• Title/Summary/Keyword: In vitro cytotoxicity

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A Novel Helicosporium Isolate and Its Antimicrobial and Cytotoxic Pigment

  • Choi, Hye Jung;Lee, Sang Myeong;Kim, Sun-Hee;Kim, Dong Wan;Choi, Young Whan;Joo, Woo Hong
    • Journal of Microbiology and Biotechnology
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    • v.22 no.9
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    • pp.1214-1217
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    • 2012
  • One Helicosporium strain, isolated from a wilted chestnut tree, evidenced in vitro antimicrobial activity against various types of bacteria and fungi, and generated a diffusible pigment. The antimicrobial compounds and the diffusible pigment of the Helicosporium sp. isolate were purified via solvent fractionation, column chromatography, and recycling preparative chromatography. Both the major antimicrobial compound and the diffusible pigment were identified as 2-methylresorcinol via nuclear magnetic resonance spectroscopy. Therefore, 2-methylresorcinol, a diffusible pigment generated by Helicosporium sp., appears to be an active antimicrobial principle. This pigment also exhibited considerable cytotoxicity against mammalian cells.

Antitumor Activity of Psorelea corylifolia

  • Ryu, Shi-Yong;Choi, Sang-Un;Lee, Chong-Ock;Zee, Ok-Pyo
    • Archives of Pharmacal Research
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    • v.15 no.4
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    • pp.356-359
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    • 1992
  • The activity-oriented fractionation of Psoralea corylifolia led to an isolation of a (+) bakuchio 1 as an activ eprinciple of its antitumoral property in vitro 1 was observed to exhibit a mild cytotoxicity against five kinds of cultured human cancer cell lines, i. e. the A549, SK-OV-3, SK-MEL-2, XF-498 and HCT15. The synthesized 2, 3-epoxide of (+)-bakuchiol 3 showed the similar activity as the (+) bakuchiol 1, whereas the other oxidation derivatives 4 and 5 including the acetyl (+) bakuchiol 2 showed a decreased activity.

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Antitumor Triterpense from Medicinal Plants

  • Ryu, Shi-Yong;Choi, Sang-Un;Lee, Seung-Ho;Lee, Chong-Ock;No, Zaesung;Ahn, Jong-Woong
    • Archives of Pharmacal Research
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    • v.17 no.5
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    • pp.375-377
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    • 1994
  • Thirteen kinds of naturally occurring or derivatised thiterpenes, reported to have an antitumoral property, were reinvestigated on the basis of their direct cytotoxicity or the inhibitory activity on cell growth against five kinds of cultured human tumor cells, i.e., A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15, in vitro. Ursonic acid III, betulinic acid VIII, betulonic acid X and glycrrhetinic acid XI were exhibitied a marked inhibition on cell growth.

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Phytochemical Constituents from the Aerial Parts of Paris verticillata (삿갓나물 지상부의 식물화학적 성분 연구)

  • Lee, Kyu-Ha;Kim, Ki-Hyun;Lee, Il-Kyun;Choi, Sang-Un;Lee, Kang-Ro
    • Korean Journal of Pharmacognosy
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    • v.39 no.2
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    • pp.91-94
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    • 2008
  • Column chromatographic separation of the MeOH extract from the aerial parts of Paris verticillata led to the isolation of three phenolics, two terpene glucosides and two pyrrolidine alkaloids. Their structures were characterized to be methyl caffeate (1), 5-hydroxy pyrrolidin-2-one (2), vanillic acid (3), benzyl alcohol glucopyranoside (4), (6S, 9R)-roseoside (5), staphylionoside H (6) and 5-methoxy pyrrolidin-2-one (7) by spectroscopic means. The isolated compounds (1-7) were for the first time reported from this source. The isolated compounds were tested for their cytotoxicity against four human tumor cell lines by SRB method in vitro.

Recognition of Pharmacophore of ar-Turmerone for its Anticancer Activity

  • Baik, Kyong-Up;Jung, Sang-Hun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.16 no.3
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    • pp.254-256
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    • 1993
  • For the evaluation of the role of .alpha., .betha.-unsaturated ketone portion of ar-tumerone for its activity, the structural variation of this structural unit was performed to omit its alkylating propery. Thus compounds 2, 3, and 4 were prepared and their cytotoxicities were determined against three different leukemiz cell lines (HL-60, K-562, and $L_{1210})$ in vitro. The biological inactivity against three different cell lines of these analogues implies that the $\alpha, \beta$-unsaturated ketone of ar-tumerone is the essential pharmacophore for its activity.

