• 생약학회지
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• 제34권1호통권132호
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• pp.14-17
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• 2003

In the course of screening Korean natural plants for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the leaves of Securinega suffruticosa showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of dihydrosecurinine, as a active principle. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$ value of dihydrosecurinine was $18.9\;{\mu}g$.

• Natural Product Sciences
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• 제21권1호
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• pp.1-5
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• 2015

Activity-guided separation of the methylene chloride-soluble fraction of the leaves of Zanthoxylum schinifolium, resulted in the isolation of four coumarinoids (1 - 4), two triterpenoids (5, 6) and three fatty acid derivatives (7 - 9) as active principles. Their chemical structures were identified as collinin (1), 8-methoxyanisocoumarin (2), 7-(6'R-hydroxy-3',7'-dimethylocta-2',7'-dienyloxy)-coumarin (3), (E)-4-methly-6-(coumarin-7'-yloxy) hex-4-enal (4), lupeol (5), epi-lupeol (6), phytol (7), hexadec-3-enoic acid (8) and palmitic acid (9), on the basis of spectroscopic (1D, 2D and MS) data analyses and comparing with the data published in the literatures. Compounds 1 and 7 showed potent cytotoxicity against Jurkat T cells with $IC_{50}$ values of 45.58 and $47.51{\mu}M$, respectively. The others showed moderate activity with $IC_{50}$ values ranging around 80.58 to $85.83{\mu}M$, while the positive control, auraptene, possessed an $IC_{50}$ value of $55.36{\mu}M$.

• Archives of Pharmacal Research
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• 제29권12호
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• pp.1119-1124
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• 2006

The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with $IC_{50}$ values of 0.7 and $1.7\;{\mu}M$, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B ($IC_{50}\;0.5\;and\;0.6\;{\mu}M,\;respectively$) compared to MAO-A ($IC_{50}\;1.3\;and\;34.6\;{\mu}M,\;respectively$). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.

• Archives of Pharmacal Research
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• 제26권11호
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• pp.906-911
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• 2003

We previously reported that the butanol (BuOH) fraction of the head of Panax ginseng exhibited gastroprotective activity in peptic and chronic ulcer models. In order to identify the active constituent, an activity-guided isolation of the BuOH faction was conducted with a HCI$.$ethanol-induced gastric lesion model. The BuOH fraction was passed through a silica-gel column using a chloroform-methanol gradient solvent system, and six fractions (frs. 1-6) were obtained. The active fr. 5 was further separated by silica-gel column, to yield 6 subfractions (subfrs. a-f). Subfr. d was composed of ginsenosides Re, Rc and $Rb_1$. The most active constituent was ginsenoside $Rb_1$ ($GRb_1$), a protopanaxadiol glycoside, which was investigated for its anti-ulcer effect. Gastric injury induced by HCI$.$ethanol, indomethacin and pyloric ligation (Shay ulcer) was apparently reduced with oral $GRb_1$ doses of 150 and 300 mg/kg. $GRb_1$ at these dosage significantly increased the amount of mucus secretion in an ethanol-induced model. The anti-ulcer effects were consistent with the result of histological examination. These results suggest that the major active constituent in the head of Panax ginseng is $GRb_1$ and that anti-ulcer effect is produced through an increase in mucus secretion.

• Natural Product Sciences
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• 제12권2호
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• pp.109-112
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• 2006

The chloroform-soluble fraction of the vinegar treated small black soybean [Glycine max (Leguminosae)] showed antiproliferative activity against human myeloid leukemia HL-60 cells, in terms of inhibition of proliferation and induction of apoptosis. Bioassay-guided chromatography of the chloroform-soluble fraction resulted in the isolation of two isoflavonoid compounds, genistein and daidzein, as active principles. Genistein showed more potent antiproliferative effects against HL-60 cells. Treatment of HL-60 cells with genistein induced apoptosis in a dose dependent manner. Apoptosis was judged by the detection of DNA fragmentation by a flow cytometry and the degree of apoptosis was assayed by RT-PCR.

