• Title/Summary/Keyword: SK-MEL-2

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Tsaokoarylone, a Cytotoxic Diarylheptanoid from Amomum tsao-ko Fruits

  • Moon, Surk-Sik;Cho, Soon-Chang;Lee, Ji-Young
    • Bulletin of the Korean Chemical Society
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    • v.26 no.3
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    • pp.447-450
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    • 2005
  • The crude methanol extract of the fruits of Amomum tsao-ko (Zingiberaceae) showed cytotoxic activity. Bioactivity-guided separation led to the isolation of a diarylheptanoid, tsaokoarylone [7-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one] (2). 2 showed cytotoxicity at 4.9 and 11.4 $\mu$g/mL ($IC_{50}$) against human nonsmall cell lung cancer A549 and human melanoma SK-Mel-2, respectively, determined by SRB colorimetric method. During purification-(4-hydroxyphenyl)-4-hydroxyhexan-2-one (4) together with three known diarylheptanoids was also isolated. Their structures were determined from interpretation of spectroscopic data (IR, UV, MS, and NMR) and synthesis confirmed the structure of 2.

Brine Shrimp Lethality of the Compounds from Phryma leptostachya L.

  • Lee, Sang-Myung;Min, Byung-Sun;Kho, Yung-Hee
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.652-654
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    • 2002
  • Brine shrimp assay-guided fractionation and isolation of the EtOAc soluble fraction of Phryma leptostachya L. (Phrymacaceae) gave two active compounds, phrymarolin II (1) and ursolic acid (2), which were identified by physicochemical and spectroscopic methods. Compound 1 exhibited potent lethality with $LD_{50}$ value of 0.0013 $\mu\textrm{g}$/ml, whereas 2 showed moderate lethality with $LD_{50}$ value of 27.0 $\mu\textrm{g}$/ml against brine shrimp. The cytotoxic activities of 1 and 2 were also evaluated against one murine and five human cancer cell lines employing the sulforhodamin B (SRB) method. Compound 2 exhibited cytotoxic activity against L1210 and SK-MEL-2 cells with $ED_{50}$ values of 3.70 and 9.27 mg/ml, respectively, whereas 1 was devoid of any cytotoxic activity against all cancer cells tested.

Antioxidative Effect and Melanogenesis of Nelumbo nucifera Stamen Extract on Cultured Human Skin Melanoma Cells Injured by Hydrogen Peroxide (연꽃수술추출물이 과산화수소로 손상된 배양 인체피부흑색종세포에 대한 항산화효과 및 멜라닌화에 미치는 영향)

  • Kim, Myoung-Seoup;Park, Yun-Jum;Sohn, Young-Woo
    • Korean Journal of Plant Resources
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    • v.23 no.2
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    • pp.145-150
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    • 2010
  • To examine the antioxidative effect and melanogenesis of Nelumbo nucifera stamen (NNS) extract on hydrogen peroxide $H_2O_2$ induced cytotoxicity in cultured human skin melanoma cells (SK-MEL-3), cell adhesion activity (CAA), tyrosinase inhibitory activity and total amount of melanin synthesis were measured by colorimetric assay. In this study, $H_2O_2$ significantly decreased CAA, and $CAA_{50}$ value of $H_2O_2$ was determined at 30 uM. In the antioxidative effect, NNS extract increased cell adhesion activity which was decreased by $H_2O_2$ induced cytotoxicity, and also, tyrosinase activity and total amount of melanin were decreased by NNS extract. These results suggested that $H_2O_2$ was highly toxic on cultured human skin melanoma cells and NNS extract showed the antioxidative and inhibitory effect of melanogenesis by the increased CAA, and the decresed tyrosinase activity and total amount of melanin synthesis.

Ircinin-1 from the Sponge Sarcotragus Species Induces of Cell Proliferation and Apoptosis in the Human Skin Cancer Cells

  • Choi, Hye-Joung;Yee, Su-Bog;Park, Hwa-Sun;Chung, Sang-Woon;Park, Sang-Eun;Jung, Jee-Hyung;Kim, Nam-Deuk
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.256.1-256.1
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    • 2002
  • We investigated the anti-proliferative effects of a new compound. ircinin-1. from the sponge Sarcotragus sp. on SK-MEL -2 human skin cancer cells. From the data of MTT assay, cell viability was decreased by ircinin-1 in a dose-dependent manner. We observed that the anti-proliferative effect of ircinin-1 was due to the induction of apoptosis, which was confirmed by observing the morphological changes. the increased ratio of pro-apoptotic protein Bax to anti-apoptotic protein Bcl-2, and cleavage of poly(ADP-ribose) polymerase protein, via activation of caspase-3. (omitted)

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CYTOTOXICITIES OF GINSENG SAPONINS AND THEIR DEGRADATION PRODUCTS AGAINST SOME CANCER CELL LINES AND STRUCTURE-ACTIVITY RELATIONSHIP (수종의 암세포주에 대한 인삼 사포닌 및 그 분해산물의 구조와 세포독성 관계)

