• Title/Summary/Keyword: Inhibitory Activity

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Characteristics of Angiotensin Converting Enzyme Inhibitory Peptides from Aroase AP10 Hydrolysate of Octopus (Aroase AP10에 의한 문어 가수분해물의 Angiotensin Converting Enzyme 저해 Peptide의 특성)

  • Park, Yeung-Beom
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.2
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    • pp.177-181
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    • 2009
  • The peptides from Aroase AP10 enzymatic hydrolysates of octopus proteins were isolated and tested for inhibitory activity against angiotensin converting enzyme (ACE). The Aroase AP10 hydrolysates were filtered through PM-10 membrane (M.W. cut-off 10,000) to obtain the peptides fractions with ACE inhibition activity. These fractions were applied to a Biogel P-2 column. Three active fractions (A, B, and C) were collected and applied to a SuperQ-Toyopearl 650S column chromatography, leading to the isolation of four active fractions (A-1, A-2, B-1, and C-1). Among the active fractions, C-1 had the highest ACE inhibitory activity ($IC_{50}=3.10{\mu}g$). The main composition of its amino acids is arginine, lysine, histidine and leucine, which cover about 60% of the total amino acids.

Anti-inflammatory Effect of Unripe Fruit of Citrus grandis Osbeck in RAW 264.7 and HaCaT Cells (RAW 264.7 및 HaCaT Cell에서 당유자 미숙과의 염증억제 효과)

  • Lee, Hye-Ja;Kang, Gyeoung-Jin;Yoon, Weon-Jong;Kang, Hee-Kyoung;Kim, Young-Suk;Kim, So-Mi;Yoo, Eun-Sook
    • Korean Journal of Pharmacognosy
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    • v.37 no.2 s.145
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    • pp.74-80
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    • 2006
  • We investigated the anti-inflammatory activities of unripe fruit of Citrus grandis Osbeck growing at Jeju Island, through the evaluation of their inhibitory effect on the production of inflammatory markers (IL-6, iNOS, COX, TARC and MDC) in RAW264.7 murine macrophage cells and HaCaT human keratinocyte cells. Among the sequential solvent fractions obtained from crude extract, hexane and chloroform $(CHCI_3)$ fractions showed potential inhibitory activity on the mRNA expressions of IL-6, iNOS and COX-2 at the concentration of $100\;{\mu}g/ml$ in RAW264.7 cells. Also, EtOAc fraction showed inhibitory activity on the thymus and activation-regulated chemokine (TARC)/CCL17 and macrophage-derived chemokine (MDC)/CCL22 at the concentration of $50\;{\mu}g/ml$ in HaCaT cells. These results suggest that the unripe fruit of C. grandis may have anti-inflammatory activity through the suppression of inflammatory markers (IL-6, iNOS, COX, TARC and MDC).

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.

Detection of Heavy Metal Ions by the Cuvette Assay Measuring Urease Inhibitory Activity (Urease 저해활성 측정 cuvette assay에 의한 중금속 이온 검출)

  • Kim, Dong-Kyung;Park, Kyung-Rim;Kang, Eun-Mi;Park, In-Seon;Kim, Nam-Soo
    • Applied Biological Chemistry
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    • v.46 no.2
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    • pp.74-78
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    • 2003
  • To determine the urease inhibitory activity of various heavy metal ions, a photometric cuvette assay for measuring ammonia production was developed. In this assay, the absorbance values at 630 m were linearly increased according to the ammonia concentrations up to 3.0 mg/l (r : 0.998). The urease inhibitions upon addition of a single species of heavy metal ions were in the decreasing order of Hg(II) > Pb(II) > Cu(II) > Cd(II) > Zn(II) ions. As expected, the urease inhibitions at a fixed concentration of a single species and at varying concentrations of other species occurred in the additive way. The above results show the applicability of the current method to the selective detection on Hg(II) ions as well as the screening of heavy metal ions possibly present at various samples.

