• 한국임상약학회지
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• 제8권2호
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• pp.139-142
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• 1998

The effects of MeOH extracts from 28 herbal medicines on monoamine oxidase (MAO) activity were investigated. MAO was purified from mouse brain and its activity was determined by fluoro-photometry using kynuramine as a substrate. Three MeOH extracts, Coptis japonica, Cinnamomum cassia and Poncirus trifoliate from the herbal medicines showed a strong inhibitory effect with less than $100\;{\mu}g/ml$ in their inhibitory amounts of $50\%$ ($IC_{50}$ values) on MAO activity. Four MeOH extracts including Evodia officinalis exhibited a mild inhibition of MAO activity with $100-200\;{\mu}g/ml$ in their $IC_{50}$ values.

• 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 $55.36{\mu}M$.

• Biomolecules & Therapeutics
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• 제7권2호
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• pp.153-157
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• 1999

The anticancer effect of medicinal plants against two oral carcinoma cells, A253 and SCC-25 were investigated in this study. Methanol extracts from 63 medicinal plants, which have anticancer activities against other cancers such as stomach, hepatocellular or colon carcinomas, were prepared and screened for their anti- oral cancer activity by using MTT assay. Thirty one samples showed anti-oral cancer activity against either cell line used, however, other 32 samples had no anti-oral cancer activity. Among these samples methanol extract of Caesalpinia sappan revealed the strongest anti-oral cancer activity. The $IC_{50}$/ values of this extract against A253 and SCC-25 cells were 16 and 25 $\mu$g/m1, respectively. Fractions of n-hexane, dichloromethane, ethylacetate, n-buthanol and water were prepared from methanol extracts of Caesalpinia sappan, Anthriscus sylvestris, Rhus japonica, Curcuma arowatica, Inula helenium, Sinoarnudinaria reticulata, and Polygonum cuspidatum, respectively. Among these 35 fractions the n-hexane fraction of Inula helenium showed the strongest anti-oral cancer activity, the $IC_{50}$/ value was 1.6$\pm$0.3 $\mu\textrm{g}$/ml. Ten other fractions showed $IC_{50}$/ values lower than 10 $\mu\textrm{g}$/ml.

• Natural Product Sciences
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• 제20권4호
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• pp.274-280
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• 2014

Six compounds were isolated from the n-BuOH fraction of the aerial parts of Aruncus dioicus var. kamtschaticus including: sambunigrin (1), prunasin (2), aruncide A (3), aruncide C (4), 1-O-caffeoyl-${\beta}$-D-glucopyranose (5), and caffeic acid (6). Their structures were confirmed by comparing the spectral data with those reported in the literature. The isolated compounds (1 - 6) were then examined for their cytotoxic effects towards MCF-7, HL-60, and HeLa cancer cell lines, as well as their DPPH radical scavenging activity. The results indicated that compound 4 possessed the strongest inhibitory effect toward HeLa cell line with $IC_{50}$ value of $5.38{\pm}0.92{\mu}M$. Compound 3 possessed selective cytotoxic activity on HL-60 cells with $IC_{50}$ value of $6.27{\pm}0.17{\mu}M$, compound 5 was found as the best in inhibiting proliferation with $IC_{50}$ value of $2.25{\pm}0.09{\mu}M$, and the other compounds showed significant inhibition with $IC_{50}$ values ranging from 6.10 to $11.27{\mu}M$. Compound 5 also displayed the strongest cytotoxic effect toward MCF-7 cell line ($IC_{50}$ $4.32{\pm}0.15{\mu}M$). Both 5 and 6 demonstrated strong radical scavenging activity ($IC_{50}$ $6.87{\pm}0.03$ and $4.33{\pm}0.22{\mu}M$, respectively). Compounds 1 and 5 were isolated for the first time from this plant.

• 한국식품과학회지
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• 제33권6호
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• pp.753-759
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• 2001

Aloe vera 껍질로부터 구내염등 항염증제재를 개발하기 위해 항염증 활성이 있는 분획을 분리, 동정하고, 염증과 관련된 효소활성에 대한 저해효과를 조사하였다. Aloe vera 껍질의 추출물을 용매에 따라 분획하였고, 활성이 우수한 ethylacetate층을 silica gel column chromatography 및 preparative thin layer chromatography를 통해 두 가지 활성물질을 정제하였다. 정제된 두 가지 물질은 UV spectrum과 FT-IR, $^1H-NMR$, 및 Mass spectrum 분석을 통해 aloe-emodin과 barbaloin으로 동정하였다. Aloe vera 분획물의 hyaluronidase 활성저해를 측정한 결과는 aloe-emodin은 $40\;{\mu}g/mL$, barbaloin은 $70\;{\mu}g/mL$의 $IC_{50}$값을 나타내었다. Leucko-cyte elastase 활성 저해를 측정한 결과는 aloe-emodin은 $50\;{\mu}g/mL$, barbaolin은 $60\;{\mu}g/mL$의 $IC_{50}$값을 나타내었다. Collagenase 활성 저해를 측정한 결과는 aloe-emodin은 $40\;{\mu}g/mL$, barbaloin은 $60\;{\mu}g/mL$의 $IC_{50}$값을 나타내었다. 또한 prostaglandin endoperoxide synthase 활성 저해를 측정한 결과는 aloe-emodin은 $40\;{\mu}g/mL$, barbaloin은 $70\;{\mu}g/mL$의 $IC_{50}$값을 나타내었다. 쥐를 이용한 carrageenan족 부종 억제효과는 aloe-emodin의 경우 100mg/kg 투여량으로 52.9%의 억제효과를 나타내었으며, 이 억제효과는 indomethacin의 약 1/10이었으며, aspirin과는 유사한 활성을 보였다. 반면 barbaloin의 경우 100mg/kg의 투여량으로 74.9%의 억제효과를 나타내었으며 이 억제효과는 indomethacin의 약 1/5이었으며, aspirin의 약 1.5배 효과를 나타내어 우수한 항염증 활성을 갖는 것으로 판단된다. 인체치은세포에 대한 독성은 aloe-emodin보다 barbaloin이 적게 나타났으며 이 두 가지 물질은 1 및 $5\;{\mu}g/mL$농도에서는 독성이 전혀 나타나지 않으나 10 및 $20\;{\mu}g/mL$에서는 독성이 있는 것으로 나타났다. 그러나 상용되고 있는chlorhexidin에 비해서는 유의적으로 독성이 적은 것으로 나타났다. 이상의 결과로 보아 aloe-emodin 과 barbaloin은 항우식 및 항염증 활성이 우수할 뿐만 아니라 치은세포의 독성이 비교적 낮아 구강병 예방제재로의 개발 가능성이 우수하다고 사료된다.

