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

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Anti-inflammatory Triterpenes and Glyceryl Glycosides from Kandelia candel (L.) Druce

  • Dat, Le Duc;Thao, Nguyen Phuong;Tai, Bui Huu;Luyen, Bui Thi Thuy;Yang, Seo Young;Kim, Sohyun;Koo, Jung Eun;Koh, Young Sang;Cuong, Nguyen The;Nam, Nguyen Hoai;Thanh, Nguyen Van;Kiem, Phan Van;Minh, Chau Van;Kim, Young Ho
    • Natural Product Sciences
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    • v.21 no.3
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    • pp.150-154
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    • 2015
  • Phytochemical investigation of Kandelia candel resulted in the isolation of six triterpenes (1 - 5) and two glyceryl glycosides (6 and 7) and their structures were determined by comparing the spectroscopic data with those of reported values. In present study, we described the inhibitory effects of fractions and isolated compounds from K. candel on pro-inflammatory cytokines (IL-12 p40, IL-6, and TNF-α) production in lipopolysaccharide (LPS) stimulated bone marrow-derived dendritic cells (BMDCs). Results indicated that compounds 3, 6, and 7 showed potent inhibition on IL-6 production (IC50 values at less than 0.5 μM, respectively). Meanwhile, compounds 6 and 7 exhibited strong inhibitory effects on the production of TNF-α (IC50 values of 1.7 ± 0.1 and 5.5 ± 0.2 μM). Compounds 1 and 3 were also showed the inhibitory effects on IL-12 p40 production (IC50 values of 8.9 ± 0.4 and 3.3 ± 0.1 μM, respectively).

공정변수에 따른 초전도 튜브의 전기적 특성변화

  • Park, C.W.;Jang, G.E.;Ha, D.W.;Seung, T.H.
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2004.11a
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    • pp.73-76
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    • 2004
  • High-temperature Superconductor(HTS) tubes were fabricated in term of different processing variables such as preheating temperature, speed of mold rotation and cooling rate by centrifugal forming method. For powder melting by induction the optimum range of melting temperatures and preheating temperature were $1050^{\circ}C{\sim}1100^{\circ}C$ and $550^{\circ}C$ for 30min, respectively. The mould roating speed was 1000rpm. A tube was annealed at $840^{\circ}C$ for 72hours in oxygen atmosphere. The plate-like grains were well developed along the roating direction and typical grain size was about more than $40{\mu}m$. It was found that Ic values increased with increasing the preheating temperature and speed of mold rotation. While Ic decreased with increasing the cooling rate. The measured Ic in $50mm{\times}70mm{\times}2.5mm$ tube was about 896Amp.

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Electrical Characteristics of HIS Tube Depending on Processing Parameters (공정변수에 따른 초전도 튜브의 전기적 특성)

  • Park, Chi-Wan;Jang, Gun-Eik;Ha, Dong-Woo;Seung, Tae-Hyun
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.18 no.5
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    • pp.468-472
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    • 2005
  • High-temperature Superconductor(HTS) tubes were fabricated in term of different processing variables such as preheating temperature, speed of mold rotation and cooling rate by centrigugal forming method. For powder melting by induction the optimum range of melting temperatures and preheating temperature were $1050{\circ}C{\sim}1100{\circ}C\;and\;550{\circ}C\;for\;30\; min$, respectively The mould roating speed was 1000 rpm. A tube was annealed at $840 {\circ}C$ for 72 hours in oxygen atmosphere. The plate-like grains were well developed along the loafing direction and typical grain size was about more than $40{\mu}$. It was found that Ic values increased with increasing the Preheating temperature and speed of mold rotation. While Ic decreased with increasing the cooling rate. The measured Ic in $50mm{\times}70mm{\times}2.5mm$ tube was about 896 Amp.

In Vitro Antioxidant and Antiproliferative Activities of Novel Orange Peel Extract and It's Fractions on Leukemia HL-60 Cells

  • Diab, Kawthar AE;Shafik, Reham Ezzat;Yasuda, Shin
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.16
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    • pp.7053-7060
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    • 2015
  • In the present work, novel orange peel was extracted with 100%EtOH (ethanol) and fractionated into four fractions namely F1, F2, F3, F4 which were eluted from paper chromatographs using 100%EtOH, 80%EtOH, 50%EtOH and pure water respectively. The crude extract and its four fractions were evaluated for their total polyphenol content (TPC), total flavonoid content (TFC) and radical scavenging activity using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Their cytotoxic activity using WST assay and DNA damage by agarose gel electrophoresis were also evaluated in a human leukemia HL-60 cell line. The findings revealed that F4 had the highest TPC followed by crude extract, F2, F3 and F1. However, the crude extract had the highest TFC followed by F4, F3, F2, and F1. Depending on the values of $EC_{50}$ and trolox equivalent antioxidant capacity, F4 possessed the strongest antioxidant activity while F1 and F2 displayed weak antioxidant activity. Further, incubation HL-60 cells with extract/fractions for 24h caused an inhibition of cell viability in a concentration-dependent manner. F3 and F4 exhibited a high antiproliferative activity with a narrow range of $IC_{50}$ values ($45.9-48.9{\mu}g/ml$). Crude extract exhibited the weakest antiproliferative activity with an $IC_{50}$ value of $314.89{\mu}g/ml$. Analysis of DNA fragmentation displayed DNA degradation in the form of a smear-type pattern upon agarose gel after incubation of HL-60 cells with F3 and F4 for 6 h. Overall, F3 and F4 appear to be good sources of phytochemicals with antioxidant and potential anticancer activities.

