• Title/Summary/Keyword: 2D cell lines

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Evaluation of Anticancer Activity of Curcumin Analogues Bearing a Heterocyclic Nucleus

  • Ahsan, Mohamed Jawed
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.4
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    • pp.1739-1744
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    • 2016
  • We report herein an in vitro anticancer evaluation of a series of seven curcumin analogues (3a-g). The National Cancer Institute (NCI US) Protocol was followed and all the compounds were evaluated for their anticancer activity on nine different panels (leukemia, non small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer) represented by 60 NCI human cancer cell lines. All the compounds showed significant anticancer activity in one dose assay (drug concentration $10{\mu}M$) and hence were evaluated further in five dose assays (0.01, 0.1, 1, 10 and $100{\mu}M$) and three dose related parameters $GI_{50}$, TGI and $LC_{50}$ were calculated for each (3a-g) in micro molar drug concentrations (${\mu}M$). The compound 3d (NSC 757927) showed maximum mean percent growth inhibition (PGI) of 112.2%, while compound 3g (NSC 763374) showed less mean PGI of 40.1% in the one dose assay. The maximum anticancer activity was observed with the SR (leukemia) cell line with a $GI_{50}$ of $0.03{\mu}M$. The calculated average sensitivity of all cell lines of a particular subpanel toward the test agent showed that all the curcumin analogues showed maximum activity on leukemia cell lines with $GI_{50}$ values between 0.23 and $2.67{\mu}M$.

Cytotoxic Polyacetylenes from Aralia cordata (독활의 세포독성 폴리아세틸렌 성분)

  • 박신영;김진웅
    • YAKHAK HOEJI
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    • v.39 no.6
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    • pp.681-688
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    • 1995
  • An n-hexane extract of the roots of Aralia cordata Thunb. (Araliaceae) was found to show significant in vitro cytotoxic activity against P388D$_{1}$ lymphocytic leukemia cell in culture. Bioactivity-directed fractionation of this extract led to the isolation of four polyacetylenes, falcarindiol (1), dehydrofalcarindiol (2), falcarindiol-8-acetate (3) and dehydrofalcarindiol-8-acetate (4). Cytotoxicity of compounds 1 and 3 was found to be better than that of compounds 2 and 4 when these compounds were tested against eight in vitro tumor cell lines, namely, A549, HCT15, DLD1, MCF7, SKOV3, HL60, K562 and P388D$_{1}$. The fact that the cytotoxicity of compounds 1 and 3 against series of tumor cell lines was much stronger than that of compounds 2 and 4 suggested that the saturated carbon chain at the termial and the hydroxyl group at the C-3 are important for the activities. The requirement for the activity was further confirmed by synthesizing and assaying the acetate derivatives of compounds 1 and 2.

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Growth Inhibition of Polysaccharide Fraction in Cell Wall Components from Enterococcus faecalis 2B4-1 against Tumor Cell Lines (Enterococcus faecalis 2B4-1 세포벽 성분 중 Polysaccharide Fraction의 종양세포 증식억제 효과)

  • Park, Sang-Jin;Kim, Jeong-Hwan;Lee, Kyung-Ho;Yang, Jong-Beom;Baek, Young-Jin;Kim, Chang-Han
    • Microbiology and Biotechnology Letters
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    • v.27 no.1
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    • pp.8-14
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    • 1999
  • This study was developed to evaluate the growth inhibition effects of cell wall components of Enterococcus faecalis 2B4-1 obtained from feces of neonates against tumor cell lines. Polysaccharide fraction (PS) shown sensitive growth inhibition effect in the cell wall components was isolated and characterized. In growth inhibition effects, residue fractin of whole cell was shown sensitive level of percent survival about 30% when administrated at ehe concentration of 100${\mu}$g/ml, and that was more effective than that of supernatant fraction against the tumor cell lines, SNU-1, 3LL, FARROW and HEC-1-B. Sensitive growth inhibition effects against SNU-1, FARROW and HEC-1-B were performed by whole cell (WC) fraction from Ent. faecalis 2B4-1. Cytoplasm fractin (CP) of WC was shown non-inhibition effect, however, the other part of WC, precipitate of disrupted cell (PD), was sensitive against the tumor cell line mentioned above. Followed by separation to peptidoglycan fraction (PG) and polysaccharide fraction (PS) were all sensitive which the latter was shown more sensitive percent survival than the former. Composed sugars of polysaccharide fraction were determined to D-glucose, L-rhamnose and D-glucosamine, and the rate fo composition was calculated to about 1:1:1 by the data of elemental analysis, IR, TLC and HPLC.

