• Title/Summary/Keyword: $IC_50$

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In Vitro Screening of the Physiological Activities of lshige foliacea Extracts (넓패(Ishige foliacea) 추출물의 생리활성 탐색)

  • Ji-Youn Kim;Da-Bin Park;Min-Gyeom Kim;Sun Joo Park;Yong-Tae Kim
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.57 no.3
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    • pp.209-215
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    • 2024
  • Ishige foliacea belongs to class Phaeophyceae and family Ishigeaceae. This study investigated the physiological activities of the Korean marine algae I. foliacea. Its solvent extracts were prepared with 70% ethanol, 80% methanol, and distilled water. The ethanol and methanol extracts had higher α-glucosidase (half-maximal inhibitory concentration, IC50: 0.67-0.73 mg/mL), xanthine oxidase (IC50: 0.25-0.28 mg/mL), and angiotensin-converting enzyme (IC50: 25.29-38.28 ㎍/mL) inhibitory activities than those of the water extract. The ethanol and methanol extracts possessed high acetylcholinesterase inhibitory activity (IC50: 0.78c0.97 mg/mL). Conversely, the water extract exhibited the highest β-secretase inhibitory activity (IC50: 0.48 mg/mL). These results indicate that I. foliacea may be useful as a functional substance in food and pharmaceuticals with anti-diabetic, anti-gout, anti-hypertension, and anti-dementia properties.

Cytotoxicity and Chemosensitizing Effect of Camellia(Camellia japonica) Tea Extracts (동백엽차와 화차의 세포독성 및 다제내성 극복효과)

  • 황은주;차영주;박민희;이장원;이숙영
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.3
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    • pp.487-493
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    • 2004
  • This study has been undertaken to increase availability of native camellia in Jeonnam as a medicinal resource and to isolate the effective components from them. Fresh leaf and flower of camellia, single camellia tea and camellia tea mixed with green tea, herbs were screened for cytotoxicity on MCF -7 (human breast adenocarcinoma pleual effusion), Calu-6 (human pulmonary carcinoma), SNU-601 (human gastric carcinoma) cells. Also their multidrug-resistance reversing activity were evaluated using drug sensitive AML-2/WT and multidrug-resistant AML-2/D100 cells. Among the camellia extracts, young leaf and camellia tea mixed with green tea had strong growth inhibitory effects in below 100 $\mu\textrm{g}$/mL against human cancer cells. In result, young leaf showed the strongest inhibitory effects on MCF -7 ($IC_{50}$/ = 100 $\mu\textrm{g}$/mL ↑), Calu-6 ($IC_{50}$/ = 79 $\mu\textrm{g}$/mL), and SNU -601 ($IC_{50}$/ = 39 $\mu\textrm{g}$/mL), and AML-2/WT ($IC_{50}$/ = 64 $\mu\textrm{g}$/mL). Chemosensitizing effect was the extracts of mature leaf ($IC_{50}$/ = 97 $\mu\textrm{g}$/mL, RF=3.0), roasted tea ($IC_{50}$/ = 76 $\mu\textrm{g}$/mL, RF = 2.6 ↑) and steam tea ($IC_{50}$/ = 70 $\mu\textrm{g}$/mL, RF=2.8 ↑) strongly potentiate vincristine cytotoxicity in AML-2/D100 cells. But their cytotoxicities to both sensitive AML-2/WT and resistant AML-2/D100 cells were in the same order of magnitude. This results indicate that crude extracts of camellia mature leaves would contain some principles which have chemosensitizing activity.

