• Title/Summary/Keyword: $IC_50$

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Cytotoxicity of Ethanol Extract of Raphanuse Sativus on a Human Lung Cancer Cell Line (인체 폐암 세포주에 대한 무의 에탄올 추출물의 세포독성)

  • 임효빈;이건순;채희정
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.2
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    • pp.287-290
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    • 2004
  • This study was desinged to investigate the cytotoxic effect of ethanonl extract of radish, Raphanuse sativus on human lung cancer cell lines (A-549) using MTT(3-〔4,5-dimethylthiazol-2-yl〕-2-yl)-2,5-diphenyltetrazolium bromide) assay. Radish trunk and radish root were extracted by a mixed solvent of water and ethanol (5 : 5, v/v) after drying, The extracts were used for anticancer activity assay. $IC_{50}$/ (50% inhibitory concentration) of radish trunk and radish root were 0.015% and 0.03%, respectively. Radish trunk extract showed higher anticancer activity than radish root extract at the same concentration of 0.01%.

Inhibitory Effects of Cuscuta japonica Extract and C. australis Extract on Mushroom Tyrosinase Activity (새삼 (Cuscuta japonica Choisy) 및 실새삼 (C. australis R.Be) 추출물의 Mushroom Tyrosinase 활성 억제 효과)

  • Lee, Sung-Ja;Bae, Jung-Mi;Suk, Kui-Duk
    • Korean Journal of Pharmacognosy
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    • v.35 no.4 s.139
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    • pp.380-383
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    • 2004
  • The purpose of this study was to evaluate mushroom Tyrosinase inhibitory activity of Cuscuta japonica Choisy and C. australis R.Be. The experimental materials were expressed juice from their stems and flowers, both water and ethanol extracts, their seeds, and two kinds of commercially available cosmetic packing Wontosa and Bupjetosa (made from seeds of C. japonica). The 50% inhibitory concentration $(IC_{50})$ of C. Japonica juice was 5.4 mg/ml. However, C. australis juice showed negligible mushroom tyrosinase inhibitory activity. The $IC_{50}$ of water extracted C. japonica seed was $54.0\;{\mu}g/ml$, water extracted product of Wontosa $50.0\;{\mu}g/ml$ and Bupjetosa $40\;{\mu}g/ml$. The $IC_{50}$ of ethanol extracted C. japonica seed was $10\;{\mu}g/ml$, Wontosa $10\;{\mu}g/ml$ and Bupjetosa $20\;{\mu}g/ml$.

Screening of Korean Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products Formation (VII) (한국약용식물의 최종당화산물 생성저해활성 검색(VII))

  • Choi, So-Jin;Kim, Young Sook;Song, Yoo Jin;Lee, Yun Mi;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.345-351
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    • 2012
  • In this study, 49 Korean herbal medicines have been investigated with an in vitro evaluation system using glycation end products (AGEs) formation inhibitory activity. Of these, 18 herbal medicines ($IC_{50}$ < $50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Of these, five herbal medicines ($IC_{50}$ < $50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, Mallotus japonicus (twigs and leaves), Rhus javanica (twigs and leaves), Boehmeria nivea (whole plants), Quercus acuta (stems), and Eurya japonica (stems) showed more potent inhibitory activity (approximately 9-37 fold) than the positive control aminoguanidine ($IC_{50}=76.47{\mu}g/ml$).

Metallicity-dependent mixing length in evolution models of red supergiant stars in IC 1613

