• Title/Summary/Keyword: Inhibition model

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Effect of Water Adulteration on the Rheology and Antibacterial Activities of Honey

  • ANIDIOBU, Vincent Okechukwu
    • The Korean Journal of Food & Health Convergence
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    • v.8 no.5
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    • pp.11-20
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    • 2022
  • Honey was diluted with different percentages of water and was analysed rheologically at room temperature of 27℃. The rheological profiles of pure and impure honey samples were measured at low shear rates (0.01-4.16s-1). This work developed a structural kinetic model, which correlated well with the rheological data. The new model was used to categorise honey samples using their average molecular weights as one of the distinctive properties. Also, the kinetics order in the new model predicts the number of active components in the "honey" undergoing deformation. Honey produced third order kinetics to depict the monomers, oligomers and water content in honey. Pure honey exhibits peculiar non-Newtonian rheological behaviour. The behaviour of water is Newtonian. Dilution of honey with different percentages of water turns the resulting fluid Newtonian from 10% dilution with water. This study analysed the antibacterial activities of honey and serially adulterated samples against Staphylococcus aureus and Pseudomonas aeruginosa. The antibacterial analyses of honey were conducted using Kirby Bauer's well diffusion method. The results indicated that pure honey exhibited a zone of inhibition against both organisms. Also, the diameter of the zone of inhibition decreased with increasing dilution of honey, suggesting a correlation with the rheological method.

Antioxidative Properties of Amaranth Cauline Leaf and Suppressive Effect against CT-26 Cell Proliferation of the Sausage Containing the Leaf

  • Lee, Heejeong;Joo, Nami
    • Food Science of Animal Resources
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    • v.38 no.3
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    • pp.570-579
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    • 2018
  • The study investigated antioxidative properties and rectal cancer cell inhibition effect of amaranth (Amaranthus cruentus L.) cauline leaves (ACL) to produce the sausage with ACL powder (ACLP). Antioxidative effects of ACLP prepared with different stem lengths (10-45 cm) were evaluated through DPPH, ABTS, reducing power, total phenol, and total flavonoid. Inhibition effect on rectal cancer cells growth was also examined with CT-26 cell. To determine appropriate ACL amounts in sausage formula, response surface methodology was used. The sausages without ACL (control) and the sausage with ACL (ACLP sausage) were the subjected to the examinations of antioxidation, growth inhibition on CT-26, and physicochemical properties (pH and water content). ACLP made from the leaf with 15 cm length stem generally showed the highest antioxidative effect through results of DPPH, ABTS, reducing power, total phenol, and total flavonoid. ACLP also showed inhibition effect on the proliferation of CT-26, depending on concentration of ACLP. The surface response model showed that 4.87 g of ACLP was optimized amount for sausage production. Physicochemical properties between optimized ACLP and control sausages were not significantly different. Higher antioxidative effect of optimized ACLP sausage extract was observed (p<0.05) in antioxidation tests than control sausage extract except for DPPH. Cell viability of CT-26 cells were higher (p<0.05) in ACLP than in control sausage extracts. These results indicate that ACLP has functional effects on antioxidation activity and growth inhibition on CT-26 cell, and thus, it should be useful as a supplement in sausage, which may some effect as ACLP itself.

Effects of Pahs and Pcbs and Their Toxic Metabolites on Inhibition of Gjic and Cell Proliferation in Rat Liver Epithelial Wb-F344 Cells