Effect of Sodium Caseinate Hydrolysates on Angiotensin-I Converting Enzyme Inhibition Activity (Sodium Caseinate 가수분해물의 Angiotensin-I Converting Enzyme 저해효과에 관한 연구)

  • Lee, Keon-Bong;Shin, Yong-Kook;Baick, Seung-Chun
    • Food Science of Animal Resources
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    • v.32 no.5
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    • pp.652-658
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    • 2012
  • This study was carried out to identify the ACE (Angiotensin converting enzyme) inhibitory activity of casein hydrolysates for development of anti-hypertensive hydrolysates. Sodium caseinate was treated with six kinds of commercial proteases such as Flavourzyme, Protamex, Neutrase 1.5, Alcalase, Protease M, and Protease S for 8 h individually, and was then treated with the enzyme combination for 4 h at $45^{\circ}C$. The hydrolysate which had the highest ACE inhibitory effect was then hydrolysed successively with three digestive enzymes: pepsin, trypsin, and ${\alpha}$-chymotrypsin, at $37^{\circ}C$ for 4 h under conditions mimicking those of the gastrointestinal tract. UF (ultra filtration) treatment was applied to one of the secondary hydrolysates to determine ACE inhibitory activity. When sodium caseinate was hydrolysed by commercial proteases, the degree of hydrolysis (DH) showed 2.54 to 4.25% and after secondary hydrolysis, DH showed 4.30 to 5.22%. ACE inhibitory activity and $IC_{50}$ values decreased, and inhibition rates increased during hydrolysis. Protamex treatment showed the lowest $IC_{50}$ value ($516{\mu}g/mL$) and Flavourzyme hydrolysate showed the highest $IC_{50}$value ($866{\mu}g/mL$). As the first hydrolysate was treated with Flavourzyme, the ACE inhibitory activity increased. Neutrase hydrolysate had the highest activity with an $IC_{50}$ value ($282{\mu}g/mL$). When Neutrase plus Flavourzyme treatment was hydrolyzed by digestive enzymes, the $IC_{50}$ value ($597{\mu}g/mL$) was decreased statistically (p<0.05). As Neutrase plus Flavourzyme hydrolysate is treated by UF with MW cut-off 10,000, permeate showed $273{\mu}g/mL$ of $IC_{50}$ value, showed no difference, but retentate which has over MW 10,000 showed statistically different $IC_{50}$ value, $635{\mu}g/mL$ (p<0.05).

Correlation Between Skin Irritation and Cytotoxicity of Anti-wrinkle Agents (화장품 원료의 피부자극성과 세포독성의 관련성)

  • 이은희;이종권;김용규;박기숙;안광수
    • YAKHAK HOEJI
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    • v.45 no.3
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    • pp.310-319
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    • 2001
  • To compare skin irritation and cytotoxicity of anti-wrinkle agents, we examined skin irritation of six anti-wrinkle agents (ascorbic acid, glycolic acid, all trans-retinoic acid, ginseng extract, retinol, EB) in New Zealand white rabbit. Cytotoxicity of these agents was determined by MTT [tetrazolium salt 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] at multi-time points in cultured HaCaT cell, a human immortalized keratinocyte cell. We then analyzed correlation between skin irritation and cytotoxicity by spearman's rank correlation analysis. All trans-retinoic acid showed the highest primary irritation index (0.92) in skin irritation test. Being all the six agents not irritant, retinal showed the most cytotoxic agents. The correlation between skin irritation and cytotoxicity ($IC_{50}$/ at different time point was 0.814, 0.757, 0.814 and 0.7 at 3, 24, 48 and 72 h, respectively. We also fecund that IC$_{20}$ and IC$_{80}$ of these agents showed similar correlation with skin irritation. These results therefore demonstrated that there is close correlation between skin irritation and cytotoxicity $IC_{50}$/ value by MTT in HaCaT cell at early time points by anti-wrinkle agents or IC$_{20}$ value. $IC_{50}$/ at earily time point or IC$_{20}$ values may be reliable alternative determinant of skin irritation.n.

