• Bulletin of the Korean Chemical Society
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• 제3권4호
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• pp.167-168
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• 1982

• Archives of Pharmacal Research
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• 제29권12호
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• pp.1164-1170
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• 2006

A triptolide-lysozyme (TP-LZM) conjugate was synthesized to achieve renal specific delivery and to reduce the side effects of triptolide. Triptolide was coupled to lysozyme through succinic via an ester bond with an average coupling degree of 1 mol triptolide per 1 mol lysozyme. The lysozyme can specifically accumulate in the proximal tubular cells of the kidney, making it a potential carrier for targeting drugs to the kidney. The structure of triptolide succinate (TPS) was confirmed by IR, $^{1}H-NMR$, MS and UV. The concentrations of triptolide in various samples were determined by reversed-phase high-performance liquid chromatography (HPLC). In this study, the physicochemical and stability profiles of TP-LZM under various conditions were investgated the stability and releasing profiles of triptolide-lysozyme (TP-LZM) under various conditions. In vitro release trails showed triptolide-lysozyme was relatively stable in plasma (less than 30% of free triptolide released) and could release triptolide quickly in lysosome (more than 80% of free triptolide released) at $37^{\circ}C$ for 24 h. In addition, the biological activities of the conjugate on normal rat kidney proximal tubular cells (NRK52E) were also tested. The conjugate can effectively reduce NO production in the medium of NRK52E induced by lipopolysaccharide (LPS) but with much lower toxicity. These studies suggest the possibility to promote curative effect and reduce its extra-renal toxicity of triptolide by TP-LZM conjugate.

• 대한교통학회지
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• 제23권3호
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• pp.61-71
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• 2005

본 연구는 Conjugate Gradient법을 적용하여 개발한 관측교통량기반 기종점 OD행렬 추정모형이 대규모 가로망에서도 적용 가능성이 있는지를 판단하기 위하여 246개죤 기준 전국 가로망에 적용하여 적용성 및 활용가능성을 판단해 보았다. 대규모 가로망에서 모형의 일치성을 분석한 결과, 모형의 상위수준과 하위수준이 내부적으로 유기적인 관계를 유지하고 있는 것으로 분석되었다. 관측링크 개수에 따라 모형의 추정력을 분석한 결과 교통량 오차는 허용오차 범위내에서 추정력을 확보하는 것으로 나z타났다. 또한 추정 기종점 OD행렬의 추정력 역시 기존의 모형을 이용한 결과치보다는 양호한 추정력을 보이고 있는 것으로 분석되었다. 더 많은 다양한 실험을 하여 개발된 모형의 알고리즘의 안정성이 확보된다면 대규모 가로망에서도 적용 가능성이 있다고 판단된다.

• 한국통신학회논문지
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• 제19권4호
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• pp.772-780
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• 1994

2-채널 결합 코드북을 사용한 벡터 양자화는 계산의 복잡성과 코드북의 기억용량을 줄일 수 있는 효과적인 방법으로 연구되었다. 본 논문에서는 FSVQ를 할 땐 나타나는 상태-코드북의 수를 줄이기 위한 방법으로 2-채널 결합 코드북을 이용하는 방법을 제안하였다. 2-채널 결합 벡터 양자화에서 입력벡터는 각 코드북의 상태데 따른 상태-코드북을 이용하여 부호화를 한다. 그리고 블록 부호화에서 나타나는 블록화 현상을 줄이며 높은 부호화 이득을 얻기 위한 방법으로 LOT를 적용하였다. 결과로 FSVQ는 일반적 벡터 양자화에 비하여 보다 높은 데이터 압축율을 얻을 수 있지만 매우 많은 상태 코드북을 가지는 단점을 가지고 있다. 그러나 2-채널 결합 코드북을 이용한 FSVQ는 하나의 코드북을 사용한 기존의 FSVQ에 비하여 PSNR면에서는 약간의 손실이 있다는 단점을 가지지만 상태-코드북의 수를 현저히 감소시킬 수 있는 장점을 갖는다. 그리고 공간영역 신호에서의 FSVQ보다 LOT영역 신호에서의 FSVQ는 블록화를 줄일 수 있을 뿐 아니라 보다 높은 PSNR을 얻을 수 있는 효율적인 방법으로 나타났다.

• 대한기계학회논문집A
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• 제22권2호
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• pp.278-288
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• 1998

An efficient and useful method to improve the local stress field in a displacement-formulated finite element solution has been proposed using the theory of conjugate approximations for a stress field and the Loubignac's iterative method for a displacement field. Validity of the proposed method has been tested through three test examples, to improve the stress field and displacement field in the whole domain and the local regions. As a result of analysis on the test examples, it is found that the stress field in the local regions are approximated to those in the whole domain within a few iterations which have satisfied the original finite element equilibrium equation. In addition, it is found that the local stress field are by far better approximated to the exact stress field than the displacement-based stress field with the reduction of the finite-element mesh-size.

• Macromolecular Research
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• 제12권5호
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• pp.534-539
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• 2004

Two biopolymers, silk fibroin (SF) and chitosan, were conjugated by tyrosinase (EC 1.14.18.1), a polyphenolic oxidase, to improve their physicochemical properties, such as their thermal properties and morphological stabilities in organic solvents. The crosslinking between SF and chitosan took place mainly through Michael addition reactions. A main reaction between the amino groups in chitosan and o-quinone, the oxidation product of the tyrosyl residue in SF, was confirmed by UV spectroscopy. Measurements of viscosity and light scattering indicated that the crosslinked SF/chitosan conjugate was compact: it had a smaller particle size because of tight bonding forces between the SF and chitosan molecular chains. Thermal decomposition of SF/chitosan conjugates crosslinked by tyrosinase occurred at higher temperatures. The adhesiveness of the SF/chitosan conjugates decreased steadily as the crosslinking reaction progressed. We propose that this new crosslinking method be used for the preparation of silk fibroin/chitosan conjugates using tyrosinase. We expect that SF/chitosan conjugates crosslinked by tyrosinase can be used preferentially in biomedical applications because of its unique properties and non-toxicity.

