• 제목/요약/키워드: $IC_50$

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물푸레나무로부터 분리된 Esculetin와 Esculin의 미백 효능 (Depigmenting Effects of Esculetin and Esculin Isolated from Fraxinus rhynchophyllaHance)

  • 홍용덕;남미희;이창석;신송석;박영호
    • 대한화장품학회지
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    • 제40권1호
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    • pp.89-94
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    • 2014
  • 물푸레나무 수피 추출물은 주요 생활성 물질로서 esculetin과 esculin을 포함하고 있다. 이 가운데, Esculetin은 B16F10 melanoma cells에서 $IC_{50}$ value $2.8{\mu}M$의 아주 좋은 melanogenesis 억제 활성을 나타내며, 이를 통해 Melan-A cell에서 melanin 합성을 감소시킨다. 더욱이, esculetin은 mushroom tyrosinase에서도 $IC_{50}$ value $40{\mu}M$의 억제 활성을 나타내어 melanin biosynthesis를 저해한다. 위의 결과들로서, 우리는 melanogenic enzyme 활성 조절에 의해 melanin 생성을 저해하는 효과적인 피부미백 물질로서 esculetin을 제안하고자 한다.

Antioxidant and Antidiabetic Activities of Eucommia ulmoides Bark

  • Qu, Guan-Zheng;Heo, Seong-Il;Wang, Myeong-Hyeon
    • Journal of Applied Biological Chemistry
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    • 제49권3호
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    • pp.82-85
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    • 2006
  • Eucommia ulmoides bark extracts by cold water, boiling water, 100% EtOH, 70% EtOH, 100% MeOH, 70% MeOH and $CHCl_3$ were assayed for their medicinal effects. The antioxidant activity of the extracts ranged from $IC_{50}$ 125.2 to $IC_{50}\;872.7{\mu}g/ml$ in the 1,1-diphenyl-2-picrylhydrazyl (DDPH) free radical-scavenging assay, and cold water extracts had the highest antioxidant activity. $CHCl_3$ extracts had the highest inhibitory effect on angiotensin I-converting enzyme (ACE) giving inhibition of up to 56.4% at a concentration of 1 mg/ml. Extracts in 100% EtOH had the greatest inhibitory effect on $\acute{a}-amylase$ activity ($IC_{50}=174.6{\mu}g/ml$), and 70% MeOH extracts had the greatest inhibitory effect on ${\alpha}-glucosidase$ activity ($IC_{50}=14.0{\mu}g/ml$). Taken together, these results provided the in vitro evidence on the ACE, amylase and glucosidase inhibitory actions of E. ulmoides bark that form the pharmacological basis for its antihypertensive and antidiabetic action.

Isolation and Characterization of a Trypsin Inhibitor and a Lectin from Glycine max cv. Large Black Soybean

  • Ye, Xiu Juan;Ng, Tzi Bun
    • Food Science and Biotechnology
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    • 제18권5호
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    • pp.1173-1179
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    • 2009
  • Trypsin inhibitors and lectins are defense proteins produced by many organisms. From Chinese 'Large Black Soybeans', a 60 kDa lectin and a 20 Da trypsin inhibitor (TI) were isolated using chromatography on Q-Sepharose, Mono Q, and Superdex 75. The TI inhibited trypsin and chymotrypsin with an $IC_{50}$ of 5.7 and $5{\mu}M$, respectively. Trypsin inhibitory activity of the TI was stable from pH 3 to 13 and from 0 to $65^{\circ}C$. Hemagglutinating activity of the lectin was stable from pH 2 to 13 and from 0 to $65^{\circ}C$. The TI was inhibited by dithiothreitol, signifying the importance of disulfide bond. The TI and the lectin inhibited HIV-1 reverse transcriptase ($IC_{50}$=44 and $26{\mu}M$), and proliferation of breast cancer cells ($IC_{50}$=42 and $13.5{\mu}M$) and hepatoma cells ($IC_{50}$=96 and $175{\mu}M$). The hemagglutinating activity of the lectin was inhibited most potently by L-arabinose. Neither the lectin nor the TI displayed antifungal activity.

