• Title/Summary/Keyword: Cytotoxicities

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Constituents and the Antitumor Principle of Allium victoriallis var. platyphyllum

  • Lee, Kyung-Tae;Choi, Jung-Hye;Kim, Dong-Hyun;Son, Kun-Ho;Kim, Won-Bae;Kwon, Sang-Hyuk;Park, Hee-Juhn
    • Archives of Pharmacal Research
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    • v.24 no.1
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    • pp.44-50
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    • 2001
  • To search for cytotoxic components from Allium victoriallis , MTT assays on each extract and an isolated component, gitogenin 3-O-lycotetroside, were performed against cancer cell lines. Cytotoxicities of most extract were shown to be comparatively weak, though $IC_50$ values of $CHCl_3$fraction was found to be <31.3-368.4 $\mu\textrm{g}/ml$. From the incubated methanol extract at $36^{\circ}C, eleven kinds of organosulfuric flavours were predictable by CG-MS performance. The most abundant peak was revealed to be 2-vinyl-4H-1,3-dithiin(1) by its mass spectrum. Further, this extract showed significant cytotoxicities toward cancer cell lies. Silica gel column chromatography of the n-butanol fraction led to the isolation of gitogenin 3-O-lycotetroside (3) along with astragalin (4) and kaempferol 3, 4'-di-O-$\beta$-D-glycoside (5). This steroidal saponin exhibited significant cytotoxic activities ($IC_50$, 6.51-36.5 $\mu\textrm{g}/ml$) over several cancer cell lines. When compound 3 was incubated for 24 h with human intestinal bacteria, a major metabolite was produced and then isolated by silica gel column chromatography. By examining parent and prominent ion peak in FAB-MS spectrum of the metabolite, the structure was speculated not to be any of prosapogenins of 3, suggesting that spiroketal ring were labile to the bacterial reaction. These suggest that disulfides produced secondarily are the antitumor principles.

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Selective Extraction of Cytotoxic Substances from Medicinal Plants using Supercritical Carbon Dioxide (초임계 이산화탄소를 이용한 약용식물 성분의 선택적 추출)

  • Choi, Young-Hae;Park, Eun-Jung;Kim, Young-Leem;Chin, Young-Won;Jeon, Seong-Ho;Joung, Seung-Nam;Yoo, Ki-Pung;Kim, Jin-Woong
    • Korean Journal of Pharmacognosy
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    • v.30 no.1
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    • pp.59-64
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    • 1999
  • Supercritical fluid extraction (SFE) technique was applied to extract cytotoxic substances from five medicinal plants including Angelica gigas, Angelica acutiloba, Aralia cordata, Spirodela polyrhiza, Bupleurum falcatum, and Acanthopanax sessiliflorus. The cytotoxicities against P388, A549, and HL-60 cell lines were determined for the supercritical carbon dioxide extracts of five plant materials employed and were compared with those of the conventional organic solvent extracts such as n-hexane, $CHCl_{3}$, and MeOH to evaluate the SFE as an alternative method to conventional organic solvent extraction. In most cases, the SFE extracts of plant materials showed enhanced cytotoxicities when compared with those of other organic solvent extracts. In addition, the optimum temperature and pressure of SFE for extraction of the cytotoxic substances were largely affected by both the plant species and the cell lines tested. These results suggested that SFE could be an alternative to the conventional organic solvent method for the selective extraction of cytotoxic compounds from plants.

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Augmentation of the Cytotoxic Effects of Anticancer Drugs by $(\pm)$-ar-Turmerone and Extracts of the Lithosperma and Scutellaria Roots against Human Leukemia Cell Lines (백혈병 세포주에 대한 $(\pm)$-ar-Turmerone, 자근 및 황금추출물에 의한 항암제의 세포독성 증강효과)

  • 이윤영;유관희;김삼용;안병준
    • YAKHAK HOEJI
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    • v.35 no.3
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    • pp.203-215
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    • 1991
  • Using the calorimetric [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT)assay, we evaluated the chemosensitivity of 8 anticancer drugs{vincristine(VCR), vinblastine(VBL), adriamycin(ADR), cisplatin(CPDD), etoposide(VP-16), cytosine arabinoside(ara-C), bleomycin (Bleo) and cyclophosphamide(CYC)} and the cytotoxicity-enhancing effects of ($\pm$)-ar-turmerone and the extracts of the crude drugs {Lithospermum eythrorhizon(LE) and Scutellaria baicalensis (SB)} on the above mentioned anticancer drugs against HL-60 and KG-1 cells among 8 anticancer drugs, VCR, VBL, ADR, and CPDD inhibited the growth of both cell lines by more than 50%, while VP-16, ara-C, Bleo, and CYC were less effective. ($\pm$)-ar-Turmerone had significant inhibitory effects against both cell lines, showing the ID$_{50}$ values of 11.730 $\mu\textrm{g}$/ml and 0.292 $\mu\textrm{g}$/ml for HL-60 and KG-1 cells. respectively. But the extracts of LE and SB roots showed no significant cytotoxic effects. According to ID$_{50}$ values, the cytotoxicities of VCR, VBL and ADR against HL-60 were enhanced two, eight and three times by mixing ($\pm$)-ar-turmerone, five, seven and three times by adding the extract of LE root, and twenty, six and three times by mixing the extract of SB root, respectively. The cytotoxicities of the above mentioned drugs against KG-1 cell were enhanced two, seven and three times by mixing ($\pm$)-ar-turmerone, two, three and three times by combining wilth the extract of LB root, and two, five and two times by adding the extract of SB root, respectively. The cytotoxicity-potentiating effects of ($\pm$)-ar-turmerone and the extracts of LE and SB roots against HL-60 cell were greater than KG-1 cell.

