• Title/Summary/Keyword: methoxy-polyethylene glycol

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Chemical Modification of Sheep Hemoglobin with Methoxy-Polyethylene Glycol

  • Jeong, Seong-Tae;Byun, Si-Myung
    • BMB Reports
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    • v.29 no.3
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    • pp.261-265
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    • 1996
  • Sheep hemoglobin (SHb) was modified with methoxy-polyethylene glycol (mPEG) to develop a potential blood substitute. mPEG has been used to decrease antigenicity and immunogenicity of foreign proteins. When the mPEG was attached to SHb, the modified hemoglobins showed decreased electrophoretic mobility on SDS-PAGE and decreased free amino groups. When the remaining free amino groups of mPEG modified SHb were determined by TNBS free amino group titration methods. about 34% of total free amino groups were modified with mPEG. This mPEG-SHb conjugate of 34% amino groups modified showed no precipitation by double immunodiffusion with polyclonal antibodies against SHb. This modified hemoglobin still has oxygen transport activity. So this antigenicity decreased hemoglobin may be used in humans as a potential blood substitute.

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Effect of Subcutaneous Methoxy Polyethylene Glycol-epoetin Beta on Anemia and Nutritional Indices in Peritoneal Dialysis Patients (복막투석 환자에서 Methoxy Polyethylene Glycol-epoetin Beta 피하 투여가 빈혈과 영양지표에 미치는 효과)

  • Kim, Kyung Sook;Lee, Jun Seop;Kim, Hye-Young;Lee, Myung Koo
    • Korean Journal of Clinical Pharmacy
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    • v.22 no.3
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    • pp.202-210
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    • 2012
  • Methoxy polyethylene glycol-epoetin beta (MPG-EPO), a continuous erythropoietin receptor activator, is a new erythropoiesis-stimulating agent with a long half-life. The purpose of this prospective study is to assess the effects of once-monthly subcutaneous MPG-EPO on hematological responses and nutritional status in peritoneal dialysis patients. Forty four patients undergoing stable peritoneal dialysis were enrolled into the study. Darbepoetin alfa therapy, in peritoneal dialysis patients, was converted to the monthly administration of subcutaneous MPG-EPO for 6 months. The starting dose of MPG-EPO was based on the previous weekly dose of darbepoetin alfa. The dose adjustments were performed to maintain the hemoglobin (Hb) levels in a target range of 10.5-11.0 g/dL. If the Hb levels exceeded 11.0 g/dL, MPG-EPO was temporarily interrupted for 1 month. The mean Hb levels were stable with the values of $9.5{\pm}1.1$ g/dL at baseline, and $10.4{\pm}0.9$ g/dL at the 6th month after conversion. The mean differences in the changes of Hb levels between the baseline and the 6th month were $0.9{\pm}1.4$ g/dL, which was statistically significant. However, the mean differences of iron, transferrin saturation and ferritin concentrations were not significant. It did not show significant differences in the changes of the nutritional parameters. These results suggest that the once-monthly subcutaneous administration of MPG-EPO for 6 months effectively maintains the Hb levels and nutritional status in peritoneal dialysis patients. Taken together, the once-monthly subcutaneous administration of MPG-EPO was practical and might improve the clinical compliance for the management of renal anemia in peritoneal dialysis patients.

Sustained Release of PLGylated G-CSF from PLGA Microsphere (PLGA 미립구로부터 PLGylated G-CSF의 서방성 방출)

  • 정경환;임형권;이시욱;강관엽;박태관
    • KSBB Journal
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    • v.17 no.1
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    • pp.33-37
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    • 2002
  • To improve in vitro release kinetic of G-CSF in PLGA microsphere, G-CSF was PEGylated with methoxy polyethylene glycol-aldehyde (mPEG-aldehyde, MW 5000). The majority of G-CSF was mono-PEGylated and it was characterized using SDS-PAGE, HPLC, and peptide mapping. The PLGA microencapsulation with the native, or PEGylated G-CSF was performed using W/O/w method, where the encapsulation efficiency was high. For the high loading of G-CSF to microsphere, G-CSF and PEGylated G-CSF were concentrated and then verified the protein stability using native gel and gel filtration chromatography. In comparison with native G-CSF, PEGylated G-CSF was released during the extended period and its maximum amount of released G-CSF was also increased.

