• Title/Summary/Keyword: Control Derivatives

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Topical or oral treatment of peach flower extract attenuates UV-induced epidermal thickening, matrix metalloproteinase-13 expression and pro-inflammatory cytokine production in hairless mice skin

  • Kwak, Chung Shil;Yang, Jiwon;Shin, Chang-Yup;Chung, Jin Ho
    • Nutrition Research and Practice
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    • v.12 no.1
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    • pp.29-40
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    • 2018
  • BACKGROUND/OBJECTIVES: Ultraviolet radiation (UV) is a major cause of skin photoaging. Previous studies reported that ethanol extract (PET) of Prunus persica (L.) Batsch flowers (PPF, peach flowers) and its subfractions, particularly the ethylacetate (PEA) and n-butanol extracts (PBT), have potent antioxidant activity and attenuate the UV-induced matrix metalloproteinase (MMP) expression in human skin cells. In this study, we investigated the protective activity of PPF extract against UV-induced photoaging in a mouse model. MATERIALS/METHODS: Hairless mice were treated with PET or a mixture of PEA and PBT either topically or orally along with UV irradiation. Histological changes and biochemical alterations of mouse skin were examined. Major phenolic compounds in PPF extract were analyzed using an ACQUITY UPLC system. RESULTS: The overall effects of topical and oral treatments with PPF extract on the UV-induced skin responses exhibited similar patterns. In both experiments, the mixture of PEA and PBT significantly inhibited the UV-induced skin and epidermal thickening, while PET inhibited only the UV-induced epidermal thickening. Treatment of PET or the mixture of PEA and PBT significantly inhibited the UV-induced MMP-13 expression, but not type I collagen expression. Topical treatment of the mixture of PEA and PBT with UV irradiation significantly elevated catalase, superoxide dismutase (SOD) and glutathione-peroxidase (GPx) activities in the skin compared to those in the UV irradiated control group, while oral treatment of the mixture of PEA and PBT or PET elevated only catalase and SOD activities, but not GPx. Thirteen phytochemical compounds including 4-O-caffeoylquinic acid, cimicifugic acid E and B, quercetin-3-O-rhamnoside and kaempferol glycoside derivatives were identified in the PPF extract. CONCLUSIONS: These results demonstrate that treatment with PET or the mixture of PEA and PBT, both topically or orally, attenuates UV-induced photoaging via the cooperative interactions of phenolic components having anti-oxidative and collagen-protective activities.

Physiological and Genetic Factors Controlling Streptomyces Regulatory Gene Expression Involved in Antibiotic Biosynthesis

  • Kim Eung Su
    • Proceedings of the Microbiological Society of Korea Conference
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    • 2002.10a
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    • pp.68-72
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    • 2002
  • While the biosynthetic gene cluster encoding the pigmented antibiotic actinorhodin is present in the two closely related bacterial species, Streptomyces lividans and Streptomyces coelicolor, it normally is expressed only in S. coelicolor---generating the deep blue colonies responsible for the S. coelicolor name. However, multiple copies of the afsR2 gene, which activates actinorhodin synthesis, result in the ability of S. lividansto also synthesize large amounts of actinorhodin. Here we report that the phenotypic property that historicially distinguishes these two Streptomycesspecies is determined conditionally by the carbon source used for culture. Whereas growth on glucose repressed actinorhodin production in S. lividans, culture on solid media containing glycerol as the sole carbon source dramatically increased the expression of afsR2 mRNA---leading to extensive actinorhodin synthesis by S. lividansand obliterating its phenotypic distinction from S. coelicolor. afsR2 transcription under these conditions was developmentally regulated, rising sharply at the time of aerial mycelium formation and coinciding temporally with the onset of actinorhodin production. Our results, which identify media-dependent parallel pathways that regulate actinorhodin synthesis in S. lividans, demonstrate carbon source control of actinorhodin production through the regulation of afsR2 mRNA synthesis. The nucleotide sequences of afsR2 revealed two putative important domains; the domain containing direct repeats in the middle and the domain homologous to sigma factor sequence in the C-terminal end. In this work, we constructed various sized afsR2-derivatives and compared the actinorhodin stimulating effects in S. lividans TK21. The experimental data indicate that the domain homologous to sigma factor sequence in the C-terminal end of afsR2 plays a critical role as an antibiotic stimulating function. In addition, we also observed that the single copy integration of afsR2 regulatory gene into S. lividans TK21 chromosome significantly activates antibiotic overproduction.

