• Title/Summary/Keyword: ${\beta}_2$ MG

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Enhanced Dissolution and Duodenal Permeation of Atorvastatin Calcium Using Bile Salt and 2-Hydroxypropyl-${\beta}$-Cyclodextrin (담즙산염과 2-히드록시프로필-${\beta}$-시클로덱스트린을 이용한 아토르바스타틴칼슘의 용출 및 십이지장 점막 투과 증진)

  • Choi, Ji-Won;Chun, In-Koo
    • YAKHAK HOEJI
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    • v.56 no.3
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    • pp.164-172
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    • 2012
  • This study was aimed to increase the solubility, dissolution and permeation rates of atorvastatin calcium (ATC) using bile salt and/or 2-hydroxypropyl-${\beta}$-cyclodextrin ($HP{\beta}CD$). From solubility studies, sodium deoxycholate (SDC) among bile salts studied was found to have the highest solubilizing effect on ATC ($4.4{\pm}0.4$ mg/ml), and the order of increasing solubility was SDC>sod. cholate>sod. glycocholate>sod. taurodeoxycholate>sod. taurocholate>conjugated bile acid. ATC solid dispersions were prepared at various ratios of drug to SDC and/or $HP{\beta}CD$, and evaluated by differential scanning calorimetry (DSC), dissolution studies and dissolution-permeation studies. DSC curves showed amorphous state of ATC in the physical mixture and solid dispersion. Dissolution rates of ATC-SDC solid dispersions and physical mixture were markedly increased at pH 6.8, but decreased at pH 1.2 with greater proportions of SDC due to the precipitation of SDC, compared with that of drug alone. On the other hand, dissolution rates of ATC-$HP{\beta}CD$ solid dispersion and physical mixture at pH 1.2 were varied with the ratio of drug to carriers. From duodenal permeation studies, it was found that fluxes of ATC (donor dose: 0.5 mg/3.5 ml) in the presence of 25 mM sodium glycocholate, SDC, sod. cholate and sod. taurocholate $(5.7{\pm}0.9$, $5.6{\pm}0.9$, $4.8{\pm}0.7$ and $4.6{\pm}0.9\;{\mu}g/cm^2/hr$, respectively) were enhanced, compared with drug alone ($3.4{\pm}0.9\;{\mu}g/cm^2/hr$). In the dissolution-permeation studies, 1 : 9 : 10 (w/w) ATC-SDC-$HP{\beta}CD$ solid dispersion increased the flux 2.2 times, compared with 1 : 5 : 4 (w/w) ATC-lactose-corn starch mixture as control. In conclusion, solid dispersions with bile salt and $HP{\beta}CD$ were found to be an effective means for increasing the dissolution and permeation rates of ATC.

Phosphodiesterase III Inhibitor Cilostazol Protects Amyloid β-Induced Neuronal Cell Injury via Peroxisome Proliferator-Activated Receptor-γ Activation (Amyloid β에 의해 유도된 신경세포 손상에 대한 phosphodiesterase III inhibitor인 cilostazol의 신경보호 효과)

