• Title/Summary/Keyword: cell growth inhibition

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Evaluation of Cytotoxicity Effects of Chalcone Epoxide Analogues as a Selective COX-II Inhibitor in the Human Liver Carcinoma Cell Line

  • Makhdoumi, Pouran;Zarghi, Afshin;Daraei, Bahram;Karimi, Gholamreza
    • Journal of Pharmacopuncture
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    • v.20 no.3
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    • pp.207-212
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    • 2017
  • Objectives: Study of the mechanisms involved in cancer progression suggests that cyclooxygenase enzymes play an important role in the induction of inflammation, tumor formation, and metastasis of cancer cells. Thus, cyclooxygenase enzymes could be considered for cancer chemotherapy. Among these enzymes, cyclooxygenase 2 (COX-2) is associated with liver carcinogenesis. Various COX-2 inhibitors cause growth inhibition of human hepatocellular carcinoma cells, but many of them act in the COX-2 independent mechanism. Thus, the introduction of selective COX-2 inhibitors is necessary to achieve a clear result. The present study was aimed to determine the growth-inhibitory effects of new analogues of chalcone epoxide as selective COX-2 inhibitors on the human hepatocellular carcinoma (HepG2) cell line. Methods: Estimation of both cell growth and the amount of prostaglandin E2 (PGE2) production were used to study the effect of selective COX-2 inhibitors on the hepatocellular carcinoma cell. Cell growth determination has done by MTT assay in 24 h, 48 h and 72 h, and PGE2 production has estimated by using ELYSA kit in 48 h and 72 h. Results: The results showed growth inhibition of the HepG2 cell line in a concentration and time-dependent manner, as well as a reduction in the formation of PGE2 as a product of COX-2 activity. Among the compounds those analogues with methoxy and hydrogen group showed more inhibitory effect than others. Conclusion: The current in-vitro study indicates that the observed significant growth-inhibitory effect of chalcone-epoxide analogues on the HepG2 cell line may involve COX-dependent mechanisms and the PGE2 pathway parallel to the effect of celecoxib. It can be said that these analogues might be efficient compounds in chemotherapy of COX-2 dependent carcinoma specially preventing and treatment of hepatocellular carcinomas.

Inhibition of Growth and Collagenase Activity of the Extract from Salvia miltiorrhiza against Microorganisms Causing Periodontal Diseases (단삼(Salvia miltiorrhiza) 추출물의 치주질환유발 세균의 생육억제 및 Collagenase 저해 활성)

  • 민응기;김용해;금상일;한영환
    • Korean Journal of Microbiology
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    • v.40 no.2
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    • pp.111-114
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    • 2004
  • This study was carried out to evaluate the inhibition of growth and collagenase activity of Salvia miltiorrhiza Bunge against microorganisms causing periodontal diseases. The ethanol extract of Salvia miltiorrhiza showed sig-nificant growth inhibition against microorganisms causing periodontal diseases. Ethanol extract was further fractionated with organic solvents in the order of hexane, chloroform and ethyl acetate. Among the fractions tested, the hexane fraction showed the highest cell growth inhibition. The minimal inhibitory concentration (MIC) of the extract against C. curvus, C. rectus, E. corrodens, F nucleatum, P. gingivalis, P. intermedia and W. succinogenes were 200, 50, 50, 250, 150, 250 and 200 ${\mu}g$/ml, respectively. The inhibition of collagenase activity by organic solvent fractions were higher than that of minocycline, and the inhibition ratio of collagenase activity was $88.2{\pm}2.1$ % in the chloroform fraction.

Growth Inhibition of Escherichia coli during Heterologous Expression of Bacillus subtilis Glutamyl-tRNA Synthetase that Catalyzes the Formation of Mischarged Glutamyl-$tRNA_{l}$$^{Gln}$