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Quantitative analysis of anthraquinones in Polygonum multiflorum Thunberg (하수오(何首烏)의 안트라퀴논 함량분석)

  • Lee, Hye-Won;Park, So-Young;Choo, Byung-Kil;Chae, Sung-Wook;Lee, A-Yeong;Kim, Ho-Kyoung
    • Korean Journal of Oriental Medicine
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    • v.13 no.3
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    • pp.157-163
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    • 2007
  • Objective: Polygonum multiflorum Thunberg (Polygonaceae) has been traditionally used as a tonic and the purgative in China and Korea. The genus Polygonum is a source of a wide range of phenolic compound, flavanoids, anthraquinones, stilbenes and tannins. In this study, three anthraquinones were isolated and quantitative determination of anthraquinones from P multiflorum has been developed for quality standardization. Methods : Three anthraquinone derivatives were isolated from a methanol extract of the radix of P. multiflorum by the chromatographic separation. Their structures were identified as emodin, physcion and ${\omega}$-hydroxyemodin on the basis of spectral data (MS, lH-NMR, 13C-NMR) and chemical analysis. HPLC analysis was performed to determine the contents of emodin, physcion, chrysophanol, rhein and ${\omega}$-hydroxyemodin in P. multiflorum from different specimens were collected from twenty Korean markets. Results: According to the results, the contents of emodin, physcion, chrysophanol, rhein and ${\omega}$-hydroxyemodin were 0.145%, 0.434%, 0.016%, 0.026%, 0.030% by HPLC, respectively. Conclusions : In these results, we have determined the contents of emodin, physcion, chrysophanol, rhein and ${\omega}$-hydroxyemodin in P. multiflorum, respectively. We hope that this study will contribute to the standardization and quality control of herbal medicine.

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Bioremediation Potential of a Tropical Soil Contaminated with a Mixture of Crude Oil and Production Water

  • Alvarez, Vanessa Marques;Santos, Silvia Cristina Cunha dos;Casella, Renata da Costa;Vitae, RonaIt Leite;Sebastin, Gina Vazquez;Seldin, Lucy
    • Journal of Microbiology and Biotechnology
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    • v.18 no.12
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    • pp.1966-1974
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    • 2008
  • A typical tropical soil from the northeast of Brazil, where an important terrestrial oil field is located, was accidentally contaminated with a mixture of oil and saline production water. To study the bioremediation potential in this area, molecular methods based on PCR-DGGE were used to determine the diversity of the bacterial communities in bulk and in contaminated soils. Bacterial fingerprints revealed that the bacterial communities were affected by the presence of the mixture of oil and production water, and different profiles were observed when the contaminated soils were compared with the control. Halotolerant strains capable of degrading crude oil were also isolated from enrichment cultures obtained from the contaminated soil samples. Twenty-two strains showing these features were characterized genetically by amplified ribosomal DNA restriction analysis (ARDRA) and phenotypically by their colonial morphology and tolerance to high NaCl concentrations. Fifteen ARDRA groups were formed. Selected strains were analyzed by 16S rDNA sequencing, and Actinobacteria was identified as the main group found. Strains were also tested for their growth capability in the presence of different oil derivatives (hexane, dodecane, hexadecane, diesel, gasoline, toluene, naphthalene, o-xylene, and p-xylene) and different degradation profiles were observed. PCR products were obtained from 12 of the 15 ARDRA representatives when they were screened for the presence of the alkane hydroxylase gene (alkB). Members of the genera Rhodococcus and Gordonia were identified as predominant in the soil studied. These genera are usually implicated in oil degradation processes and, as such, the potential for bioremediation in this area can be considered as feasible.

Comparison of biological and chemical assays for measuring the concentration of residual antibiotics after treatment with gamma irradiation

  • Nam, Ji-Hyun;Shin, Ji-Hye;Kim, Tae-Hun;Yu, Seungho;Lee, Dong-Hun
    • Environmental Engineering Research
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    • v.25 no.4
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    • pp.614-621
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    • 2020
  • Antibiotic pollution is one of the factors contributing to the spread of antibiotic-resistant bacteria in the environment. Advanced oxidation and irradiation processes have been introduced to eliminate antibiotics from water and wastewater. However, few studies have reported the toxic effects of residual antibiotics and their byproducts induced by a treatment system. In this study, we compared the efficacies of chemical (high-performance liquid chromatography (HPLC)) and biological (antimicrobial susceptibility test) assays for measuring the concentrations of residual antibiotics after gamma irradiation for degrading amoxicillin, cephradine, lincomycin, and tetracycline. The concentrations of residual antibiotics estimated using the two assay methods were almost identical, except cephradine. In the case of cephradine, inhibited bacterial growth was observed that was equivalent to twice the concentration measured by HPLC in the samples subjected to gamma irradiation. The observed inhibition of bacterial growth suggested the generation of potentially toxic intermediates following antibiotic degradation. These results indicate that biological and chemical assays should be used in concert for monitoring antibiotic contamination and the toxic derivatives of antibiotic degradation. The results demonstrate that these four antibiotics can be decomposed by 2.0 kGy gamma-irradiation without toxic effects of their byproducts.

