• Title/Summary/Keyword: $IC_{50}$ values

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Melanin Synthesis Inhibition and Radical Scavenging Activities of Compounds Isolated from the Aerial Part of Lespedeza cyrtobotrya

  • Lee, Mi-Yeon;Kim, Jin-Hee;Choi, Jung-Nam;Kim, Ji-Young;Hwang, Geum-Sook;Lee, Choong-Hwan
    • Journal of Microbiology and Biotechnology
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    • v.20 no.6
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    • pp.988-994
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    • 2010
  • The EtOAc fraction of Lespedeza cyrtobotrya showed mushroom tyrosinase inhibitory and radical scavenging activities. Four active compounds were isolated based on Sephadex LH-20 chromatography and HPLC, and the structures were elucidated, on the basis of their LC-MS and NMR spectral data, as 2-(2,4-dihydroxyphenyl)-6-hydroxybenzofuran (1), eriodictyol-7-O-glucopyranoside (2), haginin A (3), and dalbergioidin (4), respectively. Compound (1) showed mushroom tyrosinase inhibitory activity with an $IC_{50}$ value of $5.2\;{\mu}M$ and acted as a competitive inhibitor. Furthermore, $37.3\;{\mu}M$ of compound 1 reduced 50% of the melanin content on human melanoma (MNT-1) cells. The radical scavenging activities of compounds 1, 2, 3, and 4 were shown to have $IC_{50}$ values of 11.0, 24.5, 9.0, and $36.5\;{\mu}M$, respectively, in an ABTS system and $IC_{50}$ values of 42.7, 36.0, 37.7, and $61.7\;{\mu}M$, respectively, in a DPPH system. The mushroom tyrosinase inhibitory activity of the EtOAc fraction of Lespedeza cyrtobotrya was contributed by compounds 1, 3, and 4, and its radical scavenging activity was contributed by compounds 1-4.

Inhibition Effect of ACE (Angiotensin Converting Enzyme) and Kinetics of Aloe Acethylmannan (알로에 아세칠만난의 ACE (Angiotensin Converting Enzyme) 저해효과 및 동력학적 분석)

  • Ryu, Il-Whan;Shin, Yong-Seo
    • Korean Journal of Food Science and Technology
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    • v.29 no.6
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    • pp.1269-1274
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    • 1997
  • This study was researched to purify and characterize variety bioactive material acethylmannan from Aloe vera. Purified acethylmannan was mannose (67%), acetyl group (23%) and the rest glucose, galactose that consisting of long chain polydispered ${\beta}-1,4$ linked mannan polymers. The sugar and acetyl group in molecular were linked molar ration one third. $IC_{50}$ value (i.e that concentration which exhibits 50% more enzyme inhibition than control) on angiotensin converting enzyme were 0.58 mM. This compound were found to be a competitive inhibition of Angiotensin Converting Enzyme with apparent Ki values of 0.068 mM.

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4D-QSAR Study of p56Ick Protein Tyrosine Kinase Inhibitory Activity of Flavonoid Derivatives Using MCET Method

  • Yilmaz, Hayriye;Guzel, Yahya;Onal, Zulbiye;Altiparmak, Gokce;Kocakaya, Safak Ozhan
    • Bulletin of the Korean Chemical Society
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    • v.32 no.12
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    • pp.4352-4360
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    • 2011
  • A four dimensional quantitative structure activity relationship analysis was applied to a series of 50 flavonoid inhibitors of $p56^{lck}$ protein tyrosine kinase by the molecular comparative electron topological method. It was found that the -log (IC50) values of the compounds were highly dependent on the topology, size and electrostatic character of the substituents at seven positions of the flavonoid scaffold in this study. Depending on the negative or positive charge of the groups correctly embedded in these substituents, three-dimensional bio-structure to increase or decrease -log (IC50) values in the training set of 39 compounds was predicted. The test set of 11 compounds was used to evaluate the predictivity of the model. To generate 4D-QSAR model, the defined function groups and pharmacophore used as topological descriptors in the calculation of activity were of sufficient statistical quality ($R^2$ = 0.72 and $Q^2$ = 0.69). Ligand docking approach by using Dock 6.0. These compounds include many flavonoid analogs, They were docked onto human families of p56lck PTKs retrieved from the Protein Data Bank, 1lkl.pdb.

