• Title/Summary/Keyword: Binding ability

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Antioxidative and Inhibition Activities on Helicobacter pylori of Spice Extracts (향신료 추출물의 항산화활성 및 Helicobacter pylori 저해효과)

  • Cha, Won-Seup;Kim, Jeung-Hoan;Lee, Kyoung-Hwan;Kwon, Hyo-Jung;Yoon, So-Jung;Chun, Sung-Sook;Choi, Ung-Kyu;Cho, Young-Je
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.3
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    • pp.315-320
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    • 2006
  • For the purpose of developing natural antioxidant, the antioxidative and antimicrobial activities of phenolics isolated from spices were determined. The total phenolics contents of spices were more than 20 mg/g in water and 60% ethanol extracts of all spice, oregano and sage. Electron donating ability assay showed high inhibition rate in water extracts of all spice, nutmeg, white pepper, oregano and sage and 60% ethanol extracts of oregano and nutmeg. Antioxidant protection factor (PF) was higher than 1.2 in 60% ethanol extracts of sage, all spice and oregano and water extracts of sage. The 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid radical decolorization (ABTS) was inhibited by more than 90% by water and 60% ethanol extracts of all spice and oregano. TBARS (thiobarbituric acid reactive substances) were $0.7{\mu}M$ in the control and $0.2{\mu}M$ in water and 60% ethanol extracts the each spices. The water extracts of each spices did not have antimicrobial activity against H. pylori; however, the 60% ethanol extracts from oregano revealed the high antimicrobial activity as clear zone of 10 mm and inhibition rate of 77.2% with $200{\mu}g/mL$ of phenolics content. The result suggests that spices extract may be useful as potential sources of anti-Helicobacter pylori, antioxidant.

Analysis of Amino Acid Residues Affecting the Activity of QscR, a Quorum Sensing Receptor of Pseudomonas aeruginosa (녹농균(Pseudomonas aeruginosa)의 쿼럼 센싱 수용체인 QscR의 활성에 영향을 미치는 아미노산 잔기 분석)

  • Park, Su-Jin;Kim, Soo-Kyoung;Lee, Joon-Hee
    • Korean Journal of Microbiology
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    • v.48 no.3
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    • pp.180-186
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    • 2012
  • Pseudomonas aeruginosa, a Gram-negative bacterium, is an ubiquitous and opportunistic human pathogen, which expresses many virulence factors through quorum sensing (QS) regulation. QscR, one of the QS signal receptors of P. aeruginosa, has unique features that make it possible to distinguish QscR from other QS receptors. In the present study, we focused on amino acid residues responsible for such a broad signal specificity of QscR. Thus we constructed mutant QscRs: $QscR_{T72I}$, $QscR_{R132M}$, and $QscR_{T140I}$ by substituting $72^{nd}$ threonine, $132^{nd}$ arginine, and $140^{th}$ threonine residues with isoleucine, methionine, and isoleucine, respectively by site-directed mutagenesis. When we examined the activity of these mutant QscRs, $QscR_{R132M}$ failed to respond to N-3-oxododecanoyl homoserine lactone (3OC12-HSL), but $QscR_{T72I}$ and $QscR_{T140I}$ remained the ability to respond to 3OC12-HSL despite much reduction of the sensitivity. When we treated a variety of acyl-HSLs with different structure, $QscR_{T72I}$ and $QscR_{T140I}$ showed better responsiveness to N-decanoyl HSL (C10-HSL) or N-dodecanoyl HSL (C12-HSL) that has no oxo-moiety at $3^{rd}$ carbon of acyl group than to 3OC12-HSL, and $QscR_{R132M}$ showed no responsiveness to any acyl-HSLs tested here. In addition, $QscR_{T72I}$ and $QscR_{T140I}$ were inhibited by 5f, a QscR inhibitor as similarly as wild type QscR was. These results suggest that while the $130^{th}$ arginine is crucial in both activity and acyl-HSL binding of QscR, the $72^{nd}$ and $140^{th}$ threonines are important in the activity, but they are little responsible for the discrimination of acyl-HSLs or competitive inhibitor.

