• Title/Summary/Keyword: Vehicle activity

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Preparation and Characterization of Tributyrin Sub-micron Emulsion as Carrier for Paclitaxel

  • Fei, Xiang;Xu, Wenting;Yue, Yuan;Lee, Mi-Kyung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.5
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    • pp.295-300
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    • 2011
  • Paclitaxel is a well known anticancer agent and has been a pharmaceutical challenge because of its extremely poor water-solubility and susceptibility to the p-glycoprotein (p-gp)-mediated efflux in multi-drug resistant (MDR) cancer cells. Tributyrin (TB), a triglyceride with relatively short fatty acid chains, was chosen as solubilizing vehicle for paclitaxel based on the solubility study (26.6 mg/mL). Tributyrin (10%) o/w emulsion containing paclitaxel (5%), egg phosphatidylcholine (5%) and pegylated phospholipid (0.5%) was prepared by high pressure homogenization to obtain submicron-sized emulsion. The mean particle size of the resultant TB emulsion was 395.5 nm. Paclitaxel in TB emulsion showed higher anticancer activity against human breast cancer cell line, MCF-7, than free form delivered in DMSO solution. On the other hand, its anticancer activity was significantly reduced in MCF-7/ADR, a MDR variant cancer cell line of MCF-7, and recovered by the presence of verapamil, suggesting of the susceptibility to the p-gp mediated efflux even though paclitaxel was encapsulated into emulsion. The TB emulsion showed great potential as a promising vehicle for water-insoluble anticancer agent, paclitaxel.

Effect of Sophorae Radix-Skin Lotion on Acne (고삼(苦蔘) 추출물을 함유한 화장수의 여드름에 대한 효과)

  • Baek, Sang-Chul;Jo, Eun-Hee;Mendgerel, Mendgerel;Park, Min-Cheol
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.24 no.1
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    • pp.111-120
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    • 2011
  • Background & Objective : Sophorae Radix has been known as an useful plant with anti-inflammatory and anti-bacterial activity. Therefore, Sophorae Radix is expected to mitigate and prevent acne by inhibiting the activity of the sebaceous glands and acne bacterium. To evaluate anti-inflammation effect of Sophorae Radix, we applied Sophorae Radix-skin lotion on the patients with acne. Methods : The Sophorae Radix-skin lotion was prepared by dissolving 1% ethanol extract of Sophorae Radix in skin lotion vehicle and treated 2 times everyday for 4 weeks on faces. Follow-up was performed with Janus facial analysis system. Results : Sophorae Radix-skin lotion reduced sebum and porphyrin. However, the Sophorae Radix-skin lotion didn't significantly reduced sebum and porphyrin compared with skin lotion vehicle control group. Conclusion : These results showed that the Sophorae Radix-skin lotion could be used as a pharmaceutical material with anti-inflammatory effects by reducing sebum and porphyrin in acne patient with further clinical research.

Attenuation of insulin resistance using steamed Polygonatum odoratum var pluriflorum extract in rat skeletal muscle cells L6 myoblast (렛 근육세포 L6에서 둥굴레 추출물의 인슐린저항성 개선)

  • Choi, Mi-Ae
    • The Korea Journal of Herbology
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    • v.31 no.1
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    • pp.1-5
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    • 2016
  • Objectives : The purpose of this study was to investigate inhibitory effects of steamed Polygonatum odoratum extract (POE) on insulin resistance in rat skeletal muscle cells, L6 cells.Methods : Polygonatum odoratum (P. odoratum) extract was extracted with ethyl acetate. Activity of α-glucosidase in POE was measured for blood glucose regulation. MTT assay was examined for cell toxicity. Western blot analysis for measurement of adiponectine, peroxisome proliferator-activated receptorγ (PPARγ), insulin receptor substrate (IRS), glucose transporter 4 (Glut-4) and phosphorylation of serine/threonine-specific protein kinase (Akt) expressions were performed. Akt signaling pathway were analyzed with LY294002, which is a specific PI3K/Akt inhibitor.Results : The results revealed that POE inhibited α-glucosidase activity. Treatment of POE in L6 cells inhibited the differentiation of L6 cells compared to those of vehicl control. Additionally, protein expressions of adiponectine, PPARγ, IRS and Glut-4 were significantly regulated compared to those of vehicle control (p < 0.05), respectively. Futhermore, phosphorylation of Akt was increased in L6 cells treated with POE compared to that of vehicle control (p < 0.05). pAkt expression was significantly accentuated with Akt inhibitor (LY294002).Conclusions : These results suggest that POE may have potential as a natural agent for prevention/improvement of diabetes, especially, regulation of blood glucose. Therefore, further additional study should be conducted to elucidate in depth the pharmaceutical efficacy of these.