  • Chun, Sang-Hyun;Yoon, Sung-Chul;Oh, Heeyoung
    • The Bulletin of The Korean Astronomical Society
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    • v.46 no.2
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    • pp.50.2-50.2
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    • 2021
  • There is increasing evidence that the convective mixing length (α) in stellar evolution models depends on metallicity of stars. In order to confirm a more precise metallicity-dependent mixing length trend, we investigate the effective temperature and metallicity of 14 red supergiant stars (RSGs) in the irregular dwarf galaxy IC 1613 using the near-infrared spectra observed with the MMIRS on the MMT telescope. From the synthetic spectral fitting to the observed spectra, we find that the mean metallicity is about [Fe/H]=0.69 with a weak bimodal distribution. We also find that the effective temperature of RSGs in IC 1613 is higher by about 250 K than that of the SMC on average. We compare the RSG position with stellar evolutionary tracks on the HR diagram, finding that models with α = 2.2-2.4 H_p can best reproduce the effective temperatures of the RSGs in IC 1613. It is evident that the mixing length values for IC 1613 is lower than that of the Milky Way. This result supports our previous study on a metallicity-dependent mixing length: mixing length decreases with decreasing metallicity of host galaxies. However, this dependency becomes relatively weak for RSGs having a metallicity equal to or less than the SMC metallicity.

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Antioxidative Effect and Neuraminidase Inhibitory Activity of Polyphenols Isolated from a New Korean Red Waxy Sorghum (Sorghum bicolor L. cv. Hwanggeumchalsusu) (황금찰수수(Sorghum bicolor L. cv. Hwanggeumchalsusu) 유래 에탄올 추출물 및 폴리페놀계 화합물의 항산화 활성 및 뉴라미니데이즈 억제 효과)

  • Ra, Ji-Eun;Seo, Kyung Hye;Ko, Jee Yeon;Lee, Mi-Ja;Kang, Hyeon Jung;Kim, Sun Lim;Chung, Ill-Min;Seo, Woo Duck
    • Journal of Life Science
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    • v.25 no.7
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    • pp.786-794
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    • 2015
  • To identify nutritional and therapeutic properties of the new Korean red waxy sorghum cultivar ‘Hwanggeumchalsusu (HGC)’, we assayed the antioxidative effects and neuraminidase inhibitory activity. A methanol and 70% ethanol extract of HGC exhibited strong antioxidative effects (IC50 values of 83.2±2.7 for DPPH) and 85.6±2.4 μg/ml for ABTS) and neuraminidase (ND) inhibitory activity (IC50 values of 1.8±0.1 from extracted with methanol and 3.4±0.1 μg/ml from extracted with 70% ethanol) compared with that of the control, noncolored sorghum cultivar ‘Huinchalsusu (HC)’ (IC50> 200 μg/ml). We isolated nine polyphenols, Gallic acid (1), Protocatecuic acid (2), p-Hydroxy benzoic acid (3), Vanillic acid (4), Caffeic acid (5), Ferulic acid (6), Luteolinidin (7), Apigeninidin (8), Luteolin (9), from the HGC - methanol extract, to determine whether they were the active components Luteolinidin of one kind of polyphenols from the HGC, exhibited significant antioxidative effects (IC50 values of 10.9±0.5 μM for DPPH and 8.6 0.6 μM for ABTS) and neuraminidase (ND) inhibitory activity (IC50 values of 26.3±0.6) showed noncompetitive inhibition model. The binding affinity of the ND inhibitors in molecular docking experiments correlated with their ND inhibitory activities. These results suggest that HGC may be utilized to serve as a potential effective antioxidant and inhibitor of ND.

Antiplatelet and Antithrombotic Activities of Lindera obtusiloba Extract in vitro and in vivo

