• The KIPS Transactions:PartB
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• v.8B no.6
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• pp.669-674
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• 2001

In order to reflect the aggregation situation in the aggregation process, aggregation based on situation assessment (ASA) method was proposed in [1]. It consists of the situation assessment model (SAM) and the ASA algorithm. In the SAM, the value of parameter, p, is transformed into the nearest integer value [1]. The integer-typed output of SAM is used as input for an aggregation. The integer-typed output of SAM indicates the current degree of aggregation situation. The ASA algorithm produces at most finite several aggregation results between min and max. In the sequel, the ASA method can not properly handle the applications with the more sophisticated aggregation results between min and max. In order to solve this problem, we propose two improved ASA (I-ASA) methods. In these I-ASA methods, we allow the value of parameter of SAM to be a real number, and suggest two improved ASA algorithms to make continuous aggregation results between min and max. These I-ASA methods can handle both a precise aggregation and an approximate aggregation. Therefore, when compared to the ASA method [1], the proposed I-ASA methods have advantages in that they can handle the applications with the more sophisticated aggregation results and can be used in the more general applications for aggregations.

• Journal of Pharmaceutical Investigation
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• v.37 no.1
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• pp.45-49
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• 2007

Dextran-5-aminosalicylic acid conjugate (dextran-5-ASA) was in vitro-evaluated as a polymeric colon-spe-cific prodrug of 5-aminosalicylic acid (5-ASA). Chemical stability of dextran-5-ASA in the pH 1.2 or 6.8 buffer solutions was investigated at 37 for 6 hrs. The dextran backbone was not degraded and no 5-ASA release was detected. Moreover, dextran-5-ASA neither liberated 5-ASA in the homogenates of the small intestine of rats nor was transported across Caco-2 cell monolayers, suggesting no significant loss of dextran-5-ASA during transit through the upper intestine. Furthermore, incubation of dextran-5-ASA in 10% cecal contents of rats released about 37% and 55% of 5-ASA bound to dextran in 8 hr and 24 hr, respectively. While that with either esterase or dextranase failed to liberate 5-ASA from the polymeric prodrug, incubation of dextran-5-ASA with both esterases and dextranse released 5-ASA up to about 24% of 5-ASA bound to dextran. These results suggest that, after oral administration of dextran-5-ASA, the polymeric prodrug is delivered specifically to and releases 5-ASA in the large intestine, and reveal that the 5-ASA release by cleavage of the ester bond requires precedent depolymerization of the dextran backbone.

• Archives of Pharmacal Research
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• v.26 no.4
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• pp.264-269
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• 2003

5-Aminosalicylic acid (5-ASA) is an active ingredient of therapeutic agents used for Crohn s disease and ulcerative colitis. Because it is absorbed rapidly and extensively in the upper intestine, delivery of the agent specifically to the colon is necessary. We selected taurine as a colon-specific promoiety and designed 5-aminosalicyltaurine (5-ASA-Tau) as a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA). It was expected that introduction of taurine would restrict the absorption of the prodrug and show additive effect to the anti-inflammatory action of 5-ASA after hydrolysis. 5-ASA-Tau was prepared in good yield by a simple synthetic route. The apparent partition coefficient of 5-ASA-Tau in 1-octanol/pH 6.8 phosphate buffer or $CHCl_3$/pH 6.8 phosphate buffer was 0.10 or 0.18, respectively, at $37^{\circ}C$. To determine the chemical and biochemical stability in the upper intestinal environment, 5-ASA-Tau was incubated in pH 1.2 and 6.8 buffer solutions, and with the homogenates of tissue and contents of stomach or small intestine of rats at $37^{\circ}C$. 5-ASA was not detected from any of the incubation medium with no change in the concentration of 5-ASA-Tau. On incubation of 5-ASA-Tau with the cecal and colonic contents of rats, the fraction of the dose released as 5-ASA was 45% and 20%, respectively, in 8 h. Considering low partition coefficient and stability in the upper intestine, 5-ASA-Tau might be nonabsorbable and stable in the upper intestine. After oral administration, it would be delivered to the colon in intact form and release 5-ASA and taurine. These results suggested 5-ASA-Tau as a promising colon-specific prodrug of 5-ASA.

• Korea-Australia Rheology Journal
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• v.18 no.1
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• pp.1-8
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• 2006

Blend of bisphenol-A polycarbonate (PC) and (acrylonitrile-styrene-acrylic rubber) terpolymer (ASA) having excellent balance in the interfacial properties and mechanical strength was developed for the automobile applications. Since interfacial adhesion between PC and styrne-acrylonitrile copolymer (SAN) matrix of ASA is not strong enough, two different types of compatibilizers, i.e, diblock copolymer composed of tetramethyl polycarbonate (TMPC) and SAN (TMPC-b-SAN) and poly(methyl methacrylate) (PMMA) were examined to improve interfacial adhesion between PC and SAN. TMPC-b-SAN was more effective than PMMA in increasing interfacial adhesion between PC and SAN matrix of ASA (or weld-line strength of PC/ASA blend). When blend composition was fixed, PC/ASA blends exhibited similar mechanical properties except impact strength and weld-line strength. Impact strength of PCI ASA blend at low temperature was influenced by rubber particle size and its morphology. PC/ASA blends containing commercially available PMMA as compatibilizer also exhibited excellent balance in mechanical properties and interfacial adhesion.

• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2381-2384
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• 2014

A solid-phase synthetic approach is reported for the synthesis of an ascorbic acid (ASA)-dipeptide conjugate that exhibited enhanced antioxidant activity. The N-terminal amino group of dipeptide (Ala-Ala) on a resin support was first activated by 1,1'-carbonyldiimidazole (CDI), and then reacted with an ASA derivative. The addition of a base, triethylamine (TEA), promoted nucleophilic acylation of ASA derivative and yielded a desired product (ASA-Ala-Ala) with enhanced purity, when cleaved from the resin. Compared to the approach where a C3 hydroxyl group of ASA was first activated with CDI and then reacted with the amino group of dipeptide on the resin, this new approach allowed a significant reduction of a total reaction time from 120 h to 8 h at $25^{\circ}C$. As-prepared ASA-dipeptide conjugate (ASA-Ala-Ala) showed improved antioxidant activity compared to ASA.

• Korean Journal Plant Pathology
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• v.13 no.1
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• pp.63-68
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• 1997

In the screening of antiviral materials produced by actinomycetes, an isolate named B25 was fond to produce an antibiotic substance ASA, which showed a strong inhibitory activity against tobacco mosaic virus (TMV) infection. ASA was purified from culture broth of B25 by silica gel column chromatography, preparative TLC, and reversed phase HPLC. Also MS, IR, UV spectrum, and melting point of ASA were determined and analysed. ASA was white powder soluble in dimethyl sulfoxide, chloroform, and ethyl acetate, having absorption peaks at 223 and 328 nm in UV-VIS spectrum, and had a molecular weight of 548. ASA showed strong inhibitory effect on TMV infection when it was applied as a mixture of TMV to the upper surface of leaves of a local lesion host (Nicotiana tabacum c. Xanthi-nc). It also showed antimicrobial effect against yeast and some phytopathogenic fungi.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.179-186
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• 1998

Dextran-5-aminosalicylic acid ester (dextran-5-ASA) was synthesized as a colon-specific prodrug of 5-aminosalicylic acid (5-ASA) which is active against inflammatory bowel diseases. Chemical stability of dextran-5-ASA in the bath of pH 1.2 or 6.8 was investigated at $37^{\circ}C$ for 6 hrs, and 5-ASA was not released on such conditions. Depolymerization (%) of dextran-5-ASA by dextranase with the degree of substitution (DS) of 18, 23, or 30 was 92, 62 or 45 in 8 hrs respectively, but was not affected by the MW of dextran (9,000, 40,600, 80,200 or 580,000). Distribution of 5-ASA in dextran, determined by gel filtration chromatography, appeared to be relatively uniform. Incubation of dextran-5-ASA (DS 18) in cecal contents of rats released 20% (28 g) and 35% (49 g) of 5-ASA in 8 hrs and 24 hrs, respectively, but no 5-ASA was liberated from small intestinal contents.

• Proceedings of the Korea Technical Association of the Pulp and Paper Industry Conference
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• 2000.04a
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• pp.48-48
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• 2000