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Synthesis and Preliminary Cytotoxicity Evaluation of New Diarylamides and Diarylureas Possessing 2,3-Dihydropyrrolo[3,2-b]quinoline Scaffold

  • Kim, Hyun-Jin;El-Gamal, Mohammed I.;Lee, Yong Sup;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2480-2486
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    • 2013
  • A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.

Structure-Activity Relationship Studies of Isoquinolinone Type Anticancer Agent

  • Cheon, Seung-Hoon;Park, Joon-Suck;Lee, Joon-Yeol;Lee, You-Na;Yi, Hyo;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.24 no.4
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    • pp.276-280
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    • 2001
  • Substituted isoquinolin-1-ones (1) were synthesized to test their in vitro anticancer activity. 3-Biphenyl-H-methylisoquinolin-1-one (7) showed the most potent anticancer activity against five different human cancer cell lines.

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Pheophytin Content and Fibrinolytic Activity of Silkworm Feces in the Different Larval Stages of Silkworms

  • Ahn, Mi-Young;Ryu, Kang-Sun;Kim, Iksoo;Kim, Jin-Won;Lee, Heui-Sam;Lee, Yong-Ki;Kim, Eun-Sun
    • International Journal of Industrial Entomology and Biomaterials
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    • v.5 no.2
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    • pp.195-199
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    • 2002
  • In order to find potential anticancer agents, we extracted pheophytin in the silkworm feces from various larval stages by water, chloroform and methanol extraction. The cytotoxicity of the pheophytin extracts of various silkworm feces was measured in the CT-26 cells originated from murine metastatic colon cancer, by dye uptake assay. The cytotoxicity of those pheophytins in 2nd, 3rd and 4th instars was better than remaining larval stages. The in vitro anticoagulant and fibyinolytic activities of ethanol extract from varietal mulberry leaves, mulberry branches and silkworm feces and pheophytin extracts from silkworm feces obtained at various larval stages were evaluated in order to find effective therapeutic drugs for the treatment of myocardial and cerebral thrombosis. The fibrinolytic activity was tested using the activated partial thromboplastin time (APTT) and thrombin time (TT) was measured for blood clotting activity. With regards to the fibrinolytic system, ethanol extracts of silkworm feces were better than varietal mulberry leaves and mulberry branches. The pheophytin extracts from 7th days of 5th instar contained the highest percentage of pheophytin and good fibrinolytic activity.

Antioxidant and Cytoprotective Activity of the Olive Leaf (Olea europaea L. var. Kalamata) Extracts on the Mouse Embryonic Fibroblast Cell

  • Ha, Ju-Yeon;Goo, Sun-Young;Sung, Jung-Suk;Shin, Han-Seung
    • Food Science and Biotechnology
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    • v.18 no.4
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    • pp.965-970
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    • 2009
  • Oleuropein content of olive leaf extracts (OLE; ethanol extract) was evaluated by high performance liquid chromatography analysis. Oleuropein contents were $4.21{\pm}0.57$, $3.92{\pm}0.43$, $0.32{\pm}0.03$, $5.76{\pm}0.32$, and $32.47{\pm}0.25$ mg/100 g for ethanol extract, and hexane, chloroform, ethyl acetate, and butanol fraction, respectively. The removal of DPPH free radical increased in OLE and all 5 fractions of OLE in a concentration dependent manner. In order to investigate the antioxidant effect of OLE in vitro, 80%(v/v) ethanol OLE, $H_2O_2$, or combined treatment of 80%(v/v) ethanol OLE and $H_2O_2$ were applied on mouse embryonic fibroblast (MEF) cells. Cells were damaged by oxidative stress decreased their viability followed by increasing concentration of $H_2O_2$, but co-treatment of OLE and $H_2O_2$ showed an increase in cell growth about 20% compare to the cells treated with $H_2O_2$. OLE suppresses cytotoxicity induced by $H_2O_2$ in dose dependent manner. OLE treatment on MEF cells was also examined by analyzing cell cycle and apoptotic rate using flow cytometry. Apoptotic and necrotic cell accumulation was decreased in addition of OLE to $H_2O_2$ compare to the oxidative damaged cells. Taken together, these results demonstrated that OLE suppresses cytotoxicity induced by $H_2O_2$ and protect cells against oxidative stress on MEF cells.