• Biomedical Science Letters
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• v.24 no.3
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• pp.150-156
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• 2018

Tankyrases are multifunctional poly (ADP-ribose) polymerases that regulate a variety of cellular processes including WNT signaling, telomere maintenance, regulation of mitosis, and many others. Tankyrases interact with target proteins and regulate their interactions and stability through poly (ADP-ribosyl) ation. In addition to their roles in telomere maintenance and regulation of mitosis, tankyrase proteins regulate tumor suppressors such as AXIN, PTEN, and AMOT. Therefore, tankyrases can be effective targets for cancer treatment. Tankyrase inhibitors could affect a variety of pathways that are carcinogenic (essential for the unlimited proliferation of human cancer cells), including WNT, AKT, YAP, telomere maintenance, and regulation of mitosis. Recently, new aspects of the function and mechanism of tankyrases have been reported and several tankyrase inhibitors have been identified. Also, it has been proposed that the combination of conventional chemotherapy agents with tankyrase inhibitors may have synergistic anti-cancer effects. Based on this, it is expected that more advanced and improved tankyrase inhibitors will be developed, enabling new therapeutic strategies against cancer and other tankyrase linked diseases. This review discusses tankyrase function and the role of tankyrase inhibitors in the treatment of cancer.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2004.05a
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• pp.118-118
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• 2004

• The Korean Journal of Food And Nutrition
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• v.19 no.2
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• pp.176-182
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• 2006

Sorghum bicolor L. Moench(Sorghum, Su-Su) is a major cereal food crop used in many parts of the world. It is used as a human food resource and folk medicines in Asia and Africa. The stem of sorghum has been used as a digestive aid and an anti-diarrheal agent. Sorghum hybrids contain high levels of diverse phenolic compounds that may provide health benefits. High levels of polyflavanols, anthocyanins, phenolic acids, and other antioxidant compounds have been reported in sorghums, which have also been shown to possess various biological activities such as anti-mutagenic, anti-carcinogenic, and HMG-CoA reductase inhibitory activities. In an in vitro experiment, we examined mice splenocyte proliferation and production of three types of cytokine($IL-1{\beta},\;IL-6,\;TNF-{\alpha}$) by peritoneal macrophages cultured with ethanol and water extracts of Sorghum bicolor L. Moench. A single cell suspension of splenocytes was prepared and the cell proliferation of the splenocytes was examined by MTT assay. The splenocyte proliferation was increased when water extracts of Sorghum bicolor L. Moench were used as supplements in all concentrations investigated. The production of cytokine($IL-1{\beta},\;IL-6,\;TNF-{\alpha}$) by activated peritoneal macrophage was detected by ELISA using the cytokine kit. $IL-1{\beta},\;IL-6,\;and\;TNF-{\alpha}$ production by activated macrophages were increased by supplementation with Sorghum bicolor L. Moench water extracts. This study suggests that supplementation of with Sorghum bicolor L. Moench water extracts may enhance immune function by regulating the splenocyte proliferation and enhancing the cytokine production by activated macrophages in vitro.

• Preventive Nutrition and Food Science
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• v.22 no.2
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• pp.149-155
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• 2017

The effects of Korean solar salt on an azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced colon cancer C57BL/6 mouse model were studied. Korean solar salt samples (SS-S, solar salt from S salt field; SS-Yb, solar salt from Yb salt field), nine-time-baked bamboo salt (BS-9x, made from SS-Yb), purified salt (PS), and SS-G (solar salt from $Gu\acute{e}rande$, France) were orally administered at a concentration of 1% during AOM/DSS colon cancer induction, and compared for their protective effects during colon carcinogenesis in C57BL/6 mice. SS-S and SS-Yb suppressed colon length shortening and tumor counts in mouse colons. Histological evaluation by hematoxylin and eosin staining also revealed suppression of tumorigenesis by SS-S. Conversely, PS and SS-G did not show a similar suppressive efficacy as Korean solar salt. SS-S and SS-Yb promoted colon mRNA expression of an apoptosis-related factor and cell-cycle-related gene and suppressed pro-inflammatory factor. SS-Yb baked into BS-9x further promoted these anti-carcinogenic efficacies. Taken together, the results indicate that Korean solar salt, especially SS-S and SS-Yb, exhibited anti-cancer activity by modulating apoptosis- and inflammation-related gene expression during colon carcinogenesis in mice, and bamboo salt baked from SS-Yb showed enhanced anti-cancer functionality.

