• Archives of Pharmacal Research
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• v.28 no.3
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• pp.285-289
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• 2005

Two new sulfated saponins designated as certonardosides P$_{2}$ and I$_{3}$ (1 and 2) were isolated from the brine shrimp active fraction of the MeOH extract of the starfish Certonardoa semiregularis. The structures were determined on the basis of spectral analysis. Compounds 1 and 2 were tested for cytotoxicity against five human tumor cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15), and compound 1 displayed significant cytotoxicity against the SK-MEL-2 skin cancer cell.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.636-639
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• 2002

The extract of the root of Polygonum multiflorum exhibited a significant antioxidant activity assessed by the DPPH radical scavenging activity in vitro. The bioassay-guided fractionation of the extract yielded a stilbene glucoside, (E)-2,3,5,4'-tetrahydroxystilbene-2-Ο-$\beta$-d-glucopyranoside (1) as an active constituent responsible for the antioxidant property. Compound 1 demonstrated a moderate DPPH radical scavenging activity ($IC_{50}$, 40 $\mu$M), while the corresponding deglucosylated stilbene 2 exhibited a much higher activity ($IC_{50}$, 0.38 $\mu$M).

• Archives of Pharmacal Research
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• v.26 no.2
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• pp.147-150
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• 2003

To find anticancer agents from higher plants, DNA strand-scission assay method was employed for bioassay-guided fractionation as well as for screening the crude extracts. During the screening, an ethyl acetate extracts of the heartwood of Caesalpinia sappan L. (Leguminosae) exhibited potent DNA strand-scission activity. Therefore, the ethyl acetate extracts of the dried heartwood of C. sappan was subjected to the bioassay-guided fractionation, which led to the isolation of a known compound, brazilin (1) as the active constituent. In addition, caesalpine J (2) was also isolated as an inactive constituent.

• YAKHAK HOEJI
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• v.60 no.3
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• pp.107-111
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• 2016

Inhibitory activities of 1,5-diarylimidazole analogs with methylthiophenyl group on prostaglandin $E_2$ ($PGE_2$) production from LPS-treated RAW 264.7 cells, were evaluated and compared with those of the corresponding analogs with 4-methanesulfonylphenyl group. Among the tested nineteen analogs with methylthiophenyl group, fourteen analogs showed strong inhibitory activities (>88%) when compared with the reference compound NS-398, and fifteen analogs have similar inhibitory activities with those of parent analogs with 4-methanesulfonylphenyl group. Those results suggest that most of 1,5-diarylimidazole analogs with methanesulfonylphenyl group can be also active even after they are metabolized by reduction.

• Bulletin of the Korean Chemical Society
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• v.31 no.11
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• pp.3318-3326
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• 2010

Five new series of 3,4-ethylenedioxythiophene derivatives carrying important pharamacophores, viz., amide, ester, ether and active secondary aryl moieties have been designed and synthesized through multistep reactions starting from thiodiglycolic ester and diethyl oxalate. They have been characterized by elemental and spectral data. All the target compounds have been screened for their anticonvulsant activity at three different models viz. maximal electroshock (MES), subcutaneous metrazole (scMET), and 6 Hz screen and evaluated for their neurotoxicity in rotorod model. Compound 6a emerged as lead with no neurotoxicity. All the five series of compounds are safe in the toxicity studies at the maximum dose of 300 mg/kg of body weight. Amongst the tested compounds, the ester pharmacophore with thioamide fragment has showed better activity than the other analogs.

• 한국약용작물학회:학술대회논문집
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• 2010.10a
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• pp.430-430
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• 2010

In this study ethanol extracts of aerial part of Geranium thunbergii Sieb. et Zucc. was investigated for their ability to inhibit a-glucosidase, and thus was fractionated using two organic solvents, including dichloromethane, ethyl acetate. The ethyl acetate-soluble fraction, which manifested potent enzyme inhibitory properties, was then followed by tracking down the active compound by combining HPLC micro-fractionation to an enzyme assay in 96-well plate. The ${\alpha}$-glucosidase inhibitory activity profile showed that two peaks exhibited potent inhibitory activity, and then the structural analyses of the two peaks were carried out by HPLC-UV-MS. The main ${\alpha}$-glucosidase inhibitory compounds in the ethyl acetate-soluble fractions of ethanol extracts of Geranium thunbergii Sieb. et Zucc. were tentatively identified as geraniin and kaempferol-7-rhamnoside.

