• Title/Summary/Keyword: in vitro cancer research

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The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

  • Yin, Jie;Kwon, Gu-Joong;Wang, Myeong-Hyeon
    • Nutrition Research and Practice
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    • v.1 no.3
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    • pp.189-194
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    • 2007
  • This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its $IC_{50}$ values ranged from 47.1 to $210.5\;{\mu}g/ml$ and $IC_{50}$ of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and $56.5\;{\mu}g/ml$, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.

Lignans from the Roots of Berberis amurensis

  • Park, Hyun-Bong;Lee, Kyu-Ha;Kim, Ki-Hyun;Lee, Il-Kyun;Noh, Hyung-Jun;Choi, Sang-Un;Lee, Kang-Ro
    • Natural Product Sciences
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    • v.15 no.1
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    • pp.17-21
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    • 2009
  • Column chromatographic separation of the alcoholic extract from the roots of Berberis amurensis yielded eight phenolic constituents including six lignans, hanultarin (1), (-)-secoisolariciresinol (3), (+)-lyoniresinol (5), (+)-syringaresinol (6), (+)-syringaresinol-O-$\beta$-D-glucopyranoside (7), liriodendrin (8), and two phenylpropanoids, 4-glucosyloxy-3-methoxyphenyl trans-propenoic ethyl ester (2), trans-ferulic acid (4). The structures were determined on the basis of NMR spectroscopic data. All isolated compounds(1-8) were reported for the first time from this source. Compound 1 exhibited moderate cytotoxicity against four human cancer cell lines in vitro using sulforhodamin B bioassay.

Synthesis and in vitro Antitumor Activity of 2-Alkyl, 2-Aryl, and 2-Piperazinyl Benzimidazole-4, 7-dione Derivatives

  • Ahn, Chan-Mug;Tak, Jung-Ae;Choi, Sun-Ju
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.288-301
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    • 2000
  • A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

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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.

Cellular-uptake Behavior of Polymer Nanoparticles into Consideration of Biosafety

  • Do, Jeong-Hoe;An, Jeong-Ho;Joun, Yong-Seung;Chung, Dong-June;Kim, Ji-Heung
    • Macromolecular Research
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    • v.16 no.8
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    • pp.695-703
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    • 2008
  • Nanoparticles have tremendous potential in cancer prevention, detection and augmenting existing treatments. They can target tumors, carry imaging capability to document the presence of tumors, sense pathophysiological defects in tumor cells, deliver therapeutic genes or drugs based on the tumor characteristics, respond to external triggers to release an appropriate agent, document the tumor response, and identify the residual tumor cells. Nanoparticles < 30 nanometers in diameter show unexpected and unique properties. Furthermore, particles < 5 nanometers in size can easily penetrate cells as well as living tissues and organs. This study evaluated the safety of nano materials in a living body and the relationship between the living tissue and synthetic nano materials by examining the in-vitro cytotoxicity of poly(lactic-co-glycolic) acid (PLGA) nano-spheres and fluorescein isothiocynate(FITC)-labeled dendrimers as polymer nanoparticles. PLGA was chosen because it has been used extensively for biodegradable nanoparticles on account of its outstanding bio-compatibility and its acceptance as an FDA approved material. The dendrimer was chosen because it can carry a molecule that recognizes cancer cells, a therapeutic agent that can kill those cells, and a molecule that recognizes the signals of cell death. Cytotoxicity in L929 mouse fibroblasts was monitored using MTT assay. Microscopic observations were also carried out to observe cell growth. All assays yielded meaningful results and the PLGA nanoparticles showed less cytotoxicity than the dendrimer. These nano-particles ranged in size from 10 to 100 nm according to microscopy and spectroscopic methods.