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1-Methyl Substituent and Stereochemical Effects of 2-Phenylcyclopropylamines on the Inhibition of Rat Brain Mitochondrial Monoamine Oxidase A and B

  • Kang, Gun-Il;Hong, Suk-Kil;Choi, Hee-Kyung
    • Archives of Pharmacal Research
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    • v.10 no.1
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    • pp.50-59
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    • 1987
  • (E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

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Screening of Antithrombotic Peptides from Soybean Paste by the Microplate Method (Microplate법에 의한 된장유래의 항혈전 펩타이드 탐색)

  • Shon, Dong-Hwa;Lee, Kyung-Ae;Kim, Seung-Ho;Ahn, Chang-Won;Nam, Hee-Sop;Lee, Hyung-Jae;Shin, Jae-Ik
    • Korean Journal of Food Science and Technology
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    • v.28 no.4
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    • pp.684-688
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    • 1996
  • In order to search for antithrombotic peptides from soybean paste, the inhibitory activity of water extract of soybean paste and its peptide fractions on ADP-induced aggregation of washed platelets was assayed. Soybean paste extract treated with ultrafiltration (M.W. cut off, 3,000 daltons) was found to have inhibitory activity of 90% at the dose of $96\;{\mu}g/ml$ by the method of turbidometric aggregometer. Soybean paste extract was fractionated to 19 fractions (No. B-18) by Dowex 50W X-2 ion exchange column chromatography and activity test was performed by the microplate method. All of the fractions had antithrombotic activity $(IC_{50},\;101,000\;{\mu}g/ml)$, and most fractions had higher activity than positive control, RGDS $(IC_{50}.\;205\;{\mu}g/ml)$. Especially, basic fractions No.16-18 showed higher activity than soybean paste extract $(IC_{50},\;30\;{\mu}g/ml)$. The fraction No.16 with the highest activity $(IC_{50},\;10\;{\mu}g/ml)$ was purified and analysed for amino acid composition. The results showed that histidine, arginine, and alanine were major residues in the peptide part of the fraction.

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Synthesis of (5R,8R)-2-(3,8-Dimethyl-2-oxo-1,2,4,5,6,7,8,8α-octahydroazulen-5-yl) Acrylic Acid (Rupestonic Acid) Amide Derivatives and in vitro Inhibitive Activities against Influenza A3,B and Herpes Simplex Type 1 and 2 Virus

  • Yong, Jian-Ping;Lv, Qiao-Ying;Aisa, Haji Akber
    • Bulletin of the Korean Chemical Society
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    • v.30 no.2
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    • pp.435-440
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    • 2009
  • 19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a~2l, 3a~3g were synthesized and preliminarily evaluated in vitro against influenza virus $A_3$,B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus $A_3\;(TC_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;19.2\;{\mu}$mol/L, SI = 6.3) and B (T$C_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;29.9\;{\mu}$mol/L, SI = 4.0); 2g was more active against influenza $A_3$ virus at very low cytotoxicity ($TC_{50}\;>\;2092.1\;{\mu}mol/L,\;IC_{50}=\;143.7\;{\mu}mol/L,$ SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;11.3\;{\mu}mol$/L, SI = 17.7 ) and HSV-2 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;20.7\;{\mu}mol$/L , SI = 9.7).

Antioxidative Properties of Artemisia princeps Pamp (약쑥(Artemisia princeps Pamp)의 항산화작용)

  • Hong, Jung-Hee;Jeon, Jeong-Lan;Lee, Ju-Hyun;Lee, In-Seon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.36 no.6
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    • pp.657-662
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    • 2007
  • Antioxidant properties of Artemisia princeps Pamp were determined using in vitro assay systems against 1,1-diphenyl-picrylhydrazyl (DPPH) radical, superoxide ($O_2{^-}$), hydrogen peroxide ($H_2O_2$), hydroxyl radical ($HO{\cdot}$) and nitric oxide (NO) radical, as well as rat liver microsomal lipid peroxidation. Among the five solvent fractions, ethyl acetate fractions showed the highest total polyphenol and flavonoid contents at $311.35{\mu}g/mg\;and\;92.73{\mu}g/mg$, respectively. Ethyl acetate fractions, except for $H_2O_2$ scavenging activity, also showed the highest scavenging activity; the 50% inhibitory concentration ($IC_{50},\;{\mu}g/mg$) values for DPPH, superoxide, $HO{\cdot}$ and NO radical scavenging were 52.71, 26.47, 58.92 and 65.94, respectively. Additionally, the highest inhibition of rat liver microsomal lipid peroxidation was observed by ethyl a cetate fraction.

