• Title/Summary/Keyword: binding agent

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Strongylocentrotus intermedius Extract Suppresses Adiposity by Inhibiting Adipogenesis and Promoting Adipocyte Browning via AMPK Activation in 3T3-L1 Cells

  • Lakshi A. Dayarathne;Jasmadi;Seok-Chun Ko;Mi-Jin Yim;Jeong Min Lee;Ji-Yul Kim;Gun-Woo Oh;Dae-Sung Lee;Won-Kyo Jung;Sei-Jung Lee;Jae-Young Je
    • Journal of Microbiology and Biotechnology
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    • v.34 no.8
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    • pp.1688-1697
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    • 2024
  • The current study aimed to determine whether Strongylocentrotus intermedius (S. intermedius) extract (SIE) exerts anti-obesity potentials employing 3T3-L1 cells as in vitro model. Herein we reported that treatment of SIE for 6 days reduced lipid accretion and triglyceride content whereas it increased the release of free glycerol. The inhibited lipid accumulation and induced lipolysis were evidenced by the downregulation of lipogenesis proteins, such as fatty acid synthase and lipoprotein lipase, and the upregulation of hormone-sensitive lipase expression. Furthermore, the downregulation of adipogenic transcription factors, including peroxisome proliferator-activated receptor gamma, CCAAT/enhancer-binding protein α, and sterol regulatory element-binding protein 1, highlights that reduced lipid accumulation is supported by lowering adipocyte differentiation. Additionally, treatment activates brown adipocyte phenotype in 3T3-L1 cells by inducing expression of brown adipose tissue-specific proteins, such as uncoupling protein 1 and peroxisome proliferator-activated receptor-γ coactivator 1α. Moreover, SIE induced the phosphorylation of AMP-activated protein kinase (AMPK). The pharmacological approach using AMPK inhibitor revealed that the restraining effect of SIE on adipogenesis and promotion of adipocyte browning were blocked. In GC-MS analysis, SIE was mainly composed of cholest-5-en-3-ol (36.71%) along with saturated and unsaturated fatty acids which have favorable anti-obesity potentials. These results reveal that SIE has the possibility as a lipid-lowering agent for the intervention of obesity.

Radiolabeling of NOTA and DOTA with Positron Emitting $^{68}$Ga and Investigation of In Vitro Properties (양전자 방출핵종 $^{68}$Ga을 이용한 NOTA와 DOTA의 표지 및 시험관내 특성 연구)

  • Jeong, Jae-Min;Kim, Young-Ju;Lee, Yun-Sang;Lee, Dong-Soo;Chung, June-Key;Lee, Myung-Chul
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.4
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    • pp.330-336
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    • 2009
  • Purpose: We established radiolabeling conditions of NOTA and DOTA with a generator-produced PET radionuclide $^{68}$Ga and studied in vitro characteristics such as stability, serum protein binding, octanol/water distribution, and interference with other metal ions. Materials and Methods: Various concentrations of NOTA 3HCl and DOTA 4HCl were labeled with 1 mL $^{68}$GaCl$_3$ (0.18$\sim$5.75 mCi in 0.1 M HCl in various pH. NOTA 3HCl (0.373 mM) was labeled with $^{68}$GaCl$_3$(0.183$\sim$0.232 mCi/0.1 M HCl 1.0 mL) in the presence of CuCl$_2$, FeCl$_2$, InCl$_3$, FeCl$_3$, GaCl$_3$, MgCl$_2$ or CaCl$_2$ (0$\sim$6.07 mM) at room temperature. The labeling efficiencies of $^{68}$Ga-NOTA and $^{68}$Ga-DOTA were checked by ITLC-SG using acetone or saline as mobile phase. Stabilities, protein bindings, and octanol distribution coefficients of the labeled compounds also were investigated. Results: $^{68}$Ga-NOTA and $^{68}$Ga-DOTA were labeled optimally at pH 6.5 and pH 3.5, respectively, and the chelates were stable for 4 hr either in the reaction mixture at room temperature or in the human serum at 37$^{\circ}C$. NOTA was labeled at room temperature while DOTA required heating for labeling. $^{68}$Ga-NOTA labeling efficiency was reduced by CuCl$_2$, FeCl$_2$, InCl$_2$, FeCl$_3$ or CaCl$_3$, however, was not influenced by MgCl$_2$ or CaCl$_2$. The protein binding was low (2.04$\sim$3.32%). Log P value of $^{68}$Ga-NOTA was -3.07 indicating high hydrophilicity. Conclusion: We found that NOTA is a better bifunctional chelating agent than DOTA for $^{68}$Ga labeling. Although, $^{68}$Ga-NOTA labeling is interfered by various metal ions, it shows high stability and low serum protein binding.