Use of Bioluminescent Indicator Acinetobacter Bacterium for Screening and Characterization of Active Antimicrobial Agents

  • Haleem Abd-El;A.M. Desouky;Zaki Sahar A.
    • Journal of Microbiology and Biotechnology
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    • v.16 no.11
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    • pp.1706-1712
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    • 2006
  • Because of the need for new antimicrobial substances with novel mechanisms of action, we report here the use of an Acinetobacter reporter system for high-throughput screening of active antimicrobial agents. The bioreporter Acinetobacter strain DF4/PUTK2 carrying luciferase genes luxCDABE was chosen because of its ecological importance and it is widespread in nature. This bioreporter is genetically engineered to emit light constitutively that can be measured in real time by luminometry. Hence, this reporter system was employed to determine the bacteriostatic actions of spent-culture supernatants derived from twelve bacterial isolates. Out of the results, the strongest bioluminescence inhibitory effect of the supernatants was recorded with Bacillus cereus strain BAC (S5). Subsequently, ethyl acetate extracts of extracellular products of strain BAC (S5) were separated by a thin-layer chromatography (TLC). Based on the bioluminescence inhibitory assay, three fractions were found to have antimicrobial activity. One fraction (C) having the strongest antimicrobial activity was further purified using TLC and characterized by IR, $^1H$ NMR, mass spectrometry, SDS-PAGE, and amino acid composition analysis. The results predicted the presence of 2-pyrrolidone-S-carboxylic acid (PCA) and the octadeconic-acid-like fatty acid. Fraction C also demonstrated a broad inhibitory activity on several Gram-negative and Gram-positive bacteria. In conclusion, the Acinetobacter reporter system shows great potential to be a reliable, sensitive, and real-time indicator of the bacteriostatic actions of the antimicrobial agents.

Synthesis of Sulfonamide Derivatives as New Herbicidal Compounds and Studies on Biological Activity (새로운 Sulfonamide 유도체의 합성과 Acetolactate Synthase (ALS) 저해)

  • Chae, Jong-Kun;Lee, Jae-Seob;Choi, Jung-Do;Shin, Jung-Hyu
    • Applied Biological Chemistry
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    • v.41 no.1
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    • pp.99-103
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    • 1998
  • Triazolopyrimidine sulfonanilide (TP) derivative is one of excellent herbicide compounds. We have synthesized three classes of a new sulfonamide derivative (TPP) as Acetolactate synthase (ALS) inhibitors, in which the benzene ring in TP skeleton was converted to substituted pyrimidyl ring and examined their inhibitory activities on barley for ALS. $I_{50}$ values of the inhibitors ranged from 0.005 to 2 mM. Comparing the $I_{50}$ value of each class of TPP derivatives, the substituents in pyrimidine and triazolopyrimidine ring were found to affect the degree of ALS inhibition. TPP with substituted methyl group in pyrimidine ring showed higher inhibitory activity than that with methoxy group, while the substitution of the cyclopentano group in triazolopyrimidine ring gave very large inhibitory activity than that of methyl group. The present study established that variation of the electron density by substitution at heterocyclic ring is a very important factor for ALS inhibition, but showed no dependence on steric effect by substituents.

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Constituents of the seeds of Cornus officinalis with Inhibitory Activity on the Formation of Advanced Glycation End Products (AGEs) (산수유 씨의 최종당화산물 생성저해활성 성분)

  • Lee, Ga-Young;Jang, Dae-Sik;Lee, Yun-Mi;Kim, Young-Sook;Kim, Jin-Sook
    • Applied Biological Chemistry
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    • v.51 no.4
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    • pp.316-320
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    • 2008
  • Ten compounds, (+)-pinoresinol (1), (-)-balanophonin (2), gallicin (3), vanillin (4), 4-hydroxybenzaldehyde (5), coniferaldehyde (6), betulinic acid (7), ursolic acid (8), 5-hydroxymethyl furfural (9), and malic acid (10), were isolated from a EtOAc-soluble fraction of the seeds of Cornus officinalis. The structures of these compounds were elucidated by spectroscopic methods as well as by comparison with reported values. Compounds 1, 2, and 4-7 were isolated from this species for the first time. All the isolates (1-10) were subjected to an in vitro bioassay to evaluate their inhibitory activity against advanced glycation end products (AGEs) formation. Among these, compounds 2 and 3 showed the significant inhibitory activity on AGEs formation with $IC_{50}$ values of 27.81 and 18.04${\mu}M$, respectively.

