• Title/Summary/Keyword: IC values

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A New Histone Deacetylase Inhibitor, MHY4381, Induces Apoptosis via Generation of Reactive Oxygen Species in Human Prostate Cancer Cells

  • Richa, Sachan;Dey, Prasanta;Park, Chaeun;Yang, Jungho;Son, Ji Yeon;Park, Jae Hyeon;Lee, Su Hyun;Ahn, Mee-Young;Kim, In Su;Moon, Hyung Ryong;Kim, Hyung Sik
    • Biomolecules & Therapeutics
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    • v.28 no.2
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    • pp.184-194
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    • 2020
  • Histone deacetylase (HDAC) inhibitors represent a novel class of anticancer agents, which can be used to inhibit cell proliferation and induce apoptosis in several types of cancer cells. In this study, we investigated the anticancer activity of MHY4381, a newly synthesized HDAC inhibitor, against human prostate cancer cell lines and compared its efficacy with that of suberoylanilide hydroxamic acid (SAHA), a well-known HDAC inhibitor. We assessed cell viability, apoptosis, cell cycle regulation, and other biological effects in the prostate cancer cells. We also evaluated a possible mechanism of MHY4381 on the apoptotic cell death pathway. The IC50 value of MHY4381 was lower in DU145 cells (IC50=0.31 µM) than in LNCaP (IC50=0.85 µM) and PC-3 cells (IC50=5.23 µM). In addition, the IC50 values of MHY4381 measured in this assay were significantly lower than those of SAHA against prostate cancer cell lines. MHY4381 increased the levels of acetylated histones H3 and H4 and reduced the expression of HDAC proteins in the prostate cancer cell lines. MHY4381 increased G2/M phase arrest in DU145 cells, and G1 arrest in LNCaP cells. It also activated reactive oxygen species (ROS) generation, which induced apoptosis in the DU145 and LNCaP cells by increasing the ratio of Bax/Bcl-2 and releasing cytochrome c into the cytoplasm. Our results indicated that MHY4381 preferentially results in antitumor effects in DU145 and LNCaP cells via mitochondria-mediated apoptosis and ROS-facilitated cell death pathway, and therefore can be used as a promising prostate cancer therapeutic.

Quantifying the Interactive Inhibitory Effect of Heavy Metals on the Growth and Phosphorus Removal of Pseudomonas taeanensis

  • Yoo, Jin;Kim, Deok-Hyun;Oh, Eun-Ji;Chung, Keun-Yook
    • Korean Journal of Soil Science and Fertilizer
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    • v.51 no.1
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    • pp.35-49
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    • 2018
  • This study was initiated to quantitatively evaluate the effects of five heavy metals (Cd, Cu, Zn, Pb, and Ni) on growth and P removal efficiencies of Pseudomonastaeanensis, known as the phosphorus accumulating microorganism. The heavy metals were added individually and with the binary mixture to the batch culturing system of Pseudomonastaeanensis. $IC_{50}$ and $EC_{50}$ were used to quantitatively evaluate their effects on the growth and phosphorus removal efficiency of Pseudomonas taeanensis in those treatments. Additionally, additive index value method was used to evaluate the interactive effects of heavy metals for Pseudomonas taeanensis in this study. As those heavy metals were singly added to Pseudomonastaeanensis, the greatest inhibitory effect on its growth and P removal efficiency was observed in Cd, whereas, the smallest effect was found in Ni. As the concentrations of all heavy metals added were gradually increased, its growth and P removal efficiency was correspondingly decreased. Specifically, $IC_{50}$ of Pseudomonas taeanensis for Cd, Cu, Zn, Pb, and Ni were $0.44mg\;L^{-1}$, $5.12mg\;L^{-1}$, $7.46mg\;L^{-1}$, $8.37mg\;L^{-1}$ and $14.56mg\;L^{-1}$, respectively. The P removal efficiency of Pseudomonas taeanensis was 81.1%. $EC_{50}$ values of Pseudomonas taeanensis for Cd, Cu, Zn, Pb, and Ni were $0.44mg\;L^{-1}$, $4.08mg\;L^{-1}$, $7.17mg\;L^{-1}$, $8.90mg\;L^{-1}$ and $11.26mg\;L^{-1}$, respectively. In the binary treatments of heavy metals, the lowest $IC_{50}$ and $EC_{50}$ were found in the Cd + Cu treatment, whereas, the highest $IC_{50}$ and $EC_{50}$ were found in the Zn + Pb and Pb + Ni treatments, respectively. Most of the interactive effects for the binary mixture treatments of heavy metals were antagonistic. Based on the results obtained from this study, it appears that they could provide the basic information about the toxic effects of the respective individual and binary treatments of heavy metals on the growth and P removal efficiency of other phosphorus accumulating organisms.