  • Baick, Ji-Won;Yoon, Jang-Ho;Suk Namgoong;Dieter Soll;Kim, Sung-Il;Eom, Soo-Hyun;Hong, Kwang-Won
    • Journal of Microbiology
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    • v.42 no.2
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    • pp.111-116
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    • 2004
  • It is known that Bacillus subtilis glutamyl-tRNA synthetase (GluRS) mischarges E. coli $tRNA_{1}$$^{Gln}$ with glutamate in vitro. It has also been established that the expression of B. subtilis GluRS in Escherichia coli results in the death of the host cell. To ascertain whether E. coli growth inhibition caused by B. subtilis GluRS synthesis is a consequence of Glu-$tRNA_{1}$$^{Gln}$ formation, we constructed an in vivo test system, in which B. subtilis GluRS gene expression is controlled by IPTG. Such a system permits the investigation of factors affecting E. coli growth. Expression of E. coli glutaminyl-tRNA synthetase (GlnRS) also amelio-rated growth inhibition, presumably by competitively preventing $tRNA_{1}$$^{Gln}$ misacylation. However, when amounts of up to 10 mM L-glutamine, the cognate amino acid for acylation of $tRNA_{1}$$^{Gln}$, were added to the growth medium, cell growth was unaffected. Overexpression of the B. subtilis gatCAB gene encoding Glu-$tRNA^{Gln}$ amidotransferase (Glu-AdT) rescued cells from toxic effects caused by the formation of the mis-charging GluRS. This result indicates that B. subtilis Glu-AdT recognizes the mischarged E. coli Glu-$tRNA_{1}$$^{Gln}$, and converts it to the cognate Gln-$tRNA_{1}$$^{Gln}$ species. B. subtilis GluRS-dependent Glu-$tRNA_{1}$$^{Gln}$ formation may cause growth inhibition in the transformed E. coli strain, possibly due to abnormal protein synthesis.

Antiproliferative Effect of RST Associated with the Inhibition of Cyclooxygenase-2 Expression and Prostaglandin E2 Release in Human Lung Carcinoma Cells (산두근 추출물이 인체폐암세포의 COX-2 발현 및 PGE2 생성에 미치는 영향)

  • Kim, Kang-Tae;Eom, Hyun-Sup;Chi, Gyoo-Yong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.21 no.4
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    • pp.907-915
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    • 2007
  • In this study the effect of water extract of Sophora tonkinensis Gapnep (RST) was investigated on the growth of human lung carcinoma A549 cells. Exposure of A549 cells to RST resulted in the growth inhibition in a dose-dependent manner as measured by MTT assay. The antiproliferative effect by RST treatment in A549 cells was associated with morphological changes such as membrane shrinking and cell rounding up. RST treatment did not induce the cell cycle arrest and the levels of tumor suppressor p53 as well as cyclin-dependent kinase inhibitor p21(WAF1/CIP1). It was found that RST treatment decreased the levels of cyclooxygenase (COX) -2 mRNA and protein expression without significant changes in the expression of COX-1 and inducible nitric oxide synthase (iNOS), which was correlated with a decrease in prostaglandin E2 (PGE2) synthesis. RST treatment also slightly inhibited the levels of human telomerase reverse transcriptase (hTERT) mRNA and protein expression, and the activity of telomerase. Taken together, these findings suggested that RST-induced inhibition of human lung carcinoma A549 cell growth was aoosciated with the inhibition of COX-2 expression and PGE2 production. These results provided important new insights into the possible molecular mechanisms of the anti-cancer activity of RST.

Resveratrol Anglog 3,5,2',4'-Tetramethoxy-trans-stilbene, Potentiates the Inhibotion of Cell Growth and Induces Apoptosis in Human Cancer Cells

  • Nam, Kyung-Ae;Kim, Sang-hee;Heo, Yeon-Hoi;Lee, Sang-Kook
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.441-445
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    • 2001
  • Resveratrol, a trihydroxystilbene found in grapes and several plants, has been shown to be active in inhibiting multistage carcinogenic process. Using resveratrol as the prototype, we synthesized several analogs and evaluated their growth inhibitory effect using cultured human cancer cells. In the present report we show that one of the resveratrol analogs, 3, 5,2',4'-tetramethoxy-trans-stilbene, potentiated the inhibition of cancer cell growth. Prompted by the strong growth Inhibitory activity of the compound ($IC_{50}$; $0.8{\mu}$ g/ml) compared to resveratrol ($IC_{50}$; $18{\mu}$ug/ml) in cultured human colon cancer cells (Col2), we performed an action mechanism study using the compound. The compound induced the accumulation of cellular DNA contents in the sub-CO phase DNA contents of the cell cycle by in a time-dependent manner. The morphological changes were also consistent with an apoptotic process. This result indicated that the compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.