Affecting Factors on the Variation of Atmospheric Concentration of Polycyclic Aromatic Hydrocarbons in Central London

  • Baek, Sung-Ok;Roger Perry
    • Journal of Korean Society for Atmospheric Environment
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    • v.10 no.E
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    • pp.343-356
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    • 1994
  • In this study, a statistical investigation was carried out for the evaluation of any relationship between polycyclic aromatic hydrocarbons (PAHss) associated with ambient aerosols and other air quality parameters under varying meteorological conditions. Daily measurements for PAHs and air quality/meteorological parameters were selected from a data-base constructed by a comprehensive air monitoring in London during 1985-1987. Correlation coefficients were calculated to examine any significant relationship between the PAHs and other individual variables. Statistical analysis was further Performed for the air quality/meteorological data set using a principal component analysis to derive important factors inherent in the interactions among the variables. A total of six components were identified, representing vehicle emission, photochemical activity/volatilization, space heating, atmospheric humidity, atmospheric stability, and wet deposition. It was found from a stepwise multiple regression analysis that the vehicle emission component is overall the most important factor contributing to the variability of PAHs concentrations at the monitoring site. The photochemical activity/volatilzation component appeared to be also an important factor particularly for the lower molecular weight PAHs. In general, the space heating component was found to be next important factor, while the contributions of other three components to the variance of each PAHs did not appear to be as much important as the first three components in most cases. However, a consistency for these components in their negative correlations with PAHs data was found, indicating their roles in the depletion of PAHs concentrations in the urban atmosphere.

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Comparison of Oral versus Rectal Administration of Processed-Scutellaria baicalensis on Colonic Inflammation in Mice

  • Choi, Yeon-Ah;Kim, Dae-Ki;Chun, Myung-Kwan;Choi, Hoo-Kyun;Lee, Young-Mi
    • Journal of Pharmaceutical Investigation
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    • v.39 no.5
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    • pp.381-386
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    • 2009
  • We previously showed that the water extracts of rice wine-baked Scutellaria baicalensis Georgi (RWBS) ameliorated colonic inflammation more than crude Scutellaria baicalensis (CS) after oral administration. The aim of this study is to compare the effect of rectal and oral administration of RWBS in the experimental colitis. Experimental colitis was induced in mice by daily treatment with 5% dextran sulfate sodium (DSS) in the drinking water for 7 days. Water was used as vehicle of oral administration, while Carbopol/PEG mucoadhesive gel was used as vehicle of rectal administration. RWBS and RWBS gel (RWBSG) were administered once per day for 7 days. RWBS and RWBSG significantly attenuated the disease activity index (DAI) calculated as the sum of scores of body weight loss, stool consistency and rectal bleeding. Furthermore, RWBS and RWBSG reduced the mucosal myeloperoxidase activity and COX-2 (cyclooxygenase-2) expression in colon tissue. Anti-inflammatory effect of CS on colonic inflammation was increased by baking with rice wine in both oral and rectal administration. Moreover, anti-inflammatory effects of oral administration on colonic inflammation was greater than those of rectal administration. Further study would be required for the development of intra-rectal formulation.