  • Baek N.I.;Kim S.I.;Lee Y.H.;Kim D.S.;Park J.D.;Lee C.B.
    • Proceedings of the Ginseng society Conference
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    • 1993.09a
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    • pp.132-137
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    • 1993
  • Several Prosapogenins and sapogenins obtained by acid hydrolysis or alkaline cleavage of Korean red ginseng saponins were separated and identified by spectral and physical methods. Some of these degradation products showed the cytotoxic activities against various cancer cell lines, that is, A549, SK - OV - 3, L121O, P388 and K562. The significant difference of activity between stereoisooers was not approved and the activity was inversely proportional to the number of sugars binding to sapogenins. It was clear that diol type prosapogenins and sapogenins were more cytotoxic than triol type ones.

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Novel Benzoylurea Derivatives as Potential Antitumor Agents; Synthesis, Activities and Structure-Activity Relationships

  • Hwang, Ki-Jun;Park, Kyung-Ho;Lee, Chong-Ock;Kim, Beom-Tae
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.781-785
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    • 2002
  • A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

Antitumor Activity of 23, 24-dihydrocucurbitacin D Isolated from Bryonia alba L.

  • Sohn, Hyung-Ok;Lee, Young-Gu;Lim, Heung-Bin;Kwon, Nyoun-Soo;Goorgen V. Aprikian;Lee, Dong-Wook
    • Toxicological Research
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    • v.16 no.4
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    • pp.263-267
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    • 2000
  • The cytotoxic and antitumor activity of 23,24-dihydrocucurbitacin D (dhc D) isolated from Bryonia alba L. was examined. Our results showed that dhc D strongly inhibited the viability of the cultured cancer cells, A-549, COLO 205, SK-MEL-2, and L121O. It also exhibited effective antitumor activity in ICR mice, which had been intra peritoneally implanted with sarcoma 180 ascites tumor cells. The dhc D also strongly inhibited the viability of immortalized macrophages RAW 264.7, but not normal peritoneal macrophages. These results indicate that dhc D has antiproliferative effect on cancer cells and it may more sensitive on immortalized cells than normal cells.

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Lupane Derivatives-I: Synthesis and Cytotoxic Activity (루판 유도체의 합성 및 세포독성-I)

  • You, Young-Jae;Kim, Yong;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.46 no.5
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    • pp.295-300
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    • 2002
  • To observe the structure-activity relationship of lupane derivatives both on cytotoxic and antiangiogenic activity, twelve lupane derivatives were prepared; their antiangiogenic and cytotoxic activities were evaluated. Among them, four compounds were more cytotoxic than betulinic acid. Carboxylic acid at C28 seemed to be essential for cytotoxic activity. But, a selective cytotoxicity toward SK-MEL-2 was not observed. As for antiangiogenic activity, none of the compounds except lupeol showed antiangiogenic activity at 30 $\mu\textrm{g}$/mL.

Effects of Gleditsia spina (GS) water extract on Gene Expression of Human Melanoma cells, by using Microarry technique (DNA chip을 이용한 조각자 추출물의 인간유래 악성 종양에 미치는 영향)

  • Park, Yong-Ho;Kim, Jong-Han;Park, Su-Yeon;Choi, Jeong-Hwa
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.21 no.1
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    • pp.55-69
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    • 2008
  • Objective : This study was designed to investigated effects of Gleditsia spina (GS) on human derived melanoma cells Methods : The genetic profile for the effect of medicine on human derived melanoma cells of SK-MEL-2, was measured by using microarray technique, and the functional analysis on these genes was conducted. The network of total protein interactions was measured by using cytoscape program. Results : Total 253 genes were up-regulated and 439 genes down-regulated in cells treated with GS. Genes induced or suppressed by GS were all mainly concerned with metabolic process, regulation of biological process and protein binding. Conclusion : Suggest the possibility of GS as anti-cancer drug and cosmetic agent, and also suggest that related mechanisms are involved in regulation of intra-cellular metabolism in melanoma cells.

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Synthesis and Evaluation of Cytotoxicity of Novel Arylsulfonylimidazolidinones Containing Sulfonylurea Pharmacophore

  • Jung, Sang-Hun;Song, Jae-Shin;Lee, Hui-Soon;Choi, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.570-580
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    • 1996
  • Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones 3 and 4-phenyl-3-arylsulfonylimidazolones 4 and evaluation of their cytotoxic activity against eleven human cancer cell lines and two murine leukemia cell lines in vitro were performed. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolones (3) has been found to be the potential anticancer agent. Compounds 3b, 3c, and 3d exhibit strong activity as indicated by their $IC_{50}$ values 0.39, 3.19, $0.31{\mu}g/mL$ against A549 and 0.80, 0.48, $0.0007{\mu}g/mL$against SK-Mel-2, respectively. These compounds also possess much more potent activity (10-1000 times) than LY186641 against eleven other cell lines.

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