  • Miroslav, Machala;Jan, Vondracek;Katerina, Chramostova;Lenka, Sindlerova;Pavel, Krcmar;Martina, Pliskova;Katerina, Pencikova;Brad, Upham
    • Environmental Mutagens and Carcinogens
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    • v.23 no.2
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    • pp.56-62
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    • 2003
  • The liver progenitor cells could form a potential target cell population fore both tumor-initiating and -promoting chemicals. Induction of drug-metabolizing and antioxidant enzymes, including AhR-dependent CYP1A1, NQO-1 and AKR1C9, was detected in the rat liver epithelial WB-F344 "stem-like" cells. Additionally, WB-F344 cells express a functional, wild-type form of p53 protein, a biomarker of genotoxic events, and connexin 43, a basic structural unit of gap junctions forming an important type of intercellular communication. In this cellular model, two complementary assays have been established for detection of the modes of action associated with tumor promotion: inhibition of gap junctional intercellular communication (GJIC) and proliferative activity in confluent cells. We found that the PAHs and PCBs, which are AhR agonists, released WB-F344 cells from contact inhibition, increasing both DNA synthesis and cell numbers. Genotoxic effects of some PAHs that lead to apoptosis and cell cycle delay might interfere with the proliferative activity of PAHs. Contrary to that, the nongenotoxic low-molecular-weight PAHs and non-dioxin-like PCB congeners, abundant in the environment, did not significantly affect cell cycle and cell proliferation; however both groups of compounds inhibited GJIC in WB-F344 cells. The release from contact inhibiton by a mechanism that possibly involves the AhR activation, inhibition of GJIC and genotoxic events induced by environmental contaminants are three important modes of action that could play an important role in carcinogenic effects of toxic compounds. The relative potencies to inhibit GJIC, to induce AhR-mediated activity, and to release cells from contact inhibition were determined for a large series of PAHs and PCBs and their metabolites. In vitro bioassays based on detection of events on cellular level (deregulation of GJIC and/or proliferation) or determination of receptor-mediated activities in both ?$stem-like^{\circ}{\times}$ and hepatocyte-like liver cellular models are valuable tools for detection of modes of action of polyaromatic hydrocarbons. They may serve, together with concentration data, as a first step in their risk assessment.

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A STUDY OF IONIC DISSOCIATION ON VARIOUS CALCIUM HYDROXIDE PASTES USING MOLECULAR SIEVING MODEL (분자체 모델을 이용한 수종의 수산화칼슘 제재의 이온 용출에 관한 연구)

  • Lee, Kyoung-Sun;;;Lee, Seung-Jong
    • Restorative Dentistry and Endodontics
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    • v.27 no.6
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    • pp.632-643
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    • 2002
  • The purpose of this study was two-fold. First was to evaluate whether the molecular sieving model was appropriate for ionic dissociation experiment. Second was to compare the dissociation of calcium and hydroxyl ions from five types of calcium hydroxide pastes (Pure calcium hydroxide paste, DT temporary $dressing^{\circledR},{\;}Metapaste^{\circledR},{\;}Chidopex^{\circledR},{\;}Metapex^{\circledR}$) in three vehicles (aqueous, viscous and oily) and the antibacterial effect. Each calcium hydroxide pastes was placed into 0.65ml tube with cap and then 15% polyacrylamide gel was placed onto calcium hydroxide pastes. After the gel was hardened, the tubes were filled with tridistilled water (pH 7.14) and closed with cap. The tubes were stored in $37^{\circ}C$ 100% incubator The pH reading and the concentration of calcium ions were taken at 1, 4, 7. 10, and 14 days. The brain heart infusion agar plates with S. mutans and A. actinomycetemcomitans were used far antibacterial activity test. Middle of agar plate was filled with the calcium hydroxide pastes. The plates were incubated at $37^{\circ}C$ and observations were made to detect the zones of inhibition. These data were evaluated statistically by use of the analysis of variance and duncan test. The results were as follows. 1. In fresh mixing state, the pH of five types of calcium hydroxide pastes were measured between 12.5 and 12.8. 2. The pH was increased in all five types of calcium hydroxide pastes compared with control group. In 14 days, Pure calcium hydroxide paste (11.45) and DT temporary $dressing^{\circledR}$ (11.33) showed highest pH, followed by $Metapaste^{\circledR}$ (9.49), $Chidopex^{\circledR}$ (8.37) and $Metapex^{\circledR}$ (7.59) 3. Calcium was higher in all five types of calcium hydroxide pastes compared with control group. In 14 days, Pure calcium hydroxide paste (137.29 mg%) and DT temporary $dressing^{\circledR}$ (124.6 mg%) showed highest value, followed by $Metapaste^{\circledR}$ (116.74 mg%), $Chidopex^{\circledR}$ (111.84 mg%) and $Metapex^{\circledR}$ (60.22 mg%). 4. The zones of bacterial inhibition were seen around all five types of calcium hydroxide pastes. $Chidopex^{\circledR}{\;}and{\;}Metapex^{\circledR}$ groups which include iodoform were observed significantly larger zone of inhibition in A. actinomycetemcomitans compared with the other calcium hydroxide groups (p<0.05) However, $Metapex^{\circledR}$ showed the least antibacterial effect on S. mutans compared with other groups (p<0.05). The molecular sieving model was found to be acceptable in dissociation experiment of hydroxyl and calcium ions when compared with the previous tooth model study. But this model was not appropriate for the antibacterial test.