  • Park, Sun-Haeng;Kim, Ji-Hyun;Bae, Sun-Sik;Hong, Ki-Whan;Choi, Byung-Tae;Shin, Hwa-Kyoung
    • Journal of Life Science
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    • v.21 no.5
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    • pp.647-655
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    • 2011
  • The neurotoxicity of aggregated amyloid ${\beta}$ ($A{\beta}$) has been implicated as a critical cause in the pathogenesis of Alzheimer's disease (AD). It can cause neurotoxicity in AD by evoking a cascade of apoptosis to neuron. Here, we investigated the neuroprotective effects of cilostazol, which acts as a phosphodiesterase III inhibitor, on $A{\beta}_{25-35}$-induced cytotoxicity in mouse neuronal cells and cognitive decline in the C57BL/6J AD mouse model via peroxisome proliferator-activated receptor (PPAR)-${\gamma}$ activation. $A{\beta}_{25-35}$ significantly reduced cell viability and increased the number of apoptotic-like cells. Cilostazol treatment recovered cells from $A{\beta}$-induced cell death as well as rosiglitazone, a PPAR-${\gamma}$ activator. These effects were suppressed by GW9662, an antagonist of PPAR-${\gamma}$ activity, indicative of a PPAR-${\gamma}$-mediated signaling. In addition, cilostazol and rosiglitazone also restored PPAR-${\gamma}$ activity levels that had been altered as a result of $A{\beta}_{25-35}$ treatment, which were antagonized by GW9662. Furthermore, cilostazol also markedly decreased the number of apoptotic-like cells and decreased the Bax/Bcl-2 ratio. Intracerebroventricular injection of $A{\beta}_{25-35}$ in C57BL/6J mice resulted in impaired cognitive function. Oral administration of cilostazol (20 mg/kg) for 2 weeks before $A{\beta}_{25-35}$ injection and once a day for 4 weeks post-surgery almost completely prevented the $A{\beta}_{25-35}$-induced cognitive deficits, as did rosiglitazone. Taken together, our findings suggest that cilostazol could attenuate $A{\beta}_{25-35}$-induced neuronal cell injury and apoptosis as well as promote the survival of neuronal cells, subsequently improving cognitive decline in AD, partly because of PPAR-${\gamma}$ activation. The phosphodiesterase III inhibitor cilostazol may be the basis of a novel strategy for the therapy of AD.

Anti-wrinkle Activity of $\beta$-carotene Extracted & Purified from Recombinant Escherichia coli (재조합 대장균으로부터 추출.정제된 베타-카로틴의 주름개선 활성)

  • Jo, Ji-Song;Ku, Bo-Mi;Kang, Sang-Soo;Lee, Jae-Ran;Kim, You-Geun;Lee, He;Kim, Sung-Bae;Kim, Seon-Won;Kim, Chang-Joon;Chung, In-Young
    • KSBB Journal
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    • v.23 no.6
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    • pp.513-518
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    • 2008
  • This paper described the extraction/purification of $\beta$-carotene from recombinant E.coli and evaluation of anti-wrinkle activity of purified $\beta$-carotene. No significant differences in extraction yields were observed when hexane or isobutyl acetate was used. However, extraction from wet-cell cake resulted in 2-fold higher amount of $\beta$-carotene than that from dry cells. Disruption of 5 g-wet cells by ultrasonic homogenizer, acetone dehydration, extraction with isobutyl acetate resulted in 36 mg of $\beta$-carotene corresponding to 61.2% of recovery. The formation and separation of $\beta$-carotene crystal improved the purity. 633 mg of $\beta$-carotene crystal with 93% purity was obtained from 223 g/L of wet-cell cake harvested from 2.5-L fed-batch culture broth. The cultures of normal human primary fibroblast were performed to investigate the effect of $\beta$-carotene on cytotoxicity as MTT assay and anti-wrinkle activity as collagen synthesis assays. $1.7{\mu}M$ of $\beta$-carotene was found to be optimal concentration at which 1.4-fold higher amount of collagen was synthesized than that in absence of $\beta$-carotene. This indicates that highly purified $\beta$-carotene can be obtained from recombinant E.coli by applying simple method with less toxic solvent and can be used in functional cosmetics as anti-wrinkle agent.

The physicochemical characteristics and antioxidant capacities of commercial tea products from Phellinus baumii, Ganoderma lucidum (상황버섯과 영지버섯 차류 제품의 이화학적 특성 및 항산화능)