Screening of Extracts from Red Algae in Jeju for Potentials MarineAngiotensin - I Converting Enzyme (ACE) Inhibitory Activity

  • Cha, Seon-Heui;Lee, Ki-Wan;Jeon, You-Jin
    • ALGAE
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    • v.21 no.3
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    • pp.343-348
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    • 2006
  • This study was conducted to screen in vitro angiotensin - I converting enzyme (ACE) inhibitory activities of methanol (MeOH) and aqueous extracts at 20°C and 70°C, respectively, prepared from twenty-six red algae obtained from the coast of Jeju Island in Korea. Among aqueous extracts at 20°C (20AE) from red algae Lomentaria catenata showed the strongest ACE inhibitory activity and Lithophyllum okamurae recorded the second highest activity. From MeOH extract at 20°C (20ME) Ahnfeltiopsis flabelliformis possessed the strongest ACE inhibitory activity. Remarkable activities from MeOH extracts at 70°C (70ME) were observed in Grateloupia filicina, Sinkoraena lancifolia and Grateloupia lanceolata. However, no significant activity was found in aqueous extracts at 70°C (70AE). The IC50 values, which are concentrations required to inhibit 50% activity of ACE, for ACE inhibitory activities of 20AE from Lithophyllum okamurae and L. catenata were 13.78 and 12.21 μg mL–1, respectively. The IC50 values of 20ME from A. flabelliformis and Laurencia okamurae were 13.84 and 106.15 μg mL–1. Those of the 70ME from Bonnemaisonia hamifera, Grateloupia filicina, Sinkoraena lancifolia, G. lanceolata, Gracilaria vermiculophylla and L. okamurae ranged from 25.82 to 124.69 μg mL–1.

Quality Characteristics of Jelly with Black Garlic (흑마늘을 이용한 기능성 젤리의 품질 특성)

  • Lee, Ji-Yeon;Yoon, Ho-Young;Kim, Mee-Ree
    • Journal of the Korean Society of Food Culture
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    • v.25 no.6
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    • pp.832-838
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    • 2010
  • In this study, the quality characteristics of jelly with black garlic (0, 10, 20, and 30%) were evaluated. The pH of jelly with black garlic decreased according to the amount of black garlic added. The sugar content of the jelly increased significantly with added black garlic. Lightness, redness, and yellowness decreased with increasing black garlic content. Moreover, the textural properties, which included hardness, springiness, cohesiveness, gumminess, and chewiness decreased in jelly that contained black garlic compared to the controls. Additionally, the antioxidant activity of jelly that contained black garlic increased in a concentration dependent manner. The $IC_{50}$ values of the DPPH radical scavenging activity for jelly that contained 10, 20 and 30% black garlic were 132.47, 50.97, 40.06, and 30.41 mg/mL, respectively. The $IC_{50}$ values of the hydroxyl radical scavenging activity of jelly decreased as the black garlic concentration increased. Finally, sensory results showed that the scores of over-all preference and buying intention for jelly with 20% black garlic were the highest.

Antioxidant Activity of Several Cabbage (Brassica oleracea L.) Cultivars

  • Yang, Sung-Ryeul;Songzhuzhao,;Boo, Hee-Ock
    • Korean Journal of Plant Resources
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    • v.28 no.3
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    • pp.312-320
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    • 2015
  • Total phenol, flavonoid and antioxidant components of cabbage leaf samples derived from different cultivar were determined. Total phenol compound content showed the highest amount in methanol extracts from ‘YR Howol’ cultivar (11.72 ㎎/g), followed by ‘Harutame’ (10.66㎎/g), ‘Winstar’ (10.34 ㎎/g) and YR Hero (10.20 ㎎/g). The highest amount of total flavonoid content was observed from the methanol extracts of Harutame (5.39 ㎎/g), followed by Winstar (4.28 ㎎/g), Wialhowol (4.10 ㎎/g). The SOD enzyme activity showed a high activity of ‘YR Hogeo’ cultivar, and the cultivar of ‘YR Howol’ cultivar showed the lowest activity of SOD. The activity of CAT and APX showed higher values ‘Ogane’ and ‘YR Hogeol’ cultivars than the other cultivars. The POD activities showed relatively high values ‘Ogane’ and ‘YR Howol’ cultivars compared with other cultivars. The free radical (DPPH) scavenging activity showed lower IC50 values of ‘Harutame’ (15.71) and ‘YR Howol’ cultivar (16.88), however methanol extract of ‘YR Hero’ cultivar (22.49) being the highest. The extracts of all cabbage cultivars in the reaction solution of pH 1.2 could be decomposed nitrite more than 50%. Especially, the cultivar ‘YR Hogeol’ and ‘Ogane’ showed a relatively high nitrite scavenging activity for each 60.13% and 57.20% respectively. The IC50 values of antioxidant activity determined by ABTS were lower in ‘Harutame’ (17.04) and ‘YR Howol’ cultivar (17.97), and its results observed similar with values obtained from the same extracts by DPPH method. The result of this study suggests that the methanol extract of Brassica oleracea L. contains the high amount of phenolic and higher radical scavenging activities.

