• Proceedings of the Korean Society of Toxicology Conference
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• 2005.05a
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• pp.177-177
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• 2005

• Biomolecules & Therapeutics
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• v.30 no.5
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• pp.435-446
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• 2022

The present study evaluated the anti-cancer activity of histone deacetylase (HDAC)-inhibiting CKD-581 in multiple myeloma (MM) and its pharmacological mechanisms. CKD-581 potently inhibited a broad spectrum of HDAC isozymes. It concentration-dependently inhibited proliferation of hematologic cancer cells including MM (MM.1S and RPMI8226) and T cell lymphoma (HH and MJ). It increased the expression of the dishevelled binding antagonist of β-catenin 3 (DACT3) in T cell lymphoma and MM cells, and decreased the expression of c-Myc and β-catenin in MM cells. Additionally, it enhanced phosphorylated p53, p21, cleaved caspase-3 and the subG1 population, and reversely, downregulated cyclin D1, CDK4 and the anti-apoptotic BCL-2 family. Finally, administration of CKD-581 exerted a significant anti-cancer activity in MM.1S-implanted xenografts. Overall, CKD-581 shows anticancer activity via inhibition of the Wnt/β-catenin signaling pathway in hematologic malignancies. This finding is evidence of the therapeutic potential and rationale of CKD-581 for treatment of MM.

• BMB Reports
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• v.53 no.10
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• pp.512-520
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• 2020

T-cell-based cancer immunotherapies, such as immune checkpoint blockers (ICBs) and chimeric antigen receptor (CAR)-T-cells, have significant anti-tumor effects against certain types of cancer, providing a new paradigm for cancer treatment. However, the activity of tumor infiltrating T-cells (TILs) can be effectively neutralized in the tumor microenvironment (TME) of most solid tumors, rich in various immunosuppressive factors and cells. Therefore, to improve the clinical outcomes of established T-cell-based immunotherapy, adjuvants that can comprehensively relieve multiple immunosuppressive mechanisms of TME are needed. In this regard, recent studies have revealed that metformin has several beneficial effects on anti-tumor immunity. In this mini-review, we understand the immunosuppressive properties of TME and how metformin comprehensively enhances anti-tumor immunity. Finally, we will discuss this old friend's potential as an adjuvant for cancer immunotherapy.

• BMB Reports
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• v.49 no.3
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• pp.167-172
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• 2016

Kaiso is a Pox Virus and Zinc Finger (POZ-ZF) transcription factor with bi-modal DNA-binding specificity. Here, we demonstrated that Kaiso expression is inversely correlated with glucocorticoid receptor (GR) expression in breast carcinomas. Knockdown of Kaiso increased GR expression, while overexpression of Kaiso inhibited GR expression in breast cancer cells. Furthermore, Kaiso repressed GR proximal promoter-reporter activity in a dose-dependent manner. Remarkably, ChIP experiments demonstrated that endogenous Kaiso was associated with the GR promoter sequence in a methylation-dependent manner. Since glucocorticoids inhibit chemotherapyinduced apoptosis and have been widely used as a co-treatment of patients with breast cancer, we assessed the role of Kasio in GR-mediated anti-apoptotic effects. We found that overexpression of Kaiso attenuated the anti-apoptotic effects of glucocorticoids in breast cancer cells. Our findings suggest that GR is a putative target gene of Kaiso and suggest Kaiso to be a potential therapeutic target in GC-combination chemotherapy in breast cancer.

• Natural Product Sciences
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• v.29 no.2
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• pp.113-119
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• 2023

Descurainia sophia seeds methanol extract showed significant anti-influenza activity and we tried to isolate anti-influenza compounds from the D. sophia extract. D. sophia seeds were extracted with 80% methanol and fractionated with n-hexane, ethyl acetate, CHCl₃ and n-butanol. The anti-influenza activity of each fraction was assessed using sulforhodamine B (SRB) method in A549 cells, human-derived lung cancer cells. The ethyl acetate and CHCl₃ fractions showed the most potent anti-influenza activity. Seven compounds were isolated from CHCl₃ fraction and identified 1-decanol (1), 2-(3,4-dihydroxy-2-methylenebutoxy)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (2), daucosterol (3), isorhamnetin (4), quercetin (5), sinapic acid (6), and helveticoside (7) by spectroscopic data such as UV, IR, ¹H-NMR, ¹³C-NMR and mass spectroscopy. Anti-influenza activities of isolated compounds were evaluated using SRB method in A549 cells. Compounds 3, 4 and 7 had significant anti-influenza activity in a dose-dependent manner.