• Journal of Ginseng Research
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• v.41 no.4
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• pp.435-443
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• 2017

Panax ginseng is one of the most universally used herbal medicines in Asian and Western countries. Most of the biological activities of ginseng are derived from its main constituents, ginsenosides. Interestingly, a number of studies have reported that ginsenosides and their metabolites/derivatives-including ginsenoside (G)-Rb1, compound K, G-Rb2, G-Rd, G-Re, G-Rg1, G-Rg3, G-Rg5, G-Rh1, G-Rh2, and G-Rp1-exert anti-inflammatory activities in inflammatory responses by suppressing the production of proinflammatory cytokines and regulating the activities of inflammatory signaling pathways, such as nuclear factor-${\kappa}B$ and activator protein-1. This review discusses recent studies regarding molecular mechanisms by which ginsenosides play critical roles in inflammatory responses and diseases, and provides evidence showing their potential to prevent and treat inflammatory diseases.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.470-475
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• 1994

The butanol extract of paulownia tomentosa stem showed antibacterial activity against staphyl ococcus aureus (SG511, 285 and 503), Streptococcus pyogenes (A308 and A77) and Streptococcus farcium MD8b etc. The most active compound of the extractg was identified to be campneoside I, which had a minimal inhibitory concentration(MIC) of $150{\;}{\mu}g/ml$ against Strptococcus and Staphylococcus species. From such antibacterial activity, the methoxy group of campneoside I was posulated to be the essential element for the antibacterial activity.

• International Journal of Oral Biology
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• v.35 no.4
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• pp.177-184
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• 2010

In our present study, we investigated the effects of continentalic acid on Streptococcus mutans (S. mutans) biofilm. Methanol extract of Aralia continentalis (A. continentalis) was suspended in water and sequentially partitioned with CHCl3, ethyl acetate (EtOAc), and n-butanol (n-BuOH). The CHCl3 fraction showed the highest activity and an antibacterial compound against S. mutans was isolated from this preparation through various chromatography methods by bioassay guided fractionation. MS, $^1H-NMR$ and $^{13}C-NMR$ analysis showed that the active principle was continentalic acid which was confirmed to show significant inhibitory effects against S. mutans biofilm. These results may provide some scientific rationale for the traditional use these extracts for the treatment of dental diseases.

• Journal of Ginseng Research
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• v.36 no.1
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• pp.1-15
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• 2012

The major commercial ginsengs are Panax ginseng Meyer (Korean ginseng), P. quinquifolium L. (American ginseng), and P. notoginseng (Burk.) FH Chen (Notoginseng). P. ginseng is the most commonly used as an adaptogenic agent and has been shown to enhance physical performance, promote vitality, increase resistance to stress and aging, and have immunomodulatory activity. These ginsengs contain saponins, which can be classified as dammarane-type, ocotillol-type and oleanane-type oligoglycosides, and polysaccharides as main constituents. Dammarane ginsenosides are transformed into compounds such as the ginsenosides $Rg_3$, $Rg_5$, and $Rk_1$ by steaming and heating and are metabolized into metabolites such as compound K, ginsenoside $Rh_1$, proto- and panaxatriol by intestinal microflora. These metabolites are nonpolar, pharmacologically active and easily absorbed from the gastrointestinal tract. However, the activities metabolizing these constituents into bioactive compounds differ significantly among individuals because all individuals possess characteristic indigenous strains of intestinal bacteria. To overcome this difference, ginsengs fermented with enzymes or microbes have been developed.