• Title/Summary/Keyword: Cytotoxity

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Anti-Proliferation Effects of Benzimidazole Derivatives on HCT-116 Colon Cancer and MCF-7 Breast Cancer Cell Lines

  • Al-Douh, Mohammed Hadi;Sahib, Hayder B.;Osman, Hasnah;Hamid, Shafida Abd;Salhimi, Salizawati M.
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.8
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    • pp.4075-4079
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    • 2012
  • Benzimidazoles 1-4 were obtained using modified synthesis methods and studied for their ability to inhibit cell proliferation of colon cancer cell HCT-116 and breast cancer cell MCF-7 using MTT assays. In the HCT-116 cell line, benzimidazole 2 was found to have an $IC_{50}$ value of $16.2{\pm}3.85{\mu}g/mL$ and benzimidazole 1 a value of $28.5{\pm}2.91{\mu}g/mL$, while that for benzimidazole 4 was $24.08{\pm}0.31{\mu}g/mL$. In the MCF-7 cell line, benzimidazole 4 had an $IC_{50}$ value of $8.86{\pm}1.10{\mu}g/mL$, benzimidazole 2 a value of $30.29{\pm}6.39{\mu}g/mL$, and benzimidazole 1 a value of $31.2{\pm}4.49{\mu}g/mL$. Benzimidazole 3 exerted no cytotoxity in either of the cell lines, with $IC_{50}$ values $>50{\mu}g/mL$. The results suggest that benzimidazoles derivatives may have chemotherapeutic potential for treatment of both colon and breast cancers.

Autophagic Degradation of Caspase-8 Protects U87MG Cells Against H2O2-induced Oxidative Stress

  • Zhang, Yi-Bo;Zhao, Wei;Zeng, Rui-Xia
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.7
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    • pp.4095-4099
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    • 2013
  • Oxidative stress induces apoptosis in many cellular systems including glioblastoma cells, with caspase-8 activation was regarded as a major contribution to $H_2O_2$-induced cell death. This study focused on the role of the autophagic protein p62 in $H_2O_2$-induced apoptosis in U87MG cells. Oxidative stress was applied with $H_2O_2$, and cell apoptosis and viability were measured with use of caspase inhibitors or autophagic mediators or siRNA p62, GFP-p62 and GFP-p62-UBA (del) transfection. We found that $H_2O_2$-induced U87MG cell death was correlated with caspase-8. To understand the role of p62 in MG132-induced cell death, the levels of p62/SQSTM1 or autophagy in U87MG cells were modulated with biochemical or genetic methods. The results showed that the over-expression of wild type p62/SQSTM1 significantly reduced $H_2O_2$ induced cell death, but knockdown of p62 aggravated the process. In addition, inhibition of autophagy promoted p62 and active caspase-8 increasing $H_2O_2$-induced apoptosis while induction of autophagy manifested the opposite effect. We further demonstrated that the function of p62/SQSTM1 required its C-terminus UBA domain to attenuate $H_2O_2$ cytotoxity by inhibition of caspase-8 activity. Our results indicated that p62/SQSTM1 was a potential contributor to mediate caspase-8 activation by autophagy in oxidative stress process.

The Cytotoxic and Apoptotic Effect of Pseudomonas aeruginosa Exotoxin A on Human Leukemia K-562 Cells (인간 백혈병 세포에서 Psuedomonas aeruginosa exotoxin A에 대한 세포독성과 세포자멸사 효과)