Synthesis and Application of Caffeic Acid Methoxy Polyethylene Glycol Ester (카페산 메톡시 폴리에틸렌글리콜 에스테르의 합성 및 응용)

  • Lee, Hyun-Gi;Jeong, Noh-Hee
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.3
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    • pp.259-266
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    • 2011
  • Caffeic acid is a kind of phytochemicals occurred in coffee, which is worked as a carcinogenesis restrainer and antioxidants on the human body. In this study, as one type of caffeic acid derivatives, methoxypolyethylene glycol caffeate(MPC) was synthesized by the esterification between caffeic acid and methoxypolyethylene glycol with N,N'-dicyclohexyl carbodiimide, 4-dimethylamino pyridine. The synthesized product was confirmed by using FT-IR and $^1H$-NMR, thin-layer chromatography. And these compound was investigated as antioxidant, Tyrosinase hindrance and skin moisturizers. In the free radical scavenging study, antioxidant effect of MPC was averagely high than the red ginseng extract that be used as a natural antioxidants. The result of Tyrosinase anti-activity test was better than embryo bud of rice extract at low concentration. At the iNOS anti-activity tested by using Raw 264.7 cell, and confirmed anti-inflammatory function. For the MPC handled with sodium lauryl sulfate, was tested for the skin moisture content and skin moisture loss.

Synthesis and Biological Evaluation of Water-Soluble Oleanolic Acid Derivatives for use as Melanogenesis Inhibitors (멜라닌 생합성 억제제로서 수용성 Oleanolic Acid 유도체의 합성 및 활성 평가)

  • An, Hyun-Jin;Yoon, Young-kyung;Lee, Jae-Duck;Jeong, Noh-Hee
    • Applied Chemistry for Engineering
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    • v.31 no.6
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    • pp.653-659
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    • 2020
  • This study was focused on the synthesis of methoxy polyethylene glycol-oleanolic acid ester (mPEG-OA derivative) and investigation of its water solubility and anti-melanogenic effects. mPEG-OA derivative was identified by 1H and 13C NMR and FT-IR spectroscopic measurements. The water solubilities of mPEG-OA derivative and OA were found to be 13 and 0.013 mg/mL and that of mPEG-OA was found to be 1000-fold higher than that of OA. The effects of mPEG-OA derivative and OA on cell viability were measured using B16F10 melanoma cells. The viability of cells treated with mPEG-OA derivative (250 μM) increased 4-fold compared to that of cells treated with OA (62.5 μM). At mPEG-OA derivative and OA concentrations where the cell viability was unaffected, the inhibitory effect of mPEG-OA derivative and OA on the melanogenesis in B16F10 melanoma cells were 36 and 35% at 50 and 10 μM, respectively. The expression level of microphthalmia-associated transcription (MITF) was also reduced in B16F10 melanoma cells treated with mPEG-OA and OA. Overall, mPEG-OA derivative showed excellent water solubility and inhibitory effects of the melanogenesis, which could be used as a potential formulation for use in whitening functional cosmetic material.

