• Journal of the Korean Society of Food Science and Nutrition
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• v.29 no.2
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• pp.322-328
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• 2000

This study was performed to determine the antimutagenic and cytotoxic effect of the Phellinus linteus methanol extract on Salmonella typhimurium TA98, TA100 and human cancer cell lines. In the Ames test, methanol extract of P. linteus alone did not exhibit any mutagenicity but showed substantial inhibitory effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), 4-nitroquinoline-nitroquinoline-1-oxide(4NQO), 3-amino-1,4-dimethyl-5H-pyrdo[4,3-blindol(Trp-P-1) and benzo(α)pyrene(B(α)P). The methanol extracts of P. linteus(200㎍/plate) showed approximately 78.3%, 78.7% and 88.1% inhibitory effect on the mutagenesis induced by 4NQO, Trp-P-1 and B(α)P. The anticancer effects of P. linteus extract against human breast adenocarcinoma(MCF7), human lung carcinoma (A549), human fibrosarcoma (HT1080), human hepatocelular carcinoma (Hep3B) and human epitheloid carcinoma (HeLa) were investigated. The treatment of 1mg/mL P. linteus extracts had the highest cytotoxicity against MCF7 (92.0%), followed by Hep3B (84.9%), A549 (84.2%) and HT1080 (82.9%). In contrast 1mg/mL treatment of P. linteus extracts had only 10∼40% cytotoxicity on normal human liver cell (WRL68).

• YAKHAK HOEJI
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• v.44 no.5
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• pp.399-405
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• 2000

We have synthesized a novel platinum (II) coordination complex containing trans-ι-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis (diphenylphosphino)ethane (DPPE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt (trans-ι-DACH) (DPPE)].2NO$_3$(PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against MKN-45/S, MKN-45/ADR and MKN-45/CDDP cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells, and human renal cortical tissues, determined using the MTT assaying technique, the ($^3$H)-thymidine uptake and the glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum (II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• YAKHAK HOEJI
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• v.50 no.6
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• pp.421-428
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• 2006

Water extracts, ethanol extracts, and juice of Cusuta japonica, C, australis, and C. chinensis were prepared, and their cytotoxicity, antioxidant activity and inhibitory effects on tyrosinase activitiy and melanin biosynthesis were estimated by using melanoma Clone M-3. From this study; the following conclusions were attained. Extracts of Cuscuta japonica, C. australis, and C. chinensis showed noticeable cytotoxicity except ethanol extracts from the stem of C. australis. A maximual cytotoxicity was observed with tile ethanol extract from the seed of C, australis (87.39%). While the ethanol extract from the seed of C. japonica (91.88%) showed the most pronounced inhibitory effect on melanin biosynthesis, the water extract from the stem of C. japonica (1.05%) possessed very little inhibitory effect. The most inhibitory effect on tyrosinase activity was observed with the water extract from the stem of C. australis (76.67%). Howeverr the water extract from the stem of C. japonica showed a very poor effect on the inhibition of tyrosinase activity All the preparations, except extracts from the seed of C. australis were able to remove reactive oxygen species (ROS) in a dose-dependent manner. The juice of C. japonica demonstrated the strongest activity (59.02%).

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.548-555
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• 2006

Three diterpenes (1, 8, and 9), three triterpenes (3, 4, and 7), one saponin (11), four sterols (2, 5, 6, and 12), and one cerebroside (10) were isolated from the EtOH extract of the aerial parts of Aralia cordata by repeated silica gel column chromatography. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in literatures. All isolated compounds were evaluated for their cytotoxicity against L1210, K562, and LLC tumor cell lines using MTT assay. Of which, $3{\beta},5{\alpha}-dihydroxy-6{\beta}-methoxyergosta-7,22-diene$ (6) showed a potent cytotoxicity against all cell lines with $IC_{50}$ values of 11.7, 11.9, and $15.1\;{\mu}M$, respectively, while compounds 1, 5, and 11 showed a moderate or weak cytotoxicity. These isolates were also examined for their inhibitory activity against COX-1 and COX-2. Although most compounds, except for 2, 10, and 12, showed a strong inhibitory activity against COX-1, they exhibited a moderate or weak inhibitory activity against COX-2.

• The Korean Journal of Physiology and Pharmacology
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• v.23 no.1
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• pp.37-45
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• 2019

To study the effect of nicorandil pretreatment on ketone body metabolism and Acetyl-CoA acetyltransferase (ACAT1) activity in hypoxia/reoxygenation (H/R)-induced cardiomyocytes. In our study, we applied H9c2 cardiomyocytes cell line to evaluate the cardioprotective effects of nicorandil. We detected mitochondrial viability, cellular apoptosis, reactive oxygen species (ROS) production and calcium overloading in H9c2 cells that exposed to H/R-induced cytotoxicity. Then we evaluated whether nicorandil possibly regulated ketone body, mainly ${\beta}$-hydroxybutyrate (BHB) and acetoacetate (ACAC), metabolism by regulating ACAT1 and Succinyl-CoA:3-ketoacid coenzyme A transferase 1 (OXCT1) protein and gene expressions. Nicorandil protected H9c2 cardiomyocytes against H/R-induced cytotoxicity dose-dependently by mitochondria-mediated anti-apoptosis pathway. Nicorandil significantly decreased cellular apoptotic rate and enhanced the ratio of Bcl-2/Bax expressions. Further, nicorandil decreased the production of ROS and alleviated calcium overloading in H/R-induced H9c2 cells. In crucial, nicorandil upregulated ACAT1 and OXCT1 protein expressions and either of their gene expressions, contributing to increased production of cellular BHB and ACAC. Nicorandil alleviated cardiomyocytes H/R-induced cytotoxicity through upregulating ACAT1/OXCT1 activity and ketone body metabolism, which might be a potential mechanism for emerging study of nicorandil and other $K_{ATP}$ channel openers.