Cytotoxic and antioxidant properties of four plants belonging to the genus Solanum

  • Dongre, Santoshkumar H.;Badami, Shrishailappa;Godavarthi, Ashok;S., Mahendran;P., Vijayan;B., Suresh
    • Advances in Traditional Medicine
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    • 제8권1호
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    • pp.86-92
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    • 2008
  • The aim of the study was to evaluate in vitro antioxidant and cytotoxic activities of the methanolic extracts of leaves of Solanum sisymbrifolium, Solanum anguivi multiflora, Solanum barbisetum and Solanum jasminoides. In the in vitro antioxidant screening using ABTS [2,2'-azino-bis (3-ethylbenzo-thiazoline-6-sulphonic acid) diammonium salt] method, the methanol extracts of Solanum jasminoides, Solanum barbisetum and Solanum anguivi multiflora exhibited potent antioxidant activity with $IC_{50}$ values 31.25 $\pm$ 0.35, 40.33 $\pm$ 0.57 and 54.33 $\pm$ 0.57 ${\mu}g$/ml, respectively. Solanum barbisetum also showed potent activity in DPPH [1,1-diphenyl-2-picryl hydrazyl] method with an $IC_{50}$ value of 55.33 $\pm$ 1.66 ${\mu}g/ml. In the cytotoxicity studies, the methanol extract of Solanum barbisetum exhibited moderate activity against Vero, HEp-2, HeLa and A-549 cell lines with $IC_{50}$ values in the range of 83.30 - 127.30 ${\mu}g$/ml. Solanum anguivi multiflora extract also showed moderate activity against Hep-2 cell line with $IC_{50}$ value of 80.13 ${\mu}g$/ml. Solanum barbisetum possessing both the activities requires further investigation.

Cyclic Nucleotide Phosphodiesterases as Possible Targets for Ginsenosides

  • Lugnler, C.;Kim, N.D
    • 고려인삼학회:학술대회논문집
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    • 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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    • pp.216-223
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    • 1998
  • Cyclic nucleotide phosphodiesterases (PDEs) represent the unique enzymatic system degrddinf cAMP and cGMP which play a major role in the regulation of cell physiology. To investigate a possible molecular mechanism of ginsenosides, their activities were evaluated on PDEs which are recently described is new therapeutic targets. PDEs are classified into 7 families according to their genes (PDEI to PDE7) and are differently distributed in tissues. The IC50 values of ginsenosides were determined on PDEI to PDE 5 chromatographically isolatetl from bovine aorta. The results show that total ginseng saponin extract preferentially inhibits PDE 1 and PDE4 at concentrations nearby 200 ug/ml. Protopanaxadiol (PPD) fraction acts preferentially on PDE4 with and IC50 value of 100 nlml and inhibits also PDEI and PDE5 at 14 to 2 fold higher concentrations, respectively. Protopanaxatriol (PPT) fraction preferentially inhibits PDE 1 with and IC50 value of 170 ug/ml. Compound Rgl, originated from PPT fraction, and RC3 (5) represent the most active compounds towards PDE 1 with IC50 values around 80 UM. However Rg3 (R), epimer of Rgl (5) has no effect on the various PDEs tested, excepted on PDE3 rich is sligthly sensitive Compound Rbl, originated from PPD, acts on both PDEI and PDE4. It if two fold less active than Rgl and Rg3 (5) on PDEI. Taken together, these results mainly suggest that PDEI and PDE4 inhibitions could be a molecular mechanism which would participate in ginsenoside mechanisms, especially the effect of PPD on blood vessel and on CNS.

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Monoamine Oxidase Inhibitory Components from the Roots of Sophora flavescens

  • Hwang Ji-Sang;Lee Seon A;Hong Seong Su;Lee Kyong Soon;Lee Myung Koo;Hwang Bang Yeon;Ro Jai Seup
    • 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.

Antioxidant Activities and Determination of Phenolic Acids from Leaves of Perilla frutescens

  • Lee, Jin-Hwan;Kang, Nam-Suk;Ha, Tae-Joung;Ko, Jong-Min;Han, Won-Young;Suh, Duck-Yong;Park, Ki-Hun;Baek, In-Youl
    • Journal of Applied Biological Chemistry
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    • 제49권1호
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    • pp.11-15
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    • 2006
  • Two catecholic phenolic acids (1 and 2) obtained from 80% methanolic extract of Perilla frutescens var. frutescens leaves through chromatography showed strong DPPH (1: $IC_{50}$ = 15.5 ${\mu}M$, 2: $IC_{50}$ = 11.7 ${\mu}M$) and ABTS (1: $IC_{50}$ = 5.5 ${\mu}M$, 2: $IC_{50}$ = 4.6 ${\mu}M$) radicals scavenging abilities. Antioxidant compounds contents of 1 and 2 as determined by $C_{18}$ reversed phase HPLC coupled with diode-array detector were 2.98 and 2.26 mg/g, respectively.