Acetolactate Synthase Activity Inhibition and Herbicidal Activity of Sulfonylurea and Imidazolinone Herbicides (Sulfonylurea 및 imidazolinone계 제초제(除草劑)의 살초작용(殺草作用)과 acetolactate synthase 활성(活性) 억제작용(抑制作用))

  • Hwang, I.T.;Hong, K.S.;Cho, K.Y.
    • Korean Journal of Weed Science
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    • v.15 no.1
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    • pp.54-62
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    • 1995
  • Acetolactate synthase activity inhibition and herbicidal activities were investigated with 2 sulfonylureas [chlorsulfuron{2-chloro-N-{{(4-methoxy-6-methyl-1,3,5-triazin-2-yl) amino} carboxyl} benzenesulfonamide}, metsulfuron-methyl{methyl-2{{{{(4-methoxy-6-methyl-1,3,5-triazin-2-yl)amino}carbonyl}amino}sulfonyl}benzoic acid}, and 2 imidazoli-nones [imazethapyr{2-{4,5-dihydro-4-methyl-4-(1-methyl)-5-oxo-1H-imidazol-2-yl}-5-ethyl-3-pyridinecarboxylicacid}, imazaquin{2-{4,5-dihydro-4-methyl-4-(1-methyl)-5-oxo-1H-imidazol-2-yl}-3-quinoline carboxylic acid} herbicides. A broad weeding spectrum was observed with the treated herbicides at low application rates. Both corn(Zea mays L.) and sorghum(Sorghum bicolor Moench) were very sensitive to the two herbicide groups. Although legumes, such as soybean(Glycine max Merr.), clover(Trifolium repense L.), and indian jointvetch(Aeschnomene indica L.) were sensitive to the sulfonylureas, they were tolerant to the imidazolinones. On the contrary, wheat(Triticum aestivum L.) and barley(Hoderum sativum Jess.) showed the reverse responses of the legumes to the two herbicide groups. Quackgrass(Agropyron repens(L.) P. Beauv.). however, was commonly tolerant to the two herbicide groups. Degrees of crop injury and acetolactate synthase inhibition also varied with the crops examined. The 50% inhibition concentrations of sulfonylureas on acetolactate synthase in vitro activity($IC_{50}$) from corn, wheat, and soybean did not relate to the greenhouse herbicidal activities ($GI_{50}$). With chlorsulfuron, for example, wheat had more than 100 times higher $GI_{50}$ than corn and soybean, but the $IC_{50}$ was 4 to 10 times lower. Similar observation was made with metsulfuron-methyl. However, closer relationships between $IC_{50}$ and $GI_{50}$ were found with the imidazolinones. When imazethapyr was applied, the order of $GI_{50}$ values against com, wheat, and soybean was the same as that of $IC_{50}$.

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Secondary Metabolites with Anti-complementary Activity from the Stem Barks of Juglans mandshurica Maxim

  • Li, Zi-Jiang;Chen, Shilin;Yang, Xiang-Hao;Wang, Rui;Min, Hee-Jeong;Wu, Lei;Si, Chuan-Ling;Bae, Young-Soo
    • Journal of the Korean Wood Science and Technology
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    • v.46 no.2
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    • pp.118-124
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    • 2018
  • Juglans mandshurica is a fast growing hard species, which is a tree in family of Juglandaceae and has a wide distribution in China, Korea and eastern Russia. Plant materials from J. mandshurica have extensively been used in folk medicines to prevent or cure gastric, esophageal, lung and cardiac cancer. As one chain of our searching for anticomplementary agents from natural sources, two epimeric ellagitannins, [2,3-O-4,4',5,5',6,6',-hexahydroxydiphenoyl (HHDP))-(${\alpha},{\beta}$)-D-glucose] (I) and pedunculagin (II) were purified from 70% acetone extracts of the stem barks of J. mandshurica by Thin Layer Chromatography and Sephadex LH-20 column chromatography approaches. The chemical structures of the isolated compounds were characterized by MS, NMR, and a careful comparation with published literatures. The epimeric ellagitannins I and II exhibited inhibitory properties against a classical pathway of complementary system with 50 % inhibitory concentrations ($IC_{50}$) values of 65.3 and $47.7{\mu}M$, respectively, comparing with riliroside ($IC_{50}=104{\mu}M$) and rosmarinic acid ($IC_{50}=182{\mu}M$), which were used as positive controls. Thus, the work indicated both the two secondary metabolites possess excellent inhibitory activity and might be developed as potential anticomplementary chemicals.

