoptotic effects of MEJG were confirmed by cleavage of poly (ADP-ribose) polymerase (PARP). Collectively, these results suggest that MEJG may exert the anticancer effect in HT29 cells by inducing apoptosis via both the intrinsic and extrinsic pathways.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.1
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• pp.14-19
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• 2012

This study was conducted on the antioxidant activity and in vitro anticancer effects of rough rice (Oryza sativa L.) by germination periods. Rough rice was germinated at $37^{\circ}C$ for 8 days and then extracted with 70% ethanol. It was then analyzed for total polyphenol content, reducing power, antioxidant activities, and in vitro anticancer effects. Total polyphenol content increased from 3.12 mg/g for raw rough rice to 4.05 mg/g at 4 days of germination. Also reducing power increased from 0.96 to 1.25 (p<0.05). DPPH radical scavenging activity increased from 29.25% at 0 day to 34.82% at 2 days. ABTS radical scavenging activity increased from 3.05 mg AA eq/100 g at 0 day to 3.84 mg AA eq/100 g at 4 days, and then decreased afterward. The anticancer effect of ethanol extract at 4 days on stomach cancer cell line (AGS) and colon cancer cell line (HCT-116) showed higher values compared with raw rough rice extract. These results suggest that the best germination periods for increasing biological activities may be 3~4 days.

• Journal of the East Asian Society of Dietary Life
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• v.21 no.6
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• pp.871-876
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• 2011

In the present study, we investigated the compositions, antioxidant activities and anti-tumor effects of Artemisia princeps Pampanini (APD) as well as blanched leaves (CNBD) and dried leaves (CND) from Cirsium setidens Nakai on HepG2 cells. Water and ash contents were increased in CND. Protein and lipid contents were increased in CNBD. K, Ca, Mg, Fe and Cu contents of CND were higher than those of CNDB and APD. P contents was significantly decreased in CND. Yields of CND was reached high levels, but TPC, TFC, acacetin, apigenin, cynarin contents, and antioxidant activity were higher in APD. Viability of HepG2 liver cells was significantly decreased in APD. Therefore, extracts of APD are more effective preventing the liver cancer than extracts of CND and CNBD.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.226-235
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• 1993

DA-125, a new anthracycline antitumor antibiotic, was administered to Sprague-Dawley rats intravenously for 4 weeks to investigate the repeated dose toxicity Focal alopecia was noted in three female rats receiving 1.0mg/kg/day. In rats receiving 1.0 mg/kg/day, weight gain decreased in both sexes after first or second week. Hematological examination revealed lower counts of total leukocyte and increased numbers of platelet after second week. At terminal necropsy, atrophy of thymus and spleen was observed. Lymphocytic depletion of thymus and atrophy of white pulp in spleen were observed microscopically. A decrease in the number of hematopoietic cells in the bone marrow and degeneration of germinal epithelia in testes were also observed. These treatment-related effects were mainly confined to rats receiving 1.0 mg/kg/day. And toxic effects with microscopic changes were not observed in rats receiving 0.2 mg/kg/day or 0.04 mg/kg/day.