• 대한한의학회지
• /
• 제32권3호
• /
• pp.35-43
• /
• 2011

Objectives: This study was performed to screen target-specific inhibitors of ${\beta}$-catenin/TCF signaling whose functional activation plays an important role in early events in carcinogenesis. Methods: To investigate the activation or suppression of ${\beta}$-catenin/TCF transcription, we established a transiently transfected cell line with a constitutively active ${\beta}$-catenin mutant gene whose product is not degraded. This cell line was also co-transfected with luciferase reporter gene constructs containing either an optimized (TOPflash) or mutant (FOPflash) TCF-binding element. We investigated cytotoxic effects using a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium salt (MTS) assay. To find effective inhibitors of ${\beta}$-catenin/TCF signaling from medicinal herbs, the crude extracts of 99 types of medicinal herbs were screened using a luciferase assay system in HEK-293 and SH-SY5y cells. Results: At a concentration of $50{\mu}g$/ml, extracts of Angelica koreanae radix, Cannabis sativa semen, Ephedrae intermedia Schrenk radix, and Vitis rotundifolia fruit showed the following inhibitory effects on ${\beta}$-catenin/TCF signaling: $40{\pm}5.6%$, $23{\pm}6.1%$, $8{\pm}5.1%$, and $22{\pm}9.8%$ in ${\beta}$-catenin-activated HEK-293 cells and $9{\pm}4.7%$, $39{\pm}8.1%$, $39{\pm}6.4%$, and $42{\pm}10.1%$ in ${\beta}$-catenin-activated SH-SY5y cells, respectively. Crude extracts of E. radix were isolated by silica gel column chromatography, and two non-polar fractions of these extracts showed inhibitory effects on ${\beta}$-catenin/TCF signaling. Conclusions: In this study, we established a transiently transfected cell line as a screening system and found that various medicinal herb extracts had inhibitory effects on ${\beta}$signaling.

• Molecules and Cells
• /
• 제24권1호
• /
• pp.113-118
• /
• 2007

The brains of Alzheimer's disease (AD) patients are characterized by large deposits of amyloid beta peptide ($A{\beta}$). $A{\beta}$ is known to increase free radical production in nerve cells, leading to cell death that is characterized by lipid peroxidation, free radical formation, protein oxidation, and DNA/RNA oxidation. In this study, we selected an extract of Gardenia jasminoides by screening, and investigated its ameliorating effects on $A{\beta}$-induced oxidative stress using PC12 cells. The effects of the extract were evaluated using the 2',7'-dichlorofluorescein diacetate (DCF-DA) assay and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay. To find the active component, the ethanol extract was partitioned with hexane, chloroform, and ethyl acetate, respectively, and the active component was purified by silica-gel column chromatography and HPLC. The results suggested that Gardenia jasminoides extract can reduce the cytotoxicity of $A{\beta}$ in PC 12 cells, possibly by reducing oxidative stress.

• 생약학회지
• /
• 제39권3호
• /
• pp.233-236
• /
• 2008

In order to find the antioxidative components, fractionation of Cyperus amuricus (Cyperaceae) methanol extract was performed by measuring the DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging effect. Three compounds, 3,4-dimethoxy benzoic acid (1), 4-hydroxybenzoic acid (2), and piceatannol (3) were isolated from the active ethylacetate soluble fraction of C. amuricus through repeated silica gel and Sephadex LH-20 column chromatography. Among them, compound 3 showed the significant antioxidative effect on DPPH free radical scavenging test. These compounds are reported for the first time from this plant.

• 한국식품과학회지
• /
• 제34권1호
• /
• pp.114-117
• /
• 2002

연교의 메탄올 추출물로부터 caspase 저해물질을 분리하였으며, ESI-MS, $^1H-NMR$, $^13C-NMR$, DEPT 등의 기기분석 자료에 의하여 rengyolone으로 동정하였다. 이 물질은 $IC_{50}\;6.25\;{\mu}g/mL$의 농도에서 etoposide가 처리된 U937 세포주의 caspase-3 유도 저해를 나타내었다. 또한 rengyolone은 $Interleukin-1{\beta}$가 처리된 D10S 세포에서 caspase-1의 유도저해활성을 나타내었으며, $IC_{50}$값은 $7.5\;{\mu}g/mL$이었다.

