• Title/Summary/Keyword: Activity-guided isolation

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Antioxidative Constituents of the Aerial Parts of Galium spurium

  • Yang, Seok-Won;Park, Sae-Rom;Ahn, Dal-Rae;Yang, Jae-Heon;Kim, Dae-Keun
    • Biomolecules & Therapeutics
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    • v.19 no.3
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    • pp.336-341
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    • 2011
  • As part of an ongoing search for natural plants with antioxidant compounds by measuring the radical scavenging effect on 1,1-diphenyl- 2-picrylhydrazyl (DPPH), a total extract of the twigs of Galium spurium L. (Rubiaceae) was found to show potent antioxidant activity. Subsequent activity-guided fractionation of the methanolic extract led to the isolation of nine compounds, asperulosidic acid methyl ester (1), asperuloside (2), caffeic acid (3), kaempferol-3-O-L-rhamnopyranoside (4), quercetin-3-O-[${\alpha}$-Lrhamnopyranosyl($1{\rightarrow}6$)-${\beta}$-D-glucopyranoside] (5), isorhamnetin-3-O-glucopyranoside (6), quercetin-3-O-${\alpha}$-L-rhamnopyranoside (7), kaempferol-3-O-[${\alpha}$-L-rhamnopyranosyl($1{\rightarrow}6$)-${\beta}$-D-glucopyranoside] (8), and quercetin (9). Their structures were elucidated by spectroscopic studies. Compounds 1, 3-8 were isolated for the first time from this plant. Among them, compounds 3 and 9 showed the significant radical scavenging effects on DPPH, and compounds 3 and 7 showed the potent riboflavin originated superoxide quenching activities.

Antioxidant Activity of Flavonoids Isolated from Vitex rotundifolia (순비기나무(Vitex rotundifolia)로부터 분리한 플라보노이드 성분의 항산화 활성)

  • Kim, You-Ah;Lee, Jung-Im;Hong, Joo-Wan;Jung, Myoung-Eun;Seo, Young-Wan
    • Ocean and Polar Research
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    • v.33 no.3
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    • pp.255-263
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    • 2011
  • The aim of this investigation was to evaluate antioxidant activity of crude extracts from the halophyte Vitex rotundifolia, their solvent fractions, and isolated compounds (1-3). Antioxidant capacity was determined by measuring DPPH radical, and authentic $ONOO^-$ and $ONOO^-$ generated from 3- morpholinsydnonimine (SIN-1) in vitro as well as degree of occurrence of intracellular ROS, NO and GSH in mouse macrophage Raw 264.7 cells. From comparative analysis, MeOH extract, n-BuOH, and 85% aq. MeOH solvent fractions showed significant antioxidant effect in DPPH radical and $ONOO^-$ assay systems. Activity-guided purification of n-BuOH and 85% aq. MeOH fractions led to the isolation of flavonoids 1-3. Among them, compound 1 exhibited excellent antioxidant effect in all bioassay systems tested. On the other hand, compounds 2 and 3 revealed potent inhibitory effect against $ONOO^-$ generated from SIN-1, comparable with the positive control penicillamine.

Topical Anti-inflammatory Activity of Dianemycin Isolated from Streptomyces sp. MT 2705-4

  • Lee, Song-Jin;Kim, Hyun-Pyo;Park, Byung-Keun;Ahn, Soon-Cheol;Lee, Hyun-Sun;Ahn, Jong-Seog
    • Archives of Pharmacal Research
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    • v.20 no.4
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    • pp.372-374
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    • 1997
  • In order to develop new anti-inflammatory agents having different action mechanisms compared with nonsteroidal and steroidal anti-inflammatory drugs, the culture broths of various actinomycetes isolated from soil were screened using an in vivo mouse ear edma assay and one strain (Streptomyces sp. MT 2705-4: KCTC 8651 P) was selected. Activity-guided purification led to the isolation of a polyether compound, dianemycin. Topically, dianemycin showed a potent anti-inflammatory activity in mouse ear edema induced by croton-oil or arachidonic acid.$ED_{50}$value of dianemycin was found to be 0.8 mg,/ear compared to 0.4 mg/ear of prednisolone in croton-oil ear edema. However, dianemycin did not show the inhibitory activity in UV-erythema and delayed hypersensitivity reaction. These results indicate that dianemycin is a potential topical anti-inflammatory agent.