• Journal of Applied Biological Chemistry
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• v.55 no.3
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• pp.191-194
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• 2012

Novel pyrazolinecarbothioamide (5) was synthesized from chalcone (3) which was prepared from 2'-hydroxy-1'-acetonaphthone (1) and 2-methoxy benzaldehyde (2). Treatment of pyrazolinecarbothioamide (5) on HCT116 cancer cell showed upregulation of p21 and downregulation of cyclin D1 protein. Flowcytometer analysis revealed that pyrazolinecarbothioamide (5) controls the expression of cell cycle regulatory proteins, which blocks cell cycle progression of HCT116 cancer cell at the G1 phase.

• The Korean Journal of Food And Nutrition
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• v.35 no.5
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• pp.359-368
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• 2022

In this study, the quality characteristics of kimchi, such as its salinity, pH, and acidity, were measured and compared, and the HT-29 human colon cancer cells were used to show the anticancer effects of kimchi. The kimchi samples used herein included standard kimchi (SK), turnip kimchi (TK), and turnip-powder-added kimchi (TPK). The measured pH and acidity of TK and TPK showed no significant differences with those of SK. Compared to SK and TK, TPK had higher DPPH scavenging activity and higher total flavonoid content, confirming its antioxidant activity. The cancer cell growth inhibition rates of TK and TPK were significantly higher than that of SK. In HT-29 cells treated with TPK, the mRNA expression of Bcl-xL, an anti-apoptosis-related gene, was lower, and the mRNA expressions of the apoptosis-related genes Bax, Bad, and caspase-9 were higher. TPK showed significantly higher levels of mRNA expressions for the cell-cycle-related genes p53 and p21 than the other samples, in addition to suppression effects on cancer cell proliferation. Compared to SK, TK and TPK suppressed the growth of colon cancer cells and showed higher anticancer effects. Therefore, it is shown that kimchi with added turnip powder had high anticancer effects.

• Mycobiology
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• v.37 no.1
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• pp.21-27
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• 2009

In the present study, the anti-cancer effects of ginseng fermented with Phellinus linteus (GFPL) extract were examined through in vitro and in vivo assays. GFPL was produced by co-cultivating ginseng and Phellinus linteus together. Ginsenoside Rg3, Rh1 and Rh2 are important mediators of anti-angiogenesis and their levels in GFPL were enriched 24, 19 and 16 times, respectively, more than that of ginseng itself through the fermentation. GFPL exhibited distinct anti-cancer effects, including growth inhibition of the human lung carcinoma cell line A549, and promotion of immune activation by stimulating nitric oxide (NO) production in Raw 264.7 cells. Further evidence supporting anti-cancer effects of GFPL was its significant prolongment of the survival of B16F10 cancer cell-implanted mice. These results suggest that the GFPL may be a candidate for cancer prevention and treatment through immune activation and anti-angiogenic effects by enriching Rg3, Rh1 and Rh2.

• Journal of the Korean Society of Food Culture
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• v.35 no.4
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• pp.400-405
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• 2020

Evodiae Fructus is the dried unripe fruit of Evodia rutaecarpa, and has traditionally been used for treating stomachache and diarrhea. Evodiamine and rutaecarpine, the major biologically active compounds of Evodiae Fructus, are reported to have anti-oxidative and anti-inflammatory effects, as well as inhibit proliferation and metastasis of various cancer cells. The current study investigates the anti-oxidative and anti-cancer effects of the Evodiae Fructus extract, considering varying concentrations of methanol extraction (40, 80, and 95%). High contents of total phenolic compounds were determined in the order of extracts 80, 95, and 40%. Evaluating contents of the 95, 80, and 40% extracts revealed 36.77, 7.29, and 1.86 ㎍/mg evodiamine, respectively, and 53.02, 17.16, and 3.79 ㎍/mg rutaecarpine, respectively, with the highest content of both compounds obtained in the 95% extract. DPPH radical scavenging activity was observed to be inversely proportional to the contents of total phenolic compounds, with decreasing SC₅₀ values obtained in the order 80, 95, and 40% extract. The 95 and 80% extracts exerted toxicity to AGS gastric cancer cells, but the 40% extract was non-toxic. Evodiamine is a known anti-cancer agent, and could be responsible for the observed toxicity. Cleavage of PARP, and Caspase-3, -7, -8 and -9 was observed in the 95% extract-treated AGS cells, indicating that cell toxicity exerted by the 95% extract could be attributed to apoptosis.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.4
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• pp.1331-1336
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• 2015

Natural glycoproteins can induce apoptosis of tumor cells and exert anti-tumor activity by immunomodulatory functions, cytotoxic and anti-inflammation effects, and inhibition of endothelial growth factor. Given their prospects as novel agents, sources of natural antitumor glycoproteins have attracted attention and new research directions in glycoprotein biology are gradually shifting to the direction of cancer treatment and prevention of neoplastic disease. In this review, we summarize the latest findings with regard to the tumor suppressor signature of glycoproteins and underlying regulatory mechanisms.