Transformation of Mouse Liver Cells by Methylcholanthrene Leads to Phenotypic Changes Associated with Epithelial-mesenchymal Transition

  • Oh, Jiyun;Kwak, Jae-Hwan;Kwon, Do-Young;Kim, A-Young;Oh, Dal-Seok;Je, Nam Kyung;Lee, Jaewon;Jung, Young-Suk
    • Toxicological Research
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    • v.30 no.4
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    • pp.261-266
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    • 2014
  • Environmental pollutants such as polycyclic aromatic hydrocarbons (PAHs) have been implicated in cancer development and progression. However, the effects of PAHs on carcinogenesis are still poorly understood. Here, we characterized a mouse cancer cell line BNL 1ME A. 7R.1 (1MEA) derived by transformation of non-tumorigenic liver cell line BNL CL.2 (BNL) using 3-methylcholanthrene (3MC), a carcinogenic PAH. RT-PCR and immunoblot analysis were used to determine the expression level of mRNA and proteins, respectively. To determine functionality, cell motility was assessed in vitro using a transwell migration assay. Both mRNA and protein levels of E-cadherin were significantly decreased in 1MEA cells in comparison with BNL cells. While the expression levels of mesenchymal markers and related transcription factors were enhanced in 1MEA cells, which could lead to increase in cell motility. Indeed, we found that 7-day exposure of BNL cells to 3-MC reduced the level of the adhesion molecule and epithelial marker E-cadherin and increased reciprocally the level of the mesenchymal marker vimentin in a dose-dependent manner. Taken together, these results indicate that the process of epithelial-mesenchymal transition (EMT) may be activated during premalignant transformation induced by 3-MC. A mechanism study to elucidate the relation between 3-MC exposure and EMT is underway in our laboratory.

Isolation and Identification of Cytotoxic and Biological Active Toxin from the Puffer Fish Arothron stellatus

  • Veeruraj, Anguchamy;Pugazhvendan, Sampath Renuga;Ajithkumar, Thipramalai Thankappan;Arumugam, Muthuvel
    • Toxicological Research
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    • v.32 no.3
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    • pp.215-223
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    • 2016
  • This study is to investigate the biological, biochemical and cytotoxic effects of puffer fish (Arothron stellatus) toxin extracts under in-vitro condition. Extracted toxins from various organs of puffer fish were purified by using active charcoal column, and Bio-gel-P2 column chromatography. The lethality of toxin was tested in crabs, which consists of neurotoxic compounds. The degree of the brine shrimp lethality assay was found directly proportional to the concentration of the toxin extracts, which was well supported by hemolytic assay. The experimental results suggested that the gonad was found higher toxins than the liver and muscles. The mortality rate of brine shrimp nauplii was increased with the raise of concentrations of toxin level. Among the different doses and time dependent cytotoxic effect of human cervical carcinoma (HeLa) cells were showed $4.0{\mu}g/mL$ of toxin, which was effectively inhibited cancer cell proliferation. HPLC and TLC analysis was revealed that the A. stellatus toxin contains tetrodotoxin (TTX), related compounds 4-epi TTX and anhydro-TTX. The present results suggested that the A. stellatus contain TTX as a major and anh-TTX as a minor toxin. It could be the potential candidate in the field of anticancer drug discovery against human cervical cancer cells. The present data is confirming that the puffer fish toxin as an interesting source of novel bioactive natural compounds with potent applications in pharmacology.

In Vitro Antioxidant and Antiproliferative Activities of Novel Orange Peel Extract and It's Fractions on Leukemia HL-60 Cells

  • Diab, Kawthar AE;Shafik, Reham Ezzat;Yasuda, Shin
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.16
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    • pp.7053-7060
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    • 2015
  • In the present work, novel orange peel was extracted with 100%EtOH (ethanol) and fractionated into four fractions namely F1, F2, F3, F4 which were eluted from paper chromatographs using 100%EtOH, 80%EtOH, 50%EtOH and pure water respectively. The crude extract and its four fractions were evaluated for their total polyphenol content (TPC), total flavonoid content (TFC) and radical scavenging activity using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Their cytotoxic activity using WST assay and DNA damage by agarose gel electrophoresis were also evaluated in a human leukemia HL-60 cell line. The findings revealed that F4 had the highest TPC followed by crude extract, F2, F3 and F1. However, the crude extract had the highest TFC followed by F4, F3, F2, and F1. Depending on the values of $EC_{50}$ and trolox equivalent antioxidant capacity, F4 possessed the strongest antioxidant activity while F1 and F2 displayed weak antioxidant activity. Further, incubation HL-60 cells with extract/fractions for 24h caused an inhibition of cell viability in a concentration-dependent manner. F3 and F4 exhibited a high antiproliferative activity with a narrow range of $IC_{50}$ values ($45.9-48.9{\mu}g/ml$). Crude extract exhibited the weakest antiproliferative activity with an $IC_{50}$ value of $314.89{\mu}g/ml$. Analysis of DNA fragmentation displayed DNA degradation in the form of a smear-type pattern upon agarose gel after incubation of HL-60 cells with F3 and F4 for 6 h. Overall, F3 and F4 appear to be good sources of phytochemicals with antioxidant and potential anticancer activities.