• Archives of Pharmacal Research
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• 제29권2호
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• pp.135-139
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• 2006

Activity-guided fractionation of the ethanol extract of the whole plant from Solanum lyratum resulted in the isolation of a new pregnane derivative glycoside, 16-dehydropregnenolone 3-O-${\alpha}$-L-rhamnopyranosyl-($1{\to}2$)-${\beta}$-D-glucopyranosid uronic acid (2), as well as other six known compounds: 16-dehydropregnenolone (1), allopregenolone (3), protocatechuic acid (4), vanillic acid (5), caffeic acid (6), and scopoletin (7). The structures of the isolated compounds were elucidated on the basis of their spectral data and chemical evidences. Compounds 1, 3, 4 were isolated for the first time from this plant. Cytotoxic activities of the isolated compounds were evaluated. Compound 1 exhibited significant cytotoxic activity against A375-S2, HeLa, SGC-7901, and Bel-7402 with $IC_{50}$ values of $13.1{\pm}0.9,\;21.5{\pm}1.0,\;40.2{\pm}0.7$, and $49.8{\pm}1.2\;{\mu}g/mL$, respectively.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.190-194
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• 2005

In our search for monoamine oxidase (MAO) inhibitors from natural resources, we found that the methanol extract of the roots of Sophora flavescens showed an inhibitory effect on mouse brain monoamine oxidase (MAO). Bioactivity-guided isolation of the extract yielded two known flavonoids, formononetin (1) and kushenol F (2), as active compounds along with three inactive compounds, oxymatrine (3), trifolirhizin (4), and ${\beta}$-sitosterol (5). Formononetin (1) and kushenol F (2) showed significant inhibitory effects on MAO in a dose-dependent manner with $IC_{50}$ values of 13.2 and $69.9\;{\mu}M$, respectively. Formononetin (1) showed a slightly more potent inhibitory effect against MAO-B ($IC_{50}:\;11.0\;{\mu}M$) than MAO-A ($IC_{50}:\;21.2\;{\mu}M$). Kushenol F (2) also preferentially inhibited the MAO-B activity than MAO-A activity with the $IC_{50}$ values of 63.1 and $103.7\;{\mu}M$, respectively.

• Archives of Pharmacal Research
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• 제23권4호
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• pp.344-348
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• 2000

80% Aqueous MeOH extracts from the wood of Caesalpinia sappan, which showed remarkable anticonvulsant activity, were fractionated using EtOAc, n-BuOH, and $H_2$O. Among them, the EtOAc fraction significantly inhibited the activities of two GABA degradative enzymes, succinic semialdehyde dehydrogenase (SSADH) and succinic semialdehyde reductase (SSAR). Repeated column chromatographies for the fraction guided by activity test led to the isolation of the two active principal components. Their chemical structures were determined to be sappanchalcone and brazilin based on spectral data. The pure compounds, sappanchalcone (1) and brazilin (2), inactivated the SSAR activities in a dose dependent manner, whereas SSADH was inhibited partially by sappanchalcone and not by brazilin.

• 생약학회지
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• 제41권3호
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• pp.174-179
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• 2010

Activity guided isolation of 80% acetone extract from the barks of Acer ginnala Maxim. yielded five gallotannins [6-galloyl-1,5-anhydroglucitol (ginnalin B) (1), acertannin (3,6-digalloyl-1,5-anhydroglucitol) (2), methyl gallate (3), acertannin (2,6-digalloyl-1,5-anhydroglucitol) (4) and gallic acid (5)]. All of these isolated compounds from Acer ginnala(1-5) were firstly isolated from Acer ginnala Maxim. And contents of compounds from barks of Acer ginnala (Comp. 1: 0.73$\pm$0.002%, Comp. 2: 0.48$\pm$0.001%, Comp. 3: 0.66$\pm$0.002%, Comp. 4: 1.05$\pm$0.002% and Comp. 5: 0.29$\pm$0.001%) were evaluated by HPLC analysis. And, in order to evaluate anti-oxidative activities on Comp. 1-5 isolated from Acer ginnala, DPPH radical scavenging activity was measured in vitro. All of these isolated compounds from Acer ginnala exhibited potent DPPH radical scavenging activities.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.633-636
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• 1997

In the course of searching for PAF receptor antagonists, pregomisin (1) and chamigrenal (2) were isolated from the fruits of Schizandra chinensis Baill by the bioactivity-guided isolation. Both compounds showed PAF antagonistic activity and the $IC_{50}$ values were $4.8{\times}10^{-5} M and 1.2{\times}10^{-4}M,$ respectively. In addition, the $^{13}C$ NMR assignments of 1 and 2 using DEPT, HMQC, COLOC and HMBC were reported for the first time.