• 공업화학
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• 제5권3호
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• pp.524-536
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• 1994

생체적합성이 좋은 천연고분자인 chitosan에 수용성의 비닐계 단량체인 polyethyleneglycol monomethacrylate series를 그라프트중합시켜 그 반응조건과 물성을 검토하였다. 그라프트중합은 ethylene oxide 부가몰수에 따라 PE-90, PE-200, PE-350의 세 가지 단량체에 ceric ammonium nitrate(CAN)를 개시제로 사용하였으며, 중합에서 개시제의 농도, 단량체의 농도, 반응온도, 반응시간이 총전환율, 그라프트율, 그라프트효율에 미치는 영향을 조사하여 최적조건을 규명하였다. 반응은 개시제농도 $4{\sim}5{\times}10^{-3}M$, 단량체농도 0.5~0.6M, 반응시간 2~3시간, 반응온도 $40^{\circ}C$에서 최고의 그라프트율과 총전환율을 나타냈다. 합성한 공중합체의 열적 성질, 용해성 및 점성도를 검토한 결과 고농도의 개시제를 사용하면 그라프트 중합체는 chitosan의 특성을 급격히 감소시켰다. 고유점성도의 경우, chitosan-g-PE-90이 2.81dl/g, chitosan-g-PE-200이 3.01dl/g, chitosan-g-PE-350이 4.93d1/g으로 증가하는 경향이 나타났다. 공중합체를 막으로 성형하여 그라프트율과 polyethyleneglycol monomethacrylates의 ethylene oxide 부가몰수에 따른 공중합체의 기계적 물성과 함수율을 측정하였다. 가교화 공중합체막은 150분 이내에 함수율이 평형에 이르렀다. 공중합체의 물성은 그라프트율과 ethylene oxide 부가몰수의 영향을 받았으며 chitosan의 기계적 물성과 함수율이 공중합체에서 증가되었음을 확인하였으며 그라프트율이 증가함에 따라 vitamin $B_{12}$의 투과량도 증가하였다.

• Macromolecular Research
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• 제17권10호
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• pp.734-738
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• 2009

Biodegradable, pH-sensitive, glycol chitosan (GC) hydrogels were prepared using divinyl adipate (DVA) as a crosslinker and acetic acid as a catalyst. DVA has highly reactive double vinyl ester groups and GC contains a high density of hydroxyl groups, with two in every glucosamine unit. The transesterification reaction between vinyl esters and hydroxyl groups produced crosslinked GC hydrogels. The initial crosslinking reaction was monitored by measuring the viscosity of the reaction mixture. When DVA was added to the GC solution and heated to $50^{\circ}C$, the viscosity of the GC solution gradually increased, implying a crosslinking reaction and hydrogel formation. A new peak from the ester group was observed in the FTIR spectra of the GC hydrogels, confirming the crosslinking reaction. The synthesized GC hydrogel showed pH-dependent water absorbency, mainly due to the presence of amine groups ($-NH_2$) at the C-2 position of the glucosamine unit of GC. The water absorbency greatly increased at acidic pH and slightly decreased at alkaline pH. The GC hydrogel gradually degraded in $37^{\circ}C$ water due to hydrolysis of the ester bonds, which were intermolecular crosslinking sites. A red dye, 5-carboxyltetramethyl-rhodamine (CTMR), was entrapped in the GC hydrogels as a model compound. CTMR was released from GC hydrogels in two steps: an initial burst release mainly due to desorption and diffusion, and a second sustained release possibly due to gradual degradation.

• Macromolecular Research
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• 제14권5호
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• pp.573-578
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• 2006

Three different, polymer-platinum conjugates (hydrogels, microparticles, and nanoparticles) were synthesized by complexation of cis-dichlorodiammineplatinum(II) (cisplatin) with partially succinylated glycol chitbsan (PSGC). Succinic anhydride was used as a linker to introduce cisplatin to glycol chitosan (GC). Succinylation of GC was investigated systematically as a function of the molar ratio of succinic anhydride to glucosamine, the methanol content in the reaction media, and the reaction temperature. By controlling the reaction conditions, water-soluble, partially water-soluble, and hydrogel-forming PSGCs were synthesized, and then conjugated with cisplatin. The complexation of cisplatin with water-soluble PSGC via a ligand exchange reaction of platinum from chloride to the carboxylates induced the formation of nano-sized aggregates in aqueous media. The hydrodynamic diameters of PSGC/cisplatin complex nano-aggregates, as determined by light scattering, were 180-300 nm and the critical aggregation concentrations (CACs), as determined by a fluorescence technique using pyrene as a probe, were $20-30{\mu}g/mL$. The conjugation of cisplatin with partially water-soluble PSGC, i.e., borderline between water-soluble and water-insoluble PSGC, produced micro-sized particles $<500{\mu}m$. Cisplatin-complexed PSGC hydrogels were prepared from water-insoluble PSGCs. All of the cisplatin-incorporated, polymer matrices released platinum in a sustained manner without any significant initial burst, suggesting that they may all be useful as slow release systems for cisplatin. The release rate of platinum increased with the morphology changes from hydrogel through microparticle to nanoparticle systems.