Lipoxygenase Inhibitors from Paeonia lactiflora Seeds

  • Kim, Hyo-Jin;Chung, Shin-Kyo;Park, Sang-Won
    • Preventive Nutrition and Food Science
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    • 제4권3호
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    • pp.163-166
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    • 1999
  • Previously, the methanolic extract of Paeonia lactiflora seeds was shown to have strong ingibitory activity against soybean liposygenase (SLO). Four phenolic compounds were isolated from the seeds by solvent fractionation Sephadex LJ-20 column chromatography and preparative HPLC, and three of them showed strong SLO inhibitio and were characterized as trans-resveratrol, $\varepsilon$-viniferin and luteolin by UV, IR, 1H-NMR, 13C-NMR and MS spectrometry. trans-Resveratrol (IC50=1.02$\mu$M), $\varepsilon$-viniferin (IC50=0.81$\mu$M) and luteolin (IC50=10.01$\mu$M), first found in the above seeds, exhibited a potent SLO inhibitory activity although their activity was lower than that of a well-known lipoxygenase inhibitor, nordihydroguaiaretic acid (NDGA) (IC50=0.57$\mu$M). These results suggest that Paenia lactiflora seeds, now an unused plant seed, may be developed into useful sources of anti-inflammatory drugs.

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Optimization of the Extraction of Polyphenols and Flavonoids from Argania spinosa Leaves using Response Surface Methodology

  • Rajaa Moundib;Hamadou Sita;Ismail Guenaou;Fouzia Hmimid
    • Natural Product Sciences
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    • 제29권2호
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    • pp.83-90
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    • 2023
  • To our knowledge, this is the first study aiming to optimize the extraction conditions of total phenolic compounds (TPC) and total flavonoids contents (TFC) from Argania spinosa leaves using Response Surface Methodology (RSM) with a Box-Behnken design (BBD). The optimal conditions obtained were 5% (w/v) solvent-to-solid ratio, 72.33% ethanol concentration, and 10h ours as an extraction time, which resulted in an extract with maximum TPC (131.63 mg GAE/g dw) and TFC (10.66 mg QE/g dw). Under the optimal extraction conditions, the antioxidant activity of the extracts of leaves of argan tree showed a moderate antiradical capacity of DPPH (IC50 = 0,130 mg/mL) and ABTS (IC50 = 0.198 mg/mL). However, the leaves of argan tree showed a very interesting reducing power of Iron (IC50 = 0.448 mg/ml) which is similar to that of the ascorbic acid (IC50 = 0.371 mg/mL).

옻나무 칠액성분(漆液成分) 중 Urushiol의 암세포(癌細胞) 증식억제(增殖抑制) 효과(效果) - in vitro 세포독성효과(細胞毒性效果) - (In vitro Cytotoxin Activity of Urushiol in the Sap of Rhus verniciflua STOKES)

  • 나천수;정남철;오광인
    • 한국산림과학회지
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    • 제87권2호
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    • pp.260-269
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    • 1998
  • 본 연구는 전통적인 민간요법으로 많이 이용되고 있는 옻나무의 옻칠액의 주성분인 urushiol의 암세포증식억제 효과를 검정하기 위하여 L1210(mouse 혈액암세포), PC-9(인체폐암세포), A427(인체폐암세포), KATO III(인체위암세포)에 대한 urushiol의 세포독성을 검정하였다. Urushiol은 column chromatography에서 hexane과 acetone을 혼합하여 step-wise법으로 용출한 분획을 암세포주 L1210, PC-9, A427, KATO III에 투여했다. 그 결과 암세포 증식억제효과는 hexane : acetone(9 : 1) 분획이 가장 높았고, 그외 50%억제농도($IC_{50}$)는 A427 에서 $0.018{\mu}g/m{\ell}$로 가장 우수하였다. 이들 암세포에 대한 urushiol의 hexane: acetone(9 : 1)분획의 50%억제농도($IC_{50}$)를 시판용 tetraplatin 비교한 결과 urushiol이 tetraplatin에 대하여 L1210에서 3.4배, PC-9 에서 3.9배, A427에서 105.5배의 낮은 농도에서도 동일한 억제효과를 나타냈고, KATO III에서는 다소 높았다.

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