Effect On the Air Permeability of Composting Bulking Agent (퇴비화 첨가제의 공기투과성에 대한 분석)

  • Kim, Byung Tae
    • Journal of the Korea Organic Resources Recycling Association
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    • v.20 no.3
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    • pp.71-82
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    • 2012
  • Common bulking agents in composting system include woody materials such as sawdust and woodchips. These bulking agents are mainly used for the purpose of the proper control of C/N ratio and moisture content in the composting. The topic for the effect on air permeability of bulking agents has far received relatively little attention in the composting field. This study investigated the effect of bulk density, moisture content, air-filled porosity, particle size and air flow rate on air permeability of several mixture ratios of sawdust and woodchip bulking agent. Increasing the moisture contents, the air-filled porosity was decreased and the particle size was increased for all kinds of bulking agent mixtures. Especially, with the increasing of mixing ratio of woodchip, these effects were sharply magnified. The air permeability respond to air-filled porosity was very similar to that for moisture content which was anticipated the linear relationship between air-filled porosity and moisture content. Above the region of moisture content 0.25 or 0.43(d.b.)(20 or 30% w.b.), the pressure drop decreased even though air-filled pore spaces were filling with water. Especially, to the particle size of 5 mm the pressure drop was decreased exponentially, so the air permeability was dramatically improved. By the water had the role of binding of the small particles, the macropores less resistances to air flow were created in the matrix. The effect of particle size on air permeability was much stronger than that of air-filled porosity or moisture content. And it is needed the preparing of initial particle size above 5 mm for efficient composting.

Human Neutrophil Elastase: Rapid Purification, Metal binding Stoichiometry and Modulation of the Activity by Chelating Agents (사람의 백혈구 내에 있는 Elestase: 순수부리, 금속이온의 화학량, 그리고 Chelating 효과에 의한 활성도 조절)

  • Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.24 no.1
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    • pp.111-123
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    • 1988
  • Neutrophil elastases were purified by a three step procedure consiting of one Sephadex G-75 and two HPLC elutions. The elastases cross-reacted with antibodies to human neutrophil elastase. Three bands with molecular weights between 26,000 and 29,700 were observed by gel electrophoresis. At each stage of purification the quantity of Zn increased, reaching molar ratio of 2:1 with elastase in the most purified samples. Calcium content. was seletively elevated during the earlier stages of purification but decreased to a ratio of 0.25 to 1 with elastase at the final step of purfication. Neutrophil elastase could be inhibited by EDTA, EGTA and 1,10-phenanthroline. EGTA inhbition was noncompetitive inhibition and reversible only if the time of preincubation was relatively short, indicating the instability of the apoenzyme. The concentration of chelator required to show significant inhibition of elastase was also dependent upon the stage of purity and the ionic strength of the reaction mixture. Inhibition by EGTA, followed by the removal of EGTA, could be reversed by Zn. In the presence of EGTA the enzyme could be returened to full activity by the addition of Zn, Mn and Ca, but not Mg or Na. All of the above evidence strongly supports human neturophil elastase could be a metalloenzyme as well as a serine protease.

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Effects and Mechanisms of Silkworm Powder as a Blood Glucose-Lowerinly Agent

  • Ryu, Kang-Sun;Lee, Heui-Sam;Kim, Iksoo
    • International Journal of Industrial Entomology and Biomaterials
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    • v.4 no.2
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    • pp.93-100
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    • 2002
  • Cocoon production, which is a representative of traditional sericulture shifted into silkworm powder production in the spring of 1995. This, infect, signifies the change from the dress-centered textile business to the bio-industry and the functional resource industry. One of the most outstanding shifting is utilization of silkworm larvae for anti-diabetic agent. In Asian countries including Korea, silkworm powder derived from the domestic silkworm (Bombyx mori L.) has long been favored for anti-diabetic agent, but its efficacy was not tested until last decade by modern scientific methods. In this article, we reviewed the major researches on the silkworm powder as a blood glucose-lowering substance. After the beginning test of the efficacy of silkworm powder by a cooperative research between Department of Sericulture and Entomlogy, NIAST, RDA and Kyung Hee University, substantial data have been accumulated so far, In a serial experiment to select best condition, the fifth instar larvae prepared by freeze dry method turned out to have the best blood glucose-lowering effect. In the pharmacological experiment to understand the mechanism of silkworm powder in small intestine, the silkworm powder turned out to inhibit the activity of ${\alpha}$-glucosidase, by competitively binding to $\alpha$-type disaccharides. The animal experiment showed that the extract of silkworm powder prevents a rapid increase of blood glucose level after meal and prevents hunger and law blood glucose level during empty stomach. In the experiment to isolate the major component of silkworm powder, which exerts blood glucose-lowering effect, 1-deoxynojirimy-cin (DNJ) was eventually mass-purified, and it turned out that DNJ isolated from silkworm powder was excellent in its blood glucose-lowering effect. In the experiment to understand the personal difference of the efficacy of the silkworm powder, clinical candidates were divided on the basis of the criterion of traditional Chinese medicine: Tae-Yang, Tae-Um, So-yang, and So-Um. The result showed that silkworm powder has a tendency to reduce blood glucose level at fasting and at 2 hours after meal, and this trend was somewhat obvious in the Tae-Um body type. In summary, we reviewed scientific papers on the efficacy of silkworm powder and its purified DNJ as a blood glucose-lowering agent. These suggest that silkworm powder truly possesses blood glucose-lowering effect as documented in the traditional Chinese medicine, although further researches will be required to develop them as "medical" resource instead of functional food.

