• 제목/요약/키워드: 5-$HT_{1A}$

검색결과 599건 처리시간 0.033초

Neuroprotective and Anti-Neuroinflammatory Activities of Anthraquinones Isolated from Photorhabdus temperata Culture Broth

  • Yang, Eun-Ju;Kim, Seo-Hyun;Lee, Kyeong-Yeoll;Song, Kyung-Sik
    • Journal of Microbiology and Biotechnology
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    • 제28권1호
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    • pp.12-21
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    • 2018
  • Photorhabdus temperata (PT), a gram-negative bacterium, lives symbiotically within entomopathogenic nematodes. The insecticidal compounds derived from Photorhabdus are used as biopesticides in agriculture. However, the physiological properties are not well characterized. In the course of our screening for neuroprotective and anti-neuroinflammatory substances from natural products, the culture broth of PT showed considerable activities. By activity-guided purification, five anthraquinones, namely, 3-methoxychrysazine (1), 1,3-dimethoxy-8-hydroxy-9,10-anthraquinone (2), 1,3,8-trihydroxy-9,10-anthraquinone (3), 3,8-dihydroxy-1-methoxy-9,10-anthraquinone (4), and 1,3,4-trimethoxy-8-hydroxy-9,10-anthraquinone (5), were isolated from the ethyl acetate fraction of the PT culture broth. Among the isolated compounds, $75{\mu}M$ 3 significantly protected mouse hippocampal neuronal cells (HT22) against 5 mM glutamate-induced cell death via the inhibition of reactive oxygen species production, $Ca^{2+}$ influx, and lipid peroxidation. Additionally, 3 and 4 effectively suppressed the interferon-${\gamma}$-induced neuroinflammation of mouse-derived microglial cells (BV2) at 10 ng/ml, via the reduction of nitric oxide, interleukin-6, and tumor necrosis factor-${\alpha}$. Anthraquinones 3 and 4 derived from the PT culture broth are a potential starting point to discover neuroprotective and anti-neuroinflammatory drug leads. The novel compound 5 is reported for the first time in this study.

Antioxidant and Anti-Inflammatory Effect of Probiotic Lactobacillus plantarum KU15149 Derived from Korean Homemade Diced-Radish Kimchi

  • Han, Kyoung Jun;Lee, Ji-Eun;Lee, Na-Kyoung;Paik, Hyun-Dong
    • Journal of Microbiology and Biotechnology
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    • 제30권4호
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    • pp.591-598
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    • 2020
  • Lactobacillus plantarum KU15149 was demonstrated to have probiotic behavior and functions, including antioxidant and anti-inflammatory activity. L. plantarum KU15149 obtained from homemade diced-radish kimchi has a high survival rate under artificial gastric acid (pH 2.5, 0.3% pepsin) and bile salt (0.3% oxgall) conditions. However, L. plantarum KU15149 did not produce β-glucuronidase, which is known to be a carcinogenic enzyme with resistance to several antibiotics, such as gentamycin, kanamycin, streptomycin, tetracycline, and ciprofloxacin. L. plantarum KU15149 strongly adhered to HT-29 cells and had high antioxidant activity in terms of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical-scavenging and β-carotene bleaching assays. L. plantarum KU15149 also exhibited a pronounced inhibition of nitric oxide (NO) production, along with expression of nitric oxide synthase (iNOS) and cyclooxygenase -2 (COX-2) as well as pro-inflammatory cytokines, such as TNF-α, IL-1β, and IL-6, when RAW 264.7 cells were stimulated with LPS. Therefore, L. plantarum KU15149 exhibited pharmaceutical functionality as a potential probiotic.