  • Lee, Jung-Ok;Kim, Chul-Young;Lee, Seung-Woo;Oak, Min-Ho
    • Biomolecules & Therapeutics
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    • v.18 no.2
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    • pp.205-210
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    • 2010
  • Several studies have shown that plant-derived polyphenols reduce cardiovascular accidents in high-risk patients and the inhibition of platelet function may be responsible for part of this benefit. Lindera obtusiloba is widely used in traditional herbal medicine for the treatment of cardiovascular and inflammatory diseases. Therefore, the antiplatelet and antithrombotic activities of Lindera obtusiloba Extracts (LOE) on in vitro platelet aggregation, radical scavenging activity and in vivo murine pulmonary thrombosis were examined. LOE was able to directly scavenge the stable DPPH radical in a concentration-dependent manner and its $IC_{50}$ value was 3.9 ${\pm}$ 0.1 ${\mu}g$/ml. LOE significantly inhibited collagen- and ADP-induced platelet aggregation in a concentration-dependent manner and its $IC_{50}$ value is 0.9 ${\pm}$ 0.1 mg/ml and 0.4 ${\pm}$ 0.1 mg/ml respectively. The inhibitory effect of LOE was comparable to aspirin ($IC_{50}$ values were 1.0 ${\pm}$ 0.5 and 1.0 ${\pm}$ 0.7 mg/ml, respectively). Furthermore, oral administration of LOE suppressed the death of mice with pulmonary thrombosis induced by intravenous injection of collagen plus epinephrine. Taken together, our results suggest LOE may be a promising candidate for antithrombotic agent, and the antithrombotic effect of LOE may be due to, at least in part, antiplatelet activity.

Inhibitory Potential of Thelephoric Acid on CYP2J2 Activities in Human Liver Microsomes (Thelephoric acid의 CYP2J2 효소 활성 저해제 평가)

  • Wu, Zhexue;Lee, Boram;Song, Kyung-Sik;Liu, Kwang-Hyeon
    • Journal of Life Science
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    • v.23 no.9
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    • pp.1126-1132
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    • 2013
  • Cytochrome P450 2J2 (CYP2J2) is an enzyme mainly found in human extrahepatic tissues, with predominant expression in the cardiovascular system. CYP2J2 plays important roles in the metabolism of endogenous metabolites and therapeutic drugs, such as arachidonic acid, astemizole, ebastine, and terfenadine. CYP2J2 is also overexpressed in human cancer tissues and cancer cell lines and may represent a potential target for therapy of human cancers. In this study, 10 natural products obtained from plants and microorganisms were screened as potential CYP2J2 inhibitors. Among them, thelephoric acid showed strong inhibition of astemizole O-demethylation activity ($IC_{50}=3.23{\mu}M$) in a dose-dependent manner. Evaluation of the substrate dependency of the inhibitory activity of thelephoric acid showed that it strongly inhibited CYP2J2-mediated ebastine hydroxylation ($IC_{50}=5.32{\mu}M$) and terfenadine hydroxylation ($IC_{50}=3.27{\mu}M$) in a substrate nondependent manner. The present data suggest that this compound might be a potential candidate for further evaluation for anticancer activity.

Anti-tumor activities of Naesosungma-tang (내소승마탕(內消升麻湯)의 항암효과(抗癌效果) 연구(硏究))

  • Shim, Sang-Hee;Park, Su-Yeon;Kim, Jong-Han;Choi, Jung-Hwa
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.19 no.1
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    • pp.79-92
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    • 2006
  • This study was carried out to evaluate antioxidative, cytotoxic and chemosensitizing effects for anti-tumor activities of Naesosungma-tang (NST). The results were as follows ; 1. The oxidative effects were measured by DPPH radical scavenging activity. NST water extract was showed more effective than ethanol extract and also various solvent fractions from NST showed effective in the following order : butanol fraction > ethyl acetate fraction > hexane fraction > aqueous fraction. 2. NST water extract was showed cytotoxic effects on the human cancer cells Calu-6 cell and SNU-601 cell, but not on MCF-7 cell. 3. The viability of cells was measured in 4 kinds of solvent fractions from water extract of NST by MTT assay. The results were as followings : 1) On the NIH3T3 cell, $IC_{50}$ value was $200{\sim}300\;{\mu}g/m{\ell}$ in three fractions except aqueous fraction. 2) On the Caco-2 cell, effective only in the butanol fraction. 3) On the Calu-6 cell, most effective in hexane fraction($IC_{50}:80\;{\mu}g/m{\ell}$) and effective in ethyl acetate and butanol fraction($IC_{50}:100{\sim}120\;{\mu}g/m{\ell}$). 4) On the MCF-7 cell, $IC_{50}$ value was similar in three fractions except aqueous fraction. 5) On the SNU-601 cell, $IC_{50}$ value was within $100\;{\mu}g/m{\ell}$ in three fractions except aqueous fraction. 6) On the HCT-1l6 cell, $IC_{50}$ value was $150{\sim}200\;{\mu}g/m{\ell}$ in three fractions except aqueous fraction. 7) On the AML-2/WT cell, not effective in four kinds of solvent fractions. 4. In combined effects of NST and vincristine on AML-2/D100 cell, water and ethanol extracts of NST and hexane fraction of water extracts of NST more effectively inhibited proliferation of AML-2/D100 cell. These results Suggest that NST has antioxidative and cytotoxic effects against Caco-2, Calu-6, MCF-7, SNU-601, HCT116 and NIH3T3 cell especially Calu-6 and SNU-601 cell, and also chemosensitizing effects against AML-2/D100 cell in combined vincristine.