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A Study of Mode of Action of Fluazifop-butyl- II. Fluazifop-butyl Effect on Cell Division, Cell Enlargement, and Protein Synthesis in Oat(Avena sativa L.) Roots (Fluazifop-butyl의 제초기구(除草機構)에 관한 연구(硏究)- 제2보(第II報) Fluazifop-butyl이 귀리뿌리의 세포분열(細胞分裂), 세포신장(細胞伸張) 및 단백질합성(蛋白質合成)에 미치는 영향(影響))

  • Kim, Jae-Cheol
    • Korean Journal of Weed Science
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    • v.6 no.2
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    • pp.168-173
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    • 1986
  • The effects of varying concentrations and duration of fluazifop-butyl [(${\pm}$)-butyl [2- [4- [(5-(trifluoro methyl)-2-pyridinyl] oxy] phenoxy] propanate] treatment on cell division, cell enlargement, and protein synthesis were studied. Oat (Avena staiva L.) were treated from 0 to 48 hr with concentration ranging from $1{\times}10^{-6}M$ to $1{\times}10^{-3}M$ of fluazifop-butyl in the cell division study. There was a significant reduction in the mitotic indices of oat roots treated with $1{\times}10^{-4}M$ after 6 hr. After 18 hr treatment, All herbicide treatment inhibited cell division significantly. After 24 hr treatment almost 100% inhibition of cell division occurred at $1{\times}10^{-4}M$ to $1{\times}10^{-3}M$ while 20% inhibition of cell division occurred at $1{\times}10^{-6}M$ concentration at same exposure period. The greatest inhibition of cell division occurred between 0 to 18 hr. The avena coleoptile straight- growth test were used to determine the influence of fluazifop-butyl on eoleoptile growth. Significant inhibition of elongation of oat coleoptiles were observed at $1{\times}10^{-7}M$ to $1{\times}10^{-3}M$ after 24 hr incubation. Protein incorporation study showed that the $1{\times}10^{-4}M$ of fluazifop-butyl caused 60% inhibition of protein synthesis. It was concluded that the growth of inhibition of plants caused by fluazifop-butyl results from inhibition of cell division, cell enlargement, and protein synthesis.

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Antitumor Activity of Gamdutang Aqua-Acupuncture Solution (감두약침액의 암세포 성장 저해 효과)

  • 조경희;한상훈;임종국;손윤희;이임태;남경수
    • Journal of Life Science
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    • v.9 no.6
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    • pp.677-683
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    • 1999
  • Gamdutang aqua-acupuncture solution (GAS), Gamdutang water-extracted solution (GWS) and Dae-Gamdutang aqua-acupuncture solution (DGAS) were prepared and tested for antitumor activities. It was shown to possess considerable toxicity toward various tumor cell lines. Concentration of 5 $\times$ and 10$\times$ of GAS resulted in more than 70% inhibition of growth in Ehrlich ascites tumor cells (EATC), Hepa1c1c7 and A549. GAS at concentrations of 5$\times$ and 10$\times$ revealed more than 60% inhibition in HeLa. GWS showed more than 50% inhibition of growth with EATC and HeLa at concentrations of 5$\times$ and 10$\times$, respectively. Toxicity assay with GWS in Hepa1c1c7 and A549 revealed that more than 80% inhibition of growth at the concentration of 5$\times$ and 10$\times$. In morphological study, the number of cells were decreased, and the shape of cells was round-form in EATC, Hepa1c1c7, A549, HeLa with GAS.