• Korean Journal of Plant Resources
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• v.31 no.6
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• pp.604-611
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• 2018

This study was conducted to explore the immune activity, anticancer activity and nitrile scavenging activities of methanol extracts from the various organs of four Korean resource plants. The immune responses from both human T and B cell line was significantly enhanced in the cell growth compared to control while the cell growth was influenced at a certain period of culture. The results revealed that the cell growth of both human T and B cell was altered in a time dependent manner. Among tested several resource plants, the flower extract of E. japonicum demonstrated a pronounced cytotoxicity against HCT-116 cell with an IC50 value $132.08{\mu}g\;ml-1$. The flower extract from Corylopsis coreana had a promising scavenging activity against pH 1.2 compared to other species. Taken together, the studied resource plants have influenced significantly in response to immunity and also have the potential cytotoxicity and nitric scavenging activities. However, the species E. japonicum exhibited the pronounced activities from several resource plants. The result from this investigation suggests that the extracts of studied resource plant could be an addition to basic medicine for some diseases.

• The Korean Journal of Physiology and Pharmacology
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• v.27 no.5
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• pp.471-479
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• 2023

Disulfiram (DSF), a medication for alcoholism, has recently been used as a repurposing drug owing to its anticancer effects. Despite the crucial role of dendritic cells (DCs) in immune homeostasis and cancer therapy, the effects of DSF on the survival and function of DCs have not yet been studied. Therefore, we treated bone marrow-derived DCs with DSF and lipopolysaccharide (LPS) and performed various analyses. DCs are resistant to DSF and less cytotoxic than bone marrow cells and spleen cells. The viability and metabolic activity of DCs hardly decreased after treatment with DSF in the absence or presence of LPS. DSF did not alter the expression of surface markers (MHC II, CD86, CD40, and CD54), antigen uptake capability, or the antigen-presenting ability of LPS-treated DCs. DSF decreased the production of interleukin (IL)-12/23 (p40), but not IL-6 or tumor necrosis factor-α, in LPS-treated DCs. We considered the granulocyte-macrophage colony-stimulating factor (GM-CSF) as a factor to make DCs resistant to DSF-induced cytotoxicity. The resistance of DCs to DSF decreased when GM-CSF was not given or its signaling was inhibited. Also, GM-CSF upregulated the expression of a transcription factor XBP-1 which is essential for DCs' survival. This study demonstrated for the first time that DSF did not alter the function of DCs, had low cytotoxicity, and induced differential cytokine production.

• Archives of Pharmacal Research
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• v.19 no.4
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• pp.286-291
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• 1996

Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$, bibenzyl, $2,2^I-dimethylbibenzyl$, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.

• Advances in Traditional Medicine
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• v.1 no.2
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• pp.45-51
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• 2000

This study was carried out to evaluate cytotoxicity of the methanol extract from Sophora flavescens Ait. against L1210 (lymphocytic leukemia) and $P388D_1$ (lymphoid neoplasma) Cells in vitro. We have determined cytotoxicity by the MTT (3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazolium bromide) assay. The order of cytotoxicity of Sophora flavescens Ait. extracts against L1210 and $P388D_1$ cells in vitro is as follows: Fr. 4 > Fr. 3 > Fr. 5 > Fr. 2 > Fr. 1. These results suggest that the fraction 4 of the methanol extracts from Sophora flavescens Ait. may be a valuable choice for the development of antitumor agents. In order to develop an antimicrobial agent, dried Sophora flavescens Ait. was extracted with hot methanol, and then antimicrobial activity (MIC test) was investigated. In this study, the fraction 3 of the methanol extracts from the roots of S. flavescens showed strong growth inhibition activity against gram-positive and gram-negative bacteria (MIC, $3.125\;{\mu}g/ml$) such as S. mutans, S. epidermidis and P. putida. These results indicate that fractions 3 and 4 inhibit tumor cells and bacteria.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.16
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• pp.7003-7006
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• 2015

Background: Nanoparticles of gold and silver are offering revolutionary changes in the field of cancer therapy. N-heterocyclic carbene (NHC) metal complexes possess diverse biological activities and are being investigated as potential chemotherapeutic agents. The purpose of this study was to examine the cytotoxicity and possible mechanisms of action of two types of newly synthesized nanofiber composites containing BIAN N-heterocyclic gold carbene complexes in two types of human cancer cells, namely breast cancer (MCF7) and liver cancer (HepG2) cells and also in normal human embryonic kidney cells (HEK 293). Materials and Methods: Cytotoxicity was assessed by MTT cell viability assay and oxidative stress by checking the total glutathione level. Results: Both compounds affected the cell survival of the tested cell lines at very low concentrations (IC50 values in the micro molar range) as compared to a well-known anti-cancer drug, 5 fluorouracil. A 60-80% depletion in total glutathione level was detected in treated cells. Conclusions: Reduction in total glutathione level is one of the biochemical pathways for the induction of oxidative stress which in turn could be a possible mechanism of action by which these compounds induce cytotoxicity in cancer cell lines. The in vitro toxicity towards cancer cells found here means that these molecules could be potential anticancer candidates.