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Antioxidant Constituents of the Aerial Parts of Curcuma longa (강황 지상부의 항산화 성분)

  • Ahn, Dalrae;Lee, Eun Byeol;Ahn, Min-Sil;Lim, Hye Won;Xing, Ming Ming;Tao, Chao;Yang, Jae Heon;Kim, Dae Keun
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.274-278
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    • 2012
  • As part of ongoing study focused on the discovery of natural antioxidants from Korean plants by measuring the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging effect and superoxide quenching activity, ethanol extract of the aerial parts of Curcuma longa (Zingiberaceae) was found to show potent antioxidant activities. Subsequent activity-guided fractionation of the ethanol extract led to the isolation of two phenolic compounds, 1,2,3,4,6-penta-O-galloyl-${\beta}$-D-glucopyranoside (1) and gallic acid (2), as antioxidant compounds. Their structures were elucidated by spectroscopic studies. Compounds 1 and 2 were isolated for the first time from this plant. These compounds showed the significant antioxidative effects during the DPPH free radical scavenging test, and the riboflavin- and xanthine-originated superoxide quenching activity tests.

Anti-oxidative Activities of 3'-Hydroxygenkwanin from the Flower Buds of Daphne genkwa in Caenorhabditis elegans

  • Park, Sung-Hoon;Cui, Xun;Ahn, Dalrae;Lee, Eun Byeol;Cha, Dong Seok;Jeon, Hoon;Zee, Ok Pyo;Kim, Youn-Chul;Kim, Dae Keun
    • Natural Product Sciences
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    • v.20 no.2
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    • pp.80-85
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    • 2014
  • In the course of screening for antioxidant compounds from natural plants in Korea by measuring the radical scavenging effect, a methanol extract of the flower buds of Daphne genkwa S. et Z. (Thymelaeaceae) was found to show a potent antioxidant activity. Subsequent activity-guided fractionation of methanol extract of D. genkwa led to the isolation of four compounds from the ethyl acetate soluble fraction. The chemical structures were elucidated as genkwanin (1), 3'-hydroxygenkwanin (2), apigenin (3), and tiliroside (4) by spectroscopic techniques. Among them, compound 2 showed the significant anti-oxidative effect on DPPH. And compound 2 showed the significant riboflavin-and xanthine-originated superoxide quenching activities. To verify the antioxidant enzymatic activities of compound 2, the SOD enzymatic activity was measured spectrophtometrically using prepared Caenorhabditis elegans homogenates. The results showed that compound 2 was able to elevate SOD activity of C. elegans in a dose dependent manner. Moreover, compound 2 decreased the intracellular ROS accumulation of worms.

Antidiabetic Stilbene and Anthraquinone Derivatives from Rheum undulatum

  • Choi Sang Zin;Lee Sung Ok;Jang Ki Uk;Chung Sung Hyun;Park Sang Hyun;Kang Hee Chol;Yang Eun Young;Cho Hi Jae;Lee Kang Ro
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1027-1030
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    • 2005
  • The antidiabetic-activity-guided fractionation and isolation of the $80\%$ EtOH extracts obtained from cultivated Korean Rhubarb rhizomes (Rheum undulatum, Polygonaceae) led to the isolation and characterization of one stilbene, desoxyrhapontigenin(1) and two anthraquinones, emodin (2) and chrysophanol (3). Their structures were established by chemical and spectroscopic methods. Compounds 1, 2, and 3 inhibited postprandial hyperglycemia by 35.8, 29.5, $42.3\%$, respectively.

Antidiabetic Coumarin and Cyclitol Compounds from Peucedanum japonicum

  • Lee, Sung-Ok;Choi, Sang-Zin;Lee, Jong-Hwa;Chung, Sung-Hyun;Park, Sang-Hyun;Kang, Hee-Chol;Yang, Eun-Young;Cho, Hi-Jae;Lee , Kang-Ro
    • Archives of Pharmacal Research
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    • v.27 no.12
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    • pp.1207-1210
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    • 2004
  • The antidiabetic activity-guided fractionation and isolation of the 80% EtOH extracts from Peucedani Radix (Peucedanum japonicum, Umbelliferae) led to the isolation and characterization of a coumarin and a cyclitol as active principles, that is, peucedanol 7-O-${\beta}$ -D-glucopyranoside (1) and myo-inositol (2). Their structures were identified by spectroscopic methods. Compound 1 showed 39% inhibition of postprandial hyperglycemia at 5.8 mg/kg dose, and compound 2 also significantly inhibited postprandial hyperglycemia by 34% (P<0.05).