  • Kim, Ha-Na;Son, Eun Ji;Chung, Shin-Kyo
    • Food Science and Preservation
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    • v.24 no.1
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    • pp.153-157
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    • 2017
  • This study was conducted to investigate the physicochemical characteristics, antioxidant capacities of Phellinus linteus and Ganoderma lucidum commercial tea products. The physicochemical characteristics included pH, Hunter's color values, soluble solid contents, evaporation residues, and ${\beta}$-glucan contents. The antioxidant capacities were measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities, ferric reducing antioxidant power (FRAP), and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activities, total phenolic contents (TPC), and total flavonoid contents (TFC). The pH, soluble solid contents, evaporation residues, and ${\beta}$-glucan contents were in the range of 4.43-7.05, $0.40-0.73^{\circ}Brix$, 62.04-258.84 mg/100 g, and 15.51-62.32 mg%, respectively. Hunter's color values (L, a, and b) indicated 41.76-55.02, -0.49-5.06, and 17.41-28.32, respectively. The antioxidant capacities showed $32.63-367.81{\mu}M$ GAE (DPPH radical scavenging activities), $321.86-1,035.19{\mu}M$ TE (FRAP), $703.50-1,091.83{\mu}M$ (ABTS radical scavenging activities), $286.56-916.00{\mu}M$ (TPC), and $85.33-635.33{\mu}M$ (TFC). Overall, P. linteus liquid tea 2 (PL2) and G. lucidum liquid tea 1 (GL1) showed high antioxidant capacities (p<0.05). The TPC and TFC were highly correlated with DPPH radical scavenging activities, FRAP, and ABTS radical scavenging activities (r=0.7298-0.9743), but the ${\beta}$-glucan contents were not correlated well with antioxidant activities tested (r=0.3146-0.6663).

Antioxidant Component and Sensory Evaluation of Mixed Cereals (혼합잡곡의 항산화 물질과 기호도)

  • Lee, Kyung-Haeng
    • The Korean Journal of Food And Nutrition
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    • v.28 no.2
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    • pp.196-201
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    • 2015
  • To improve functionality of rice, we manufactured mixed cereals and mixed cereals with taste materials and evaluated their antioxidant component (ascorbic acid, tocopherols, polyphenols and flavonoids) contents and sensory evaluation. Ascorbic acid content in water extract of the control was 6.68 mg%, and mixed cereals were 18.23 and 21.84 mg%, respectively. Ascorbic acid content in methanol extract of the control was lower than those of mixed cereals too. ${\beta}$-Tocopherol was the only tocopherol detected in the control. However, tocopherols detected in mixed cereals were ${\alpha}$-, ${\beta}$-. ${\gamma}$-, ${\delta}$-tocopherol and ${\alpha}$-, ${\gamma}$-tocotrienol, with a highest content of ${\gamma}$-tocopherol. Total tocophenols content of the control was 1.26 mg%, whereas, those of mixed cereals were 19.24 and 39.32 mg%, respectively. Polyphenols contents in water extract of the control was 2.20 mg%, and mixed cereals were 14.38 and 21.91 mg%, respectively. In addition, polyphenols contents in methanol extract of mixed cereals were higher than that of the control, too. Flavonoids were undetected in water extract of the control, but flavonoids contents of mixed cereals were 42.45 and 32.54 mg%, respectively. In methanol extracts, flavonoids contents of the control and mixed cereals were not significantly different. The sensory parameters including taste, flavor, color, texture and overall acceptance of control were lower than those of mixed cereals. Especially, mixed cereals with taste materials was the highest acceptance.

Factors Effecting the Bioavailability of Carotenoid in Elderly Korean Women (한국 여자 노인의 Carotenoid Bioavailability에 미치는 요인 조사)