Whitening and Anti-wrinkling Effects of Fractions from Prunus persica Flos (도화(Prunus persica Flos) 분획물의 미백 및 주름개선 효과)

  • Lee, Jin-Young;An, Bong-Jeun
    • Microbiology and Biotechnology Letters
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    • v.40 no.4
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    • pp.364-370
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    • 2012
  • In this study, the compounds of Prunus persica Flos were extracted with 70.0% acetone and were purified using a sephadex-LH-20 column chromatography. As a result, eight fractions were isolated. For whitening effects, the tyrosinase inhibitory activity was determined to be 92.2% in Fr.-8 isolated from P. persica Flos at 1.000 ppm. The melanoma cell-originated tyrosinase inhibitory effect of Fr.-8 from P. persica Flos was approximately 63.4% at 100 ppm. The inhibitory activity on melanin synthesis by Fr.-8 isolated from P. persica Flos was about 71.7% at 100 ppm concentration. For anti-wrinkling effects, the elastase inhibition activities by Fr.-5, 7 isolated from P. persica Flos were around 71.4 and 74.5% respectively at 1,000 ppm. The collagenase inhibition activity and collagen synthesis by Fr.-8 isolated from P. persica Flos was about 80.0% at 100 ppm. All these findings suggested that the fractions of P. persica Flos have great potential as cosmeceutical ingredients with whitening and anti-wrinkling effects.

Isolation of Streptomyces sp. KK565 as a Producer of ${\beta}-Amyloid$ Aggregation Inhibitor

  • Hwang, Sung-Eun;Im, Hyung-Min;Kim, Dong-Hoon;Shin, Hyun-Ju;Shin, Dong-Hoon;Park, Jeong-Eun;Jo, In-Ho;Kim, Chang-Jin;Yoo, Jong-Shin;Kang, Jong-Min;Lim, Dong-Yeon;Ahn-Jo, Snag-Mee;Kwon, Ho-Jeong
    • Journal of Microbiology and Biotechnology
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    • v.13 no.5
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    • pp.809-814
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    • 2003
  • ${\beta}-amyloid$ ($A{\beta}$) peptides from the proteolytic processing of ${\beta}-amyloid$ precursor protein (${\beta}-APP$) aggregates in the brain to form senile plaques, and their aggregation plays a key role in pathogenesis of Alzheimer's disease (AD). To isolate an active compound that has an $A{\beta}$ aggregation-inhibitory activity, 2,000 microbial metabolite libraries were screened based on their ability to inhibit $A{\beta}$ aggregation by using both Congo red and thioflavin T assays. As a result, a water-soluble fraction of a soil microorganism, KK565, showed a potent $A{\beta}$ aggregation-inhibitory activity. The strain was identified as Streptomyces species, based on the cultural and morphological characteristics, the presence of diaminopimelic acid in the cell wall, and the sugar patterns for the whole-cell extract. In addition, the purification of active principle resulted in identifying a heat-unstable protein responsible for the $A{\beta}$ aggregation-inhibitory activity.

Antioxidant Activities and Tyrosinase Inhibitory Effects of Different Extracts from Pleurotus ostreatus Fruiting Bodies

  • Alam, Nuhu;Yoon, Ki-Nam;Lee, Kyung-Rim;Shin, Pyung-Gyun;Cheong, Jong-Chun;Yoo, Young-Bok;Shim, Mi-Ja;Lee, Min-Woong;Lee, U-Youn;Lee, Tae-Soo
    • Mycobiology
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    • v.38 no.4
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    • pp.295-301
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    • 2010
  • We evaluated the antioxidant activity and tyrosinase inhibitory effects of Pleurotus ostreatus fruiting bodies extracted with acetone, methanol, and hot water. The antioxidant activities were tested against $\beta$-carotene-linoleic acid, reducing power, 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activity, and ferrous chelating ability. Furthermore, phenolic acid and flavonoid contents were also analyzed. The methanol extract showed the strongest $\beta$-carotene-linoleic acid inhibition as compared to the other exracts. The acetone extract (8 mg/mL) showed a significantly high reducing power of 1.54 than the other extracts. The acetone extract was more effective than other extracts for scavenging on 1,1-diphenyl-2-picrylhydrazyl radicals. The strongest chelating effect (85.66%) was obtained from the acetone extract at 1.0 mg/mL. The antioxidant activities of the extracts from the P. ostreatus fruiting bodies increased with increasing concentration. A high performance liquid chromatography analysis detected seven phenolic compounds, including gallic acid, protocatechuic acid, chlorogenic acid, naringenin, hesperetin, formononetin, and biochanin-A in an acetonitrile and 0.1 N hydrochloric acid (5 : 1) solvent extract. The total phenolic compound concentration was $188{\mu}g$/g. Tyrosinase inhibition of the acetone, methanol, and hot water P. ostreatus extracts increased with increasing concentration. The results revealed that the methanol extract had good tyrosinase inhibitory ability, whereas the acetone and hot water extracts showed moderate activity at the concentrations tested. The results suggested that P. ostreatus may have potential as a natural antioxidant.