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Immunostimulation Effects of Cell Wall Components Isolated from Lactobacillus plantarum

  • TAE BOO CHOE;KANG, KWAN YUEB;SUNG HO PARK
    • Journal of Microbiology and Biotechnology
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    • v.4 no.3
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    • pp.195-199
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    • 1994
  • Immunostimulation effects of the cell wall components isolated from Lactobacillus plantarum were investigated by studying the macrophage s tumorcidal activity, splenocyte proliferation, anticomplementary activity and the inhibition of peritoneal tumor cell growth measured with ICR mice inoculated with sarcoma 180. The immunopotentiating cell wall components were a complex of peptidoglycan and exopolysaccharides. The tumorcidal activity of macrophage against Yacl and B16 tumor cells was enhanced when the cell wall components were added into the macrophage s culture medium. They also stimulated splenocytes to proliferate up to the same level as when the concanavalin A was added into the splenocyte's culture medium. The complementary activity was inhibited by 50% when the cell wall components were incubated with the sheep red blood cells treated with hemolysin and guinea pig complement. This result confirmed that the cell wall components had an antitumor effect, because the anticomplementary activity is usually accompanied by an antitumor activity at the same time. This fact was confirmed again by the inhibition of the growth of sarcoma 180 when the cell wall components were injected intraperitoneally into ICR mice inoculated with sarcoma 180. As a result, it is concluded that the cell wall components isolated from Lactobacillus plantarum had multifunctional immunostimulation effects in vitro and in vivo.

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Melittin Inhibits Human Prostate Cancer Cell Growth through Induction of Apoptotic Cell Death

  • Park Hye-Ji;Lee Yong-Kyung;Song Ho-Seub;Kim Goon-Joung;Son Dong-Ju;Lee Jae-Woong;Hong Jin-Tae
    • Toxicological Research
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    • v.22 no.1
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    • pp.31-37
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    • 2006
  • It was previously found that melittin inhibited $NF-{\kappa}B$ activity by reacting with signal molecules of $NF-{\kappa}B$ which is critical contributor in cancer cell growth by induction of apoptotic cell death. We here investigated whether melittin inhibits cell growth of human prostate cancer cells through induction of apoptotic cell death, and the possible signal pathways. Melittin ($0{\sim}1\;{\mu}g/ml$) inhibited prostate cancer cell growth in a dose dependent manner. Conversely related to the growth inhibitory effect, melittin increased the induction of apoptotic cell death in a dose dependent manner. Melittin also inhibited DNA binding activity of $NF-{\kappa}B$, an anti-apoptotic transcriptional factor. Consistent with the induction of apoptotic cell death and inhibition of $NF-{\kappa}B$, melittin increased the expression of pro-apoptotic proteins caspase-3, and Bax but down-regulated anti-apoptotic protein Bcl-2. These findings suggest that melittin could inhibit prostate cancer cell growth, and this effect may be related with the induction of apoptotic cell death via inactivation of $NF-{\kappa}B$.

Quantitative Analysis of Bergenin in Astilbe rubra and Growth Inhibition Effect of Ethanol Extract on Hela Cells (노루오줌으로부터 Bergenin의 함량 분석 및 에탄올 추출물의 자궁경부암세포 성장 억제 효과)

  • Kim, A Hyeon;Nho, Jong Hyun;Woo, Kyeong Wan;Gang, Ju Eun;Sim, Mi Ok;Kim, Min Suk;Ham, Seong Ho;Cho, Hyun Woo
    • Korean Journal of Pharmacognosy
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    • v.49 no.1
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    • pp.47-54
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    • 2018
  • Astilbe rubra (AR) is a perennial, belongs to the Saxifragaceae family, it contains tannin and triterpene. AR has been used in republic korea to improve toxication, fever, pain and convulsion. Recently, number of natural products have been analyzed for potential pharmacological activities including anti-cancer, anti-obesity and anti-diabetic medication. Consequently, we investigated the growth inhibition effect of Astilbe rubra water extract (WAC), ethanol extract (EAC) and bergenin on Hela cell (human adenocarcinoma cell). From whole plant of A. rubra, bergenin was isolated by column chromatography and its structures were identified by $^1H$, $^{13}C$ NMR and IT TOF-ESI MS. High extraction efficiency of bergenin was shown at 0.95% under 60 min reflux extraction with 50% MeOH. The MTS assay showed that EAC (ethanol extract) treatment increased cell death in a dose-dependent manner. Moreover, EAC treatment on Hela cell increased apoptotic cell death and caspase-3 activity. Results suggest that EAC has growth inhibition effect on Hela cells, but not WAC and bergenin. $500{\mu}g/mL$ EAC treatment inhibited Hela cell at $60.2{\pm}1.5%$.