Quality characteristics and functionalities of Korean and Japanese spring Baechu cabbages and the kimchi prepared with such cabbages (한국산 및 일본산 봄배추와 이를 이용하여 제조한 김치의 품질특성과 기능성)

  • Park, So-Eun;Bong, Yeon-Ju;Kim, Hee-Young;Park, Kun-Young
    • Food Science and Preservation
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    • v.20 no.6
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    • pp.854-862
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    • 2013
  • We examined the quality characteristics and functionalities of Korean and Japanese spring Baechu cabbages and the kimchi prepared with them. To study the physiochemical properties of the cabbages and the kimchis, we measured their water content, pH, acidity, microbial counts, and springiness. On the third week of the kimchi fermentation at $5^{\circ}C$, their sensory properties and in vitro DPPH radical scavenging and anticancer activities using AGS human gastric cancer cells were determined. The Japanese Baechu contained 97.1% water, and the Korean Baechu, 92.4%. The comparison of the textures of the raw Baechu and the brined Baechu showed that the Korean Baechu had higher springiness scores than the Japanese Baechu. After four-week fermentation, the springiness score of the kimchi with Korean Baechu was 53.5%, significantly higher than the 41.4% of the kimchi with Japanese Baechu. The kimchi prepared with Korean Baechu had a low total bacterial count but higher Lactobacillus sp. and Leuconostoc sp. counts than the kimchi with Japanese Baechu. The kimchi prepared with Korean Baechu had the highest overall acceptability score in the sensory evaluation test. The DPPH radical scavenging activity of the kimchi with Korean Baechu was 83.2%, and that of the kimchi with Japanese Baechu, 46.1%. When the AGS human gastric cancer cells were treated with the kimchis, the kimchi prepared with Korean Baechu showed a 45% cancer cell growth inhibition rate, and the kimchi with Japanese Baechu, 26%, at 1 mg/mL of methanol extracts. At the 2 mg/mL concentration, the kimchis with Korean Baechu and Japanese Baechu showed 97% and 74% inhibition, respectively. The Korean Baechu showed better quality than the Japanese Baechu, and the kimchi prepared with the Korean Baechu showed better kimchi quality and functionality than the Japanese Baechu.

Secondary Metabolites Isolated from Ganoderma lucidum and Their Anti-inflammatory Activity (영지버섯(Ganoderma lucidum)으로 부터 분리한 이차대사산물 및 이들의 항 염증 활성)

  • Kim, Hye Ji;Koo, Man Hyung;Lee, Jun Hyuck;Suh, Sung-Suk;Youn, Ui Joung
    • Korean Journal of Pharmacognosy
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    • v.50 no.3
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    • pp.232-238
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    • 2019
  • Phytochemical study of Ganoderma lucidum (Polyporaceae) let to the isolation of five lanostane triterpenoid (1-5), along with two nitrogen derived phenolic compounds, N-phenylethylformamide (6) and N-acetylphenethylamine (7). The structures of the compounds were determined by 1D and 2D NMR, and MS experiments, as well as by comparison of their data with published values. Compounds 6 and 7 were isolated for the first time from the genus Ganoderma and this species. All the compounds were evaluated for cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production induced by lipopolysaccharide (LPS) in mouse macrophage RAW 264.7 cells in vitro. Among the isolates, compounds 2 and 3 showed moderate inhibitory activity against NO production.