The Physiological Activities of Bark Extract of Albizia julibrissin (자귀나무(A. julibrissin) 수피 추출물의 생리활성)

  • Lee, Yang-Suk;Kim, Kwang-Kon;Kim, Nam-Woo
    • Food Science and Preservation
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    • v.18 no.1
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    • pp.79-86
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    • 2011
  • Three bark extracts of Albizia julibrissin were prepared using water (AW), 70% (v/v) ethanol (AE), and hot water (AHW). Organic solvent fractions were analyzed for total flavonoids and polyphenols, antioxidant activities, and inhibitory activities against xanthine oxidase. Total flavonoid and polyphenol contents of the AHW extract were 8.57 mg/g and 108.67 mg/g, respectively. The SOD-like activities of all extracts, assayed at 1.0 mg/mL, were 10.46-16.73%. The nitrite-scavenging ability of the AHW extract, assayed at pH 1.2, was 60.82%, and the $IC_{50}$ value was $770.18\;{\mu}g$/mL. The electron-donating ability of the AHW extract, at 0.3 mg/mL, was 92.30%; the $IC_{50}$ values of the AW and AHW extracts were $31.31\;{\mu}g$/mL and $36.22\;{\mu}g$/mL, respectively; thus higher than that of ascorbic acid ($39.06\;{\mu}g$/mL). Xanthine oxidase inhibition by the AHW extract, at 1.0 mg/mL, was 94.05%. These results indicate that the AHW of A. julibrissin has potential as a natural antioxidant, for addition to foods and nutraceuticals.

Screening of $\alpha$-amylase and $\alpha$-glucosidase Inhibitors from Brazilian Plant Extracts for Treatment of Rumen Acidosis (100종 브라질 식물 추출물로부터 반추동물 산독증 예방치료를 위한 $\alpha$-amylase 및 $\alpha$-glucosidase 저해제의 선별)

  • Kim, Mi-Sun;An, Seon-Mi;Jung, In-Chang;Kwon, Gi-Seok;Sohn, Ho-Yong
    • Food Science and Preservation
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    • v.17 no.2
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    • pp.290-296
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    • 2010
  • To develop anti-acidosis and anti-diabetes agentsfrom natural products, the inhibitory activities of Brazilian plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among 100 different ethanol extracts tested, those of Acacia jurema Mart., Anacardium humile A. St.-Hil., Cedrela odorata L., and Guazuma ulmifolia Lam showed good inhibitoryactivities toward both enzymes. In addition, an extract of Plumeria drastica Mart. showed specific inhibition of $\alpha$-amylase, whereas that of Eugenia uniflora L. demonstrated strong inhibition of the enzyme. IC50 values of $\alpha$-amylase inhibition suggested that the extract of A. humile A. St.-Hil., which has been used as an anti-diabetes medicine in Brazil, had potent inhibitory activity. The IC50 for the A. humile A. St.-Hil. extract ($91.2{\mu}g/mL$) was similar to that of acarbose ($50.5{\mu}g/mL$). This activity of A. humile A. St.-Hil. was not reduced by heat or acid treatment. Moreover, treatment with HCl (0.01 M) for 1 h increased the inhibitory activity from 57.5% to 81.2%. Also, the extract did not cause hemolysis of human red blood cells at levels up to 1 mg/mL. The results indicate that the extract of A. humile A. St.-Hil. is potentially useful as an anti-acidosis and anti-diabetes agent.

Anti-Oxidative and Inhibitory Effect of Saussurea involucrata on MMP-1 in UVA-irradiated Human Dermal Fibroblast (설련의 항산화능와 사람 섬유아세포에서 UVA에 의한 MMP-1발현 저해효과)

  • Sim, Gwan-Sub;Kim, Jin-Hwa;Na, Young;Lee, Dong-Hwan;Lee, Bum-Chun;Zhang, Yong-He;Pyo, Hyeong-Bae
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.4 s.54
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    • pp.329-335
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    • 2005
  • In order to investigate the effects of Saussurea involucrata on (relationship between) aging (and Saussurea involucrata), we examined the activities of antioxidation, in vitro MMP inhibition and UVA-induced MMP-1 expression in human dermal fibroblasts. S. involucrata showed scavenging activities radicals and reactive oxygen species (ROS) with the $IC_{50}$ values of $3.89{\mu}g/mL$ against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and $67.29{\mu}g/mL$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. At the concentration of $1000{\mu}g/mL$, S. involucrata showed 93.27% inhibition on lipid peroxidation of linoleic acid. S. involucrata inhibited the activities of MMP-1 in a does-dependent manner and the $IC_{50}$ value calculated from semi-log plots was $97.18{\mu}g/mL$. Also, UVA induced MMP expression in human dermal fibroblasts was reduced 42.86% by treatment with S. involucrata, and MMP-1 mRNA expression was reduced in a dose-dependent manner. Therefore S. involucrata was able to significantly inhibit MMP expression in protein and mRNA level. All these results suggested that S. involucrata might act as an anti-aging agent by antioxidation and reducing UVA-induced MMP-1 production.

