• Title/Summary/Keyword: A549 Cell

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Screening of Anticancer Potential of Celecoxib and its Derivatives (셀레콕시브 및 그 합성유도체들의 항암활성 스크리닝)

  • Park, Jeong-Ran;Kang, Jin-Hyoung;Kuh, Hyo-Jeong;Noh, Ji-Young;Ryu, Hyung-Chul;Park, Sang-Wook;Ko, Dong-Hyun;Cho, Il-Hwan;Lee, Joo-Y.;Hwang, Daniel-H.;Kim, In-Kyung
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.105-112
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    • 2003
  • Selective COX (cyclooxygenase)-2 inhibitors including celecoxib have been shown to induce apoptosis and cell cycle changes in various tumor cells. New inhibitors are recently being developed as chemomodulating agents. We evaluated celecoxib and screened 150 synthetic compounds for anti-proliferative activities in vitro. Effects of celecoxib on COX activity, cell growth, cell cycle distribution, and apoptosis induction were determined in A549 COX-2 overexpressing human non-small cell lung cancer (NSCLC) cells. The COX inhibition of celecoxib increased with concentration up to 82% at $1\;{\mu}M$ after 24 hr exposure. Forty ${\mu}M$ and $50\;{\mu}M$ of ce1ecoxib induced $G_1$ arrest, and TUNEL-positive apoptotic cells, respectively. Among 150 compounds, several compounds were selected for having greater COX-2 inhibitory activity and higher selectivity than celecoxib with growth inhibitory activity. Celecoxib showed concentration-dependent COX inhibitory activity, and ability to induce cell cycle arrest and apoptosis in human NSCLC cells in vitro. Among synthetic analogues screened, several compounds showed promising in vitro activity as COX-2 inhibitory anticancer agents, which warrant further evaluation in vitro and in vivo.

Studies on Biological Activities of the Polysaccharides and Oligosaccharides of Orostachys japonicus (와송 다당체 및 올리고당류의 생리 활성)

  • Kim Ki Hoon;Kim Eun Young;Kim Yea Oon;Baek Geum Ok;Kim Han Bok;Lee Dong Seok
    • Korean Journal of Microbiology
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    • v.40 no.4
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    • pp.334-341
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    • 2004
  • Polysaccharides were prepared from Orostachys japonicus by extration with hot steam water (OJPl). The OIPl fraction was further purified by Sephadex G-50 gel filtration chromatography to produce FI (polysaccharides) and FII (oligosaccharides) fraction. The average molecular masses o fFI and FII fraction were determined to be 3050 kDa and 13 kDa, respectively. The antimicrobial activity of OIPl was tested against 8 strains of bacteria and one strain of yeast by the disc diffusion method, fluorescein diacetate (FDA) method and broth dilution method. The OIPl exhibited a very strong growth inhibition to Candida albicans. The OIPl remarkably sup­pressed the growth of Salmonella typhimurium and Staphylococcus aureus. The OIPl showed higher growth inhibition to Escherichia coli and Pseudomonas aeruginosa than propolis, positive control. When the anticancer activity of the OIPl, FI or FII was examined against human cancer cell lines and the Sarcoma 180 cells, these widely suppressed the proliferation of cell lines in the MTT assay and morphology study. Especially, they remarkably inhibited the growth of A549, HeLa and AGS cells. Also treatment of cancer cells with OJPl, FI or FII induced apoptotic cell death characterized by DNA fragmentation. The OJPl, FI or FII exhibiting various biological activities such as antimicrobial activity and anticancer activity is expected to be developed as new biohealth products.

Polyphenol and Flavonoid Contents, Antioxidative and Cancer Cell Inhibitory Effects of Domestic Tomatoes (우리나라 토마토의 폴리페놀 및 플라보노이드 함량, 항산화활성 및 암세포 억제활성)

  • Choi, Suk-Hyun
    • The Journal of the Korea Contents Association
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    • v.21 no.12
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    • pp.879-887
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    • 2021
  • This study was carried out for elucidating bioacive properties of three domestic tomato cultivars. Total polyphenol and flavonoid of Rafito, Momotaro and Medison were 10.44±1.84, 11.14±1.95, 12.26±1.82 and 3.62±0.57, 3.24±0.35, 3.87±0.60 mg/g(dry weight) respectively. Domestic tomatoes showed DPPH and ABTS radical scavenging activities. All of tomatoes had no cytotoxicity for normal liver cell, but showed remarkable growth inhibitory effect against cervical cancer cell and liver cancer cell. These results suggested that domestic tomatoes can be used as a bioactive food material.