  • Chang, Jeong-Hyun;Kwon, Heun-Young
    • Korean Journal of Clinical Laboratory Science
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    • v.39 no.2
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    • pp.68-75
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    • 2007
  • After reports on regression of cancer in humans and animals infected with microbial pathogens date back more than 100 years, much effort has been spent over the years in developing a wild type or attenuated bacterial and purified bacterial proteins for the treatment of cancer. Pseudomonas aeruginosa exotoxin A (ETA) is known to inhibit cell growth and trigger significant cell death in various cancer cells. Although ETA induces apoptosis of cancer cells, its exact mechanism of action is not known yet. Four different assays were performed in this study: morphological assessment of apoptotic cells, cell cytotoxity, annexin-V binding assay, and cell cycle analysis. The proliferation and survival of the K-562 cells treated with ETA were decreased in a dose dependent manner. In addition, the apoptotic body of K-562 cells was induced by ETA treatment in a dose dependent manner. The ETA-induced apoptosis was confirmed by annexin-V binding assay. Flow cytometric analysis was examined to ascertain whether ETA could arrest the cell cycle at the sub-G1 phase. Our results suggest that P. aeruginosa ETA inhibits cell growth and induces apoptosis in human leukemia K-562 cells.

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Anti-inflammatory and Anti-cancer Effects of Sterol-rich Fraction from Nannochloropsis oculata by using Saponification (해양미세조류(Nannochloropsis oculata)로부터 saponification을 통한 Sterols 분획물의 항염증 및 항암 효능 평가)

  • Kim, Junseong;Lakmal, H.H. Chaminda;Lee, Ji-Hyeok;Lee, WonWoo;Jeon, You-Jin
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.47 no.6
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    • pp.770-775
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    • 2014
  • The green microalga of the genus Nannochloropsis (class Eustigmatophyceae) is a leading candidate for biofuel production due to its ability to accumulate high oil content (28.7% of cellular ash-free dry weight). We investigated the anti-inflammatory and anticancer activities of sterol-rich fraction from nannochloropsis oculata n-hexane (NOH) extract after saponification of the microalga. Among the fractions with n-hexane, chloroform and ethyl acetate, the n-hexane fraction showed the highest anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophage as well as anticancer activity against human leukemia HL-60 cells without the cytotoxity. And the sterol-rich fraction was obtained from the n-hexane fraction by open silica column under the gradient solvent condition with 100% hexane (1L), hexane : ethyl acetate (20 : 1, 10 : 1, 5 : 1, 1 : 1, v/v). Among the four fractions (NOH-1~4), especially NOH-1 contained the highest content of sterols. NOH1 showed the highest HL-60 (about 85%) and NO inhibitory activities at the concentration of $100{\mu}g/mL$. These results demonstrated that the sterol-rich fraction from N. oculata might be a useful candidate as anti-inflammatory and anticancer agents for anti-inflammatory and anticancer activity.

Effect of LED Irradiation on Proliferation of Human Epidermal Keratinocyte for Convergence (LED조사가 인간 피부 각질세포의 증식에 미치는 융복합적인 영향)

  • Park, Jeong-Sook;Kim, Mi Hye;Lee, Jae-Hyeok
    • Journal of Digital Convergence
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    • v.14 no.11
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    • pp.639-644
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    • 2016
  • The purpose of this study is to determine the effect of the light-emitting-diode (LED) to investigate proliferation of human epidermal keratinocyte and collagen, procollagen expression. In order to determine whether LED irradiation can safely be applied to human skin, the proliferative effects of LED irradiation were determined by MTS assay in Human Epidermal Keratinocytes. Wavelength of 470nm LED irradiation increased mRNA expression of collagen, procollagen without cytotoxity. Our results suggest that 470nm LED irradiation may have a proliferative effects and collagen synthesis property. In order to determine whether LED irradiation can safely be applied to human skin, the cytotoxic effects of LED irradiation were determined by MTS assay in Human Dermal Fibroblasts (HDF). As far as we know, this is the first report demonstrating in vitro collagen synthesis activity of 470nm LED irradiation and being a scientific basis for the cosmetic.