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Syntheses and in vitro Antitumor Activities of 8-Azaxanthine and Its Derivatives (8-Azaxanthine과 그 유도체의 합성 및 시험관내 항암 활성)

  • Lee, Bong Hun;Shin, Jung Hee;Jang, Tae Sik;Park, Jang Su;Kang, Shin Won
    • Journal of the Korean Chemical Society
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    • v.41 no.7
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    • pp.357-361
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    • 1997
  • 8-Azaxanthine (1), 3-${\beta}$-D-ribofuranosyl-8-azaxanthine (2), 3-${\beta}$-D-ribofuranosyl-8-azaxanthine-5'-monophosphate (3), and 3-${\beta}$-D-ribofuranosyl-8-azaxanthine-5'-(3-pyridinylcarbonyl)monophosphate (4) were synthesized. The in vitro antitumor activities of the synthesized compounds against P388 mouse leukemia, FM3A mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. 2 with unnatural N-3 and C-1' glycoside bond had activity against three tumor cell lines and $IC_{50}$s of these compounds were 0.05, 0.06, and 0.06 ${\mu}mol/mL$ against three tumor cell lines, respectively. But these compounds had no antibacterial activity. $IC_{50}$s against U937 human histiocytic lymphoma cells were verified with the structural modification: $IC_{50}$s of 1, 2, 3, and 4 were 0.33, 0.06, 0.25, and 0.33 ${\mu}mol/mL$, respectively.

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Chlorogenic Acid Isomers from Sorbus commixta of Ulleung Island Origin and Their Inhibitory Effects against Advanced Glycation End Product (AGE) Formation and Radical Scavenging Activity (울릉 마가목의 클로로겐산 이성체의 최종당화산물의 생성 저해 및 라디칼 소거 활성)

  • Kim, Tae Hoon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.8
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    • pp.1208-1213
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    • 2016
  • Advanced glycation end product (AGE) formation and reactive oxygen species are potential therapeutic targets for the prevention of diabetic nephropathy and other pathogenic complications. Activity-guided isolation of an ethylacetate-soluble portion of 80% methanolic extract from fruits of Sorbus commixta of the Ulleung Island origin using AGE formation inhibition assay led to the isolation and identification of three caffeoylquinic acid derivatives of a previously known structure, 3-O-caffeoylquinic acid (neochlorogenic acid; 1), 4-O-caffeoylquinic acid (cryptochlorogenic acid; 2), and 5-O-caffeoylquinic acid (chlorogenic acid; 3). The structures of these compounds were confirmed by interpretation of nuclear magnetic resonance and mass spectrometry data. Among the isolates, the major metabolite, neochlorogenic acid (1) showed the most potent inhibitory effect against AGE formation with an $IC_{50}$ value of $167.5{\pm}3.5{\mu}M$. Furthermore, all isolated chlorogenic acid isomers were evaluated for their radical scavenging activity against peroxynitrite, and structurally related isomers 1, 2, and 3 exhibited potent inhibitory effects in this radical scavenging assay. This result suggests that the monocaffeoyl quinic acid derivatives isolated from S. commixta might be beneficial for the regulation of diabetic complications and related diseases.