• Title/Summary/Keyword: Cytotoxic Effect

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Celecoxib, a COX-2 Selective Inhibitor, Induces Cell Cycle Arrest at the G2/M Phase in HeLa Cervical Cancer Cells

  • Setiawati, Agustina
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.4
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    • pp.1655-1659
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    • 2016
  • Celecoxib, a selective inhibitor of COX-2, showed cytotoxic effects in many cancer cell lines including cervical cancer cells. This study investigated the effect of celecoxib on cell cycle arrest in HeLa cervical cancer cells through p53 expression. In vitro anticancer activity was determined with the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) method. A double staining method was applied to investigate the mechanism of cell death, cell cycling was analyzed by flow cytometryand immunocytochemistry was employed to stain p53 expression in cells. Celecoxib showed strong cytotoxic effects and induced apoptosis with an $IC_{50}$ value of $40{\mu}M$. It induced cell cycle arrest at G2/M phase by increasing level of p53 expression on HeLa cells.

Induction of Apoptosis with Moringa oleifera Fruits in HCT116 Human Colon Cancer Cells Via Intrinsic Pathway

  • Guon, Tae-Eun;Chung, Ha Sook
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.227-234
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    • 2017
  • Moringa oleifera Lam (M. oleifera, Moringaceae) is a tree of the Moringaceae family that can reach a height of between 5 and 10 m. The current paper presents cytotoxic effect of M. oleifera fruits and its flavonoids 1 and 2. The viability of HCT116 human colon cancer cells were 38.5% reduced by $150{\mu}g/mL$ of ethanolic extracts in a concentration-dependent manner; in addition, we observed the apoptotic features of cell shrinkage and decreased cell size. Bcl-2 family proteins were regulated as determined by Western blotting analysis, suggesting that M. oleifera fruits and their flavonoids 1 and 2 induced apoptosis through an intrinsic pathway. Based on our findings, 70% ethanolic extracts of M. oleifera fruits and flavonoids 1 and 2 might be useful as cytotoxic agents in colorectal cancer therapy.

2- or 6-(1-Azidoalkyl)-5,8-Dimethoxy-1,4-Napyhthoquinone: Synthesis, Evaluation of Cytotoxic Activity, Antitumor Activity and Inhibitory Effect on DNA Topoisomerase-I

  • Chae, Gyu-Han;Song, Gyu-Yong;Kim, Yong;Cho, Hoon;Sok, Dai-Eun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.22 no.5
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    • pp.507-514
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    • 1999
  • 6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2-an 6-(1-azidoalkyl)-DMNQ derivatives.

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Synthesis and Structure-activity Relationship of Cytotoxic $5,2^I,5^I$-Trihydroxy-7,8-dimethoxyflavanone Analogues

  • Min, Byung-Sun;Ahn, Byung-Zun;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.543-550
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    • 1996
  • Analogues of $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone, a naturally-occurring compound, which had been reported to have potent antitumor activity, were synthesized and examined for the cytotoxicity against three cancer cell lines. Among the intermediate chalcones and synthetic 5-hydroxy-7, 8-dimethoxyflavanone analogues, $({\pm})2^{l}, 5^{l}-dibenzyloxy-5, 7, 8-trimethoxyflavanone$ exhibited about 2-8 times stronger activity than $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone against L1210, K562 and A549 cancer cell lines. In the structure-activity relationship, it is suggested that among analogues of 5-hydroxy-7, 8-dimethoxyflavanone, the existence of two oxygenated groups of para-relation at $C-2^{I} and C-5^{I}$ positions on flavanone B-ring, may be necessary to exhibit effective cytotoxic activity.

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Cytotoxic Constituents of Diadema setosum

  • Minh, Chau-Van;Kiem, Phan-Van;Huong, Le-Mai;Kim, Young-Ho
    • Archives of Pharmacal Research
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    • v.27 no.7
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    • pp.734-737
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    • 2004
  • 5,8-Epidioxycholest-6-en-3-ol (1), cholesterol (2), glycerol 1-palmitate (3) and glycerol 1,3-dioleate-2-stearate (4) were isolated from the methanol extract of the sea urchin Diadema setosum, which was collected from the Halong sea, Vietnam. Chemical structures were established based on extensive 1D, 2D-NMR, FAB-MS, EI-MS spectroscopic data and GC-MS analysis. The NMR spectral data of compound 1 were reassigned by using HMQC and HMBC. Compound 1 was found to have strong cytotoxic effect against various cancer cell lines, such as KB ($IC_{50}$, 2.0 $\mu\textrm{g}$/mL), FL($IC_{50}$, 3.93 $\mu\textrm{g}$/mL), and Hep-2 ($IC_{50}$, 2.4 $\mu\textrm{g}$/mL) by in vitro assay.