The Effects of Hoechunyanggyeok-san on hyperglycemia and Dyslipidemia in db/db mice (회춘양격산(回春凉膈散)이 db/db 마우스의 고혈당 및 지질대사에 미치는 효과)

  • Jang, Soo-Young;Jung, Yu-Sun;Shin, Hyeon-Cheol
    • The Journal of Internal Korean Medicine
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    • v.35 no.1
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    • pp.70-78
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    • 2014
  • Objectives : Hoechunyanggyeok-san (HYS) is a traditional herbal medicine, which has been clinically used for treating febrile and inflammatory diseases. HYS has been reported to be a useful treatment for diabetes, atherosclerosis and hyperlipidemia in the type 1 diabetic model. However, the mechanism of the effects of HYS against hyperglycemia and hyperlipidemia is poorly understood. In the present study, we investigated the underlying mechanism of ameliorative effect of HYS on hyperglycemia and hyperlipidemia in vivo. Methods : HYS (10, 50 mg/kg/day, p.o.) was administered every day for 2 weeks to db/db mice and its effect was compared with vehicle-treated db/db mice. To confirm serum glucose and triglyceride (TG) changes, serological testing was performed. The levels of sterol regulatory element-binding protein-1 (SREBP-1) activity and Sirtuin1 (SIRT1), AMP-activated protein kinase (AMPK), and acetyl-CoA carboxylase ${\alpha}$ ($ACC{\alpha}$) expression were analyzed by western blot analysis. Results : The administration of HYS significantly decreased the elevated serum glucose and TG in db/db mice. HYS administration increased the levels of SIRT1 and AMPK expression compared with the vehicle-treated group. Moreover, HYS treatment significantly inhibited SREBP-1 activity and $ACC{\alpha}$ expression in the liver, while the vehicle-treated group exhibited their increase. Conclusions : In conclusion, HYS is suggested to have an improvement effect on hyperglycemia and hyperlipidemia by activating the SIRT1/AMPK signaling pathway and inhibiting SREBP-1.

The Relevance of Driving under the Influence and Bicycle Riding under the Influence and the Factors Affecting Driving under the Influence in Korea Adults: The Korea National Health and Nutrition Examination Survey (한국 성인의 자전거 음주운전과 차량 음주운전과의 관련성 및 차량 음주운전의 영향요인: 국민건강영양조사 원시자료를 이용하여)

  • Chae, Sun-Ok;Lee, Sang-Min
    • The Journal of the Korea Contents Association
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    • v.18 no.9
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    • pp.411-423
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    • 2018
  • This study was conducted to identify the correlation between driving under the influence (DUI) and bicycle riding under the influence and the impact factors of DUI among Korean adults. The participants were 3,385 Korean adults. Data were collected Seventh Korea National Health and Nutrition Examination Survey. The pervasiveness of DUI was 7.8% of the adult population in Korea. The relevance of DUI and bicycle riding under the influence was a statistically significant difference. The factors affecting of DUI were bicycle riding under the influence, aerobic physical activity, one-time drinking, frequency of binge drinking, experience aboard a driving under the influence vehicle. To prevent DUI among Korean Adults, we would need to encourage aerobic physical activity in daily and workplace, recognize that bicycle drunk riding can lead to drunk vehicle driving, and that management of alcohol use disorders and be planning to the vehicle driving before drinking.

Indoor Air Pollution of a High-rise Apartment Caused by Combustion Sources in Winter (겨울철 연소오염원에 의한 도심 고층 아파트의 실내공기오염)

  • Kim, Jong Bum;Lee, Gwangjae;Ryu, Sung Hee;Lee, Jae Young;Woo, Sung-Ho;Lee, Seung-Bok;Kim, Kyung Hwan;Yun, Seong-Taek;Bae, Gwi-Nam
    • Particle and aerosol research
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    • v.10 no.3
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    • pp.119-130
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    • 2014
  • Home is a major living environment of children. In urban area, indoor air at home could be severely influenced by combustion sources such as vehicle exhaust and cooking. In this work, the air quality of a high-rise apartment was investigated by monitoring combustion-related air pollutants at both indoor and outdoor in winter of 2014. From 48-h continuous monitoring data, large amount of $NO_x$ was observed at the balcony of the high-rise apartment during the morning traffic hours. It deteriorated indoor air quality of the apartment. During the cooking activity, high peak episodes of ultrafine particles were seen. It was concluded that effects of vehicle exhaust and cooking activity on the indoor air of the high-rise apartment could be easily checked by $NO_x$ and ultrafine particle indicators, respectively.