• Preventive Nutrition and Food Science
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• 제16권4호
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• pp.328-332
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• 2011

After preparation of acetone, ethanol, methanol, and water extracts (10 g/300 mL) of dried persimmon (Diospyros kaki cv. Fuyu) flower-buds, total phenolic contents (TPC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (RSA), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) RSA, reducing power (RP), and tyrosinase inhibitory activity of the extracts were evaluated. The methanol extracts produced the highest TPC (113.39 mg gallic acid equivalents/g), DPPH RSA ($IC_{50}=40.25\;{\mu}g/mL$), ABTS RSA ($IC_{50}=58.17\;{\mu}g/mL$) and RP ($IC_{50}=69.43\;{\mu}g/mL$) activities while the water extracts generated the lowest values. The ethanol extract showed the highest tyrosinase inhibitor activity (88.90%) at a concentration of 1 mg/mL. These results indicated that persimmon flower-buds may be a useful source of natural antioxidants.

• Natural Product Sciences
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• 제9권2호
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• pp.105-108
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• 2003

During our research program to find DNA strand-scission agents from higher plants, the MeOH extracts of the stems of Mucuna birdwoodiana Tutcher. (Leguminosae) exhibited the most potent activity with an $IC_{50}$ value of $4.9\;{\mu}g/ml$. Thus, detailed laboratory investigation was performed, and led to the isolation of known compounds, $({\pm})$-catechin (1) and (-)-epicatechin(2) as active principles. Compounds 1 and 2 showed significant activity of DNA strand-scission with $IC_{50}$ values of 10.8 and $7.5\;{\mu}g/ml$, respectively (positive control, bleomycin: $IC_{50}\;3.3\;{\mu}g/ml$.

• Bulletin of the Korean Chemical Society
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• 제31권10호
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• pp.2854-2860
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• 2010

Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

• Natural Product Sciences
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• 제18권1호
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• pp.1-7
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• 2012

Among 90 Vietnamese medicinal plant extracts investigated for their antioxidant activity by DPPH assay at various concentrations from $10-100{\mu}g/mL$, 67 showed an inhibition rate over 50% at $100{\mu}g/mL$; 47 had greater than 50% inhibition at $50{\mu}g/mL$; 17 showed over 50% inhibition at $25{\mu}g/mL$. 8 extracts which exhibited strong inhibitory activity more than 50% inhibition at $10{\mu}g/mL$ were further tested for lipid peroxidation inhibition by TBA assay. They displayed activity with $IC_{50}$ values from 30.6 to $158.9{\mu}g/mL$. Until now, this is the first report on antioxidant activity of the female flower of Borassus flabellifer, and the stem of Combretum latifolium, Embelia ribes, Spatholobus parviflorus, and Tetrastigma erubescens. Fractionations of the EtOAc extract prepared from S. parviflorus led to the isolation of protocatechuic acid (1), ferulic acid (2), epicatechin (3), and gallic acid (4). These compounds showed significant DPPH inhibitory activity with $IC_{50}$ values from 6.5 to $23.6{\mu}M$.

• Natural Product Sciences
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• 제19권4호
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• pp.366-371
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• 2013

Seventeen compounds (1 - 17), ${\beta}$-sitosterone (1), lupenone (2), arborinone (3), ${\beta}$-sitosterol (4), lupeol (5), epi-lupeol (6), taraxerol (7), betulinic acid (8), 24R-methyllophenol (9), germanicol (10), hexatriacontane (11), nonacosan-1-ol (12), benzoic acid (13), tetradecyl(E)-ferulate (14), di(2-ethylhexyl) phthalate (15), trilinolein (16) and monopalmitin (17), were isolated from the methylene chloride-soluble fraction of the cork of Euonymus alatus Sieb. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 6, 11, 13 and 14 were isolated for the first time from this plant. Compound 4 showed moderate cytotoxic activity with an $IC_{50}$ value of 6.22 ${\mu}M$ in HL-60 cell line. Compound 9 exhibited moderate cytotoxic activity with $IC_{50}$ values of 63.31, 15.45, 15.14 and 21.72 ${\mu}M$ in four kinds of human cancer cell lines, Jurkat T, HeLa, HL-60 and MCF-7, respectively. Compound 17 showed moderate cytotoxic activity with an $IC_{50}$ value of 70.71 ${\mu}M$ in Jurkat T cell line. In addition, compounds 2, 3, 14 and 16 exhibited weak antioxidant activity with $IC_{50}$ values of 151.76, 170.79, 137.46 and 139.37 ${\mu}M$, respectively.