Thin-Film Composite (TFC) Membranes with Hydrophilic Ethyl Cellulose-g-poly(ethylene glycol) (EP) Substrates for Forward Osmosis (FO) Application (친수성을 가지는 에틸셀룰로스-폴리에틸렌글리콜 가지형 고분자의 정삼투 복합막 지지층으로의 응용)

  • Yu, Yun Ah;Kim, Jin-joo;Kang, Hyo;Lee, Jong-Chan
    • Korean Chemical Engineering Research
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    • v.54 no.4
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    • pp.510-518
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    • 2016
  • Ethyl cellulose-g-poly(ethylene glycol) (EP) was synthesized by esterification of carboxylic acid functionalized methoxy polyethylene glycol (MPEG-COOH) with ethyl cellulose (EC) in order to develop a hydrophilic substrate for thin-film composite (TFC) membrane in a forward osmosis (FO) system. A porous EP substrate, fabricated by a non-solvent induced phase separation method, was found to be more hydrophilic than the EC substrate due to the presence of polyethylene glycol (PEG) side chains in the EP. Since the EP substrate exhibits smaller water contact angles and higher porosity, the structural parameter (S) of TFC-EP is smaller than that of TFC-EC, indicating that internal concentration polarization (ICP) within porous substrates can occur less when TFC-EP is used as a membrane. For example, the water flux value of the TFC-EP is 15.7 LMH, whereas the water flux value of the TFC-EC is only 6.6 LMH. Therefore, we strongly believe that the TFC-EP could be a promising candidate with good FO performances.

Supramolecular Hydrogels Instantaneously Formed by Inclusion Complexation between Amphiphilic Oligomers and $\alpha$-Cyclodextrins

  • Zhao, Sanping;Lee, Jong-Hwi
    • Macromolecular Research
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    • v.17 no.3
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    • pp.156-162
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    • 2009
  • Supramolecular hydrogels were instantaneously fabricated by mixing aqueous solutions of $\alpha$-cyclodextrins ($\alpha$-CDs) and amphiphilic methoxy (polyethylene glycol) (MPEG)-$\varepsilon$-caprolactone (CL) oligomer, which was synthesized via the ring-opening polymerization of the CL monomer using low-molecular-weight MPEG ($M_n$ of MPEG=2,000 g/mol) as an initiator. The supramolecular structure of the hydrogels was revealed by X-ray diffraction (XRD) analyses. Rheological studies of the hydrogels revealed an elastic character when the number of CL units in the oligomer was more than 2, and the obtained hydrogels showed high storage modulus but relatively low shearing viscosity due to the low-molecular-weight character of the oligomer, which was more preferable for use as an injectable delivery system. The physical properties of the hydrogels could be modulated by controlling the chain morphology and concentration of the oligomers, as well as the feed molar ratio of the oligomer to $\alpha$-CD. The components of the supramolecular hydrogels are biocompatible and can readily be eliminated from the body. These features render the supramolecular hydro gels suitable as drug delivery systems and tissue engineering scaffolds.

The Effects of the Coplymerization Conditions in Synthesis of Polycarboxylic Type Superplasticizer on Interfacial Properties and on Cement Mortar Fluidity (Polycarboxylate계 콘크리트 유동화제의 합성에 있어서 공중합 조건에 따른 계면물성 변화 및 이의 시멘트 몰탈의 물성에 미치는 영향)

  • Kim, Young-Ho
    • Applied Chemistry for Engineering
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    • v.21 no.4
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    • pp.463-468
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    • 2010
  • The polycarboxylic (PC) type concrete superplasticizer was synthesized. The effects of ethylene oxide group number and its molecular weight on the properties of the polycarboxylic type concrete superplasticizer and the concrete motar properties were studied. To investigated of the interfacial properties of the premixed-concrete with the superplasticizer, the type and the amount of polyethylene glycol, meta acrylate added, and type of the initialization agent were studied. Also the interfacial properties of the superplasticizer aqueous phase, the wettability on the cement particle, the fluidity of the cement mortar, and the strength properties of the concrete were measured. For a high fluidity of the cement mortar and a high strength of concrete, a low value of the surface tension and contact angle were required for PC. To have a good performance for PC, the reaction condition of 1.3 mol ratio of MA against to MPEG was suitable with KSP initiator.