Protective Effect of Taurine on TNBS-induced Inflammatory Bowel Disease in Rats

  • Son, Mi-Won;Ko, Jun-Il;Doh, Hyoun-Mie;Kim, Won-Bae;Park, Tae-Sun;Shim, Mi-Ja;Kim, Byong-Kak
    • Archives of Pharmacal Research
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    • v.21 no.5
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    • pp.531-536
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    • 1998
  • We had previously reported that the protective effect of taurine against indomethacin-induced gastric mucosal injury was due to its antioxidant effects, which inhibited lipid peroxidation and neutrophil activation. In this study, we examined the effect of taurine on reducing the inflammatory parameters of trintrobenzene sulfonic acid (TNBS)-induced inflammatory bowel disease (IBD) in rats. In order to induce IBD, ethanolic TNBS was given to rats intracolonically. Then they received 500 mg/kg.day of taurine orally and were sacrificed one week after IBD induction. While ulceration and inflammation of distal colon with formation of granuloma in the vehicle-treated IBD rats two days after administration of TNBS were observed, treatment with taurine ameliorated colonic damage and decreased the incidence of diarrhea and adhesion. also, colon weight as an index of tissue edema, which was mardedly increased in the IBD rats, became significantly lower after administration of TNBS were observed, treatment with taurine ameliorated colonic damage and decreased the incidence of diarrhea and adhesion. Also colon weitht as an index of tissue edema, which was markedly increased in the IBD rats, became significantly lower after taruine treatment. Myeloperoxidase (MPO) activity in the vehicle-treated IBD rats was substantially increased, compared with that of normal control. the taurine-treated animals significantly reduced MPO activity (35% lower) when compared with that of the vehicle-treated animals. Taurine treatment decreased both basal and formyl-methionyl leucyl phenylalanine-stimulated reactive oxygen generation from colonic tissue in the IBD rats. These results suggest that the administration of taurine reduce the inflammatory parameters in this IBD rat model by increasing defending capacity against oxidative damage.

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Chitosan-Based Film of Tyrothricin for Enhanced Antimicrobial Activity against Common Skin Pathogens Including Staphylococcus aureus

  • Han, Sang Duk;Sung, Hyun Jung;Lee, Ga Hyeon;Jun, Joon-Ho;Son, Miwon;Kang, Myung Joo
    • Journal of Microbiology and Biotechnology
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    • v.26 no.5
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    • pp.953-958
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    • 2016
  • Chitosan-based film-forming gel is regarded as a promising vehicle for topical delivery of antimicrobial agents to skin wounds, since it protects from microbial infection and the cationic polymer itself possesses antibacterial activity. In this study, possible synergistic interaction against common skin pathogens between the cationic polymer and tyrothricin (TRC), a cyclic polypeptide antibiotic, was investigated, by determining the concentration to inhibit 90% of bacterial isolates (MIC). The addition of the polysaccharide to TRC dramatically reduced the MIC values of TRC by 1/33 and 1/4 against both methicillin-resistant and methicillin-susceptible Staphylococcus aureus, respectively. The synergism of TRC and chitosan combination against both strains was demonstrated by the checkerboard method, with a fractional inhibitory concentration index below 0.5. Moreover, co-treatment of TRC and chitosan exhibited antibacterial activity against Pseudomonas aeruginosa, due to the antibacterial activity of chitosan, whereas TRC itself did not inhibit the gram-negative bacterial growth. These findings suggested that the use of chitosan-based film for topical delivery of TRC could be an alternative to improve TRC antimicrobial activity against strains that are abundant in skin wounds.