• 공업화학
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• 제7권1호
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• pp.59-66
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• 1996

양말단에 아미노기가 결합된 일련의 bisamino-PEG($Jeffamine^{(R)}ED$)를 함유한 키토산 비드들을 알칼리 용액을 사용한 capillary extrusion method에 의해 제조하였다. 제조된 각각의 비드들에 대한 swelling kinetics를 조사한 결과, 키토산비드 내부에 PEG 사슬이 길어질수록 팽윤이 늦게 진행되었다. 또한 키토산 비드에 함유된 bisamino-PEG들의 방출현상을 정량적으로 알아 보기 위해 양말단의 1차 아민기에 fluorescamine을 결합시킨 후, UV spectra로 방출과정을 추적하였다. 실험결과 키토산 비드 내부에 있는 PEG 사슬이 길수록 방출시간은 $Jeffamine^{(R)}ED$-600 < $Jeffamine^{(R)}ED$-900 < $Jeffamine^{(R)}ED$-2001 순으로 지연되는 경향을 나타내었다. 이는 PEG 사슬이 길어질수록 키토산과의 수소결합에 의한 상호작용이 강화되고 그 결과 방출기간이 지연된 것으로 사료된다.

• Journal of Veterinary Science
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• 제25권2호
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• pp.30.1-30.16
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• 2024

Background: Biofilms, such as those from Staphylococcus epidermidis, are generally insensitive to traditional antimicrobial agents, making it difficult to inhibit their formation. Although quercetin has excellent antibiofilm effects, its clinical applications are limited by the lack of sustained and targeted release at the site of S. epidermidis infection. Objectives: Polyethylene glycol-quercetin nanoparticles (PQ-NPs)-loaded gelatin-N,O-carboxymethyl chitosan (N,O-CMCS) composite nanogels were prepared and assessed for the on-demand release potential for reducing S. epidermidis biofilm formation. Methods: The formation mechanism, physicochemical characterization, and antibiofilm activity of PQ-nanogels against S. epidermidis were studied. Results: Physicochemical characterization confirmed that PQ-nanogels had been prepared by the electrostatic interactions between gelatin and N,O-CMCS with sodium tripolyphosphate. The PQ-nanogels exhibited obvious pH and gelatinase-responsive to achieve on-demand release in the micro-environment (pH 5.5 and gelatinase) of S. epidermidis. In addition, PQ-nanogels had excellent antibiofilm activity, and the potential antibiofilm mechanism may enhance its antibiofilm activity by reducing its relative biofilm formation, surface hydrophobicity, exopolysaccharides production, and eDNA production. Conclusions: This study will guide the development of the dual responsiveness (pH and gelatinase) of nanogels to achieve on-demand release for reducing S. epidermidis biofilm formation.

• BMB Reports
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• 제44권3호
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• pp.193-198
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• 2011

The chitinase-producing strain SC081 was isolated from Korean traditional soy sauce and identified as Bacillus atrophaeus based on a phylogenetic analysis of the 16S rDNA sequence and a phenotypic analysis. A gene encoding chitinase from B. atrophaeus SC081 was cloned in Escherichia coli and was named SCChi-1 (GQ360078). The SCChi-1 nucleotide sequences were composed of 1788 base pairs and 596 amino acids, which were 92.6, 89.6, 89.3, and 78.9% identical to those of Bacillus subtilis (ABG57262), Bacillus pumilus (ABI15082), Bacillus amyloliquefaciens (ABO15008), and Bacillus licheniformis (ACF40833), respectively. A recombinant SCChi-1 containing a hexahistidine tag at the amino-terminus was constructed, overexpressed, and purified in E. coli to characterize SCChi-1. $H_6SCChi$-1 revealed a hydrolytic band on zymograms containing 0.1% glycol chitin and showed the highest lytic activity on colloidal chitin and acidic chitosan. The optimal temperature and pH for chitinolytic activity were $50^{\circ}C$ and pH 8.0, respectively.