Effect of Unsaturation on the Stability of C18 Polyunsaturated Fatty Acids Vesicles Suspension in Aqueous Solution

  • Teo, Yin Yin;Misran, Misni;Low, Kah Hin;Zain, Sharifuddin Md.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.1
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    • pp.59-64
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    • 2011
  • Degree of unsaturation in fatty acid molecules plays an important role in the formation of vesicles. Vesicle formation from C18 fatty acids with different amount of double bonds such as oleic acid, linoleic acid and linolenic acid with the incorporation of 1,2-dipalmitoyl-sn-glycerol-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DPPE-PEG2000) have been examined by TEM. Critical vesicular concentrations (CVC) of the vesicle suspension are determined by turbidity and surface tension methods. The CVC of fatty acids increases when the amount of unsaturation in the alkyl chain increases. On the other hand, stability of vesicle suspension has been examined by using particle size and zeta potential at $30^{\circ}C$. There was a dramatic decrease in particle size measurement from mono-unsaturation to tri-unsaturation which could be due to the effect of fluidity in the membrane bilayer caused by different degree of unsaturation. The values of zeta potential for vesicles that were formed without the incorporation of DPPE-PEG2000 were in the range of -70 mV to -100 mV. It has been observed that the incorporation of DPPEPEG2000 to the vesicle reduces the magnitude of zeta potential. However, this phenomenon does not obviously seen in fatty acid vesicles formed by linoleate-linoleic acid and linolenate-linolenic acid. We therefore conclude that the addition of DPPE-PEG2000 does not effectively improve the stability of the linoleate-linoleic acid and linolenatelinolenic acid vesicle at pH 9.0 after the evaluation of their particle size and zeta potential over a period of 30 days. Although the vesicles formed were not stable for more than 10 days, they have displayed the potential in encapsulating the active ingredients such as vitamin E and calcein. The results show that the loading efficiencies of vitamin E are of encouraging value.

Amphotericin B Aggregation Inhibition with Novel Nanoparticles Prepared with Poly(${\varepsilon}$-caprolactone)/Poly(N,N-dimethylamino-2-ethyl methacrylate) Diblock Copolymer

  • Shim, Yong-Ho;Kim, You-Chan;Lee, Hong-Joo;Bougard, Francois;Dubois, Philippe;Choi, Ki-Choon;Chung, Chung-Wook;Kang, Dae-Hwan;Jeong, Young-Il
    • Journal of Microbiology and Biotechnology
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    • v.21 no.1
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    • pp.28-36
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    • 2011
  • Diblock copolymers composed of poly(${\varepsilon}$-caprolactone) (PCL) and poly(N,N-dimethylamino-2-ethyl methacrylate) (PDMAEMA), or methoxy polyethylene glycol(PEG), were synthesized via a combination of ring-opening polymerization and atom-transfer radical polymerization in order to prepare polymeric nanoparticles as an antifungal drug carrier. Amphotericin B (AmB), a natural antibiotic, was incorporated into the polymeric nanoparticles. The physical properties of AmB-incorporated polymeric nanoparticles with PCL-b-PDMAEMA and PCL-b-PEG were studied in relation to morphology and particle size. In the aggregation state study, AmB-incorporated PCL-b- PDMAEMA nanoparticles exhibited a monomeric state pattern of free AmB, whereas AmB-incorporated PCL-b- PEG nanoparticles displayed an aggregated pattern. In in vitro hemolysis tests with human red blood cells, AmBincorporated PCL-b-PDMAEMA nanoparticles were seen to be 10 times less cytotoxic than free AmB (5 ${\mu}g$/ml). In addition, an improved antifungal activity of AmBincorporated polymeric nanoparticles was observed through antifungal activity tests using Candida albicans, whereas polymeric nanoparticles themselves were seen not to affect activity. Finally, in vitro AmB release studies were conducted, proving the potential of AmB-incorporated PCL-b-PDMAEMA nanoparticles as a new formulation candidate for AmB.