MODULATION OF INTRACELLULAR pH BY $Na^+/H^+$ EXCHANGER AND $HCO_3^-$ TRANSPORTER IN SALIVARY ACINAR CELLS ($Na^+/H^+$ exchanger와 $HCO_3^-$ transporter에 의한 흰쥐 타액선 선세포내 pH 조절)

  • Park, Dong-Bum;Seo, Jeong-Taeg;Sohn, Heung-Kyu;Lee, Jong-Gap
    • Journal of the korean academy of Pediatric Dentistry
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    • v.25 no.2
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    • pp.352-367
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    • 1998
  • Intracellular pH (pHi) plays an important role in the regulation of cellular processes by influencing the acitivity of various enzymes in cells. Therefore, almost every type of mammalian cell possesses an ability to regulate its pHi. One of the most prominent mechanisms in the regulation of pHi is $Na^+/H^+$ exchanger. This exchanger has been known to be activated when cells are stimulated by the binding of agonist to the muscarinic receptors. Therefore, the aims of this study were to compare the rates of $H^+$ extrusion through $Na^+/H^+$ exchanger before and during muscarinic stimulation and to investigate the possible existence of $HCO_3^-$ transporter which is responsible for the continuous supply of $HCO_3^-$ ion to saliva. Acinar cells were isolated from the rat mandibular salivary glands and loaded with pH-sensitive fluoroprobe, 2', 7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein(BCECF), for 30min at room temperature. Cells were attached onto the coverglass in the perfusion chamber and the changes in pHi were measured on the iverted microscope using spectrofluorometer. 1. By switching the perfusate from $HCO_3^-$-free to $HCO_3^-$-buffered solution, pHi decreased by $0.39{\pm}0.02$ pH units followed by a slow increase at an initial rate of $0.04{\pm}0.007$ pH units/min. The rate of pHi increase was reduced to $0.01{\pm}0.002$ pH units/min by the simultaneous addition of 1 mM amiloride and $100{\mu}M$ DIDS. 2. An addition and removal of $NH_4^+$ caused a decrease in pHi which was followed by an increase in pHi. The increase of pHi was almost completely blocked by 1mM amiloride in $HCO_3^-$-free perfusate which implied that the pHi increase was entired dependent on the activation of $Na^+/H^+$ exchanger in $HCO_3^-$-free condition. 3. An addition of $10{\mu}M$ carbachol increased the initial rate of pHi recovery from $0.16{\pm}0.01$ pH units/min to $0.28{\pm}0.03pH$ units/min. 4. The initial rate of pHi decrease induced by 1mM amiloride was also increased by the exposure of the acinar cells to $10{\mu}M$ carbachol ($0.06{\pm}0.008pH$ unit/min) compared with that obtained before carbachol stimulation ($0.03{\pm}0.004pH$ unit/min). 5. The intracellular buffering capacity ${\beta}1$ was $14.31{\pm}1.82$ at pHi 7.2-7.4 and ${\beta}1$ increased as pHi decreased. 6. The rate of $H^+$ extrusion through $Na^+/H^+$ exchanger was greatly enhanced by the stimulation of the cells with $10{\mu}M$ carbachol and there was an alkaline shift in the activity of the exchanger. 7. An intrusion mechanism of $HCO_3^-$ was identified in rat mandibular salivary acinar cells. Taken all together, I observed 3-fold increase in $Na^+/H^+$ exchanger by the stimulation of the acinar cells with $10{\mu}M$ carbachol at pH 7.25. In addition, I have found an additional mechanism for the regulation of pHi which transported $HCO_3^-$ into the cells.