Cytotoxicity and Physiological Activity of SunbangHwalmyung-um (선방활명음의 항암 및 항산화효과 검증)

  • Lee, Jin-Tae;Lee, Chang-Eon;Son, Jun-Ho;Lee, In-Cheol;Lee, Jin-Young;Park, Tae-Soon;Jang, Min-Jung;Song, Mi-Ae;Jee, Seon-Young;An, Bong-Jeun
    • The Korea Journal of Herbology
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    • v.20 no.3
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    • pp.51-58
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    • 2005
  • Objectives : The purpose of this research was physiological activities and investigate cytotoxicity of Sunbanghwalmyung-um extract. Methods : Physiological activity and a cytotoxicity were examined through the hot water and ethanol extracts from Sunbanghwalmyung-um and its ingredient. Results : The electron donating ability(EDA) was 66.9%, 71.3% in 1000 ppm water extract and ethanol extract. Above 90% from 1000 ppm ethanol extract showed a higher activities and it is Rhei Radix et Rhizoma, Lonicerae Flos, Gleditsiae Spina, Glycyrrhizae Radix, Myrrh. SOD-like activity was weak as 12.24%, 16.62% in 700 ppm. In water and ethanol extracts cytotoxicity were against G361, B16F10, MDA, A549, high cytotoxity over 70%. Rhei Radix et Rhizoma, Gleditsiae Spina, Trichosanthis Radix, Paeoniae Radix Rubra showed high cytotoxicity in water and ethanol extracts. Conclusions : We observed physiological activities and investigated cytotoxicity of Sunbanghwalmyung-um and its ingredients. The results also demonstrated in food or cosmetic industry.

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BIOCOMPATIBILITY OF RETROGRADE FILLING MATERIALS (역충전재의 생체적합성에 관한 연구)

  • Im, Mi-Kyung
    • Restorative Dentistry and Endodontics
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    • v.25 no.1
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    • pp.63-70
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    • 2000
  • The properties of ideal retrograde filling materials include the ability to seal the root canal system in three dimensions and well tolerated by periradicular tissues. Biocompatibility testing has been done mainly with cytotoxicity tests using cell culture. Little attention has been paid to the potential adverse influence on the inflammatory and immune reaction in the periapical tissue. The purpose of this study was to investigate the effects of retrograde filling materials on human mononuclear cells in vitro. Freshly mixed and set specimens from six materials (Z100, Tetric Ceram, Fuji II, Fuji II LC, F2000, Compoglass Flow, and ZOE) were eluated with cell culture medium for 24 hours. Cytotoxic effects of these extracts were evaluated by determining cell viability and enzyme activity using MTT and lactate dehydrogenase (LD). The production of inflammatoy bone resorptive cytokine, TNF-${\alpha}$ was measured from human peripheral blood mononuclear cells (PBMC) exposed to the extracts by means of Endogen Human TNF-${\alpha}$ ELISA kit (Wobrun, MA, U.S.A.). Eluates and diluted (1 : 10) eluates with cell culture medium from freshly mixed Fuji IT had cytotoxic effects on mononuclear cells using MTT and LD. However, eluates from set Fuji II were not cytotoxic. Eluates form set ZOE exhibited cytotoxicity with LD test. TNF-${\alpha}$ levels were high in eluates from freshly mixed Fuji II and Z100. Diluted eluates from freshly mixed Z100 and F2000 stimulated the production of TNF-${\alpha}$. However, there were no significant difference in TNF-${\alpha}$ levels compared to controls. These results indicate that some materials could possibly stimulate bone resorption in the periapical tissue by means of the production of bone resorptive cytokine.