Anti-Proliferation Effects of Benzimidazole Derivatives on HCT-116 Colon Cancer and MCF-7 Breast Cancer Cell Lines

  • Al-Douh, Mohammed Hadi;Sahib, Hayder B.;Osman, Hasnah;Hamid, Shafida Abd;Salhimi, Salizawati M.
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.8
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    • pp.4075-4079
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    • 2012
  • Benzimidazoles 1-4 were obtained using modified synthesis methods and studied for their ability to inhibit cell proliferation of colon cancer cell HCT-116 and breast cancer cell MCF-7 using MTT assays. In the HCT-116 cell line, benzimidazole 2 was found to have an $IC_{50}$ value of $16.2{\pm}3.85{\mu}g/mL$ and benzimidazole 1 a value of $28.5{\pm}2.91{\mu}g/mL$, while that for benzimidazole 4 was $24.08{\pm}0.31{\mu}g/mL$. In the MCF-7 cell line, benzimidazole 4 had an $IC_{50}$ value of $8.86{\pm}1.10{\mu}g/mL$, benzimidazole 2 a value of $30.29{\pm}6.39{\mu}g/mL$, and benzimidazole 1 a value of $31.2{\pm}4.49{\mu}g/mL$. Benzimidazole 3 exerted no cytotoxity in either of the cell lines, with $IC_{50}$ values $>50{\mu}g/mL$. The results suggest that benzimidazoles derivatives may have chemotherapeutic potential for treatment of both colon and breast cancers.

Synthesis of New Boron Derived Compounds; Anticancer, Antioxidant and Antimicrobial Effect in Vitro Glioblastoma Tumor Model

  • Koldemir-Gunduz, Meliha;Aydin, Hasan Emre;Berikten, Derya;Kaymak, Gullu;Kose, Dursun Ali;Arslantas, Ali
    • Journal of Korean Neurosurgical Society
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    • v.64 no.6
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    • pp.864-872
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    • 2021
  • Objective : The aim of our study is to investigate the cytotoxic, antioxidant, and antimicrobial effects of newly synthesized boron compounds in U87MG glioblastoma cell treatment. Methods : We synthesized boron glycine monoester (BGM) and boron glycine diester (BGD) structures containing boron atoms and determined their cytotoxic activities on glioblastoma by the MTT method. The inhibitory concentration 50 (IC50) value was calculated with GraphPad Prism 5.0 program. The IC50 values were administered 48 hours on U87MG glioblastoma cell. Catalase (CAT), acid phosphatase (ACP) and alkaline phosphatase (ALP) enzyme activity, malondialdehyde (MDA), total glutathione (GSH), and total protein levels were detected using spectrophotometric methods. We determined the antimicrobial activities of BGM and BGD with the disc diffusion method. Results : After 48 hours of BGM and BGD application to U87MG glioblastoma cells, we found the IC50 value as 6.6 mM and 26 mM, respectively. CAT and ACP enzyme activities were decreased in BGM and BGD groups. MDA which is a metabolite of lipid peroxidation was increased in both boron compounds groups. GSH level was reduced especially in BGD group. BGM and BGD have been found to be antimicrobial effects. Conclusion : Boron compounds, especially the BGM, can provide a new therapeutic approach for the treatment of glioblastoma with their anticancer, antioxidant, and antimicrobial effects.

Antioxidant and Tyrosinase Inhibitory Activities from Seed Coat of Brown Soybean

  • Lee, Jin-Hwan;Baek, In-Youl;Ko, Jong-Min;Kang, Nam-Suk;Shin, Seong-Hyu;Lim, Sea-Gyu;Oh, Ki-Won;Shin, Sang-Ouk;Park, Keum-Yong;Park, Ki-Hun;Ha, Tae-Joung
    • Food Science and Biotechnology
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    • v.17 no.1
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    • pp.1-7
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    • 2008
  • Soybeans with brown, black, and yellow seed coats were compared to total phenolic contents and antioxidant activities including 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radicals. Also, 3 seed coats were examined for inhibitory activities on tyrosinase and lipoxygenase-1 on the basis of spectrophotometric and polarographic methods. Among seed coat extracts, 80% methanol extract of brown soybean seed coat showed the highest total phenolic contents ($68.9{\pm}3.29\;mg$ GAE/g) as well as exhibited potent scavenging effects on the DPPH ($IC_{50}=4.3\;{\mu}g/mL$) and ABTS ($IC_{50}=3.7\;{\mu}g/mL$) radicals. In a polarographic experiment, this extract was potentially inhibited the oxidation of L-tyrosine and L-3,4-dihydroxy-phenylalanin (L-DOPA) catalyzed by mushroom tyrosinase with $IC_{50}$ values of 12.4 and $63.7\;{\mu}g/mL$, respectively. It was also detected inhibition of the tyrosinase catalyzed oxidation of L-DOPA with an $IC_{50}$ value of 120.3 mg/mL in UV spectrophotometric experiment. In addition, this extract inhibited the linoleic acid peroxidation catalyzed by lipoxygenase-1 with an $IC_{50}$ value of $4.0\;{\mu}g/mL$. These results suggest that brown soybean may possess more beneficial effect on human health than black and yellow soybeans.

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.