Pancreatic Lipase Inhibitors Isolated from the Leaves of Cultivated Mountain Ginseng (Panax ginseng) (산양삼 잎으로부터 Pancreatic lipase 저해 활성물질의 분리)

  • Hong, Ju-Yeon;Shin, Seung-Ryeul;Bae, Man-Jong;Bae, Jong-Sup;Lee, In-Chul;Kwon, O-Jun;Jung, Ji-Wook;Kim, Yong-Han;Kim, Tae-Hoon
    • Food Science and Preservation
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    • v.17 no.5
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    • pp.727-732
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    • 2010
  • Activity-guided fractionation of an ethyl acetate (EtOAc)-soluble portion of an ethanolic extract from the leaves of cultivated mountain ginseng, using pancreatic lipase inhibition assay, led to the isolation and identification of three flavonoids of a previously described structure, kaempferol-3-O-sophoroside (I), kaempferol-3-O-${\beta}$-Dglucopyranoside (astragalin, II) and kaempferol (III). All compounds (I.III) showed pancreatic lipase inhibitory activities, with $IC_{50}$ values ranging from $20.3{\pm}2.2$ to $9.1{\pm}1.5$ ${\mu}M$, kaempferol (III) showed the most potent inhibitory activity with an $IC_{50}$ of $9.1{\pm}1.5$ ${\mu}M$. The level of activity may depend on the number of C-3 glucosyl group(s) linked to the kaempferol backbone, and the isolated compounds may have promise as pancreatic lipase inhibitors.

Dietary Iron Intake of Koreans Estimated using 2 Different Sources of Iron Contents are Comparable: Food & Nutrient Database and Iron Contents of Cooked Foods in the Korean Total Diet Study (우리 국민의 철 섭취량 평가: 식품별 영양성분 함량자료와 한국형 총식이조사 기반 추정량 비교)

  • Lee, Jeeyeon;Kwon, Sung Ok;Yeoh, Yoonjae;Seo, Min Jeong;Lee, Gae Ho;Kim, Cho-il
    • Korean Journal of Community Nutrition
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    • v.27 no.3
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    • pp.245-253
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    • 2022
  • Objectives: This study was conducted to find out if the dietary iron intake of Koreans estimated by 2 different methods (iron content sources) using the food intake data from the Korea National Health and Nutrition Examination Survey (KNHANES) are comparable. One method was based on the KNHANES's Food & Nutrient Database (FND) derived mainly from the Korean Food Composition Table and the other used the iron content (IC) of food samples processed in the Korean Total Diet Study (KTDS). Methods: Dietary intake data from the 2013-2016 KNHANES was used to select representative foods (RFs) in KTDS for iron analysis. Selection of the RFs and cooking methods for each RF (RF × cooking method pair) was performed according to the 'Guidebook for Korean Total Diet Studies' and resulted in a total of 132 RFs and 224 'RF × cooking method' pairs. RFs were collected in 9 metropolitan cities nationwide once or twice (for those with seasonality) in 2018 and made into 6 composites each, based on the origin and season prior to cooking. Then, the RF composites prepared to a 'table ready' state for KTDS were analyzed by Inductively Coupled Plasma-Mass Spectrometry (ICP-MS). Dietary iron intake of the Korean population was estimated using only RFs' intake data based on the 2 sources of iron content, namely FND-KNHANES and IC-KTDS. Results: RFs in KTDS covered 92.0% of total food intake of Koreans in the 2016-2018 KNHANES. Mean iron intake of Koreans was 7.77 mg/person/day by IC-KTDS vs 9.73 mg/person/day by FND-KNHANES. The major food groups contributing to iron intake were meats (21.7%), vegetables (20.5%), and grains & cereals (13.4%) as per IC-KTDS. On the other hand, the latter source (FND-KNHANES) resulted in a very different profile: grains & cereals (31.1%), vegetables (16.8%), and meats (15.3%). While the top iron source was beef, accounting for 8.6% in the former, it was polished rice (19.2%) in the latter. There was a 10-fold difference in the iron content of polished rice between 2 sources that iron intakes excluding the contribution by polished rice resulted in very similar values: 7.58 mg/person/day by IC-KTDS and 7.86 mg/person/day by FND-KNHANES. Conclusions: This study revealed that the dietary iron intake estimated by 2 different methods were quite comparable, excluding one RF, namely polished rice. KTDS was thus proven to be a useful tool in estimating a 'closer-to-real' dietary intake of nutrients for Koreans and further research on various nutrients is warranted.