Carbofuran Cytotoxicity on Rat Fibroblast Cells and Compensation Effects of Phenobarbital Sodium and 3-Methycholanthrene on Its Toxicity (살충제 Carbofuran이 쥐의 NIH3T3 섬유모세포에 끼치는 독성 및 Phenobarbital Sodium과 3-Methylcholanthrene에 의한 보상효과)

  • Han, Seong-Soo;Rim, Yo-Sup
    • Korean Journal of Environmental Agriculture
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    • v.16 no.2
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    • pp.149-155
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    • 1997
  • This study was carried out to investigate the effects of phenobarbital sodium(PB) and 3-methylcholanthrene(3-MC) on carbofuran cytotoxicity and to develop antitoxic agents based on the effectivness. Experimental groups for carbofuran cytotoxicity were divided into five groups ; medium alone and four treatments of carbofuran (1, 25, 50 and $100{\mu}M)$, and those for compensation effects were divided into six groups ; medium alone, $IC_{50}$ carbofuran and four combinations of carbofuran and PB or 3-MC($IC_{50}$ carbofuran plus 1, 25, 50, $100{\mu}M$ of PB and 3-MC, respectively). After incubation for 48 hrs under the same conditions, MTT(Tetrazolium MTT), NR(Neutral red) and SRB(Sulforhodamine B protein) assay were performed. Fifty percentage inhibition of MTT, NR, and SRB against carbofuran in rat fibroblast cell were 60.7, 82.5 and $87.0{\mu}M$, respectively. At the combination treatments of $IC_{50}$ of carbofuran and $100{\mu}M$ of PB, the significant compensation effects were observed from the results of MTT and NR but not from that of SRB absorbance. And at the combination treatments of $IC_{50}$ of carbofuran and 3-MC, the relatively significant compensation effects were found at $50{\mu}M$ 3-MC from the results of MTT and at $100{\mu}M$ 3-MC from that of NR and SRB absorbances, respectively. From the results of light microscopy, combination treatments of $carbofuran(IC_{50})$ and PB or 3-MC showed good regeneration in carbofuran toxicity of rat fibroblast cells. These results suggest that PB or 3-MC can compensate the cytotoxity of carbofuran insecticide in rat NIH3T3 fibroblast cells.

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Effect of Antioxidation and Inhibition of Melanogenesis from Ligularia stenocephala extract (곤달비추출물의 항산화와 멜라닌 생성 저해 효과)

  • Roh, Eon-Joo;Kim, Yoon-Shin;Kim, Beung-Gwan
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.1
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    • pp.87-92
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    • 2009
  • In this study, we evaluated anti-oxidation and whitening effects of Ligularia stenocephala extract for use as the cosmeceuticals. L. stenocephala was extracted by three different solvents which was n-Hexane, ethyl acetate, $H_{2}O$. The free radical (1,l-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity of extract of L. stenocephala was in the order: ethyl acetate fraction of leaf ($IC_{50}$ value of 10.512ug/mL) > ethyl acetate fraction of stem ($IC_{50}$ value of 31.877ug/mL) > $H_{2}O$ fraction of leaf ($IC_{50}$ value of 129.194ug/mL). Reactive oxygen species (ROS) scavenging activity of extract of L. stenocephala was in the order: ethyl acetate fraction of leaf ($IC_{50}$ value of 0.230mg/mL) > ethyl acetate fraction of stem ($IC_{50}$ value of 0.528mg/mL) > $H_{2}O$ fraction of leaf ($IC_{50}$ value of 0.799mg/mL). Tyrosinase inhibition activity of L. stenocephala extracts was reduced 29.477% on ethyl acetate fraction of leaf, 13.583% on ethyl acetate fraction of stems. Therefore, L. stenocephala extracts may be useful as a new antioxidant and whitening agent to inhibit melanogenesis.