  • 임재연;이해정;박선주;최혜미
    • Korean Journal of Community Nutrition
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    • v.8 no.6
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    • pp.822-830
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    • 2003
  • Carotenoid-rich foods focus one's attention on the prevention age-related diseases. This study was conducted to investigate the carotenoid status and look into the factors that affect the bioavailability of carotenoid in 121 elderly nonsmoking Korean women. Carotenoids and lipids in plasma, and nutrient intakes including carotenoid were studied. The mean plasma total-cholesterol, HDL-cholesterol, LDL-cholesterol and triacylglycerol concentrations were 220.0 mg/dl 49.5mg/dl , 139.2mg/dl and 157.4mg/dl , respectively. Significantly positive correlations were found between the plasma lutein + zeaxanthin, lycopene and $\beta$-carotene concentrations and the intake of fruits (r=0.17, r=0.20, r=0.19). However, significantly negative correlations were found between the plasma zeaxanthin, and $\beta$-carotene concentrations that adjusted for carotenoid intakes and intakes of vegetables (r=-0.21, r=-0.19), and between plasma lutein+zeaxanthin, lycopene and $\beta$-carotene concentrations that adjusted for carotenoid intakes and intakes of fruits (r= -0.21, r=-0.18, r=-0.24). After the adjustment for plasma lipids, there was no correlation between the plasma carotenoid concentrations and the carotenoid-rich foods. However, after adjustment for fiber intake, significantly strong positive correlations were found between the plasma carotenoid concentrations and carotenoid-rich foods. The plasma levels of carotenoid biomarkers (plasma carotenoid concentrations adjusted for dietary fiber intakes) decreased with age, and the plasma levels of lycopene biomarkers (plasma lycopene concentrations adjusted for dietary fiber intakes) increased with regular exercise. However alcohol drinking had no impact. These results suggested that age, physical activity, and dietary fiber intake affected the bioavailability of carotenoid. Therefore, when the elderly have carotenoid-rich foods, they should consider ways of increasing the bioavailability of carotenoid through cooking methods and Physical activity.

Carotenoid Pigments in Echiurid, Urechis unicinctus (개불의 carotenoid 색소성분)

  • KIM Soo Young;HA Bong Seuk
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.32 no.2
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    • pp.223-231
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    • 1999
  • Carotenoid pigments of echiurid, Urechis unicinctus were investigated during March, April and May as a part of comparative biochemical studies of carotenoid pigments for the marine organisms other than pisces. Total carotenoid contents were found to be 1.19 mg/100 g in March, 0.98 mg/100 g in April and 0.84 mg/100 g in May, indicating that total carotenoid content was negatively affected by the temperature of sea water that echiurid resided. The carotenoid isolated in March composed of $16.3\%$ diatoxanthin monoester, $14.8\%$ $\beta$-carotene and $12.6\%$ cynthiaxanthin monoester, $8.4\%$ cynthiaxanthin diester, $8.2\%$ zeaxanthin monoester, $7.3\%$ diatoxanthin diester $4.2\%$ astaxanthin $2.9\%$ diatoxanthin, $2.4\%$ triol, $2.3\%$ cynthiaxanthin, $1.7\%$ isocrytoxanthin, $1.5\%$ zeaxanthin diester, $0.8\%$ zeaxanthin and $0.5\%$ lutein. The carotenoid isolated in April composed of $21.9\%$ diatoxanthin monoester, $17.2\%$ cynthiaxanthin monoester and $16.6\%$ $\beta$-carotene $10.9\%$ zeaxanthin monoester, $5.6\%$ cynthiaxanthin diester, $4.9\%$ diatoxanthin diester, $3.1\%$ astaxanthin, $2.4\%$ triol, $2.3\%$ diatoxanthin, $1.7\%$ isocrytoxanthin, $1.5\%$ lutein, $1.1\%$ zeaxanthin, $1.0\%$ cynthiaxanthin and $1.0\%$ zeaxanthin diester. Similarly, the carotenoid isolated in May composed of $25.3\%$ diatoxanthin monoester, $19.7\%$ cynthiaxanthin monoester, $13.0\%$ $\beta$-carotene, and $12.6\%$ zeaxanthin monoester, $5.8\%$ cynthiaxanthin diester, $5.1\%$ diatoxanthin, $3.0\%$ astaxanthin, $2.4\%$ triol, $2.2\%$ diatoxanthin, $1.3\%$ isocrytoxanthin, $1.2\%$ zeaxanthin, $1.1\%$ zeaxanthin diester, $1.0\%$ lutein and $0.9\%$ cynthiaxanthin. Based on these data, monoester-type carotenoids ($37.1\~57.6\%$) and diester-type carotenoids ($11.5\~17.2\%$) of total carotenoids in echiurid were the major carotenoids. Meanwhile, when the sea water temperature was elevated and the contents of total carotenoid in echiurids were decreased, the contents of zeaxanthin monoester, diatoxanthin monoester and cynthiaxanthin monoester were increased, but the contents of zeaxanthin diester, diatoxanthin diester and cynthiaxanthin diseter were decreased, indicating that changes in ester-type caroteoids were differently affected by the sea water temperature.

