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      • In vitro antitumor activity of flavonoids from Sophora flavescens

        Ryu, Shi Yong 대전대학교 韓醫學연구소 1997 한의학연구소 논문집 Vol.5 No.2

        The cytotoxicity-guided fractionation of the roots of Sophora flavescens (Leguminosae) extracts led to the isolation of fifteen active principles 1∼15, responsible for the cytotoxicity against five kinds of cultured human tumor cell lines, i.e., A549(non small cell lung), SK-OV-3(ovary), SK-MEL-2(skin), XF498(central nerve system) and HCT-15(colon), evaluated by SRB method in vitro. Compounds 2∼14 were classified as unusual flavonoid occurred exclusively in this species and the proliferation of each examined tumor cells were significantly inhibited during the continuous exposure to compounds 1∼15 for 48 hours, respectively.

      • KCI등재

        白花蛇舌草 헥산分劃과 多糖體가 抗癌 및 抗轉移 活性에 미치는 影響 : Ursolic acid와 Asperuloside 병용투여시 항암 및 항전이 효과에 관한 연구

        宋圭鏞,柳時容,金聖勳 대한동의병리학회 1999 동의생리병리학회지 Vol.13 No.1

        산업기술의 발달로 인한 삶의 질의 향상과 더불어 현대의학의 발달에도 불구하고 아직도 불치의 병으로 여겨지고 있는 암에 의한 사망률은 계속 증가되고 있는 추세로 암을 치유하기 위한 연구가 활발히 전개되고 있다. 백화사설초는 항암 본초로 분류되어 암치료를 위해 한방처방에 가미되어 응용되고 있다. 그러나 백화사설초의 성분에 대한 연구는 미흡한 실정이다. 이런 점을 감안하여 본 연구실에서는 백화사설초의 용매 분획 중 헥산 분획이 수종의 암세포에 대해서 세포독성이 있음을 발견하고 물질분리를 실시하여 물질을 단리한 후 물리·화학적인 방법을 통하여 구조를 확인 한 결과 ursolic acid(UA)가 효과를 나타내는 물질이라는 것을 밝혔다. 따라서 UA의 구체적인 항암 및 항전이 효과를 검증하기 위하여 수종의 암세포에 대한 세포독성, 부착저지효과, 폐암전이 억제효과, 혈관형성 억제효과, 암전이에 관련된 유전자인 MMP-2의 발현 정도를 살펴보았고 면역세포에 미치는 영향은 물론 배당체인 asperuloside(AS)를 분리하여 UA와 병용투여하므로써 항암 및 항전이 활성의 변화를 관찰하여 항암제로서의 가능성을 타진하고자 하였다. 실험결과 UA는 수종의 암세포에 농도의존적으로 암의 성장을 억제하였으며, AS의 병용투여시 상승적인 세포독성 효과를 발휘하지 않았다. 그러나 세포부착 저지효과, 혈관형성 억제효과 및 폐암전이 효과와 같은 암전이에 관련된 실험에서 AS는 UA의 효과를 상승적으로 증가시켰을 뿐만아니라 면역세포에 대해서도 증가효과를 나타냈다. 이상의 결과로부터 UA는 항암 및 항전이 효과가 있음을 발견하였으며, AS와 같은 배당체의 병용투여는 이러한 항암 및 항전이 효과를 증가시키는 것으로 보아 암에 유효하게 사용될 수 있으리라 사료된다. Ursolic acid(UA), isolated from the Oldenlandia diffusa(Rubiaceae), is a triterpenoid compound that exist widely in food, medicinal herbs, and other plants and has been recognized to have a wide spectrum of pharmacological activity such as antiinflammatory effect, anti-HIV activity, antihyperlipidemic activity, and antitumor activity. Ursolic acid was treated either alone or in combination with asperuloside(AS), irridoidal glycoside, for the evaluation of antitumor and antimetastatic effects by several experimental parameters, for example, cytotoxicity against various cancer cell line, clonogenic assay, antiadhesion assay, CAM assay, pulmonary colonization assay, MMP-2 expression, and immunological analysis by FACS. The results were obtained as follows; Ursolic acid showed a potent cytotoxic activity in a dose dependent manner against SF295, SK-OV-3, HCT15, and UN-2 cancer cell lines, while combined treatmenmt of UA & AS didn't. However, UA & AS were more effectiv than UA only in inhibitory effect on cell adhesion of A549 cells to complex extracellular matrix in vitro and pulomonary colonization assay by B16BL/6 in vivo. In the clonogenic assay UA & AS more effectively inhibited colony formation by A549 synergistically to 97% than UA to 78%. By analysis by FACS UA & AS activated CD4(T helper cell) and CDB(cytotoxic T cell) as well as macrophage while UA activated macrophage only. UA and AS suppressed MMP-2 gene expression more effectively than UA only in a dose dependent manner. These results suggest that combined therapy of ursolic acid and asperuloside showed antitumor and antimetastatic effects than ursolic aicd only so that Oldenlandiae diffusae Herba can be effectively applied for the prevention and treatment of cancer. It also is very necessary that biological activities and their mechanism should be kept studying between different constituents isolated from same plant.

