• Title/Summary/Keyword: Activity-guided purification

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Radical Scavenging Activity of Gallic Acid from Woodfordia Fruticosa Flowers

  • Bhatt, Lok Ranjan;Yook, Chan-Nam;Choi, Hwa-Jung;Baek, Seung-Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.4
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    • pp.903-906
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    • 2008
  • Woodfordia fruticosa Kurz (Lythraceae) is used in the treatment of various ailments in traditional medicines. DPPH activity guided fractionation and purification process was used to identify the free radical-scavenging components from the flowers of this plant. The methanolic extract of the plant was first fractionated into four extracts; namely, n-hexane, chloroform, ethyl acetate and water fractions. Among them, the ethyl acetate fraction was found to be the most effective and was further subjected to activity guided-fractionation and isolation procedures. After successive column chromatography on silica gel and Sephadex LH-20, gallic acid, which is responsible for the radical scavenging activity, was isolated and its structure was elucidated by spectral methods ($^1H$ NMR, $^{13}C$ NMR) and by comparison with literature.

Cytotoxic Quassinoids from Simaba cedron

  • Hitotsuyanagi, Yukio
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.52-55
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    • 1998
  • During a survey of new antitumor substances from higher plants, we have found that the crude extract of Simaba cedron Planchon (Simaroubaceae) showed cytotoxic activity (IC$\sub$50/ 0.7 $\mu\textrm{g}$/mL) against P388 leukemia cells. Activity-guided chromatographic purification using P388 cells led to the isolation of five novel quassinoids, cedronolactones A-E (1-5) and nine known quassinoids, simalikalactone D (6), chaparrinon (7), chaparrin (8), glaucarubolone (9), glaucarubol (10), samaderine Z (11), guanepolide (12), ailanquassin A (13), and polyandrol (14). In this seminar, the structural elucidation of 1-5 and the cytotoxic activity of the isolated compounds are discussed.

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Analysis of Cytotoxic Constituent of Berberis koreana Palibin (매자나무 세포독성성분 분석)

  • Kim, Young-Kyoon;Kwak, Byung-Man
    • Journal of the Korean Wood Science and Technology
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    • v.26 no.3
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    • pp.100-107
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    • 1998
  • Methanol extracts of five Berberidaceae species were examined against tissue factor inhibitory and tumour cell growth inhibitory activity. Methanol extracts of Berberis koreana Palibin showed a strong cytotoxicity activity against SK-MEL-2 (Melanoma) tumour cell lines with more than 90% in $25{\mu}g/m\ell$ and against A549 (Lung carcinoma), SK-OV-3 (Ovarian cancer), XF498 (CNS cancer) and HCTl5 (Colon cancer), other Berberidaceae species except B. koreana species have no effect on the tumour cells. Biologically active compound, therefore, was isolated through the activity guided fractionation and purification. The structure was confirmed by NMR. FT-IR and MS to 2-(3,4-dihydroxybenzyl)-ethyl alcohol. It showed cytotoxicity activity against SNU-C4 tumour cell lines with 50.7% in $50{\mu}g/m\ell$. Methanol extracts of 5 Berberidacae species have no effect on the tissue factor inhibitory activity.

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Anti-oomycete Activity of Furanocoumarins from Seeds of Psoralea corylifolia against Phytophthora infestans

  • Shim, Sang-Hee;Kim, Jin-Cheol;Jang, Kyoung-Soo;Choi, Gyung-Ja
    • The Plant Pathology Journal
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    • v.25 no.1
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    • pp.103-107
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    • 2009
  • In the course of a searching natural antifungal compounds from plant seeds, we found that the methanol extract of Psoralea corylifolia seeds showed potent control efficacy against tomato late blight caused by Phytophthora infestans and wheat leaf rust Puccinia recondita. Under bioassay-guided purification, we isolated two furanocoumarins, psoralen and isopsoralen, with anti-oomycete activity against P. infestans. By 1-day protective application, both compounds strongly reduced the disease development of P. infestans on tomato seedlings, but hardly controlled development of leaf rust on wheat seedlings. This is the first report on the anti-oomycete activity of P. corylifolia as well as that of psoralen and isopsoralen.