Anti-Inflammatory Effect of Violapyrones B and C from a Marine-derived Streptomyces sp.

  • Lee, Hwa-Sun;An, Bong-Jeun;Kim, Hyeon Jeong;Cho, Yong Hun;Kim, Dong In;Jang, Jae Yoon;Kwak, Jae Hoon;Lee, Hyi-Seung;Lee, Yeon-Ju;Lee, Jong Seok;Shin, Hee Jae
    • Natural Product Sciences
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    • v.21 no.4
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    • pp.251-254
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    • 2015
  • Recently, we reported violapyrones B, C, H and I, unusual 3, 4, 6-trisubstituted ${\alpha}-pyrones$ derivatives, from the culture broth of the marine Streptomyces sp. 112CH148. In previous studies, violapyrones have been shown to have antibacterial and antitumor activities. However, the anti-inflammatory effect of violapyrones has not been reported yet. As part of our ongoing study for the discovery of bioactive metabolites from marine microorganisms, we found that violapyrones also have anti-inflammatory activity. In this study, we investigated the effect of violapyrones on LPS-induced inflammatory responses in vitro. Violapyrones B and C did not affect the viability of RAW 264.7 cells at concentrations up to $25{\mu}M$. However, violapyrones B and C inhibited the production of NO compared to the LPS-induced control. In addition, violapyrones B and C down-regulated the expression of iNOS protein in LPS-stimulated RAW 264.7 cells. To the best of our knowledge, this is the first report on the anti-inflammatory activity of violapyrones B and C.

Acute Toxicity of $P_2$, $B_1$, $T_{0}$, and $O_1$ in Rats and Mice

  • Yoon, Suh-young;Yoo, Kyeong-seok;Yim, Jae-woong;Kim, Bak-kwang;Cheong, Jae-hoon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.190-190
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    • 1998
  • $_2$(5,7-dipropoxychrysin), $B_1$(chrysin7-O-toluate), $T_{0}$(5-hydroxy-7-butoxy-chrysin), and $O_1$(5- hydroxy-7 -octoxychrysin) are chrysin derivatives which have isolated from Mori Cortex Radicis. They exhibited strong hypoglycemic effect, so they can be developed for hypoglycemic agents. In this study, we evaluated the acute toxicity of $P_2$, $B_1$, $T_{0}$, and $O_1$ by a single oral administration in rats and mice. The male SD rats and the male ICR mice were divided into 5 groups, and each group was treated orally with 500mg/kg $P_2$, $B_1$, $T_{0}$, and $O_1$, and control respectively. 500mg/kg is the highest dosage which can be administered to mouse. Each group of mice were subdivided as the dosage, 5mg/kg, 20mg/kg, l00mg/kg, and 500mg/kg. After oral administration, we examined food consumption, clinical signs and mortality of each group for 12 days. We also examined body weight increment of animals before and after treatment. Then organ weights were examined on 13th day. There was no toxic effect in mortality, body weight changes, food consumption, clinical signs and organ weights. We found out that the $LD_{50}$ of $P_2$, $B_1$, $T_{0}$, and $O_1$ is more than 500mg/kg in rats.

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Simultaneous Determination of Haloperidol and Its Metabolite, Reduced Haloperidol, in Plasma by Gas Chromatography Using Nitrogen Phosphorous Selective Detection (Gas Chromatography-Nitrogen Phosphorous Selective Detection을 이용한 혈장중 Haloperidol 및 대사체인 Reduced Haloperidol의 동시정량)