      • KCI등재

        Screening of Various Sources of Phytochemicals for Neuroprotective Activity against Oxygen-Glucose Deprivation in vitro

        장현주,김영섭,류시용,전향숙 한국응용생명화학회 2013 Applied Biological Chemistry (Appl Biol Chem) Vol.56 No.4

        Neuroprotective activities of 176 phytochemicals were investigated against oxygen-glucose deprivation in vitro using primary cortical neuron culture. Diterpenes (taxol and taxol C)were the most potent neuroprotective compounds. EC50 of taxol and taxol C were 0.402 and 0.452 μM, respectively. This result supports the use of an in vitro model as initial screening for neuroprotective candidates, which warrants further testing in animal models.

      • 참소리쟁이의 세포독성 성분

        김대근,최상운,류시용,이강노,지옥표 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

        Activity-guided fractionation and repeated column chromatography afforded two cytotoxic compounds R-3 and R-4 from the root of Rumex japonicus HOUTT. Compounds were identified as musizin and emodin, respectively, by the physicochemical and spectral data. Besides R-3 and R-4, two compounds R-1 and R-2, chrysophanol and physcion, respectively, were also isolated. The compound R-3 and R-4 exhibited cytotoxicity against cultured human tumor cell lines. A-549, SK-OV-3, SK-MEL-2, XF498 and HCT15 with ED_50 values ranging from 2.68 to 10.06㎍/㎖.

      • KCI등재

        Anti-osteoclastogenic diacetylenic components of Dendropanax morbifera

        김은혜,조창수,류시용,김성환,이지영 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.5

        Methanol (MeOH) extract of the aerial parts ofDendropanax morbifera (Araliaceae) has demonstrated asignificant dose-dependent inhibitory effect on theRANKL-induced differentiation of bone marrow-derivedmacrophages to osteoclasts. Bioassay-guided fractionationof the extract resulted in the isolation of a novel diacetylenecarboxylic acid (1), together with a known diacetyleniccompounds (2) as phytochemicals to strongly inhibitthe osteoclast differentiation. The chemical structure of 1was determined by spectroscopic analyses as (9Z,16S)-16-O-acetyl-9,17-octadecadiene-12,14-diynoic acid, that isacetyl derivative of 2. Two diacetylenic components of D. morbifera, 1 and 2 exhibited a dose-dependent inhibitoryeffect on the RANKL-induced formation of tartrate-resistantacid phosphatase-positive multinucleated cells withIC50 values of 2.4 and 3.1 lM, respectively. Seven otherknown components (3–9) were also isolated from theextract: dendropanoxide (3), friedelin (4), epifriedelanol(5), a-amyrin (6), b-amyrin (7), b-sitosterol (8), and stigmasterol(9). The significant anti-osteoclastogenic activitiesof 3, 4, 5, and 7 were first reported in this study.

      • KCI등재

        Inhibitory Effects of Saururus Chinensis Extracts on Osteoclast Differentiation

        심기숙,김순남,김명희,김영섭,류시용,민용기,김성환 한국생약학회 2008 Natural Product Sciences Vol.14 No.2

        Saururus chinensis is a commonly used folk herb for the treatment of edema and liver diseases in Korea. To study the biological activity of Saururus chinensis in bone metabolism, we evaluated the effect of its extracts on osteoclast differentiation in vitro using primary mouse bone marrow-derived macrophages. Methanol extract (ME) from dried roots of Saururus chinensis was partitioned into methylene chloride (MF), ethyl acetate (EF), n-butanol (BF) and water fractions (WF). Tartrate-resistance acid phosphatase (TRAP) activity assay and western blot analysis were performed to determine the effect on osteoclast differentiation and mitogen-activated protein (MAP) kinases activation. ME, MF and EF dramatically inhibited receptor activator of NF-κB ligand (RANKL)-induced formation of multinucleated osteoclasts and activation of MAP kinases. This study firstly demonstrated that ME, MF and EF of Saururus chinensis have the potential to inhibit the osteoclast differentiation, which results from the inhibition of MAP kinases activations in part.