Isolation and Evaluation of an Antitumor Constituent from Pyrolae Herba (녹수초의 항암활성물질의 분리 및 항암력 평가)

  • Bae, Ki-Hwan;Kim, Hwan-Mook;Lee, Sang-Myung
    • YAKHAK HOEJI
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    • v.40 no.2
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    • pp.225-229
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    • 1996
  • The cytotoixic effect of Pylorae Herba (Pyrola japonica Klenze) against L1210 and K-562 cells was studied in vitro. The methanolic extract of Pylorae Radix was add ed to the culture of L1210 cells and K-562 cells for the cytotoxic activity and the ED50 values of hexane, ethylacetate, buthanol and water fractions from methanolic extract were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide) assay. The active constituent isolated by bioassay guided fractionation followed by purification gave rise to a yellow needle crystal and was clarified to be chimaphilline by the comparison with the published data. The average life spans with it were not prolonged significantly on tumor growth in hybrid female mouse (BDF1-KIST) inoculated subcutaneously with P388 cells.

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Studies on the Screening of Bioactive Compound Acting on Intracellular Enzymes from Natural Products and Its Mode of Action : Inhibitory Component of Puerariae Radix on Alcohol Dehydrogenase Activity (천연물로부터의 세포내 효소 활성 조절물질의 탐색 및 기능 연구: 갈근의 알코을 탈수소효소 저해 활성 성분)

  • 이현주;오민아;최영희;이강만
    • YAKHAK HOEJI
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    • v.45 no.5
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    • pp.500-505
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    • 2001
  • Puerariae Radix is one of the medicinal plants used in oriental medicine for hangover, It has been claimed for several pharmacological effects including anti-alcohol abuse, antidipsotropic activity and anti-alcohol intoxication. In connection with Puerariae Radix effects, an activity-guided purification of active substance on alcohol dehydrogenase (hnH) was carried-out. The most active compound was isolated as puerarin (C$_{21}$H$_{20}$ O$_{9}$ ), molecular weight 416. Puerarin inhibited ADH noncompetitively against ethanol or NAD$^{+}$./.

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Activity-guided Purification of N-benzyl-N-methyldecan-1-amine from Garlic and Its Antitumor Activity against CT-26 Colorectal Carcinoma in BALB/C Mice (활성추적분리법에 의해서 순수분리한 마늘 N-benzyl-N-methyldecan-1-amine이 CT-26 세포주 이식 BALB/C mice의 항암효과)

  • Seetharaman, Rajasekar;Choi, Seong Mi;Guo, Lu;Cui, Zheng Wei;Otgonbayar, Duuriimaa;Park, Ju Ha;Kwon, Young-Seok;Kwak, Jung Ho;Kwon, Young Hee;Min, Ji Hyun;Kang, Jum Soon;Choi, Young Whan
    • Journal of Life Science
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    • v.29 no.10
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    • pp.1062-1070
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    • 2019
  • A components of garlic (Allium sativum) have anti-proliferative effects against various types of cancer. We aimed to investigate the capacity of garlic compounds to anti-tumor on a various cancer cell lines. Fractionation of garlic extract, guided by antiproliferative activity against human gastric cancer (AGS) cells, has resulted in the isolation of N-benzyl-N-methyldecan-1-amine (NBNMA). We investigated the effect of newly isolated NBNMA from garlic cloves on the inhibition of the growth of CT-26, AGS, HepG2, HCT-116, MCF7, B16F10, and Sarcoma-180 cells for in vitro and CT-26 colon carcinoma cells in vivo. NBNMA exhibited an antiproliferative effect in CT-26 cells by apoptotic cell death. NBNMA exhibited down-regulation of anti-apoptotic Bcl-2 proteins and up-regulation of apoptotic Bad protein expression in western blot analyses. In addition, NBNMA meagre activated caspase 3 and caspase 9, initiator caspases of the extrinsic and intrinsic pathways of apoptosis. NBNMA treatment at a dose of 10 mg/kg for 21 days in experimental mice implanted with tumors resulted in significant reduction of the tumor weight (43%). NBNMA exhibited both in vitro and in vivo anticancer activity. These results indicate that NBNMA has promising potential to become a novel anticancer agent from garlic cloves for the treatment of colon carcinoma cancer.