• Biomedical Science Letters
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• v.29 no.4
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• pp.211-219
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• 2023

Caffeic acid phenethyl ester (CAPE) is an active component of propolis obtained from honeybee hives. CAPE possesses anti-mitogenic, anti-carcinogenic, anti-inflammatory, and immunomodulatory activities in diverse systems, which know as displays antioxidant activity and inhibits lipoxygenase activities, protein tyrosine kinase, and nuclear factor kappa B (NF-κB) activation. This study aimed to investigate the effect of CAPE on lipopolysaccharide (LPS)-induced human neutrophil phagocytosis. Human neutrophils were cultured with various concentrations of CAPE (1, 10, and 100 µM) with or without LPS. The pro-inflammatory proteins (tumor necrosis factor-alpha [TNF-α], interleukin [IL]-6 and IL-8) levels were measured after 4 h incubation. To investigate the intracellular signaling pathway, we measured the levels of mitogen-activated protein kinases (MAPK), including phosphorylation of p38, extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) and c-Jun N-terminal kinase (JNK). Next, to evaluate the potential phagocytosis, neutrophils were labeled with iron particles of superparamagnetic iron oxide nanoparticles (SPIONs, 40 nm) for 1 h in culture medium containing 5 mg/mL of iron. The labeling efficiency was determined by Prussian blue staining for intracellular iron and 3T-wighted magnetic resonance imaging. CAPE decreased the activation of intracellular signaling pathways, including ERK1/2 and c-Jun, and expression of pro-inflammatory cytokines, including TNF-α and IL-6, but had no effect on the signaling pathways of p38 and cytokine IL-8. Furthermore, images obtained after mannan-coated SPION treatment suggested that CAPE induced significantly higher signal intensities than the control or LPS group. Together, these results suggest that CAPE regulates LPS-mediated activation of human neutrophils to reduce phagocytosis.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.4
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• pp.462-470
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• 2012

Mountain cultivated ginseng (MCG) is a type of Panax ginseng C. A. Mayer, grown in the mountains by artificial seeding. In general, it has been known that the biophysical activities of MCG is greater than that of ginseng. However, the in vivo efficacy of MCG on cancer has not been studied. In this study, we investigated the anti-carcinogenic effect of MCG and ginseng using the 7,12-dimethylbenz[a]anthracene (DMBA)-12-O-tetradecanoylphorbol- 13-acetate (TPA) two stage mouse skin carcinogenesis model. Six weeks of female ICR mice were divided into control, MCG, and ginseng diet groups and were subjected into two different experimental protocols. In the first study, each experimental diet was fed with TPA promotion for 24 weeks. The result showed that supplementation of MCG reduced tumor incidence, tumor multiplicity, and tumor size compared to those of the control and ginseng groups. In the second study, 3 groups of mice were supplied with each diet 4 weeks before DMBA tumor initiation, until the end of experiment. The result showed that tumor incidence, tumor multiplicity, and tumor size were reduced in the ginseng diet group compared to those of the control and MCG groups. TPA-induced BrdU incorporation was also significantly reduced in the ginseng diet group. Taken together, these results suggest that MCG is chemotherapeutic, whereas ginseng has a chemopreventative effect on mouse skin cancer.

• The Journal of Korean Obstetrics and Gynecology
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• v.32 no.3
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• pp.20-31
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• 2019