효율적인 wet-end시스템의 적용으로 중성 초지시스템의 이점을 최대한 구현하고 이에 따른 초지계의 안정성 및 원가절감 등을 얻기 위해서는 중성 초지 시스템에서 사용되는 사 이즈제 및 사이징 공정에 대한 연구가 매우 중요하다. 현재 중성 사이즈제로는 AKD와 A ASA가 가장 널리 사용되고 있는데, 유럽에서는 주로 AKD가 쓰이고 있으며, 미국에서는 A ASA가 50%정도 사용되고 있다 .. AKD에 비해서 ASA는 사이즈도의 발현이 매우 빨라 사이 즈 프레스에서 사이즈도가 발현되므로 사이즈 프레스에서의 픽엽 조절 및 지절감소에 유리 한 장점을 가지고 있다. 하지만 ASA는 AKD에 비해 반웅성 높아 습부에서의 가수분해되어 초지 조업성을 악화시키는 문제점을 지니고 있다. 이러한 문제를 극복하기 위해서는 ASA 유화액의 정착성을 개선시키기 위한 연구가 시급히 요청되고 있으며 여기에는 ASA의 유화 에 사용되는 양성전분의 최적화가 가장 핵심적인 기술로 평가된다. 현재 ASA용 유화제로는 양성전분이 가장 많이 사용되고 있다. ASA 에멀션 제조에 있 어서 양성전분의 역할은 음전하를 가지고 있는 ASA 입자에 홉착되여 양전하를 부여함으로 써 콜로이드 업자의 안정성을 부여할 뿐만 아니라 섬유와의 정전기적 인력을 유도하여 정착 을 증진시키는 효과를 나타낸다. ASA 유화용으로 쓰이는 양성전분 중에서는 감자전분이 가 장 효과적인 것으로 알려져 있으며 옥수수나 타피오카 둥도 쓰이고 있다. 그러나 국내의 경 우 감자전분은 옥수수전분보다 가격이 비싸다는 단점이 있으므로 저렴한 옥수수 전분을 이 용하여 ASA 유화용 변성전분의 개발이 국내 제지산업의 경쟁력 강화를 위해 시급히 요망 되고 있다. 본 연구의 목표는 옥수수 전분을 이용한 ASA용 유화안정제를 개발하고 그 효과를 극대 화시킬 수 있는 적용기술을 확립하는데 있다. 옥수수전분을 이용한 ASA 유화용 변성전분은 외국에서 소개된 바가 있기는 하지만 사이즈도 발현이 감자전분의 절반 수준으로 효과적이 지 못한 것이 문제점으로 지적된 바 있다. A ASA 유화용 전분으로는 감자전분과 옥수수전분으로 제조된 외국산 기존 제품과 본 연 구를 통해 개발된 옥수수 전분을 이용하였다. 먼저 실험실적으로 최적의 ASA 에멸션의 유 화가 가능하도록 유화조건을 설정하여 유화액의 입도가 1µm 정도가 되도록 하였다. 이들 A ASA 사이즈제를 Hw. Sw-BKP로 조성된 지료에 투입하여 수초한 후 Hercules 사이즈도 측정기를 이용하여 수초지의 사이즈도를 측정하였다. 또 사이정 효과를 극대화시키기 위한 방안을 모색하기 위해 ASA 에말션의 입도, 제타전위, 탁도 등의 평가를 병행 실시하였다. 실험 결과 기존의 방법으로 유화한 경우 수입감자양성전분이 가장 높은 사이즈도를 보였 다. 그러나, 적절한 전분변성법과 유화조건을 개선함으로써 옥수수전분을 이용하여 수입 감 자전분이나 수입 옥수수전분보다 더 우수한 ASA 사이정 효과를 나타내는 양성전분이 개발 될 수 있음을 확인하였다.

• The Korean Journal of Pharmacology
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• v.5 no.1
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• pp.57-64
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• 1969

Acetylsalicylic acid, administered intravenously in a dose of 120 mg+250 mg/h, markedly decreased the urinary excretion of sodium and chloride, and slightly depressed potassium excretion, so that the ratio of urinary concentrations of potassium to sodium increased after ASA. Osmolar and free water clearances also diminished during water diuresis, and free water reabsorption $(T^cH_2O)$ decreased after ASA during mannitol diuresis. Glomerular filtration rate and urine flow rate changed little. When infused directly into a renal artery, ASA exhibited identical action on both kidneys, indicating that the renotropic action is mediated by some endogenous humoral agents or by some metabolites of ASA. A dose of 100 mg i.v. of spironolactone, a aldosterone antagonist, slightly reversed the renal reflect when given during maximum action of ASA. Ethacrynic acid could display its full diuretic action unhindered during maximum ASA action. Above observations lead to the suggestion that acetylsalicylic acid might release aldosterone and the action on electrolyte excretion may be mediated by the mineralocorticoid.

• Mycobiology
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• v.29 no.1
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• pp.19-26
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• 2001

Defense mechanisms against anthracnose disease caused by Colletotrichum orbiculare on the leaf surface of cucumber plants after pre-treatment with plant growth promoting rhizobacteria(PGPR), amino salicylic acid(ASA) or C. orbiculare were compared using a fluorescence microscope. Induced systemic resistance was mediated by the pre-inoculation in the root system with PGPR strain Bacillus amylolquefaciens EXTN-1 that showed direct antifungal activity to C. gloeosporioides and C. orbiculare. Also, systemic acquired resistance was triggered by the pre-treatments on the bottom leaves with amino salicylic acid or conidial suspension of C. orbiculare. The protection values on the leaves expressing SAR were higher compared to those expressing ISR. After pre-inoculation with PGPR strains no change of the plants was found in phenotype, while necrosis or hypersensitive reaction(HR) was observed on the leaves of plants pre-treated with ASA or the pathogen. After challenge inoculation, inhibition of fungal growth was observed on the leaves expressing both ISR and SAR. HR was frequently observed at the penetration sites of both resistance-expressing leaves. Appressorium formation was dramatically reduced on the leaves of plants pre-treated with ASA, whereas EXTN-1 did not suppress the appressorium formation. ASA also more strongly inhibited the conidial germination than EXTN-1. Conversely, EXTN-1 significantly increased the frequency of callose formation at the penetration sites, but ASA did not. The defense mechanisms induced by C. orbiculare were similar to those by ASA. Based on these results it is suggested that resistance mechanisms on the leaf surface was different between on the cucumber leaves expressing ISR and SAR, resulting in the different protection values.