The Synergistic Antibacterial Activity of 1-Acetyl-$\beta$-Carboline and $\beta$-Lactams Against Methicillin-Resistant Staphylococcus aureus (MRSA)

  • Shin, Hee-Jae;Lee, Hyi-Seung;Lee, Dae-Sung
    • Journal of Microbiology and Biotechnology
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    • v.20 no.3
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    • pp.501-505
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    • 2010
  • 1-Acetyl-$\beta$-carboline was isolated as an anti-MRSA agent from the fermentation broth of a marine actinomycete isolated from marine sediment. The producing strain was identified to be Streptomyces sp. by phylogenetic analysis of the 16S rRNA gene sequence. The anti-MRSA agent was isolated by bioactivity-guided fractionation of the culture extract by solvent partitioning, ODS open flash chromatography, and purification with a reversed-phase HPLC. Its structure was elucidated by extensive 2D NMR and mass spectral analyses. Combination of 1-acetyl-$\beta$-carboline with ampicillin exhibited synergistic antibacterial activity against MRSA.

Constituents of Pyrus pyrifolia with Inhibitory Activity on the NO Production and the Expression of iNOS and COX-2 in Macrophages and Microglia

  • Yoo, Ji-Hye;Yang, Ki-Sook
    • Natural Product Sciences
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    • v.18 no.3
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    • pp.183-189
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    • 2012
  • It is well known that inflammation is associated with neurodegenerative disorders, including Alzheimer' disease, Parkinson's disease and ischemia. Nitric oxide (NO), a pro-inflammatory mediator, is produced by inducible NO synthase (iNOS) in microglia as well as macrophages and appears to account for neurodegeneration. In this study, we aimed to isolate NO inhibitors from Pyrus pyrifolia by activity guided purification. As a result, we identified daucosterol and ${\beta}$-sitosterol, which have not been isolated from this plant before. This article also describes NO inhibitory activities of the methanol extract of Pyrus pyrifolia fruit and the isolated compounds from this, which are lupeol, betulin, betulinic acid, ${\beta}$-sitosterol and daucosterol, in LPS-activated RAW 264.7 and BV2 cell lines. Western blot analysis was performed to clarify the underlying mechanism of NO inhibition in the two cell lines.

Bioactivity-guided isolation of ginsenosides from Korean Red Ginseng with cytotoxic activity against human lung adenocarcinoma cells

  • Yu, Jae Sik;Roh, Hyun-Soo;Baek, Kwan-Hyuck;Lee, Seul;Kim, Sil;So, Hae Min;Moon, Eunjung;Pang, Changhyun;Jang, Tae Su;Kim, Ki Hyun
    • Journal of Ginseng Research
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    • v.42 no.4
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    • pp.562-570
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    • 2018
  • Background: Lung cancer is the leading cause of cancer-related death worldwide. In this study, we used a bioactivity-guided isolation technique to identify constituents of Korean Red Ginseng (KRG) with antiproliferative activity against human lung adenocarcinoma cells. Methods: Bioactivity-guided fractionation and preparative/semipreparative HPLC purification were used with LC/MS analysis to separate the bioactive constituents. Cell viability and apoptosis in human lung cancer cell lines (A549, H1264, H1299, and Calu-6) after treatment with KRG extract fractions and constituents thereof were assessed using the water-soluble tetrazolium salt (WST-1) assay and terminal deoxyribonucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) staining, respectively. Caspase activation was assessed by detecting its surrogate marker, cleaved poly adenosine diphosphate (ADP-ribose) polymerase, using an immunoblot assay. The expression and subcellular localization of apoptosis-inducing factor were assessed using immunoblotting and immunofluorescence, respectively. Results and conclusion: Bioactivity-guided fractionation of the KRG extract revealed that its ethyl acetate-soluble fraction exerts significant cytotoxic activity against all human lung cancer cell lines tested by inducing apoptosis. Chemical investigation of the ethyl acetatesoluble fraction led to the isolation of six ginsenosides, including ginsenoside Rb1 (1), ginsenoside Rb2 (2), ginsenoside Rc (3), ginsenoside Rd (4), ginsenoside Rg1 (5), and ginsenoside Rg3 (6). Among the isolated ginsenosides, ginsenoside Rg3 exhibited the most cytotoxic activity against all human lung cancer cell lines examined, with $IC_{50}$ values ranging from $161.1{\mu}M$ to $264.6{\mu}M$. The cytotoxicity of ginsenoside Rg3 was found to be mediated by induction of apoptosis in a caspase-independent manner. These findings provide experimental evidence for a novel biological activity of ginsenoside Rg3 against human lung cancer cells.