Objectives: The seeds from Arctium lappa have been considered for its various pharmacological properties, which include anti-carcinogenic, anti-inflammatory, anti-diabetic, and anti-viral activities. Methods: In the present study, we investigated the anti-inflammatory effect of the ethanol extract from the seeds of Arctium lappa L (EAL) on cytokine-induced vascular inflammation in human umbilical vein endothelial cells (HUVEC). Results: Pretreatment with EAL significantly decreased tumor necrosis factor alpha ($TNF-{\alpha}$)-induced cell adhesion molecules expression such as intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), and endothelial-selectin (E-selectin) in a dose-dependent manner. Cell adhesion assay showed that pretreatment with EAL suppressed HUVEC-monocyte adhesion by $TNF-{\alpha}$ over $1{\mu}g/ml$ concentration. We investigated the involvement of nuclear transcription factor kappa-B ($NF-{\kappa}B$) in $TNF-{\alpha}$-induced vascular inflammation. $NF-{\kappa}B$ p65 nuclear expression was induced by $TNF-{\alpha}$, however, pretreatment with EAL was attenuated that nuclear translocation. In cytoplasm, EAL was also attenuated $TNF-{\alpha}$-induced decrease of inhibitor of ${\kappa}B-{\alpha}$ ($I{\kappa}B-{\alpha}$) expression. Moreover, EAL significantly decreased $TNF-{\alpha}$-induced production of intracellular reactive oxygen species (ROS). Conclusions: Taken together, our findings suggest that seeds of Arctium lappa L could be a therapeutic herb for prevention of cardiovascular diseases throughout the inhibition of vascular endothelial inflammation.

• Journal of Life Science
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• v.22 no.4
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• pp.538-544
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• 2012

Ethanol is known as being carcinogenic to humans. In addition, the anti-proliferative effects of ethanol have been described for a variety of tissues and cells. In this study, we investigated the anti-proliferative effects of ethanol on various cancer cells, particularly on oncogenic $ras$-transformed or-injected cells. Ethanol treatment inhibited the cell proliferation of normal control cells, but did not suppress the proliferation of various cancer cells and oncogenic $ras$-transformed cells. Furthermore, ethanol treatment did not interfere with DNA synthesis, which was induced by microinjecting the oncogenic $H-Ras^{V12}$ protein. The anti-proliferative effect of ethanol was rescued by antioxidants, such as $N$-acetylcysteine and 4-methlpyrazole. These results suggest that ethanol cytotoxicity is exerted through free radical formation, and that the anti-proliferative action site of ethanol cytotoxicity either lies upstream, or is independent of Ras.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.46-52
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• 2023

The most abundant flavanone of grapefruits, naringenin (NN), is well known for its hepatoprotective, anti-lipid peroxidation and anti-carcinogenic effects. We generated three derivatives from NN using this technique in previous studies. Among them, it was confirmed that naringenin-7-O-phosphate (N7P), whose biological and physicochemical properties were not reported, showed a water solubility 45 times higher than that of NN. Therefore, in this study, the anti-inflammatory activity was evaluated in RAW 264.7 cells to investigate the potential physiological activity of N7P. As a result, N7P showed nitric oxide (NO) inhibitory activity at concentrations that did not show toxicity. In addition, prostaglandin E₂ (PGE₂) showed significant inhibitory activity from the lowest concentration of 12.5 μM and showed increased inhibitory activity compared to NN. In addition, as a result of western blot, N7P showed increased cyclooxygenase-2 (COX-2) inhibitory activity than NN, and effectively inhibited NO and PGE₂ by significantly inhibiting their expression pathways. N7P also inhibited inflammatory cytokines, including tumor necrosis factor-α, interleukin-6. Based on these results, we propose that N7P can be used as a potent antiinflammatory agent.

• Journal of Physiology & Pathology in Korean Medicine
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• v.25 no.6
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• pp.1014-1019
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• 2011

Curcumin is a natural phytochemical present in turmeric, the ground powder of the rhizomes of Curcuma longa. Curcumin has been described as having antioxidant, anti-inflammatory, and anti-carcinogenic properties. However, it is still largely unknown whether curcumin inhibits the UVB-induced inflammatory reaction in HaCaT keratinocyte cell lines. In this study, to confirm the photoprotection properties of curcumin, HaCaT keratinocyte cells were irradiated by UVB, and then treated with curcumin. UVB irradiation induced the increased expressions of IL-$1{\beta}$, TNF-${\alpha}$, IL-6, IL-8, and COX-2 in HaCaT cells. These increased expressions of cytokines (IL-$1{\beta}$, TNF-${\alpha}$, IL-6, IL-8, and COX-2) were down-regulated by curcumin treatment in UVB-irradiated HaCaT cells. In addition skin of hairless mice were damaged by UVB irradiation, which were evidenced by atrophy of epidermis and decrease of collagen in dermis. However, these damages were protected partially by co-treatment of curcumin. Taken together, this data indicate that curcumin may be a promising photoprotection agent, when used in massage pack or sunscreen product, to reduce cell death in UV-damaged skin.