Cytotoxic Effects of Hydrolysable Tannins from Some Euphorbia Plants on the Human Tumor Cell Lines (유포르비아속 식물로부터 단리한 가수분해형 탄닌의 인체고형암 세포에 대한 세포독성효과)

  • Lee, Seung-Ho;Park, Ji-Soo;Kim, So-Young;Chung, See-Ryun;Choi, Sang-Un
    • YAKHAK HOEJI
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    • v.41 no.4
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    • pp.524-529
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    • 1997
  • Seventy three hydrolysable tannins and related compounds were isolated from seven Euphorbia plants. Among them, 28 compounds including nine gallotannins, eleven ellagitannins and eight related compounds were selected according to the structural similarity. Cytotoxicity of them on the human tumor cell lines including A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 were evaluated by the SRB method in vitro. 3,4,6-Tri-O-galloyl-D-glucose was shown to exhibit most potent cytotoxic effect($4.4{\mu}g/ml).

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THE EFFECT OF KOREAN RED GINSENG SAPONIN ON THE ALKALINE PHOSPHATASE ACTIVITY OF RAT OSTEOBLASTIC CELL(ROS17/2.8) IN CULTURE (한국 홍삼사포닌이 배양중인 쥐 조골세포의 염기성 인산분해효소 활성도에 미치는 영향)

  • Jung, Jin-Kwang;Kim, Jung-Keun;Lee, Jae-Hyoun
    • Journal of Periodontal and Implant Science
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    • v.25 no.3
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    • pp.694-702
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    • 1995
  • Using the Korean red ginseng saponin, which is known to world-wide and thd effects of it have been investigated by many reserachers for years. Ginseng saponin, one of the major components of Korea ginseng root, has many various biologic effects, such as cytotoxic effect, tumorcidal activity, protein biosynthesis and membrane modifying effect. The purpose of this study was to evaluate effects of ginseng saponin on the alkaline phosphatase activity of ROS cells in culture. After ROS cells were seeded into a 96-well plate, 96-well plate cultured until confluence was obtained. To evaluate cytotoxic effect of total saponin in cultured ROS cells, the plates were added to each total saponin concentration (0-1mg/ml). After 48hr., cells were counted by stain with 0.2% trypan blue at randomly selected field microscopically. Also, to evaluate alkaline phosphatase(ALP) activity of total saponin in cultured ROS cell, the plate was added to each total saponin concentration (0-1mg/ml) and ALP activity was assayed. To evaluate time-course of ALP activity, $31.25{\mu}g/ml$ of saponin added to 96-well plate. After culture of 6, 12, 24 and 48hr., ALP activity test was performed. To evaluate effect of cycloheximide in ALP activity, 96-well plate was added to saponin and cycloheximide. In control group, the plate was added saponin only. The results were as follows. 1. After the various concentration of total saponin was added in the medium, 500 and $1000{\mu}g/ml$ of total saponin showed cytotoxic effect of ROS(P<0.005). 2. In contrast to control group, 7.6, 15.6, 31.25, 62.5 and $250{\mu}g/ml$ of total saponin increased ALP activity significantly. 3. Otherwise, 500 and $1000{\mu}g/ml$ of total saponin decreased ALP activity significantly(P<0.005). 4. As the time span increases, $31.25{\mu}g/ml$ of total saponin increased ALP activity. 5. Cycloheximide decreased saponin-indueced ALP actitity in ROS(P<0.005). These results suggest that Ginseng total saponin stimulates the ALP activity of rat osteoblastic cells.

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Production and Characterization of Physiological Properties of Carotenoid from a Marine Bacterium Curtobacterium sp. (해양미생물로부터 Carotenoid의 생산 및 그 생리활성)