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Antifungal Activities of Essential Oils from Glehnia littoralis Alone and in Combination with Ketoconazole

  • Shin, Seung-Won
    • Natural Product Sciences
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    • v.11 no.2
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    • pp.92-96
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    • 2005
  • The antifungal activities of essential oils from the leaves of Glehnia littoralis, which is cultivated in Korea, were evaluated against pathogenic Trichophyton species by the broth dilution method and the disk diffusion test. Additionally, the effects of the oils together with ketoconazole were tested by the checkerboard titer test. The essential oil fraction and its main components showed significant inhibition of the tested Trichophyton fungi, with minimal inhibitor concentrations (MICs) in the range of 16-32 mg/ml. The results suggest that activities of this oil are based mainly on the contents of ${\alpha}-pinene$ (22.17%), the next prominent component of the oil fraction, while the first main components ${\beta}-pinene$ (57.83%) have relatively mild activity. The MICs of ${\alpha}-pinene$ and ${\beta}-pinene$ were 1-4 mg/ml and 4-32 mg/ml, respectively. Additionally the Glehnia oil fraction and its main components as well, exhibited significant synergism with ketoconazole against Trichophyton rubrum.

Effects of the Components and Extracts of Some Edible and Medicinal Plants on the Formation of Lipid Peroxide in Rat Liver Homogenate (식용 및 약용식물 추출물과 화합물이 흰쥐의 간장조직에서 과산화지질 생성에 미치는 영향)

  • 박종철;정신교;이종호;허종문;최명락;송상호;최종원
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.6
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    • pp.1159-1163
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    • 1997
  • We have studied the effect of 31 extracts and 10 components from some edible and medicinal plants on the formation of lipid peroxide in the liver homogenate of rat in vitro. The 70% acetone extracts of Allium tuberosum, Beta vulgaris var. cicla and Brassica juncea var. integrifolia, and methanol extract of Capsicum annuum decreased the formation of lipid peroxide by 33%, 58%, 62% and 56% at the concentration of 1mg/ml, respectively. And these four extracts inhibited the lipid peroxidation at the concentration of $10^{-1}$mg/ml by 17%, 46%, 49% and 45% respectively. Among the component tested, quercetin, quercitrin and isorhamnetin reduced the formation of lipid peroxide by 45%, 15% and 28% respectively at the concentration of $10^{-2}$mg/ml.

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Saprolegnia ferax에 의한$\beta$-amylase의 생산 및 특성

  • Bai, Suk;Cho, Nam-Chul;Chun, Soon-Bai
    • Microbiology and Biotechnology Letters
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    • v.25 no.2
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    • pp.109-114
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    • 1997
  • The Oomycete Saprolegnia ferax produces an extracellular $\beta$-amylase, Maximum enzyme yield was attained after 7 days of growth in YNB starch medium (pH 6.5) at 25$\circ$C. The amylase was pu- rified 24-fold by ultrafitration, HPLC DEAE column and HPLC gel filtration. The purfied enzyme was a monomeric glycoprotein with a molecular weight of about 44,000 dalton. The pH and temperature optima were 6.5 and 50$\circ$C, respectively. The enzyme was fairly stable up to 50$\circ$C and at acidic pH region (pH 4.0-7.0). The apparent Km and Vmax values of the enzyme against soluble starch were 0.77 mg/ml and 2,174 $\mu$moles/mg protein, respectively. Amino acid analysis indicated that the enzyme was enriched in alanine, glycine, leucine and acidic amino acid. Starch hydrolysis with the enzyme released maltose but not glucose, whereas maltotriose, Schardinger dextrin ($\alpha$-cyclodextrin) and pullulan were not hydrolysed by the enzyme. The enzyme was inhibited by Schardinger dextrin, p-chloromercuribenzoate(PCMB), CU$^{2+}$' and Hg$^{2+}$. Inhibition of the enzyme by PCMB could be reversed by the addition of cysteine and mercaptoethanol.

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