Effect of organic concentration on its degradation kinetics in a burial site (매몰지 내 유기물 농도가 분해 속도에 미치는 영향)

  • Lee, Chae-Young;Choi, Jae-Min;Oh, Seung-Jun;Han, Sun-Kee;Park, Joon-Kyu
    • Journal of the Korea Organic Resources Recycling Association
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    • v.21 no.1
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    • pp.62-68
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    • 2013
  • The effect of organic substance on its degradation rate in burial site was investigated using batch tests. Substrate were swine and cattle with the initial concentrations of 2, 4, 6, 8, and 10 g VS(volatile solids)/L, respectively. The highest methane production rates of swine and cattle were found at 2 g VS/L as 46.3 and 48.4 ml CH4/g VS.d, respectively. As substrate concentration increased, the methane production rate decreased. The inhibition constants were n and m that were estimated using nonlinear inhibition model. The values of n and m were inhibition constants of methane production rate and ultimate methane yield, respectively. The values of n and m were 4.9 and 0.6 on swine and 1.1 and 0.4 on cattle. The methane production rate was responded sensitively by increase and decrease of substrate concentration, whereas ultimate methane yield do not relatively. From a relation between n and m, inhibitory effect of substrate concentration was confirmed as uncompetitive inhibition.

Inhibition of Autolysis by Lipase LipA in Streptococcus pneumoniae Sepsis

  • Kim, Gyu-Lee;Luong, Truc Thanh;Park, Sang-Sang;Lee, Seungyeop;Ha, Jung Ah;Nguyen, Cuong Thach;Ahn, Ji Hye;Park, Ki-Tae;Paik, Man-Jeong;Pyo, Suhkneung;Briles, David E.;Rhee, Dong-Kwon
    • Molecules and Cells
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    • v.40 no.12
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    • pp.935-944
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    • 2017
  • More than 50% of sepsis cases are associated with pneumonia. Sepsis is caused by infiltration of bacteria into the blood via inflammation, which is triggered by the release of cell wall components following lysis. However, the regulatory mechanism of lysis during infection is not well defined. Mice were infected with Streptococcus pneumoniae D39 wild-type (WT) and lipase mutant (${\Delta}lipA$) intranasally (pneumonia model) or intraperitoneally (sepsis model), and survival rate and pneumococcal colonization were determined. LipA and autolysin (LytA) levels were determined by qPCR and western blotting. S. pneumoniae Spd_1447 in the D39 (type 2) strain was identified as a lipase (LipA). In the sepsis model, but not in the pneumonia model, mice infected with the ${\Delta}lipA$ displayed higher mortality rates than did the D39 WT-infected mice. Treatment of pneumococci with serum induced LipA expression at both the mRNA and protein levels. In the presence of serum, the ${\Delta}lipA$ displayed faster lysis rates and higher LytA expression than the WT, both in vitro and in vivo. These results indicate that a pneumococcal lipase (LipA) represses autolysis via inhibition of LytA in a sepsis model.

Pharmacokinetic and Pharmacological Evaluation of Topical Microemulsion Preparation Containing Piroxicam (마이크로에멀젼으로 제제 설계된 피록시캄 외용제의 약물동력학적 특성 및 약효 평가)

  • 윤범진;박은석;지상철
    • Biomolecules & Therapeutics
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    • v.7 no.1
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    • pp.54-58
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    • 1999
  • The pharmacological activities and pharmacokinetic aspects of a topical microemulsion (KDPM) containing 0.5% piroxicam were evaluated after its topical application compared with a commercially available 0.5% piroxicam gel (R gel). When the pharmacological activities were evaluated with the carrageenan-induced paw edema model, KDPM showed 55.6% edema inhibition, while R gel resulted in 37.1%. With the adjuvant-induced arthritis model, KDFM also resulted in the better pharmacological activities than R gel. The relative bioavailability of KDPM based on R gel was 176% in rabbits.