Evaluation for Interactive Toxic Effects of Binary Heavy Metals on Bacterial Growth and Phosphorus Removal under Co-Culture Condition of Alcaligenes sp. and Pseudomonas sp. (Alcaligenes sp.와 Pseudomonas sp.의 공동배양 조건에서 박테리아 생장 및 인 제거에 미치는 두 종 중금속의 상호적인 독성효과 평가)

  • Kim, Deok-Hyun;Park, Sang-Wook;Kim, Deok-Won;Park, Ji-Su;Oh, Eun-Ji;Yoo, Jin;Chung, Keun-Yook
    • Applied Chemistry for Engineering
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    • v.31 no.6
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    • pp.612-623
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    • 2020
  • This study was initiated to quantitatively evaluate the inhibitory effects of five heavy metals (Cd, Cu, Zn, Pb, Ni) on bacterial growth and phosphorus removal in the binary culture of Alcaligenes sp. plus Pseudomonas sp. IC50 values of Alcaligenes sp. plus Pseudomonas sp. for Cd, Cu, Zn, Pb, and Ni were 0.75, 10.93, 7.08, 13.30, and 15.78 mg/L, respectively. For the binary treatments of heavy metals, IC50 was the lowest in the treatment of Cd + Cu, whereas, it was the highest in the Ni + Pb treatment. The EC50 values for Cd, Cu, Zn, Pb, and Ni were 0.54, 11.08, 6.14, 9.33, and 13.81 mg/L, respectively. For the binary treatments of heavy metals, EC50 was the lowest in the Cd + Zn, whereas, the highest in the Zn + Ni. Based on both IC50 and EC50 values for the binary culture of bacteria with the binary mixtures of heavy metals, the most interactive effect was found to be antagonistic, though the only synergistic effect was found in Cu + Ni treatment. Therefore, our results can provide basic data on the toxic effects of heavy metals on the bacterial growth and phosphorus removal in the wastewater treatment process.

In vitro anti-cancer activity of hydrophobic fractions of Sparassis latifolia extract using AGS, A529, and HepG2 cell lines (꽃송이버섯(Sparassis latifolia) 추출물 소수성 분획의 항암 활성)

  • Choi, Moon-Hee;Han, Hyo-Kyung;Lee, Yong-Jo;Jo, Han-Gyo;Shin, Hyun-Jae
    • Journal of Mushroom
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    • v.12 no.4
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    • pp.304-310
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    • 2014
  • The use of mushrooms has immense potential in many diverse applications. Until now, more than 3,000 species are consumed around the world, and more than 100 have shown promising clinical activity against cancer and other chronic diseases. Sparassis latifolia (formerly S. crispa) is an edible mushroom that harbors ${\beta}$-glucan reported to possess immunostimulatory and anticancer properties. However there have been no reports on the anticancer activity of hydrophobic fractions of S. latifolia. In this study, the anticancer activities of S. latifolia extract and hydrophobic fractions were investigated using AGS (stomach cancer), A529 (lung cancer), and HepG2 (liver cancer) cell lines. In cytotoxicity results of A529 cells, fractions of A2, A3, A4, A6, A7, A8, A9, and A10 in all 12 fractions show low $IC_{50}$ values. For HepG2 cells, A7 fraction results in the lowest $IC_{50}$ value while A7, A8, and A11 fractions show low $IC_{50}$ values in AGS cells. S. latifolia extract lead to low cell viability in cancer cells, compared to positive control of paclitaxel. A compound with molecular weight of 181 were detected using HPLC-MS but not identified yet. As a result, the hydrophobic fractions of S. latifolia EtOH extract would be a possible candidate as natural anticancer agents in the future.

Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp. CNQ-027

  • Lee, Hyun Woo;Choi, Hansol;Nam, Sang-Jip;Fenical, William;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • v.27 no.4
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    • pp.785-790
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    • 2017
  • Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

Discovery of Epinastine-NSAID Hybrids as Potential Anti-inflammatory Agents: Synthesis and In Vitro Nitric Oxide Production Inhibitory Activity Study

  • Woo, Hyeong Ryeol;Damodar, Kongara;Lee, Yeontaek;Lim, Soon-sung;Jeon, Sung Ho;Lee, Jeong Tae
    • Journal of the Korean Chemical Society
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    • v.64 no.2
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    • pp.79-83
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    • 2020
  • A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC50) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC50), cytotoxicity concentration (CC50) and in vitro efficacy index (iEI), 6 (IC50 = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC50 = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.