  • r김종덕;강동수;김민용;최명락;임현수;백승한;서효진;김대현;공재열
    • KSBB Journal
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    • v.15 no.6
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    • pp.621-629
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    • 2000
  • A marine bacterium producing carotenoid was isolated from the Yosu coastal area of South Korea, and has been recorded as MCPBK-1. It was identified as Curtobacterium sp.. The optimum conditions of marine carotenoid fermentation from Cutobacterium sp. were pH 7.0, a temperature of $25^{\circ}C$, 4 mM fructose as a carbon source, 0.07% tryptone as a nitrogen source, 0.5 mM $M^{+2}$ ion as a mineral source and $1{\;}\mu\textrm{M}$ of cyanocobalamine as a growth factor in a $7{\;}\ell$ jar-fermentor. 13.0 mg/ml of the marine carotenoid were produced under optimum conditions. The crude marine carotenoid isolated was composed of 5 different compounds, i.e : tunaxanthin(86.6%), diatoxanthin (7.1%), ${\beta}-carotene$ (2.1%), canthaxanthin(1.9%) and cynthiaxanthin (1.9%). Physiological properties including antibacterial activity, cytotoxic effect, antioxidative effect and free radical scavenging activity were characterized with the crude carotenoid, which exhibited no antibacterial activity against E. coli and Lactobacillus bulgaricus, but a strong cytotoxic effect against cancer cells such as HepG2 (Hepatocellular carcinoma, human, ATCC HB-8065) and HeLa (Cervical carcinoma, human, ATCC CCL-2) cells, the ratios of impediment were 86.4% and 39.2%, respectively. This carotenoid, also, expressed a strong antioxidative effect (83%) against CCL-13 (diploid, monotypic hepatocyte, human, ATCC CCL-13) and exhibited free radical scavenging activity (43.4%) when using at a concentration of $50{\;}\mu\textrm{g}/ml$ of the crude carotenoid.

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Effect of Curcuma longa L. Extract on the Melanin Accumulation and Expression of Skin Fibril Proteins (울금(鬱金) 추출물의 미백 활성 및 진피 섬유구조 단백질에 미치는 효과)

  • Kim, Hae Ok
    • The Korea Journal of Herbology
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    • v.34 no.2
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    • pp.75-82
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    • 2019
  • Objectives : In this study, various biological effects of Curcuma longa L. have been studied, however, beneficial effect of Curcuma longa L. in skin health remain still unclear. In this study, Curcuma longa L. water extract (CLE) was prepared. Inhibitory effect of CLE on melanin accumulation of B16F10 cells and expression levels of skin fibril-related proteins of human skin fibroblasts (HSF) were evaluated. Methods : The cytotoxic effect of CLE in B16F10 cells and HSF were examined by MTT assay. Inhibitory effect of CLE on the ${\alpha}-MSH-$ and IBMX-induced melanin accumulation and tyrosinase activity were evaluated in B16F10 cells. The expression levels of connective tissue growth factor (CCN2), Smad2, procollagen $1{\alpha}2$, collagen $1{\alpha}2$, and fibronectin in CLE-treated HSF were analyzed by western blotting. Results : The CLE treatment (concentrations 10 to $400{\mu}g/ml$) for 72 h did not affect to the B16F10 viability. However, 200 and $400{\mu}g/ml$ of CLE treatment for 24 h showed cytotoxic effect in HSF. Therefore, the concentrations 10, 50, and $100{\mu}g/ml$ of CLE were chosen in this study. The CLE treatment for 72 h dose dependently and significantly suppressed melanin accumulation and tyrosinase activity of B16F10 cells. In addition, the CLE treatment up-regulated expression levels of skin fibril-related proteins such as CCN2, Smad2, procollagen $1{\alpha}2$, collagen $1{\alpha}2$, and fibronectin. Conclusions : In conclusion, these results suggest that the CLE could be used as a natural material for skin health.

Inhibitory Effect of Paeoniflorin on Fos-Jun-DNA Complex Formation and Stimulation of Apoptosis in HL-60 Cells

  • Kwon, Hae-Young;Kim, Kyoung-Su;Park, Se-Yeon;Lee, Dug-Keun;Yang, Chul-Hak
    • BMB Reports
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    • v.34 no.1
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    • pp.28-32
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    • 2001
  • The Fos-Jun heterodimers are part of the regulatory network of gene expression and nuclear proteins encoded by proto-oncogenes. The activation of Fos-Jun is important in the transmission of the tumor-promoting signal from the extracellular environment to the nuclear transcription mechanism. To search for the inhibitors of the Fos-Jun DNA complex formation, several natural products were screened and water-soluble paeoniflorin reduced the binding activity of the Fos-Jun heterodimer. This active compound was purified by silica gel column chromatography and HPLC. The electrophoresis mobility shift assay and reverse-phase HPLC test showed that paeoniflorin reduced the AP-l function. The cytotoxic effect of paeoniflorin was observed in HL-60. These results indicate that paeoniflorin blocks the Fos-Jun heterodimer-binding site of the AP-l DNA and it also has cytotoxic effects on human leukemia cell lines.

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