• Title/Summary/Keyword: salicylate

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Effect of Carnosine and Related Compounds on Glucose Oxidation and Protein Glycation In Vitro

  • Lee, Beom-Jun;Park, Jae-Hak;Lee, Yong-Soon;Cho, Myung-Haing;Kim, Young-Chul;Hendricks, Deloy G.
    • BMB Reports
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    • v.32 no.4
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    • pp.370-378
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    • 1999
  • The effects of carnosine and related compounds (CRC) including anserine, homocarnosine, histidine, and ${\beta}$-alanine, found in most mammalian tissues, were investigated on in vitro glucose oxidation and glycation of human serum albumin (HSA). Carnosin and anserine were more reactive with D-glucose than with L-lysine. In the presence of $10\;{\mu}M$ Cu (II), although carnosine and anserine at low concentrations effectively inhibited formation of ${\alpha}$-ketoaldehyde from D-glucose, they increased generation of $H_2O_2$ in a dose-dependent manner. Carnosine, homocarnosine, anserine, and histidine effectively inhibited hydroxylation of salicylate and deoxyribose degradation in the presence of glucose and $10\;{\mu}M$ Cu (II). In the presence of 25 mM D-glucose, copper and ascorbic acid stimulated carbonyl formation from HSA. Except for ${\beta}$-alanine, CRC effectively inhibited the copper-catalyzed carbonyl formation from HSA. The addition of 25 mM D-glucose and/or $10\;{\mu}M$ Cu (II) to low density lipoprotein (LDL) increased formation of conjugated dienes. CRC effectively inhibited the glucose and/or copper-catalyzed LDL oxidation. CRC also inhibited glycation of HSA as determined by hydroxymethyl furfural and lysine with free ${\varepsilon}$-amino group. These results suggest that CRC may play an important role in protecting against diabetic complications by reacting with sugars, chelating copper, and scavenging free radicals.

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Unilateral Parotitis and Kawasaki Disease in a Child (일측 이하선염으로 발현한 가와사키병 1례)

  • Lyu, Soo Young;Ban, Gil Ho;Park, Su Eun
    • Pediatric Infection and Vaccine
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    • v.21 no.3
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    • pp.214-218
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    • 2014
  • Kawasaki disease is generally diagnosed base on its clinical features. Sometimes unusual or atypical presentations make the diagnosis of Kawasaki disease difficult. We experienced an unusual case of Kawasaki disease presented with unilateral parotitis in a 23-month old girl. Despite of intravenous antibiotics treatment, fever and unilateral parotid swelling persisted. Skin rashes, conjunctival injections, and coronary abnormalities showed up on the 8th day of fever. After the intravenous immunoglobulin and salicylates treatment, all symptoms disappeared. Although unilateral parotitis is very unusual presentation of Kawasaki disease, in case of no response to antibiotics, Kawasaki disease should be included in the differential diagnosis.

Physico-chemical properties of green leaf volatiles (GLV) for ascertaining atmospheric fate and transport in fog

  • Vempati, Harsha;Vaitilingom, Mickael;Zhang, Zenghui;Liyana-Arachchi, Thilanga P.;Stevens, Christopher S.;Hung, Francisco R.;Valsaraj, Kalliat T.
    • Advances in environmental research
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    • v.7 no.2
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    • pp.139-159
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    • 2018
  • Green Leaf Volatiles (GLVs) is a class of biogenically emitted oxygenated hydrocarbons that have been identified as a potential source of Secondary Organic Aerosols (SOA) via aqueous oxidation. The physico-chemical properties of GLVs are vital to understanding their fate and transport in the atmosphere via fog processing, but few experimental data are available. We studied the aqueous solubility, 1-octanol/water partition coefficient, and Henry's law constant ($K_H$) of five GLVs at $25^{\circ}C$: methyl jasmonate, methyl salicylate, 2-methyl-3-buten-2-ol, cis-3-hexen-1-ol, and cis-3-hexenyl acetate. Henry's law constant was also measured at temperatures and ionic strengths typical of fog. Experimental values are compared to scarcely-available literature values, as well as estimations using group and bond contribution methods, property-specific correlations and molecular dynamics simulations. From these values, the partition coefficients to the air-water interface were also calculated. The large Henry's law constant of methyl jasmonate ($8091{\pm}1121M{\cdot}atm^{-1}$) made it the most significant GLV for aqueous phase photochemistry. The HENRYWIN program's bond contribution method from the Estimation Programs Interface Suite (EPI Suite) produced the best estimate of the Henry's constant for GLVs. Estimations of 1-octanol/water partition coefficient and solubility are best when correlating an experimental value of one to find the other. Finally, the scavenging efficiency was calculated for each GLV indicating aqueous phase processing will be most important for methyl jasmonate.