A New Sesterterpene from the Korean Sarcotragus sp. Sponge

  • Woo, Jung-Kyun;Jeon, Ju-eun;Kim, Bora;Sim, Chung J.;Oh, Dong-Chan;Oh, Ki-Bong;Shin, Jongheon
    • Natural Product Sciences
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    • v.21 no.4
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    • pp.237-239
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    • 2015
  • Sarcotragin C (1), a new sesterterpene metabolite was isolated from a Sarcotragus sp. sponge collected from Chuja Island, Korea. On the basis of the combined spectroscopic analyses, the structure of this compound was determined to be a linear norsesterterpene containing a leucine-derived ${\gamma}-lactam$ moiety. This compound exhibited moderate cytotoxicity against K562 and A549 cell-lines.

Antioxidant and Anticarcinogenic Effects of Domestic Yellow Cherry Tomato (국내산 황색 방울토마토의 항산화활성 및 암세포 생육억제 효과)

  • Choi, Suk-Hyun
    • The Journal of the Korea Contents Association
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    • v.21 no.11
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    • pp.518-527
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    • 2021
  • This study verifies the polyphenol and flavonoid contents of a dried extract, as well as its antioxidant effect and growth inhibitory effect on cancer cells to investigate the potential of yellow cherry tomatoes as a physiologically active food material. The polyphenol and flavonoid contents were determined as 10.96 ± 1.57 and 4.12 ± 0.41 mg/g, respectively. The antioxidant activity was confirmed by measuring DPPH and ABTS radical scavenging ability, and RC50-the concentration that reduces free radicals by 50%-were determined as 490.83 ± 17.35 ㎍/mL and 355.90 ± 0.79 ㎍/mL, respectively. The dried extract showed no cytotoxicity with respect to normal hepatocytes (Chang) and no growth inhibitory activity with respect to A549 lung cancer cells, whereas dried extract showed growth inhibitory activities of 15.2% and 18.4% with respect to human cervical adenocarcinoma (HeLa) and human hepatocellular carcinoma (HepG2) cells, respectively, when treated with a concentration at 100㎍/mL. The results of this study confirm the potential of yellow cherry tomatoes as a physiologically active food material by verifying their antioxidant activity and their growth inhibitory activity with respect to cervical and liver cancer cells.

DOBI is cleaved by caspases during TRAIL-induced apoptotic cell death

  • Park, Sun-Young;Shin, Jin-Na;Woo, Ha-Na;Piya, Su-Jan;Moon, Ae-Ran;Seo, Young-Woo;Seol, Dai-Wu;Kim, Tae-Hyoung
    • BMB Reports
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    • v.42 no.8
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    • pp.511-515
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    • 2009
  • Downstream of Bid (DOBI) known as Pus10, has been identified as a modulator of TRAIL-induced cell death using RNAi library screening. The crystal structure of DOBI has revealed that it is a crescent-shaped protein containing the pseudouridine synthase catalytic domain and a THUMP-containing domain. Here, we demonstrated that DOBI is expressed in various tissues such as heart and lung, and is also expressed in various tumor cells such as HeLa and A549. Although ectopic expression of DOBI does not promote TRAIL death signaling in HeLa cells, knock-down of DOBI expression using shRNA inhibited TRAIL death signaling. DOBI is cleaved into a 54 kD cleaved DOBI during cell death, and the recombinant DOBI protein can be directly cleaved by caspases-3, or -8 in vitro. Together, these data suggest that the cleaved DOBI may acquire a new function, possibly by cooperating with tBid in the mitochondrial event of cell death caused by TRAIL.

3,7-Dihydroxy-2,4,6-trimethoxyphenanthrene, A New Phenanthrene from Bulbophyllum Odoratissimum (Bulbophyllum Odoratissimum에서 추출한 새로운 페난트렌, 3,7-Dihydroxy-2,4,6-trimethoxyphenanthrene)

  • Chen, Ye-Gao;Xu, Jun-Ju;Yu, Hong;Qing, Chen;Zhang, Yan-Li;Liu, Ying;Wang, Ji-Hua
    • Journal of the Korean Chemical Society
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    • v.51 no.4
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    • pp.352-355
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    • 2007
  • A new phenanthrene derivative 3,7-dihydroxy-2,4,6-trimethoxyphenanthrene was isolated from the all plant of Bulbophyllum odoratissimum, and its structure was elucidated by extensive spectral studies and chemical transformation. The compound displayed cytotoxicity against the growth of human leukemia cell lines K562 and HL-60, human lung adenocarcinoma A549, human hepatoma BEL-7402 and human stomach cancer cell lines SGC-7901 with IC50 values of 14.23, 10.02, 3.42, 15.36 and 1.13 mg/ml respectively.