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Effect of Ginseng on Fat Accumulation in the Obese Rats Induced by High Fat Diet (인삼이 고지방식이에 의한 비만유도 Rat에서 지방축적에 미치는 영향)

  • 김신일;김영숙
    • Journal of Ginseng Research
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    • v.10 no.2
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    • pp.167-179
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    • 1986
  • Obesity is common disease resultly accumulated excess fat. In the model for obesity induced by high fat diet contains 30% fat, administration of ginseng extract inhibited increment of body weight, epididymal fat pads and enlargement of fat cell size. This was as the result of inhibition of lipogenesis in the liver and fat accumulation in the adipose tissues.

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CoMFA and CoMSIA on the Inhibition of Calcineurin-NFAT Signaling by Blocking Protein-Protein Interaction with N-(4-Oxo-1(4H)-naphthalenylidene)benzenesulfonamide Derivatives

  • Myung, Pyung-Keun;Park, Kyung-Yong;Sung, Nack-Do
    • Bulletin of the Korean Chemical Society
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    • v.26 no.12
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    • pp.1941-1945
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    • 2005
  • To raises the possibility of designing effective inhibitors, 3D-QSAR for the inhibition of calcineurin-NFAT signaling by new N-(4-oxo-1(4H)-naphthalenylidene benzenesulfonamide derivatives as inhibitors of intracellular protein-protein interactions were studied using CoMFA and CoMSIA methodology. The three templates, N-(4-oxo-1(4H)-naphthalenylidene)benzenesulfonamide (A), benzenesulfonamide (B) and 4-oxo-1(4H)-naphthalenylidene (C) were selected to improve the statistic of the present 3D-QSAR models. The best models with combination of standard field in CoMFA, and steric field and electrostatic field in CoMSIA derived from the template, B and C, because most of the compounds tend not to be aligned in template A. From the based on the CoMFA and CoMSIA contour maps, the $R_1$ and $R_2$ groups on 4-oxo-1(4H) naphthalenylidene ring are steric favor. The ortho position on the benzenesulfonyl ring is steric disfavor and the meta position is steric favor. In addition, the oxygene atom of carbonyl group will have better inhibition activities as it has a negative charge favor. From these findings, we can conclude that the analyses of the contour maps provided insight into possible modification of molecules for effective inhibitiors.

Crassirhizomae rhizoma Exhibits Anti-Allergic Activity through Inhibition of Syk Kinase in Mast Cells (Syk kinase 억제를 통한 관중의 항앨러지 효과)

  • Kim, Young-Mi
    • Korean Journal of Medicinal Crop Science
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    • v.16 no.1
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    • pp.27-32
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    • 2008
  • This study aimed to investigate the anti-allergic activity and the mechanism of action of Crassirhizomae rhizoma (CR). The extract of CR exhibited potent inhibitory activity in mast cells; its $IC_{50}$ values were $31.2{\pm}1.5{\mu}g/m{\ell}$ for rat basophile leukemia (RBL)-2H3 mast cells and $51.5{\pm}2.1{\mu}g/m{\ell}$ for bone marrow-derived mast cells by antigen stimulation. It also suppressed the expression of TNF-${\alpha}$ and IL-4 mRNAs in RBL-2H3 cells. In an in-vivo animal allergy model, it inhibited a local allergic reaction, passive cutaneous anaphylaxis (PCA), in a dose-dependent manner. With regard to the mechanism of action, CR inhibited the activating phosphorylation of Syk kinase, a key signaling protein for the activation of mast cells. Taken together, these results strongly suggested that the anti-allergic activity of CR is mediated through the inhibition of histamine release and allergic cytokine production by the inhibition of Syk in mast cells.