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Immunomodulatory Effects of Fermented Curcuma longa L. Extracts on RAW 264.7 Cells (RAW 264.7 세포에서 발효 울금 추출물의 면역조절 효과)

  • Yoo, Seon A;Kim, Ok Kyung;Nam, Da-Eun;Kim, Yongjae;Baek, Humyoung;Jun, Woojin;Lee, Jeongmin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.2
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    • pp.216-223
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    • 2014
  • Curcuma longa L. (CL) is a well known traditional medicinal plant that is also used in curries and mustards as a coloring and flavoring agent. However, CL is not usually used as a food source due to its bitter taste. We investigated the immunomodulatory effect of CL fermented by Aspergillus oryzae (FCL) on RAW 264.7 cells. FCL was extracted with cold water (CW), hot water (HW), 20% ethanol (20% EtOH) and 80% ethanol (80% EtOH), after which its effects on phagocytic activity, tumor necrosis factor-alpha (TNF-${\alpha}$), nitric oxide (NO) production, natural killer (NK) cell activity and mRNA expression of LP-BM5 eco were investigated. Phagocytic activity was increased in HW and 20% EtOH when compared to the control. The secretion of nitric oxide (NO) from RAW 264.7 cells did not change significantly relative to the control. However, TNF-${\alpha}$ was significantly increased by the addition of FCL extracts. Moreover, FCL 20% ethanol extract showed a four fold increase in NK cell cytotoxity relative to the control group. Finally, we observed suppressed mRNA expression of LP-BM5 eco in FCL extracts, especially in the 20% ethanol extracts group. These results indicate that the FCL extracts can be used as a functional material due to their effective immunomodulating activities.

Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex (새로운 Platinum (II) Complex [Pt (II)(trans-d-dach)(DPPE)] $(NO_3)_2$의 항암효과 및 신독성에 관한 연구)

  • Jung Jee-Chang;Lee Moon-Ho;Chang Sung-Goo;Rho Young-Soo
    • The Korean Journal of Pharmacology
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    • v.31 no.1 s.57
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    • pp.103-114
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    • 1995
  • Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (Ⅱ) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,2-bis(diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(trans-ddach)(DPPE).$2NO_3(PC)$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC demonstrated acceptable antitumor activity aganist P388, L-1210 lymphocytic leukemia cells and SK=OV3 human ovarian adenocarcinoma cells, and significant. activity as compared with that. cisplatin. The toxicity of PC was found quite less than thar of cisplatin using MTT, $[^3H]$ thymidine uptake and glucose consumption tests in rabbit proximal tubule cells, human kidney cortical cells and human renal cortical tissues. Based on these results, this novel platinum compound represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low toxicity.

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Cytotoxity and Antimicrobial Effects of the Extract of Poncirus trifoliata (지실 추출물의 세포독성과 항균효과)

  • Yang Hyun-Ok;Oh Hyun-Ju;Park Nang-Kyu;Choi Eun-Young;Lee Hyun-Ok;Yang Eun-Yeong;Chun Hyun-Ja;Chung Soon-Ryang;Lee Kang-Min;Baek Seung-Hwa
    • Journal of Society of Preventive Korean Medicine
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    • v.4 no.2
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    • pp.235-241
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    • 2000
  • This study was carried out to evaluate cytotoxic effects of Poncirus trifoliata Raf. extract on lymphocytic leukemia tumor (L1210) cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay The comparison of Ic50 Values of Poncirus trifoliata Raf. extract in L1210 cell lines showed that their susceptibility to these fractons decreased in the following order: adriamycin > Fr.4> Fr. 6> Fr. 5> Fr. 3> Fr. 1> Fr. 2 by the MTT assay. In order to develop an antumicrobial agent, Poncirus trifoliata Raf. was extracted wit ethanol, and then it was fractionated with several mobile phase. The antitumor activities of fractions of the ethanol soluble extract was investigated. The minimal inhibitory concentrations (MIC) of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. against microorganisms were also examined. Antimicrobial activities of ampicillin and ketoconazole as references were compared to those of fractions of the ethanol soluble extract of Poncirus trifoliata Raf. The antimicrobial activities of all fractions from the extract had growth inhibition activities against gram-positive bacteria, gram-negative bacteria and fungi $(MIC\;>\;200{\mu}g/ml)$. These results suggest that fraction 4 of the ethanol soluble extract of Poncirus trifoliata Raf. possessed the most antitumorous agent.

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