Sesquiterpene Glycosides from the whole Plant Extract of Youngia japonica (뽀리뱅이 전초로부터 분리한 Sesquiterpene 배당체)

  • Kim, Mi-Ri;Cha, Mi-Ran;Choi, Yeon-Hee;Choi, Chun-Whan;Choi, Sang-Un;Kim, Young-Sup;Kim, Young-Kyoon;Kim, Young-Ho;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.41 no.2
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    • pp.103-107
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    • 2010
  • Extensive phytochemical investigation of the methanol extract from the whole plant of Youngia japonica (Asteraceae) led us to the isolation of a new guaiane-type sesquiterpene (1), together with three related guaianolides, youngiajaponicoside A (2), crepiside H (3) and crepeside E (4). The chemical structure of 1 was elucidated by the aid of spectroscopic analyses including 2D-NMR experiments (COSY, HMBC, HMQC and ROESY). The isolated components (1-4) were evaluated for the inhibitory effect on the proliferation of four cultured human tumor cell lines such as A549, SK-OV-3, SK-MEL-2 and HCT-15, in vitro.

Study on Antitumor Activity of Sobokchukeotang and Kamisobokchukeotang (소복축어탕과 가미소복축어탕이 항암활성에 미치는 영향)

  • 신원웅;최주선;길재호;김성훈
    • The Journal of Korean Medicine
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    • v.22 no.2
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    • pp.22-30
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    • 2001
  • This study was attempted to investigate the anti-tumor and anti-metastatic effects of Sobokchukeotang(SBCT) and Kamisobokchukeotang(KSBCT). Cytotoxicity against various cancer cell lines, anti-adhesion, pulmonary colonization, anti-angiogenesis, and T/C% were evaluated. SBCT and KSBCT exhibited no cytotoxicity against HT-1080, A549, SK-OV-3, B16-F10 and SK-Mel-2 cell lines. In inhibitory effect on DNA topoisomerase I, the $IC_{50S}$ were shown $250-500{\;}\mu\textrm{g}/ml$ of SBCT and $62.5-125{\;}\mu\textrm{g}/ml$ of KSBCT respectively. In the in vivo experiments, SBCT(135.98%) and KSBCT(151.92%) apparently increased the life span of mice bearing sarcoma-180. KSBCT significantly inhibited the adhesion of HT-1080 to complex extracellular matrix in a dose-dependent manner in contrast to SBCT. In pulmonary colonization assay by B16-F10, a number of colonies in the lungs were decreased more significantly in KSBCT group than those in SBCT group. In vitro neovascularization and CAM assay, angiogenesis was more significantly inhibited in KSBCT-treated group than in SBCT- treated group. Above results suggests that KSBCT is more effectively applied to prevention and treatment of cancer than SBCT.

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A Cytotoxic Monoterpene-Neolignan from the Stem Bark of Magnolia officinalis

  • Youn, Ui-Joung;Lee, Ik-Soo;Chen, Quan Cheng;Na, Min-Kyun;Jung, Hyun-Ju;Lee, Sang-Myung;Choi, Jae-Sue;Woo, Mi-Hee;Bae, Ki-Hwan;Min, Byung-Sun
    • Natural Product Sciences
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    • v.17 no.2
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    • pp.95-99
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    • 2011
  • A monoterpene-neolignan, piperitylmagnolol (1), was isolated from the stem bark of Magnolia officinalis, together with syringaresinol (2), caffeic acid (3), and sinapaldehyde (4). The isolated compounds were established on the basis of spectroscopic and physicochemical analyses including 1D- and 2D-NMR techniques, as well as on comparing the spectral data with those in the literature and of authentic samples. Compounds 1 - 4 were tested for their cytotoxic activity against the HeLa, K562, A549, and HCT116 cancer cell lines in vitro. Of the isolates, piperitylmagnolol (1) exhibited cytotoxic activity against the tested cancer cell lines with $IC_{50}$ values of 7.7 - 9.5 ${\mu}g/ml$.