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Cytotoxic Lactones from the Pericarps of Litsea japonica

  • Ngo, Quynh-Mai Thi;Cao, Thao Quyen;Woo, Mi Hee;Min, Byung Sun
    • Natural Product Sciences
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    • v.25 no.1
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    • pp.23-27
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    • 2019
  • From the pericarps of Litsea japonica (Thunb.) Jussieu, eighteen butanolide derivatives (1 - 18) were evaluated for their cytotoxic activity against HeLa, HL-60, and MCF-7 cells. Compounds 1-9 with 2-alkylidene-3-hydroxy-4-methylbutanolides structure exhibited cytotoxic activities against cancer-cell lines. Among them, compound 8 (litsenolide $D_2$) exhibited the most potent cytotoxicity against the tested cell lines, including HeLa, HL-60, and MCF-7, with $IC_{50}$ values of $17.6{\pm}1.3$, $4.2{\pm}0.2$, and $12.8{\pm}0.0{\mu}M$, respectively. Compound 8 induced apoptosis in a dose-dependent manner. Annexin V/Propidium Iodide (PI) double staining confirmed that 8 effectively induced apoptosis in MCF-7 cells. To the best of our knowledge, we have reported cytotoxic activity of butanolides from L. japonica against these cancer-cell lines for the first time.

Cytotoxicity and Structure-activity Relationships of Naphthyridine Derivatives in Human Cervical Cancer, Leukemia, and Prostate Cancer

  • Hwang, Yu Jin;Chung, Mi Lyang;Sohn, Uy Dong;Im, Chaeuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.6
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    • pp.517-523
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    • 2013
  • Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with $IC_{50}$ values of 0.7, 0.1, and $5.1{\mu}M$, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa ($q^2$, 0.857; $r^2$, 0.984; $r^2\;_{pred}$, 0.966), HL-60 ($q^2$, 0.777; $q^2$, 0.937; $r^2\;_{pred}$, 0.913), and PC-3 ($q^2$, 0.702; $q^2$, 0.983; $r^2\;_{pred}$, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.

Reduction of Ammonia Accumulation and Improvement of Cell Viability by Expression of Urea Cycle Enzymes in Chinese Hamster Ovary Cells

  • Chung, Myung-Il;Lim, Mi-Hee;Lee, Yun-Jeong;Kim, Ik-Hwan;Kim, Ick-Young;Kim, Jung-Hoe;Chang, Kern-Hee;Kim, Hong-Jin
    • Journal of Microbiology and Biotechnology
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    • v.13 no.2
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    • pp.217-224
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    • 2003
  • Previously, we developed a CHO cell line (CHO-OTC1-Al9) that expresses the first two enzymes in the urea cycle and exhibits a higher ammonia-removing ability and faster growth rate than a vector-controlled CHO cell line (CHO-neo-5). The current study was undertaken to develop a cell line with an ammonia-removing ability higher than the cell line developed previously. To accomplish this, CHO cell lines expressing the first three, first four, or all five enzymes of the urea cycle were constructed using a stable transfection method. Finally, the CHO-AS-16, CHO-AL-19, and CHO-Arg-11 cell lines expressing the first three, first four, and all five enzymes of the urea cycle, respectively, were selected and found to exhibit higher ammonia-removing ability than the CHO-OTC1-Al9 cell line. Among the three selected cell lines, CHO-AL-19 showed the highest ammonia-removing ability and highest cell viability at a higher cell density, with 40% and 15% lower ammonia concentration in the, culture media than that of CHO-neo-5 and CHO-OTC1-A19 cell lines, respectively. CHO-AL-19 also showed 44% and 10% higher cell viability than the CHO-neo-5 and CHO-OTC-Al9 cell lines, at a higher cell density, respectively. The ammonia concentrations in the culture media were expressed as the ammonia concentration/cell, and the CHO-AL-19 cells revealed 45-60% and 20% lower ammonia concentration/cell than the CHO-neo-5 and CHO-OTC1-Al9 cells, respectively.