Improving Transmission Performance of Real Time Traffic in HMIPv6 (HMIPv6에서 실시간 트래픽의 전송 성능 향상 방안)

  • Park, Won-Gil;Kim, Byung-Gi
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.31 no.11B
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    • pp.960-968
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    • 2006
  • HMIPv6 improved the handover management of basic MIPv6 by introducing the new protocol agent MAP. In this new protocol, MAP instead of the Mobile Node intercepts all packets and redirects the packets to CoA of the Mobile Node. However, this process may degrade the network performance due to the centralization phenomenon of registration occurring in the hierarchical MAP structure. ffe propose two schemes to improve real time traffic performance. First proposal is a MAP selection mettled in which MAP is selected based on traffic characteristics. And we also propose differentiated traffic processing scheme with multi-level queues when Home Agent or Correspondent Nodes process Binding Update messages. Performances of the proposed scheme are analyzed. Analysis result shows that our model has good performance in the respect of location update cost and total cost of Mobile Nodes.

Manufacture of Water-Resistant Corrugated Board Boxes for Agricultural Products in the Cold Chain System(II) - Application Methods of Chemicals for Improving Water and Moisture Resistance of Corrugated Boards - (농산물 저온유통용 내수 골판지 상자의 제조(제2보) - 골판지의 내수 및 내습성 향상을 위한 약품 적용 방법 -)

  • Jo, Jung-Yeon;Min, Choon-Ki;Shin, Jun-Seop
    • Proceedings of the Korea Technical Association of the Pulp and Paper Industry Conference
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    • 2004.04a
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    • pp.192-210
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    • 2004
  • Application methods of chemicals were investigated tn minimize strength reduction of corrugated boards under the high humidity environment encountered in the cold chain system. Starch insolubilizers were introduced in the starch solution preparation of the Stain hall method and their insolubilization effect of starch binder were estimated. The performance of water repellent agents(WRA) and moisture proof agents(MPA) were evaluated in terms of water and moisture resistance. And effects of the combination of the chemicals and the coating method were also examined. Addition of the polyamine polyamide insolubilizer to the main part in the Stain hall process improved the binding force and water resistance of starch, which contributed to minimize the strength reduction of paper under the high humidity environment. AZC and Glyoxal type insolubilizers could not be used in the experiment due to an excessively increased viscosity of starch solution and the poor stability. Conventional WRA treatment to the base paper enhanced water and moisture resistance very slightly even though water repellency of the paper reached R10 by the treatment. MPA showed excellent performance than WRA not only in water and moisture resistance but in water repellency. Double coating on paper with MPA was more effective than the single coating at the same coating weight. A newly developed MPA showed excellent performance and runnability only by a single coating instead of a double coating.

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Dialysis Related Treatment to Increase Elimination of Toxic Agent (독성 물질 제거에 있어서 투석과 연관된 치료)

  • Kim, Heung-Soo;Shin, Gyu-Tae
    • Journal of The Korean Society of Clinical Toxicology
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    • v.1 no.1
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    • pp.6-11
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    • 2003
  • Various forms of dialytic techniques are available for detoxification. Hemodialysis, hemoperfusion and hemofiltration (hemodialfiltration) are the main treatment modalities. Because these modalities are rather invasive and expensive, it must be decided in balance of the risk and benefit to the patient. The prime consideration in the decision is based on the clinical features of poisoning; hemodialysis or hemoperfusion should be considered in general if the patient's condition progressively deteriorates despite intensive supportive therapy. The hemodialysis technique relies on passage of the toxic agent through a semipermeable membrane so that it can equilibrate with the dialysate and subsequently removed. It needs a blood pump to pass blood next to a dialysis membrane, which allows agents permeable to the membrane to pass through and reach equilibrium. Solute (or drug) removal by dialysis has numerous determinants such as solute size, its lipid solubility, the degree to which it is protein bound, its volume of distribution etc. The technique of hemoperfusion is similar to hemodialysis except there is no dialysis membrane or dialysate involved in the procedure. The patient's blood is pumped through a perfusion cartridge, where it is in direct contact with adsorptive material (usually activated charcoal) that has a coating material such as cellulose. This method can be used successfully with lipid-soluble compounds and with higher-molecular-weight compounds than for hemodialysis. Protein binding does not significantly interfere with removal by hemoperfusion. In conclusion, hemodialysis, hemoperfusion and hemofiltration can be used effectively as adjuncts to the management of severely intoxicated patients.