      • Induction of Apoptosis by Yomogin in Human Promyelocytic Leukemic HL-60 Cells

        JEONG, Seoung-Hee,KOO, Sung-Ja,HA, Joo-Hun,RYU, Shi-Yong,PARK, Hee-Juhn,LEE, Kyung-Tae WHO COLLABORATING CENTRE FOR TRADITIONAL MEDICINE 2004 東西醫學硏究所 論文集 Vol.2004 No.-

        Yomogin is an active compound isolated from Artemisia princep, a traditional Oriental medicinal herb, which has been shown to inhibit tumor cell proliferation. In this study, we investigated the effects of yomogin on the cytotoxicity, induction of apoptosis, and putative pathways of its actions in human promyelocytic leukemia cells. Yomogin-treated HL-60 cells displayed several features of apoptosis, including DNA fragmentation, formation of DNA ladders in agarose gel electrophoresis, and externalization of annexin-V targeted phosphatidylserine residues. We observed that yomogin caused activation of caspase-8, caspase-9, and caspase-3. A general caspase inhibitor (z-VAD-fmk), caspase-8 inhibitor (z-IETD-fmk) and caspase-3 inhibitor (z-DEVD-fmk), almost completely suppressed the yomogin-induced DNA fragmentation. We further demonstrated that yomogin induced Bid cleavage, mitochondrial translocation of Bax from the cytosol, and cytochrome c release from mitochondria in a caspase-8-dependent manner. Taken together, our data indicate that yomogin is a potent inducer of apoptosis and facilitates its activity via caspase-8 activation, Bid cleavage, Bax translocation to mitochondria, and subsequent release of cytochrome c into the cytoplasm, providing a potential mechanism for the anticancer activity of yomogin.

      • KCI등재후보

        Phytochemical Constituents of the Aerial Parts from Aster hispidus

        이성옥,Sang Zin Choi,최상운,류시용,이강노 한국생약학회 2004 Natural Product Sciences Vol.10 No.6

        The chromatographic separation of the MeOH extract of the aerial parts from Aster hispidus (Compositae) led to the isolation of eight compounds. Their structures were established by spectroscopic methods to be β-amyrin$ (1), oleanolic acid (2), (2R)-1, 2-O-(9Z, 12Z, $15Z-dioctadecatrienoyl)-3-O-{\beta}-D-galactopyranosyl\;glycerol$ (3), trans-phytol (4), 9, 12, 15-octadecatrienoic acid (5), kaempferol (6), 3,5-dicaffeoyl quinic acid (7), 3,4-dicaffeoyl quinic acid (8) and kaempferol-3-O-rutinoside (9). Compounds 1, 3~6 and 9 showed non-specific moderate cytotoxicity against five human tumor cell lines $(5.44{\sim}23.51\;{\mu}g/ml)$. The other compounds were of marginal activity against tested five human cancer cell lines $(9.05{\sim}>30.0\;{\mu}g/ml)$.

      • KCI등재

        참소리쟁이의 세포독성 성분

        김대근(Dae Keun Kim),최상운(Sang Un Choi),류시용(Si Yong Ryu),이강노(Kang Ro Lee),지옥표(Ok Pyo Zee) 대한약학회 1998 약학회지 Vol.42 No.3

        Activity-guided fractionation and repeated column chromatography afforded two cytotoxic compounds R-3 and R-4 from the root of Rumex japonicus HOUTT. Compounds were identified as musizin and emodin, respectively, by the physicochemical and spectral data. Besides R-3 and R-4, two compounds R-1 and R-2, chrysophanol and physcion, respectively, were also isolated. The compound R-3 and R-4 exhibited cytotoxicity against cultured human tumor cell lines, A-549, SK-OV-3, SK-MEL-2, XF498 and HCT15 with ED50 values ranging from 2.68 to 10.06mcg/ml.

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