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Screening of the Antimicrobial Activity against Helicobacter pylori and Antioxidant by Extracts from Mulberry Fruits (Morus albba L.) (품종이 다른 오디추출물의 Helicobacter pylori에 대한 항균활성 탐색과 항산화 효과)

  • Cho, Young-Je;Chun, Sung-Sook;Lee, Kyoung-Hwan;Kim, Jeung-Hoan;Kwon, Hyo-Jung;An, Bong-Jeun;Kim, Myung-Uk
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.1
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    • pp.15-20
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    • 2006
  • The water and $40\%$ ethanol extracts from mulberry fruits were tested for their antimicrobial activities against Helicobacter pylori and antioxidant. Kangwon III (Morus albba L.) was higher phenolic content (2.90 mg/g) than other water extracts. The phenolic contents of $40\%$ ethanol extracts from Kangwon III and Hihak were 3.02 mg/g and 2.46 mg/g, respectively . The ABTS [2,2'-azinobis(3-ethylbenzothiazoline-6-sulfornic acid)] radical decolorization, electron donating ability (EDA), thiobarbituric acid reactive substance (TBARS) and antioxidant protection factor (PF) were determined for water extracts and $40\%$ ethanol extracts from mulberry fruits. EDA was higher in water extracts than ethanol extract. EDA of water extract from Kangwon III was determined as $99.54\%$ while the activity of ethanol extracts was $89.61\%$ in Daechoukmyeun. The water extracts from Cheongilppong showed higher antioxidative activity than another mulberry fruits extract when evaluated by ABTS [2,2'-azinobis(3-ethylbenzothiaznoline-6-sulfornic acid)] radical decolorization, TBARS and antioxidant PF by water extracts. Kangwon III was higher phenolic content (2.90 mg/g) than other that of water extracts. $40\%$ ethanol extracts were determined that phenolic contents of Kangwon III, Hihak were 3.02 mg/g, 2.46 mg/g for each other. Antimicrobial activity showed the high value in water extracts of Cheongilppong, Kuksang 20. The result will be useful nature microbial medicine for mulberry fruits.

Evaluation of canal preparation for apical sealing with various Ni-Ti rotary instruments (수 종의 Ni-Ti 회전 기구들을 이용한 치근단 폐쇄 향상을 위한 근관 확대 평가)

  • Shin, Yoo-Seok;Shin, Su-Jung;Song, Min-Ju;Kim, Eui-Seong
    • Restorative Dentistry and Endodontics
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    • v.36 no.4
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    • pp.300-305
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    • 2011
  • Objectives: The aim of this study was to evaluate the various NiTi rotary instruments regarding their ability to provide a circular apical preparation. Materials and Methods: 50 single canal roots were selected, cut at the cementodentinal junction and the coronal 1/3 of the canals was flared using Gates Glidden burs. Samples were randomly divided into 5 experimental groups of 10 each. In group I, GT files, Profile 04 and Quantec #9 and #10 files were used. In Group II Lightspeed was used instead of Quantec. In Group III, Orifice shaper, Profile .06 series and Lightspeed were used. In Group IV, Quantec #9 and #10 files were used instead of Lightspeed. In Group V, the GT file and the Profile .04 series were used to prepare the entire canal length. All tooth samples were cut at 1 mm, 3 mm and 5 mm from the apex and were examined under the microscope. Results: Groups II and III (Lightspeed) showed a more circular preparation in the apical 1mm samples than the groups that used Quantec (Group I & IV) or GT files and Profile .04 series.(Group V)(p < 0.05) There was no significant difference statistically among the apical 3, 5 mm samples. In 5 mm samples, most of the samples showed complete circularity and none of them showed irregular shape. Conclusions: Lightspeed showed circular preparation at apical 1 mm more frequently than other instruments used in this study. However only 35% of samples showed circularity even in the Lightspeed Group which were enlarged 3 ISO size from the initial apical binding file (IAF) size. So it must be considered that enlarging 3 ISO size isn't enough to make round preparation.