• Journal of Microbiology and Biotechnology
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• 제14권2호
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• pp.337-343
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• 2004

A bacterial strain concurrently producing extracellular chitosanase and chitinase was isolated from soil and identified as a member of the $\beta$-subgroup of Proteobacteria through its 16S rRNA analysis and some biochemical analyses. The newly discovered strain, named as KNU3, had 99% homology of its 16S rRNA sequence with chitinolytic $\beta$-Proteobacterium CTE108. Strain KNU3 produced 34 kDa of chitosanase in addition to two chitinases of 68 kDa and 30 kDa, respectively. The purified chitosanase protein (ChoK) showed activity toward soluble, colloidal, and glycol chitosan, but did not exhibit any activity toward colloidal chitin. The optimum pH and temperature of ChoK were 6.0 and $70^{\circ}C$, respectively. The chitosanase was stable in the pH 4.0 to 8.0 range at $70^{\circ}C$, while enzyme activity was relatively stable at below $45^{\circ}C$. MALDI-TOF MS and N-terminal amino acid sequence analyses indicated that ChoK protein is related to chitosanases from Matsuebacter sp. and Sphingobacterium multivorum. HPLC analysis of chitosan lysates revealed that glucosamine tetramers and hexamers were the major products of hydrolysis.

• 폴리머
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• 제30권4호
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• pp.279-285
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• 2006

유전자 치료에 있어서 안전성의 장점을 지니고 있는 비바이러스성 전달체에 대한 관심도가 높아져가고 있다. 비바이러스성 전달체 중, 양이온성 리포좀이나 합성 유전자 전달체는 in vitro계에서 효율적인 DNA 전달체이지만, 낮은 생체적합성으로 인하여 in vivo 계에서의 응용성은 크게 뒤떨어지고 있다. 한편, 천연 양이온성 다당류인 키토산은 낮은 독성과 강한 양전하를 띠고 있어 유전자 전달 시스템 (gene delivery system)에 있어 아주 기대되는 전달체이다. 본 연구에서는 저분자량 수용성 키토산 (low molecular water-soluble chitosan ; LMWSC)을 이용하여 동맥 벽 세포를 표적할 수 있는 표적성 유전자 전달체를 합성하였다. 상대 점도와 Kina 적정법을 이용하여 LMWSC의 점도 평균 분자량 $(M_W)$과 탈아세틸화도 (degree of de acetylation ; DDA)를 측정하였고 구조는 FTIR, $^1H-NMR$, 그리고 $^{13}C-NMR$을 통하여 분석하였다. 동맥 벽을 표적하기 위한 유전자 전달체로서 pegylated LMWSC 의 말단에 특이성 세포 표적 펩타이드인 artery wall binding peptide (AWBP)를 결합시킴으로써 AWBP-PEG-g-LMWSC을 합성하였고 FTIR, $^1H-NMR$. zeta potentiometer. 그리고 atomic force microscopy (AFM)을 이용하여 분석하였다.

• KSBB Journal
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• 제25권3호
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• pp.297-302
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• 2010

Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drug with analgesic and antipyretic effects. The most common side effects from ketoprofen after oral administration are gastrointestinal irritation, diarrhea, abdominal pain and retention of fluid. Ketoprofen was formulated as water-soluble gels to reduce these side effects. To increase the skin permeability of ketoprofen, microsphere containing ketoprofen was prepared with chitosan and ploy-$\varepsilon$-caprolactone. And then prepared microsphere was manufactured as an adhesive hydrogel with polyvinylpyrrolidone K-25, polyethylene glycol 4000, and various permeation enhancers. The flux and permeability of ketoprofen were evaluated. As the concentration of tween 80 and enhancers increased, the flux of ketroprofen was accelerated. Also the permeation rate was facilitated by enhancers, but did not affect the lag time. From these results, the adhesive hydrogel using microsphere could be a good delivery system for ketoprofen to improve the skin permeation.

• Journal of Microbiology and Biotechnology
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• 제13권1호
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• pp.35-42
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• 2003

A 1,3 kb cellulase gene encoding novel bifunctional cellulase-chitosanase activity was cloned from biopolymer-producing alkali-tolerant B. lichenformis NBL420 in E. coli. A recombinant cellulase-chitosanase, named CelA, was expressed and purified to homogeneity. The activity staining and the enzymatic characterization of the purified CeIA revealed bifunctional activities on carboxymethyl cellulose (CMC) and glycol-chitosan. The similar characteristics of the enzymatic activities at the optimum pH, optimum temperature, and thermostability Indicated that CelA used a common catalytic domain with relaxed substrate specificity. A comparison of the deduced amino acids in the N-terminal region revealed that the mature CelA had a high homology with the previously identified bifunctional cellulase-chitosanase of Myxobacter sp. AL- 1.