Development of Pharmaceutical Dosage Form with New Sibutramine Salt (시부트라민 신규염을 이용한 새로운 시부트라민 제제의 개발)

  • Moon, Jin-Wook;Shin, Teak-Hwan;Lee, Dong-Wook;Cho, Jun-Young;Chang, Sung-Ju;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.40 no.1
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    • pp.15-21
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    • 2010
  • Sibutramine is an orally administered centrally-acting antiobesity agent and inhibits both noradrenaline(norephinephirine) and serotonin(5-HT) reuptake. These effects are contributed by its active metabolites, M1 and M2. However, as the free base form of sibutramine is an oil form in room temperature, it had the problem of handling and stability. Thus, this drug should be used in the form of acid salt form in the pharmaceutical application. Unfortunately, anhydrous sibutramine hydrochloride is highly hygroscopic and unstable. In order to solve the hygroscopicity of the anhydrous salt form, another sibutramine acid salt form must be developed as a hydrate form. In this study. to overcome these problems, various of sibutramine acid salt forms were prepared with the pharmaceutically available salts such as maleate, esylate, mandelate, camsylate, besylate, salicylate, tartrate, isethionate and malate forms, and their physicochemical properties were investigated. Sibutramine malate was selected for excellent solubility and stability among the listed salt forms above. Its pharmacokinetic parameters were evaluated in rats comparing with sibutramine HCl, resulting in similar parameters. In vitro dissolution study of sibutramine malate-loaded capsule was performed comparison with commercial product ($Reductil^{(R)}$) in pH 1.2, pH 4.0, pH 6.8 and water medium. Our results indicated that there were no significant differences in their dissolution profiles were similar in all tested medium. Thus, sibutramine malate-loaded capsule should be a potential candiate due to its excellent solubility, good stability and biosimilar absorption.

Studies on the evaluation of efficacy of functional cosmetics(I) -Studies on the in vitro SPF test method of sunscreen products (기능성화장품의 기능성평가에 관한 연구(I) -자위선차단화장품의 in vitro 시험법 연구)

  • 손경훈;김영옥;이정표;양성준;백옥진;김원희;김종갑;허문영;최상숙
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.28 no.3
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    • pp.171-184
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    • 2002
  • The present study was undertaken to develop the in vitro sunprotection factor(SPF) measurement method having good correlation with in vivo method. As in vitro method, 8% homomentyl salicylate, P3 reference standard and sunscreens on market were measured using SPF 290 analyzer and were compared the SPF with labed value. In vitro SPF of 8% HMS and P3 reference standard were 4.59 $\pm$ 0.12 and 14.94 $\pm$ 0.83. There are good correlation, correlation factor were 0.9506 and 0.9769 respectively, between the in vitro and in vivo SPF for the sunscreen creams and lotions examined. Correlation factors of makeup base & liquid goundation, lotion labled with “shake before use”, compact powder were 0.8812, 0.8632 and 0.5984. The best sample applied method of compact powder was 1:0.8 mixture with cream base. These results suggest that the in vitro test method could be used as an alternative method for SPF.

Preparation and physicochemical characterization of mouthwash granules containing menthol, thymol, eucalyptol and Methyl salicylate (멘톨, 치몰, 유칼립톨, 메틸살리실레이트를 함유하는 구강청결용 과립의 제조와 특성 연구)

  • Kim, Dong-Wook
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.12
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    • pp.329-334
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    • 2017
  • In this study, a new granular type mouthwash with equivalent antibacterial activity to marketed liquid type mouthwash was developed using a material called magnesium aluminometasilicate (Neusilin). This material adsorbs the surface of granules to improve the flowability of granules due to the formation of a eutectic mixture of the main constituents, which have improved flow properties and rapid disintegration time and little residue in the oral cavity. The characteristics of the granules were improved when the amount of Neusilin was 10% or more according to measurements of the granule properties, such as flowability. In addition, a disintegration test in artificial saliva and a sensory test in the human oral cavity were carried out to confirm the improved disintegration characteristics and sensory test results. The antimicrobial test confirmed similar antibacterial activity to that of the liquid oral cleanser already sold in the market. The granular oral cleanser composition prepared in this study can be used for the development of pharmaceuticals containing different drugs with similar characteristics as eutectic mixtures at the same time, which is considered to be useful in the development of medicines in the pharmaceutical industry.

A Study or the Effect of Electrical Stimulation on Tinnitus Treatment based on the Correlation Analysis of ABR and ECochG (ABR과 ECochG의 상관분석을 통한 전기자극이 이명치료에 미치는 영향에 관한 연구)

  • Kim, K.S.;Park, J.W.;Nam, S.H.;Im, J.J.;Choi, E.S.;Jeon, B.H.
    • Proceedings of the KOSOMBE Conference
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    • v.1997 no.11
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    • pp.87-90
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    • 1997
  • Electrical stimulation has been used or diagnosis and treatment of impairment on the auditory system. Unfortunately, there were no standard methods or theoretical background or choosing stimulus conditions because of the lack of understanding on the current propagation through the auditory pathways. Nine guniea pigs, experimental group(A) and control group(B), were used for the experiment. ABR and ECochG were obtained under our experimental conditions, before tinnitus and 1, 6, 12 hours after tinnitus induction using salicylate. Electrical stimulations were applied to the group A, and the changes on ABR/ECochG's correlation coefficients were observed. Results showed that an electrical stimulation brings ABR waveform back to the normal states well in the group A compare to the group B, which proved the effectiveness of the stimulation. Based on the results of this experiment, establishment of an electrical model which provide the quantitative information regarding diagnosis and treatment of tinnitus could be achievied.