Inhibitory Effect against Helicobacter pylori and Biological Activity of Thyme (Thymus vulgaris L.) Extracts (Thyme(Thymus vulgaris L.) 추출물의 Helicobacter pylori 억제효과 및 생리활성)

  • Kim, Jeung-Hoan;Kwon, Jung-Hyo;Lee, Kyeong-Hwan;Chun, Sung-Sook;Kwon, Oh-Jun;Woo, Hi-Seob;Cho, Young-Je;Cha, Won-Seup
    • Applied Biological Chemistry
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    • v.49 no.3
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    • pp.243-247
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    • 2006
  • The biological activity of functional food source with thyme extracts were examined. Total phenol contents in the 60% ethanol extracts $(26.8{\pm}0.35\;mg/g)$ with thyme leaf was higher than water extracts $(25.7{\pm}0.20\;mg/g)$. This HPLC analysis is significant in that physiological activity is related with phenolic compound content such as rosemarinic acid, quercetin and chlorogenic acid. Electron donating ability was shown as 90.1% in the water extracts and 77.7% in the 60% ethanol extracts. Antioxidant protection factor of 60% ethanol extracts was higher than water extracts. Helicobacter pylori of the water extracts from thyme leaves did not have antimicrobial activity, but the 60% ethanol extracts revealed the high antimicrobial activity as 9 mm of clear zone in $50\;{\mu}g/ml$ of phenol content, 10 mm in $100\;{\mu}g/ml$, 13 mm in $150\;{\mu}g/ml$ and 16 mm in $200\;{\mu}g/ml$, respectively. Angiotensin converting enzyme inhibition activity showed no inhibition activity in 60% ethanol extracts but 39.9% inhibition activity in water extracts. Xanthine oxidase inhibition activity showed high inhibition activity at 73.5% in water extracts and 100% in 60% ethanol extracts. The result suggests the development of phenol compound in thyme as anti Helicobacter pylori, antioxidant and anti-gout agents.

Changes of Pork Antigenicity by Heat, Pressure, Sonication, Microwave, and Gamma Irradiation (물리적 처리에 의한 돼지고기의 항원성 변화)

  • Kim, Seo-Jin;Kim, Koth-Bong-Woo-Ri;Song, Eu-Jin;Lee, So-Young;Yoon, So-Young;Lee, So-Jeong;Lee, Chung-Jo;Park, Jin-Gyu;Lee, Ju-Woon;Byun, Myung-Woo;Ahn, Dong-Hyun
    • Food Science of Animal Resources
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    • v.29 no.6
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    • pp.709-718
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    • 2009
  • The purpose of this study was to search for physical treatments to reduce allergenicity of pork. Physical treatments such as heating, autoclave, microwave, sonication, and irradiation have been used for food processing or reduction of allergenicity. The porcine serum albumin (PSA), known as a major allergen in pork, was extracted after physical treatments. The antigenicity of pork extracts by heating (80 and $100^{\circ}C$ for 20 min), autoclave ($121^{\circ}C$ for 5, 10, and 30 min), and microwave (for 5 and 10 min) was significantly decreased. Especially, the binding ability of p-IgG to pork extracts by autoclave for 30 min showed the greatest decrease (about 3%) in physical treatments. However, the antigenicity of pork was unaffected by sonication and irradiation treatment. These results indicated that the autoclave treatment was the most effective method to reduce the antigenicity of pork.

A Novel Synthesized Tyrosinase Inhibitor, (E)-3-(4-hydroxybenzylidene) chroman-4-one (MHY1294) Inhibits α-MSH-induced Melanogenesis in B16F10 Melanoma Cells (신규 합성물질 (E)-3-(4-하이드록시벤질리딘)크로마논 유도체의 티로시나아제 효소활성 저해 및 멜라닌 생성 억제 효과)

  • Jeon, Hyeyoung;Lee, Seulah;Yang, Seonguk;Bang, EunJin;Ryu, Il Young;Park, Yujin;Jung, Hee Jin;Chung, Hae Young;Moon, Hyung Ryong;Lee, Jaewon
    • Journal of Life Science
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    • v.31 no.8
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    • pp.719-728
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    • 2021
  • Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC50 = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.