• 한국자원식물학회지
• /
• 제10권2호
• /
• pp.183-187
• /
• 1997

본 실험은 지모의 생리, 생태적 특성과 성숙한 상태의 각 부위별 Sarsasapogenin의 함량을 비교 분석하고자, 5개의 수집종에 대해 1993년부터 '95년까지 충남농촌진흥원 특작포장에 재배하고 성숙된 지모의 각 부위별 Sarsasapogenin 함량을 T.L.C plate 방법에 의해 분석한 결과 다음과 같은 결론을 얻었다. 1. 5개 수집종 중 주로 종실(種實)형을 나타낸 것은 공주, 청양 수집종이고 영양번식(營養繁殖)형은 금산, 연기, 유성종에서 주로 분류되어 있으며, 종실(種實)형이 비종실형보다 생육(生育) 및 형태적(形態的) 특징(特徵)이 양호하였다. 2. BuOH에 엑스를 산(酸)으로 가수분해(加水分解)한 후 T.L.C 용매(溶媒) 전개조건(展開條件)인 $CHCl_3$ : MEK : EtOH의 비율을 11 : 2 : 0.5로 하여 sarsasapogenin 분리(分離)가 가능하였고 Dual wave length T.L.C scanner로 정량(定量)이 가능(可能)하였다. 3. 주근(主根)과 세근(細根)의 sarsasapogenin의 량(量)은 각각(各各) 1.67mg/10g, 1.31mg/10g으로 세근(細根)에 sarsasapogenin의 량(量)이 주근(主根)보다 1.1배(倍)로 높게 나타나 세근(細根)에 sarsasapogenin 계통(系統)의 물질(物質)이 가장 많음을 알 수 있었다. 그러나 지상부(地上部)의 sarsasapogenin 함량은 미미한 것으로 나타났다.

• Archives of Pharmacal Research
• /
• 제29권12호
• /
• pp.1074-1079
• /
• 2006

As part of our research on phytochemicals that exert protective effects against diseases related to reactive nitrogen species, we have evaluated the scavenging activity of the yellow leaves of Ginkgo biloba on $ONOO^{-}$. The methanol extract and ethyl acetate fraction obtained from yellow leaves of G. biloba evidenced a marked scavenging activity on authentic $ONOO^{-}$. Repeated column chromatography of the active ethyl acetate soluble fraction on silica gel, Sephadex LH-20, and RP-18, resulted in the purification of 15 known compounds, including sciadopitysin (1), ginkgolide B (2), bilobalide (3), isoginkgetin (4), kaempferol (5), luteolin (6), protocatechuic acid (7), bilobetin (8), amentoflavone (9), ${\beta}-sitosterol$ glucopyranoside (10), kaempferol 3-O-rhamnopyranoside (11), kaempferol 3-O-glucopyranoside (12), kaempferol $3-O-[{6^{'}-O-p-coumaroyl-{\beta}-D-glucopyranosyl(1{\rightarrow}2)-{\alpha}-L-rhamnopyranoside]$ (13), kaempferol 3-O-rutinoside (14), and 6-hydroxykynurenic acid (15). Among the compounds isolated, flavonoids (5, 6 and 11-14), protocatechuic acid (7), and 6-hydroxykynurenic acid (15) all exhibited marked scavenging activities on authentic $ONOO^{-}$. The $IC_{50}$ values of 5-7, 11-14 and 15 were as follows: $2.86{\pm}0.70,\;2.30{\pm}0.04,\;2.85{\pm}0.10,\;5.60{\pm}0.47,\;4.16{\pm}1.65,\;2.47{\pm}0.15,\;3.02{\pm}0.48,\;and\;6.24{\pm}0.27\;{\mu}M$, respectively. DL-Penicillamine ($IC_{50}=4.98{\pm}0.27\;{\mu}M$) was utilized as a positive control. However, the other compounds (1-4, 8-10) exerted no effects against $ONOO^{-}$.

• Archives of Pharmacal Research
• /
• 제26권4호
• /
• pp.279-285
• /
• 2003

In our ongoing study to identity antioxidants from natural sources, the antioxidant activity of Nelumbo nucifera stamens was evaluated for their potential to scavenge stable 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals, inhibit total reactive oxygen species (ROS) generation, in kidney homogenates using 2 ,7 -dichlorodihydrofluorescein diacetate (DCHF-DA), and scavenge authentic peroxynitrites ($ONOO^-$). A methanol (MeOH) extract of the stamens of N. nucifera showed strong antioxidant activity in the $ONOO^-$system, and marginal activity in the DPPH and total ROS systems, so were therefore fractionated with several organic solvents, such as dichloromethane ($CH_2 Cl_2$), ethyl acetate (EtOAc) and n-butanol (n-BuOH). The EtOAc soluble fraction, which exhibited strong antioxidant activity in all the model systems tested, was further purified by repeated silica gel and Sephadex LH-20 column chromatographies. Seven known flavonoids [kaempferol (1), kaempferol 3-Ο-$\beta$-D-glucuronopyranosyl methylester (2), kaempferol 3-Ο-$\beta$-D-glucopyranoside (3), kaempferol 3-Ο-$\beta$-D-galactopyranoside (4), myricetin 3 ,5 -dimethylether 3-Ο-$\beta$-D-glucopyranoside (5), kaempferol 3-Ο-$\alpha$-L-rhamnopyranosyl-(1$\rightarrow$6)-$\beta$-D-glucopyranoside (6) and kaempferol 3-Ο-$\beta$-D-glucuronopyranoside (7)], along with $\beta$-sitosterol glucopyranoside (8), were isolated. Compound 1 possessed good activities in all the model systems tested. Compounds 2 and 7 showed scavenging activities in the DPPH and $ONOO^-$ tests, while compounds 3 and 4 were only active in the $ONOO^-$ test. Conversely, compound 8 showed no activities in any of the model systems tested.