Effect of Retinoids on Human Breast Cancer Cells (인체 유방암 세포에서 retinoids의 영향에 대한 연구)

  • 윤현정;신윤용;공구
    • Environmental Mutagens and Carcinogens
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    • v.24 no.2
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    • pp.51-66
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    • 2004
  • Retinoids, better known as vitamin A, have been reported to inhibit the growth of several breast cancer cell lines in culture and to reduce breast tumor growth in animal models. Furthermore, retinoids can augment the action of other breast cancer cell growth inhibitors both in vitro and in vivo. Clinically, interest has increased in the potential use of retinoids for the prevention and treatment of human breast cancer. We have examine the effect of all-trans retinoic acid(tRA) and 9-cis retinoic acid(9-cis RA) on human breast cancer cell(MCF-10A, T47-D, MCF-7) proliferation using MTT assay and cell cycle analysis(FACS). Overexpression of cyclin D1 protein is observed in the majority of breast cancers, suggesting that dysregulated expression of cyclin D1 might be a critical event in breast cancer carcinogenesis. We investigated whether tRA and 9-cis RA might affect expression of cyclin D1 on human breast cancer cells(MCF-10A, T47-D, MCF-7) using RT-PCR and west-ern bolt. In MCF-10A cells, either tRA or 9-cis RA treatment did not affect the cell proliferation. In T47-D cells and MCF-7 cells, either tRA or 9-cis RA treatment showed the inhibition of the cell proliferation over control cells and also inhibit the estrogen stimulated cell proliferation when it was given together with estrogen. The effect of retinoids was dose- and time- dependent. T47-D cells treated with 1.0 $\muM$ tRA undergo G0/G1-phase arrest by Day 5. MCF-7 cells treated with 1.0 $\muM$ tRA undergo S-phase arrest by Day 5. All-trans retinoic acid(tRA) and 9-cis retinoic acid(9-cis RA) inhibited the cyelin D1 mRNA and protein expression levels of human MCF-7 and T47-D breast carcinoma cells in vitro. The data indicate that retinoids can reduce cyclin D1 expression levels in a variety of breast cell lines in vitro and result in inhibition of cell proliferation. tRA-mediated growth inhibition and cyclin D1 expression inhibition is more potent than 9-cis RA mediated that. tRA-mediated inhibition effect is more potent on T47-D cells than on MCF-7 cells. Our data suggest that retinoids activity is different according to property of cell lines. Future chemoprevention of breast cancer studies using retinoids will be necessary to determine the mechanism of the retinoids-mediated growth inhibition.

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PRODUCTION OF GINSENOSIDES THROUGH IN VITRO CULTURE OF GINSENG(Panax ginseng C.A. MEYER)

  • Choi K.T.;Ahn I.O.;Park J.C.
    • Proceedings of the Ginseng society Conference
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    • 1993.09a
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    • pp.143-149
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    • 1993
  • Ginseng root explants and calli induced from selected cell lines were cultured on modified Murashige and Skoog's media supplemented with different concentrations of organic or inorganic compounds and plant growth requlators to clarify the effects of chemical composition and plant growth regulators in the medium on the growth of ginseng calli and the production of ginseng saponin. For optimum growth of calli, the concentrations of 2, 4-D and sucrose were the range of 1 to 3 mg/${\ell}$l and 1 to $3\%,$ respectively. And it was clarified that sucrose, nitrogen, phosphate, calcium, magmesian plant growth regulators and their concentrations influcenced the relative biosynthesis of saponin in tissue cultures of Panax ginseng. The patterns of ginsenosides, pharmacologically useful component, were different among the cell lines and contents of ginsenosides were much higher in selected cell lines than in original cell line.