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Assessing the Systemic Toxicity in Rabbits after Sub Acute Exposure to Ocular Irritant Chemicals

  • Reshma, Cherian Sebastian;Sruthi, Sudhakaran;Syama, Santhakumar;Gayathri, Vishwanath;Mohanan, Parayanthala Valappil
    • Toxicological Research
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    • v.31 no.1
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    • pp.49-59
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    • 2015
  • Eye is a highly vascularised organ. There are chances that a foreign substance can enter the systemic circulation through the eye and cause oxidative stress and evoke immune response. Here the eyes of rabbits were exposed, for a period of 7 days, to 5 known ocular irritants: Cetyl pyridinium chloride (CPC), sodium salicylate (SS), imidazole (IMI), acetaminophen (ACT) and nicotinamide (NIC). The eyes were scored according to the draize scoring. Blood collected from the treated rabbit were analyzed for haematological and biochemical parameters. After sacrifice, histological analysis of the eye and analysis of pro-inflammatory biomarkers ($IL-1{\alpha}$, $IL-1{\beta}$, IL-8 and $TNF-{\alpha}$) in the cornea using ELISA was carried out. Spleen was collected and the proliferation capacities of spleenocytes were analyzed. Liver and brain were collected and assessed for oxidative stress. The eye irritation potential of the chemicals was evident from the redness and swelling of the conjunctiva and cornea. Histopathological analysis and ELISA assay showed signs of inflammation in the eye. However, the haematological and biochemical parameters showed no change. Spleenocyte proliferations showed only slight alterations which were not significant. Also oxidative stress in the brain and liver were negligible. In conclusion, chemicals which cause ocular irritation and inflammation did not show any systemic side-effects in the present scenario.

Flavor Components of the Fruit Peel and Leaf Oil from Zanthoxylum piperitum DC (초피(Zanthoxylum piperitum DC)의 과피와 잎의 방향성분)

  • Kim, Jung-Han;Lee, Kyung-Seok;Oh, Won-Taek;Kim, Kyoung-Rae
    • Korean Journal of Food Science and Technology
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    • v.21 no.4
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    • pp.562-568
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    • 1989
  • The essential oils from ripe fruit peel and leaf of Zanthoxylum piperitum DC were extracted by gas co-distillation method and analyzed by gas chromatography/mass spectrometry (GC/ MS) and retention index matching. The experimental results revealed the presence of over 100 volatile components. Major components were 1,8-cineol (25.47%), limonene (11.91%), geranyl acetate (9.01%), myrcene (6.15%) in fruit peel and citronellal (23.11%), 1,8-cineol (18.38%), citronellol (6.04%) in leaf. Among the components identified were the following; in fruit peel, ${\alpha}-pinene$ and 13 hydrocarbons, linalool and 8 alcohols, citronellal and 3 aldehydes, carvone and 2 kotones, methyl salicylate and 7 esters, and 1,8-cineol and oxides, and in leaf, ${\alpha}-pinene$ and 7 hydrocarbons, linalool and 7 alcohols, citronellyl acetate and 5 esters, citronellal and 1 aldehyde, carvone, and 1,8-cineol and 1 oxide.

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Microwave-Accelerated Click Chemistry: Expeditious Synthesis of Novel Triazole-linked Salicylic β-D-O-Glycosides with PTP1B Inhibitory Activity

  • Yang, Jin-Wei;Li, Cui;He, Xiao-Peng;Zhao, Hong;Gao, Li-Xin;Zhang, Wei;Shi, Xiao-Xin;Tang, Yun;Li, Jia;Chen, Guo-Rong
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3359-3365
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    • 2010
  • The incorporation of microwave irradiation with the prevalent "click chemistry" is currently of considerable synthetic interest. We describe here the introduction of such laboratorial shortcut into carbohydrate-based drug discovery, resulting in the rapid formation of a series of triazole-linked salicylic $\beta$-D-O-glycosides with biological activities. All "clicked" products were achieved in excellent yields ($\approx$ 90%) within only a quarter. In addition, based on the structural characteristics of the afforded glycomimetics, their inhibitory activities were evaluated toward protein tyrosine phosphatases 1B (PTP1B) and a panel of homologous protein tyrosine phosphatases (PTPs). Docking simulation was also conducted to plausibly propose binding modes of this glycosyl salicylate series with the enzymatic target.