• 약학회지
• /
• 제41권2호
• /
• pp.161-173
• /
• 1997

Tuber of Aconitum chiisanense(Ranunculaceae) a specific medicinal plant in Korea, which is known to have the activity to recover reduced metabolism of feeble patients and has been used to symptoms such as pain, paralysis, atonia and coldness of extremities, etc. were studied. The powdered tubers of the plant were extracted with 10% EtOH 3 times and the combined extract was dissolved in 1N HCl solution and washed with ethyl acetate. The aqueous layer was basified with solid $Na_2CO_3$ and extracted with $CHCl_3$ to obtain an alkaloidal fraction. The alkaloidal fraction was subjected to column chromatography using silica gel, alumina and Sephdex LH 20, etc. From the alkaloidal fraction, five diterpene alkaloids, mesaconitine, aconitine, hypaconitine, 8-O-ethyl 14-benzoylmesaconine and talatizamine, were isolated and identified on the basis of their physico-chemical properties and spectroscopic evidences($^1H$-, $^{13}C$-NMR, EI-MS, IR, 2D-NMR) respectively. Especially the Compound IV, 8-O-ethyl 14-benzoylmesaconine, was assumed to be an artifact resulting from mesaconitine during extraction procedures. The contents of mesaconitine, aconitine and hypaconitine in the mother tuber of this plant were 0.300%, 0.024%, and 0.068%. And that of the attached tuber(new one) of this plant were 0.336%, 0.034% and 0.240% respectively.

• 대한설비공학회:학술대회논문집
• /
• 대한설비공학회 2009년도 하계학술발표대회 논문집
• /
• pp.629-632
• /
• 2009

The polymeric desiccant rotor is made from the super absorbent polymer by ion modification. The moisture sorption capacity of the super desiccant polymer(SDP) is 4 to 5 times larger than those of common desiccant meterials such as silica gel or zeolite. It is also known that SDP can be regenerated even at the relatively low temperature. To fabricate the desiccant rotor, firstly the SDP was laminated by coating the SDP on polyethylene sheet. Then corrugated and rolled up into a rotor. The diameter, the depth, the dimensions of the corrugated channel, etc. were pre-determined from numerical simulation on the heat and mass transfer in the desiccant rotor. The dehumidification performance was tested in a climate chamber. The relevant tests were carried out at the process air inlet temperature of $32^{\circ}C$, the regeneration air inlet temperature of $60^{\circ}C$ and the inlet dew-point temperature of both the process air and the regeneration air of $18.5^{\circ}C$, when the rotation period is long, the moisture sorption is not effective. In the desiccant rotor developed in this study, the optimum rotation period is found about 350s at the regeneration temperature of $60^{\circ}C$. It was found from further experiments that the optimum rotation tends to decreases as the regeneration temperature increases. Meanwhile, the outlet temperature of the process air deceases monotonically as the rotation period increases.

• 고려인삼학회:학술대회논문집
• /
• 고려인삼학회 1987년도 Proceedings of Korea-Japan Panax Ginseng Symposium 1987 Seoul Korea
• /
• pp.29-37
• /
• 1987

This study was devised to observe the cytotoxlc activities of petroleum-ether extract of Panax ginseng root(crude Gx) and its partially purified fraction from silicon acid column chromatography(7:3 CX) against sarcoma-180(5-180) and Walker carcinosarcoma 256(Walker 256) in vivo, and murine leukemic lymphocytes(L1210) and human rectal cancer cell(HRT-18) and human colon cancer cells(HT-29 and HCT-48) in vitro . Each cell-line was cultured in medium containing serial concentrations of the crude Gx or 7:3 Gx in vitro. A highly lipid soluble compound in the extract of Panax ginseng root was cytocidal to murine leukemic cells and human colon and rectal cancer cells in vitro In the meantime, ginseng saponin derivatives did not cytotoxic effects at its corresponding concentration. The growth rates of the cancer cells in medium containing ginseng extracts were inhibited gradually to a significant degree roughly in proportion to the increase of the extract concentration. The cytotoxic activity of 7:3 Gx was about 3 times more potent than that of crude Gx, one unit of cytotoxic activity against L121f cells being equivalent to 2.54$\mu\textrm{g}$ and 0.88 $\mu\textrm{g}$ for the crude Gx and 7:3 Gx, respectively. The Rf value of the active compound on silica -gel thin layer chromatography with petroleum-ether/ethyl ether/acetic acid mixture (90:10:1, v/v/v) as a developing solvent was 0.23. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7:3 Gx treatment compared with their control group. The significantly decreased hemoglobin values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude Gx. The synthetic levels of protein, DNA and RNA in human colon and rectal cancer cells were significantly diminished by treatment with the crude Gx, which can explain a part of the origin of its anticancer activity.