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Reactive Oxygen Species and Antioxidant Enzyme Activities in Accordance with the Cytotoxicity of Farnesol Against HL-60 Cells (Farnesol의 HL-60 세포에 대한 세포독성과 활성산소 및 항산화효소 활성 변화)

  • Lim, So-Yoon;Park, Sie-Won
    • YAKHAK HOEJI
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    • v.50 no.6
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    • pp.372-380
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    • 2006
  • Farnesol in fruits, vegetables, herbs and leaves acts as bioactive component related with prevention of cancer and psychological malaise. We investigated the cytotoxic effects of farnesol on human leukemic cell, HL-60 cells, by MTT assay using 3- (4,5-Oirnethylthiazol-2-yl) -2,5-diphenyltetrazoliumbromide. Farnesol (0.1${\sim}$50 ${\mu}$g/ml) exhibited cytotoxicities against HL-60 cells in concentration and culture period dependent manner, In the cytotoxic condition induced by farnesol against HL-60 cells, the generation of reactive oxygen species such as O$_2$ and H$_2$O$_2$ were found to be considerably increased. The most prominent augmentations of O$_2$ and H$_2$O$_2$ were over five folds of controls. In an attempt to explore the response of HL-60 cells to the increased O$_2$ and H$_2$O$_2$, superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase activities of HL-60 cells treated with farnesol were measured. SOD and GPx activities were found to be remarkably elevated by addition of farnesol showing the best results of 273% and 167% of controls, respectively: All data suggest that farnesol may have played as an apoptosis inducer in HL-60 cells via production of reactive oxygen species (ROS) and HL-60 cells may have failed to overcome the damage of ROS on account of still defcient ROS scavengers including SOD and GPx.

Stereochemical Requirement at4-Position of 4-Phenyl-1-arylsulfonylimidazolidinones for their Cytotoxicities

  • Jung, Sang-Hun;Kwak, Suhk-Jun;Kim, Nam-Doo;Lee, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.23 no.1
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    • pp.35-41
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    • 2000
  • In order to investigate the stereochemical requirements of planar structure at 4-position of 4-phenyl-1-arylsulfonylimidazolidinones (1) for their cytoxicities against human cancer cell lines, the size, the distance from imidazolidinone ring, and the conformation of this moiety were variegated. Replacement of phenyl moiety with naphthyl in compounds 2 and 3 or benzyl moiety in compound 4 sharply reduced activity of 1. Conformational restriction on phenyl ring in compound 5 also resulted in the loss of activity of 1. Therefore, phenyl moiety without any substituents directly attached to imidazolidinone ring of 1 should be considered as an essential pharmacophore for this analog.

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Antimutagenic and Cytotoxicity Effects of Fermented Soybean Extract (발효콩 추출물의 항돌연변이원성 및 세포독성 효과)

  • 함승시;최승필;이효진;문선영;김수현;이득식
    • Journal of the East Asian Society of Dietary Life
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    • v.14 no.3
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    • pp.288-293
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    • 2004
  • This study was carried out to determine the antimutagenic and anticancer effects of fermented soybean using Ames test and cytotoxicity, respectively. The ethyl acetate fraction (200 g/plate) of fermented soybean in the Salmonella typhimurium TA100 strain showed 86.6% of inhibition rate against the mutagenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG). In addition, the suppression of ethyl acetate fraction with same concentration of fermented soybean in the Salmonella typhimurium TA98 and TAI00 strains showed 82.4% and 90.8% inhibition against 3-amino-l,4-dimethyl-5H-pyrido-(4,3-b)indol (Trp-P-l), respectively. The cytotoxicity effects of fermented soybean against the cell lines with human lung carcinoma (A549), human gastric carcinoma (AGS) and human breast adenocarcinoma (MCF-7) were inhibited with the increase of the extract concentration. The treatment of 1.0 mg/mL ethyl acetate fraction of fermented soybean showed strong cytotoxicities of 71.6%, 91.5% and 80.7% against A549, AGS and MCF-7, respectively.