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Tumor Uptake Rate of Alkaline $^{99m}Tc-DMSA$ in Walker Carcinosarcoma 256 Bearing Wistar Rats (염기성 $^{99m}Tc-DMSA$의 Walker 256 암육종 이식백서에서 종양섭취율에 관한 연구)

  • Lim, S.M.;Hong, S.W.;Awh, O.D.;Lee, M.C.;Koh, C.S.
    • The Korean Journal of Nuclear Medicine
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    • v.22 no.1
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    • pp.65-76
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    • 1988
  • High affinity complexes for the tumor were obtained by changing pH and composition in the preparation of $^{99m}Tc-DMSA$. The purpose of this study was to investigate the tumor affinity, and in vitro and in vivo characteristics of these complexes. The results obtained were as follows; 1) Tumor imaging agent was formed successfully at pH $6.0\sim9.0$ and renal imaging agent at pH $2.0\sim5.0$. 2) The serum protein binding of $^{99m}Tc-DMSA$ was $89.1\sim92.8%$ at pH $2.0\sim5.0$ and $11.8\sim30.5%$ at pH $6.0\sim9.0$ respectively, and it was not changed with time. 3) The T 1/2 of tumor affinity complex in blood between 3 and 6 hours after injection was $187{\pm}29$ minutes $(mean{\pm}SD)$. 4) In the blood, the radioactivity was mainly in the plasma, and less than 1% was in the cellular components. 5) In the Walker carcinosarcoma 256 bearing Wistar rats, the radioactivity in the kidney increased, and decreased in the skeleton with time. The radioactivity in the tumor showed the peak in 6 hours after injection and decreased thereafter. 6) In the tumor cell, the radioactivity localized mainly in the cytosol, the soluble fraction of the cytoplasm. This study provides the basic knowledge about tumor affinity and usefulness of $^{99m}Tc-DMSA$ in the diagnosis of malignant disease.

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Anti-Diabetic Effects of Dung Beetle Glycosaminoglycan on db Mice and Gene Expression Profiling

  • Ahn, Mi Young;Kim, Ban Ji;Yoon, Hyung Joo;Hwang, Jae Sam;Park, Kun-Koo
    • Toxicological Research
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    • v.34 no.2
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    • pp.151-162
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    • 2018
  • Anti-diabetes activity of Catharsius molossus (Ca, a type of dung beetle) glycosaminoglycan (G) was evaluated to reduce glucose, creatinine kinase, triglyceride and free fatty acid levels in db mice. Diabetic mice in six groups were administrated intraperitoneally: Db heterozygous (Normal), Db homozygous (CON), Heuchys sanguinea glycosaminoglycan (HEG, 5 mg/kg), dung beetle glycosaminoglycan (CaG, 5 mg/kg), bumblebee (Bombus ignitus) queen glycosaminoglycan (IQG, 5 mg/kg) and metformin (10 mg/kg), for 1 month. Biochemical analyses in the serum were evaluated to determine their anti-diabetic and anti-inflammatory actions in db mice after 1 month treatment with HEG, CaG or IQG treatments. Blood glucose level was decreased by treatment with CaG. CaG produced significant anti-diabetic actions by inhiting creatinine kinase and alkaline phosphatase levels. As diabetic parameters, serum glucose level, total cholesterol and triglyceride were significantly decreased in CaG5-treated group compared to the controls. Dung beetle glycosaminoglycan, compared to the control, could be a potential therapeutic agent with anti-diabetic activity in diabetic mice. CaG5-treated group, compared to the control, showed the up-regulation of 48 genes including mitochondrial yen coded tRNA lysine (mt-TK), cytochrome P450, family 8/2, subfamily b, polypeptide 1 (Cyp8b1), and down-regulation of 79 genes including S100 calcium binding protein A9 (S100a9) and immunoglobulin kappa chain complex (Igk), and 3-hydroxy-3-methylglutaryl-CoenzymeAsynthase1 (Hmgcs1). Moreover, mitochondrial thymidine kinase (mt-TK), was up-regulated, and calgranulin A (S100a9) were down-regulated by CaG5 treatment, indicating a potential therapeutic use for anti-diabetic agent.