• Archives of Pharmacal Research
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• 제29권10호
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• pp.840-844
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• 2006

For the exploration of pharmacophoric moiety of malloapelta B (1) possessing the inhibitory activity of $NF-{\kappa}B$ activation, structural variation of ${\alpha},{\beta}-unsaturated$ carbonyl motif was attempted. 1 was reduced by catalytic hydrogenation, sodium borohydride, and lithium aluminumhydride. Catalytic hydrogenation with 30 psi or 15 psi of $H_2$ gas of 1 generated 8-butyl-5,7-dimethoxy-2,2-dimethylchroman (2) and 1-(5,7-dimethoxy-2,2-dimethylchroman-8-yl)butan-1-one (3), respectively. Reduction with sodium borohydride occurred at the double bond of ${\alpha},{\beta}-unsaturated$ ketone of 1 to give 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)butan-1-one (4). Reduction of 1 with lithium aluminumhydride and then quenched with methanol and water produced unexpected products, 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-methoxy-1-butene (5) and 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-hydroxy-1-butene (6). These are formed from the isomerization of initial product 9 through the continuous conjugate carbocation intermediate 11. Addition of ethylmagnesium bromide and dimethyl malonate anion to 1 gave the conjugate adducts 7 and 8. Ethylmagesium bromide and sodium borohydride reduction unusually gave the conjugate addition due to steric congestion around carbonyl group of 1. Compound 2 exhibits the reduced inhibitory activity against $NF-{\kappa}B$ activation and the others do not show the activity. Therefore ${\alpha},{\beta}-unsaturated$ carbonyl group of 1 should be important for its inhibitory activity.

• Toxicological Research
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• 제11권2호
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• pp.295-302
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• 1995

Menadione-ghitathione conjugate (MEN-SG), a metabolite of menadione, is known to be a redoxcycler in rat hepatocyte subcellular fraction. Therefore, it was assumed that MEN-SG could exert cytotoxlclty to ral platelets, another target tissue of menadione. We first synthesized MEN-SG, the identity of which was verified by mass, $^1{H}$-NMR and UV-visible spectra. In addition, the stability of MEN-SG was investigated in biological assay system. MEN-SG was degraded in a time-dependent manner in DMSO which had been used as a vehicle and thus, tris-HCl buffer was used as a vehicle of MEN-SG despite the low solubility in it. Perchloric acid as well as platelets itself did not affect the stability of MEN-SG. Our next attempt was the evaluation of cytotoxicity of MEN-SG in rat platelets. MEN-SG did not induce cytotoxicity to rat platelets measured by two different methods, LDH release and turbidity changes. The extents of oxygen consumption by MEN-SG in intact platelets were significantly lower than those by menadione, though it had been observed that oxygen consumptions by menadione and MENSG were similar in subcellular fractioas of platelets. These results suggest that MEN-SG is not toxic to rat platelets despite its redox cycling capacity and glutathione conjugation reaction of menadione could be regarded as a detoxification process.

• 지구물리와물리탐사
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• 제10권2호
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• pp.147-153
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• 2007

CG (conjugate gradient) 법은 선형 연립방정식을 반복적으로 푸는 가장 효율적인 해법 중 하나이고, 또한 비선형 최소자승문제에도 적용할 수 있다. 자기지전류(MT) 역산 문제를 풀 때에는 최소자승문제의 목적함수 자체의 최소화에 직접 CG 법을 적용하거나, Gauss-Newton 법에 기초한 반복역산의 각 반복단계에서 모형의 변화량 계산에 CG 법을 이용할 수 있다. CG 법을 적용할 경우, 임의의 벡터에 대한 감도행렬의 영향 및 그 전치행렬의 전치행렬의 영향을 감도행렬을 직접 구하지 않고 계산할 수 있다는 장점이 있기 때문에 감도행렬의 계산 규모가 방대한 3차원 역산 문제에서 계산시간을 월등히 줄일 수 있다.

• Journal of Microbiology and Biotechnology
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• 제28권12호
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• pp.2113-2120
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• 2018

Cross-reactive material 197 ($CRM_{197}$) is a non-toxic mutant of diphtheria toxin containing a single amino acid substitution of glycine 52 with glutamic acid. $CRM_{197}$ has been used as a carrier protein for poorly immunogenic polysaccharide antigens to improve immune responses. In this study, to develop a sandwich ELISA that can detect $CRM_{197}$ and $CRM_{197}$ conjugate vaccines, we generated a human anti-$CRM_{197}$ monoclonal antibody (mAb) 3F9 using a phage-displayed human synthetic Fab library and produced mouse anti-$CRM_{197}$ polyclonal antibody. The affinity ($K_D$) of 3F9 for $CRM_{197}$ was 3.55 nM, based on Bio-Layer interferometry, and it bound specifically to the B fragment of $CRM_{197}$. The sandwich ELISA was carried out using 3F9 as a capture antibody and the mouse polyclonal antibody as a detection antibody. The detection limit of the sandwich ELISA was <1 ng/ml $CRM_{197}$. In addition, the 3F9 antibody bound to the $CRM_{197}$-polysaccharide conjugates tested in a dose-dependent manner. This ELISA system will be useful for the quantification and characterization of $CRM_{197}$ and $CRM_{197}$ conjugate vaccines. To our knowledge, this study is the first to generate a human monoclonal antibody against $CRM_{197}$ and to develop a sandwich ELISA for $CRM_{197}$ conjugate vaccines.