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Bioactive Ginseng Yogurts Fermented with Bifidobacteria: The Transformation of Ginsenosides to Compound K

  • Kim, Na-Young;Han, Myung-Joo
    • Food Quality and Culture
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    • v.1 no.1
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    • pp.18-21
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    • 2007
  • The objective of this study was to prepare bioactive ginseng yogurts containing compound K, which is transformed from ginsenosides, and to investigate the compound's cytotoxicity against tumor cells. Milk containing ginseng was fermented by Bifidobacteria KK-I and KK-2, and their activities for transforming ginsenosides to compound K were measured. Among the tested concentrations of ginseng in the milk, compound K was effectively produced in the 3% and 6% ginseng yogurts fermented for 48 hrs. These fermented ginseng yogurts were extracted with BuOH, and their cytotoxicities against tumor cells were examined. The BuOH extract of the yogurt made from the 3% ginseng milk showed cytotoxic activity against P388 and HeLa tumor cells. However, the nonfermented ginseng milk did not exhibit cytotoxicity against these cells. Therefore, we deem that the ginseng yogurt, which contained compound K, could be developed as a potential fermented drink product.

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The Effects of NOG-YONG Aqua-Aqupuncture Solution on Cytotoxicities in Primary Culture of Adult Rat Hepatocytes

  • Byun, Boo-Hyeong;Jeong, Hye-Kwang
    • Proceedings of the Korean Society of Food Hygiene and Safety Conference
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    • 2002.05a
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    • pp.147-147
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    • 2002
  • This experimental study was carried out to investigate on the safety of Nog-yong aqua-acupuncture solution in primary culture of adult rat hepatocytes. Primary culture of adult rat hepatocytes has been considered as a ideal model for toxicological studies because cultured hepatocytes maintained many liver-specific functions. In this research, we investigated the effects of Nog-yong aqua-aqupunture(1-10$\mu\textrm{g}$/ml) on cytotoxicites in primary culture of adult rat hepatocytes using LDH release assays. Hepatic glutathione level. glutathione-S-transferase activity, and albumin synthesis were not affected by treatment with Nog-yong aqua-aqupuntur alone. Nog-yong aqua-aqupuncoure solution(0.5-$10{\mu}\textrm{g}$/ml) on cytotoxicites in primary culture of adult rat hepatocytes using LDH release not significantly affected normal functional charaterists.

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Cytotoxic Activities of Herbal Drugs Against Human Cancer Cell Lines (Ⅱ) (인체암세포주에 대한 천연자원의 세포독성 검색 (Ⅱ))

  • Park, Jong-Dae;Lee, You-Hui
    • Korean Journal of Pharmacognosy
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    • v.30 no.2
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    • pp.105-110
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    • 1999
  • In our continuing search for new antineoplastic agents from natural products, one hundred and thirty-five herbal drugs were extracted with petroleum ether/ether (1:1), ethyl acetate and methyl alcohol, successively and their cytotoxicities were evaluated against A549 (human lung carcinoma) and SK-OV-3(human ovary adenocarcinoma) cell lines. Among them, fifteen kinds of ether extracts, eighteen kinds of ethyl acetate extracts and seven kinds of methanol extracts showed significant cytotoxic activities (above 70% inhibition) against A549 cell lines at a concentration of $40\;{\mu}g/ml,$ while ten kinds of ether extracts, thirteen kinds of ethyl acetate extracts and six kinds of methanol extracts demonstrated significant cytotoxic activities against SK-OV-3 cell lines at the above same concentration.

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Cytotoxic Activities of Herbal Drugs against Human Cancer Cell Lines (I) (인체암세포주에 대한 천연자원의 세포독성 검색 (I))

  • Park, Jong-Dae;Kim, Shin-Il;Lee, You-Hui
    • Korean Journal of Pharmacognosy
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    • v.29 no.4
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    • pp.323-330
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    • 1998
  • For the search of new antineoplastic agents from natural resources, two hudred and one kinds of oriental medicinal drugs were extracted with petroleum ether/ether(1:1), ethyl acetate and methyl alcohol, successively and their cytotoxicities were evaluated against A549 (human lung carcinoma) and SK-OV-3 (human ovary adenocarcinoma) cell lines. Among them, thirty kinds of ether extracts, forty-one kinds of ethyl acetate extracts and nine kinds of methanol extracts showed significant cytotoxic activities (above 70% inhibition) against A549 cell lines at a concentration of $40\;{\mu}g/ml$. And also, twenty-four kinds of ether extracts, thirty-one kinds of ethyl acetate extracts and six kinds of methanol extracts showed significant cytotoxic activities against SK-OV-3 cell lines at the same concentration.

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