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Instability of Anthocyanin Accumulation in Vitis vinifera L. var. Gamay Freaux Suspension Cultures

  • Qu Junge;Zhang Wei;Yu Xingju;Jin Meifang
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.10 no.2
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    • pp.155-161
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    • 2005
  • The inherent instability of metabolite production in plant cell culture-based bioprocessing is a major problem hindering its commercialization. To understand the extent and causes of this instability, this study was aimed at understanding the variability of anthocyanin accumulation during long-term subcultures, as well as within subculture batches, in Vitis vinifera cell cultures. Therefore, four cell line suspensions of Vitis vinifera L. var. Gamay Freaux, A, B, C and D, originated from the same callus by cell-aggregate cloning, were established with starting anthocyanin contents of $2.73\;\pm\;0.15,\;1.45\;\pm\;0.04,\;0.7\;\pm\;0.024\;and\;0.27\;\pm\;0.04$CV (Color Value)/g-FCW (fresh cell weight), respectively. During weekly subculturing of 33 batches over 8 months, the anthocyanin biosynthetic capacity was gradually lost at various rates, for all four cell lines, regardless of the significant difference in the starting anthocyanin content. Contrary to this general trend, a significant fluctuation in the anthocyanin content was observed, but with an irregular cyclic pattern. The variabilities in the anthocyanin content between the subcultures for the 33 batches, as represented by the variation coefficient (VC), were 58, 57, 54, and $84\%$ for V. vinifera cell lines A, B, C and D, respectively. Within one subculture, the VCs from 12 replicate flasks for each of 12 independent subcultures were averaged, and found to be $9.7\%$, ranging from 4 to $17\%$. High- and low-producing cell lines, VV05 and VV06, with 1.8-fold differences in their basal anthocyanin contents, exhibited different inducibilities to L-phenylalanine feeding, methyl jasmonate and light irradiation. The low-producing cell line showed greater potential in enhanced the anthocyanin production.

Inhibition of Human $CD8^+$ Cytotoxic T Lymphocyte (CTL) -mediated Cytotoxicity in Porcine Fetal Fibroblast Cells by Overexpression of Human Cytomegalovirus Glycoprotein Unique Short (US) 2 Gene

  • Park, K-W.;Yoo, J.Y.;Choi, K.M.;Yang, B.S.;Im, G.S.;Seol, J.G.
    • Asian-Australasian Journal of Animal Sciences
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    • v.22 no.1
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    • pp.20-25
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    • 2009
  • Xenotransplantation of pig organs into humans is a potential solution for the shortage of donor organs for transplantation. However, multiple immune barriers preclude its clinical application. In particular, the initial type of rejection in xenotransplantation is an acute cellular rejection by host $CD8^+$ cytotoxic T lymphocyte (CTL) cells that react to donor major histocompatibility complex (MHC) class I. The human cytomegalovirus (HCMV) glycoprotein Unique Short (US) 2 specifically targets MHC class I heavy chains to relocate them from the endoplasmic reticulum (ER) membrane to the cytosol, where they are degraded by the proteasome. In this study we transfected the US2 gene into minipig fetal fibroblasts and established four US2 clonal cell lines. The integration of US2 into transgenic fetal cells was confirmed using PCR and Southern blot assay. The reduction of Swine Leukocyte Antigen (SLA)-I by US2 was also detected using Flow cytometry assay (FACS). The FACS analysis of the US2 clonal cell lines demonstrated a substantial reduction in SLA-I surface expression. The level (44% to 76%) of SLA-I expression in US2 clonal cell lines was decreased relative to the control. In cytotoxicity assay the rate of $CD8^+$ T cell-mediated cytotoxicity was significantly reduced to 23.8${\pm}$15.1% compared to the control (59.8${\pm}$8.4%, p<0.05). In conclusion, US2 can directly protect against $CD8^+$-mediated cell lysis. These results indicate that the expression of US2 in pig cells may provide a new approach to overcome the CTL-mediated immune rejection in xenotransplantation.