  • Park, Kyoung-Ho;Lee, Min-Hwa;Shim, Chang-Koo;Lee, Myung-Gull;Park, Jong-Sei
    • Journal of Pharmaceutical Investigation
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    • v.22 no.3
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    • pp.197-204
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    • 1992
  • A gas chromatographic method using nitrogen phosphorous selective detection was developed for simultaneous determination of haloperidol and its metabolite, reduced haloperidol, in human plasma. Combelen was used as internal standard, The method involved extraction and trimethylsilylation followed by the injection of $2-4\;{\mu}l$ of benzene layer, which was used to dissolve the trimethylsilylated derivatives of haloperidol and reduced haloperidol, onto SE-54 column [5% phenyl methyl silica fused capillary column, $16m{\times}0.22\;mm$ $(I.D.){\times}0.33\;{\mu}m$ (coated thickness)]. The temperature of column oven was programmed from $200^{\circ}C\;to\;300^{\circ}C$ at the increase rate of $10^{\circ}C/min and also the temperatures of injector and detector were set at $300^{\circ}C$. Helium was used as carrier gas and its flow rate was maintained at 30 ml/min. The detection was conducted with nitrogen phosphorous selective detector. The retention times for combelen, reduced haloperidol and haloperidol were found to be 9.14, 9.75 and 9.99 min, respectively. The detection limits for haloperidol and reduced haloperidol in human plasma were both 0.2 ng/ml. The coefficients of variation of the intra-assay were generally low (below 9.8%). The mean absolute recoveries of added haloperidol and reduced haloperidol from plasma were 72% and 84%, respectively. No interferences from endogenous substances were found.

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TEVC Studies of potent Antagonists of Human $P2X_3$ Receptor

  • Moon, Hyun-Duk;Lee, Jung-Sun;Park, Chul-Seung;Kim, Yong-Chul
    • Proceedings of the Korean Biophysical Society Conference
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    • 2003.06a
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    • pp.55-55
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    • 2003
  • P2X$_3$ receptor, a member of P2 purine receptors, is a ligand-gated ion channel activated by extracellular ATP as an endogenous ligand, and highly localized in peripheral and central sensory neurons. The activation of P2X3 receptor by ATP as the pronociceptive effect has been known to initiate the pain signaling involved in chronic inflammatory nociception and neuropathic pain by nerve injury, implicating the possibility of new drug development to control pains. In this study, we have developed a two electrode voltage clamp (TEVC) assay system to evaluate the inhibitory activity of several newly synthesized PPADS and a novel non-ionic antagonist against ATP activation of human P2X3 receptor. PPADS derivatives include several pyridoxine and pyridoxic acid analogs to study the effects of phosphate and aldehyde functional groups in PPADS. All new PPADS analogs were less potent than PPADS at human P2X$_3$ receptors, however, LDD130, a non-ionic analog showed potent antagonistic property with $IC_{50}$/ of 8.34 pM. In order to uncover the structure activity relationships of LDD130, and design new structural analogs, we synthesized and investigated a few structural variants of LDD130, and the results will be discussed in this presentation.

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Patterns of Plasma Fatty Acids in Rat Models with Adenovirus Infection

  • Paik, Man-Jeong;Park, Ki-Ho;Park, Joong-Jean;Kim, Kyoung-Rae;Ahn, Young-Hwan;Shin, Gyu-Tae;Lee, Gwang
    • BMB Reports
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    • v.40 no.1
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    • pp.119-124
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    • 2007
  • Adenoviral vectors are among the most promising vectors available for human gene therapy. However, the use of recombinant adenoviral vectors, including replicationcompetent adenovirus (RCA), raises a variety of safety concerns in relation to the development of new therapies based on gene therapy. To examine how organic compounds change in rat plasma following the injection of adenovirus, $\beta$-galactosidase expressing recombinant adenovirus (designated rAdLacZ) or RCA, we investigated the content of fatty acids (FAs), which are important biochemical indicators in pathological conditions. Pattern recognition analysis on the level of FAs in rat plasma is described for the visual discrimination of adenovirus infection groups from normal controls. Plasma FAs from four control rats (normal group), and from four rats with rAdLacZ infection and six rats with RCA infection (the two abnormal groups), were examined by gas chromatography-mass spectrometry in selected ion monitoring modes as their tert-butyldimethylsilyl derivatives. In total, 20 FAs were positively detected and quantified. The results of the Student's t-test on the normal mean of two abnormal groups, the levels of three FAs (p<0.05) from rAdLacZ group and eleven FAs (p<0.05) from RCA group were significantly different. When star symbol plotting was applied to the group mean values of 20 FAs after normalization to the corresponding normal mean values, the resulting eicosagonal star patterns of the two infected groups were distorted into similar shapes, but were distinguishable from each other. Thus, these approaches will be useful for screening and monitoring of diagnostic markers for the effects of infection following the use of adenoviral vectors in gene therapy.