Antioxidant and Free Radical Scavenging Potential of Justicia gendarussa Burm. Leaves in vitro.

  • Mruthunjaya, K.;Hukkeri, V.I.
    • Natural Product Sciences
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    • v.13 no.3
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    • pp.199-206
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    • 2007
  • Antioxidant activity of 70% aqueous ethanolic extract of leaves of Justicia gendarussa (EJ) was evaluated. EJ was prepared by cold maceration method. The antioxidant potency of EJ was investigated employing various established in vitro systems, such as DPPH radical scavenging, nitric oxide (NO) scavenging, ${\beta}-carotene$ linoleic acid module system (${\beta}$ CLAMS), hydroxyl (OH) radical scavenging, anti lipid peroxidation. $IC_{50}$ values were determined in each experiment. Also, ferric ion reduction capacity of extracts in presence and absence of chelating agent (EDTA) and total antioxidant capacity were determined. Preliminary phytochemical investigation was carried out to know the nature of constituents present in the leaves and correlate it with antioxidant activity. Further total phenolic content was determined in EJ. $IC_{50}$ values of EJ were 123.09 ${\pm}$ 3.01, 643.0 ${\pm}$ 61.10, 132.3 ${\pm}$ 6.03, 68.5 ${\pm}$ 11.5 and 68.13 ${\pm}$ 1.38 ${\mu}g/mL$ in DPPH radical scavenging, NO scavenging, ${\beta}$ CLAMS, OH radical scavenging and anti lipid peroxidation activity respectively. In total antioxidant capacity assay, ascorbic acid equivalent value was found to be 205.56 ${\pm}$ 4.69 ${\mu}g/mg$ of extract. Total phenolic content was found to be 43.76 ${\pm}$ 4.27 ${\mu}g$ equivalent of gallic acid per mg of extract. Phytochemical investigation reveals the presence of flavonoids. The results indicate that EJ possess antioxidant activity and flavonoids are responsible for this activity.

Inhibition of NF-IL6 Activity by Manassantin B, a Dilignan Isolated from Saururus chinensis, in Phorbol Myristate Acetate-stimulated U937 Promonocytic Cells

  • Son, Kyung-No;Song, In-Sung;Shin, Yong-Hyun;Pai, Tong-Kun;Chung, Dae-Kyun;Baek, Nam-In;Lee, Jung Joon;Kim, Jiyoung
    • Molecules and Cells
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    • v.20 no.1
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    • pp.105-111
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    • 2005
  • Mannasantin B, a dilignan structurally related to manssantin A, is an inhibitor of NF-${\kappa}B$ transactivation. In the present study, we found that it inhibited PMA-induced expression of IL-$1{\beta}$, IL-$1{\beta}$ mRNA, and IL-$1{\beta}$ promoter activity in U937 cells with $IC_{50}$ values of about 50 nM. It also inhibited NF-IL6- and NF-${\kappa}B$-induced activation of IL-$1{\beta}$, with $IC_{50}$ values of 78 nM and $1.6{\mu}M$, respectively, revealing a potent inhibitory effect on NF-IL6. Electrophoretic mobility shift assays showed that manassantin B had an inhibitory effect on DNA binding by NF-IL6, but not by NF-${\kappa}B$. Further analysis revealed that transactivation by NF-IL6 was also inhibited. Our results indicate that manassantin B suppresses expression of IL-$1{\beta}$ in promonocytic cells by inhibiting not only NF-${\kappa}B$ but also NF-IL6 activity. Furthermore, our observations suggest that manassantin B may be clinically useful as a potent inhibitor of NF-IL6 activity.

A Design of Advanced Channel Creation in e-Passport (전자여권의 향상된 채널생성 기법 설계)

  • Lee, Gi-Sung;Jeon, Sang-Yeob;Jun, Moon-Seog
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.13 no.10
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    • pp.4814-4821
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    • 2012
  • An e-passport is equipped with bio information by adding the non-attachable IC chip with a smart function. In order to solve such a problem, the user's privacy is protected by using the BAC, PA, AA and EAC mechanisms. However, the password key used in the BAC mechanism is made of the combination of the MRZ values. As a result, it is possible to decode the password by using the indiscriminate attacking program after finding out the combined rules of MRZ. This thesis suggests the mechanism with an improved level of efficiency through the time-stamp values by using the information of images and fingerprints and checking the forge or falsification of the e-passport when establishing a safe channel between the chip of the e-passport and the decoding system.