Isolation of Inhibitory Components on Tumor Necrosis Factor-${\alpha}$ Production from Angelica koreana (강활에서 종양괴사인자 생성을 억제하는 활성성분의 분리)

  • Cho, Jae-Youl;Lee, Jong-Soo;Park, Ji-Soo;Park, Myung-Hwan
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.125-131
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    • 1998
  • The total ethanol extract of Angelica koreana radix (UmbeUiferae) showed potent inhibitory effect on tumor necrosis factors (TNF-${\alpha}$) production from LPS-stimulated RAW 264.7 cells in screening studies on 118 Korean medicinal plants. The activity-guided fractionation of the total ethanol extract resulted in the isolation of 4 compounds, including active substances. The chemical structures of the compounds isolated were established by chemical and spectrometric analyses as imperatorin, isoimperatorin, osthol and oxypeucedanin. Among them, osthol, oxypeucedariin and isoimperatorin showed significant inhibitory activities on TNF-${\alpha}$ production as 54.3${\pm}$2.1%, 33.6${\pm}$1.0% and 17.7${\pm}$3.0%, respectively, at 12.5${\mu}$g/ml.

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Isolation of Flavonol Rhamnosides from Loranthus tanakae and Cytotoxic Effect of Them on Human Tumor Cell Lines

  • Kim, Young-Kyoon;Kim, Young-Sup;Choi, Sang-Un;Ryu, Shi-Yong
    • Archives of Pharmacal Research
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    • v.27 no.1
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    • pp.44-47
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    • 2004
  • Loranthus tanakae Fr. et Sav. (Loranthaceae) is a species of mistletoe, a semiparasitic plant growing on the branches of Quercus and Betula species as host trees. In our ongoing search for bioactive compounds from endemic species in Korea, we have investigated to isolate the chemical constituents responsible for the antitumor effect of the MeOH extract of L. tanakae. The ethyl acetate soluble part of the MeOH extract demonstrated a marginal inhibition on the proliferation of the tumor cell lines such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system), and HCT-15 (colon) in vitro. Thus, the activity-guided isolation procedure upon the ethyl acetate soluble part of the extract has been carried out and finally four flavonoid rhamnopyranosides (1-4) were isolated as active principle. The structures of 1-4 were elucidated by the physicochemical and spectral data as rhamnetin 3-O-$\alpha$-L-rhamnoside (1), quercetin 3-O-$\alpha$-L-rhamnoside (2), rhamnocitrin 3-O-$\alpha$rhamnoside (3), and kaempferol 3-O-$\alpha$-L-rhamnoside (4).

Anti-allergic Actions of the Leaves of Castnea crenata and Isolation of an Active Component Responsible for the Inhibition of Mast Cell Degranulation

  • Lee, Eun;Choi, Eun-Ju;Cheong, Ho;Kim, Young-Ran;Ryu, Shi-Yong;Kim, Kyeong-Man
    • Archives of Pharmacal Research
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    • v.22 no.3
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    • pp.320-323
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    • 1999
  • The anti-allergic actions of the leaves of Castanea crenata (Fagaceae) were studied. The water extract demonstrated potent anti-allergic actions in in vivo and in vitro experiments. The oral or intraperitoneal administration of the extract (100 or 200 mg/kg) caused a significant inhibition of the 48 hr-PCA (up to 90%) and the vascular permeability induced by histamine or serotonin in rats (about 80%). The anaphylactic release of ${\beta}$-hexosaminidase for RBL-2H3 cells was also significantly inhibited by the extract in as dose-dependent manner with an IC50 value of 230 $\mu\textrm{g}$/ml. The activity-guided fractionation of the extract, based on the determination of inhibitor effect upon the release of ${\beta}$-hexosaminidase, led to the isolation of quercetin as an active principle responsible for the inhibition of degranulation.

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