Efficacy of Aprepitant in Patients with Advanced or Recurrent Lung Cancer Receiving Moderately Emetogenic Chemotherapy

  • Uchino, Junji;Hirano, Ryosuke;Tashiro, Naoki;Yoshida, Yuji;Ushijima, Shinichiro;Matsumoto, Takemasa;Ohta, Keiichi;Nakatomi, Keita;Takayama, Koichi;Fujita, Masaki;Nakanishi, Yoichi;Watanabe, Kentaro
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권8호
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    • pp.4187-4190
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    • 2012
  • Aims and Background: To evaluate the efficacy of a combination of aprepitant and conventional antiemetic therapy in patients with advanced or recurrent lung cancer receiving moderately emetogenic chemotherapy (MEC). Methods: Patients with advanced or recurrent lung cancer who were treated with MEC regimens at the Department of Respiratory Medicine, Fukuoka University Hospital, were included and classified into the following groups: control group (treatment: 5-HT3 receptor antagonists + dexamethasone) and aprepitant group (treatment: 5-HT3 receptor antagonists + dexamethasone + aprepitant). The presence or absence of chemotherapy-induced nausea and vomiting (CINV) was evaluated according to the Common Terminology Criteria for Adverse Events (CTCAE) v4.0; patients with grade 1 or above were considered positive for CINV. Food intake per day, completion of planned chemotherapy, and progression-free survival (PFS) achieved by chemotherapy were investigated. Results: The complete suppression rate of nausea in the aprepitant group was significantly higher than that in the control group (p = 0.0043). Throughout the study, the food intake in the aprepitant group was greater than that in the control group, with the rate being significantly higher, in particular, on day 5 (p = 0.003). The completion rate of planned chemotherapy was also higher in the aprepitant group (p = 0.042). PFS did not differ significantly, but tended to be improved in the aprepitant group. Conclusions: The aprepitant group showed significantly higher complete suppression of nausea, food intake on day 5, and completion of planned chemotherapy than the control group.

Antimutagenic and Cytotoxicity Effects of Agaricus blazei Murill Extracts (아가리쿠스버섯(Agaricus blazei Murill) 추출물의 항돌연변이원성 및 세포독성 효과)

  • Ji, Jeong-Hwan;Kim, Mi-Nam;Choi, Kun-Pyo;Chung, Cha-Kwon;Ham, Seung-Shi
    • Korean Journal of Food Science and Technology
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    • 제32권6호
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    • pp.1371-1378
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    • 2000
  • This study was performed to determine the antimutagenic and cytotoxic effect of Agaricus blazei Murill methanol extract on Salmonella typhimurium TA98, TA100 and human cancer cell lines using Ames test and cytotoxicity assay, respectively. In Ames test, methanol extract from A. blazei Murill did not exhibit any mutagenicity and most of the samples showed high antimutagenic effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), 4-nitroquinoline-1-oxide(4NQO), 3-amino-1,4-dimethyl-5H-pyrido [4,3-b] indol(Trp-P-1) and $benzo({\alpha})pyrene(B({\alpha})P)$. The methanol extracts of A. blazei Murill$(200\;{\mu}g/plate)$ showed approximately 92.4%, 81.9% and 83.4% inhibitory effect on the mutagenesis induced by 4NQO, Trp-P-1 and $B({\alpha})P$ against TA98 strain, whereas 87.3%, 94.7%. 92.3% and 89.9% inhibitions were observed on the mutagenesis induced by MNNG, 4NQO, Trp-P-1 and $B({\alpha})P$ against TA100 strain. The solvent fractions of methanol extracts from A. blazei Murill except water fraction showed high antimutagenic effects of $70{\sim}90%$ against mutation induced by MNNG, 4NQO. Trp-P-1 and $B({\alpha})P$. In anticancer effects of A. blazei Murill extract and fraction against cancer cell lines including human breast adenocarcinoma(MCF7), human lung carcinoma(A549), human fibrosarcoma(HT1080), human hepatocellular carcinoma(Hep3B), human epitheloid carcinoma(HeLa), human gastric carcinoma(KATO III) and human chronic myelogenous leukemia(K562) were investigated. The treatment of 1 mg/mL A. blazei Murill extracts had the highest cytotoxicity with 91.9% against HeLa, followed by KATO III(88.7%), A549(86.5%) and Hpe3B(84.3%). Whereas 1 mg/mL treatment of A. blazei Murill extracts had only $10{\sim}40%$ cytotoxicity on human normal liver cell (WRL68).

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Hematological Characteristics of Olive Flounder (Paralichthys olivaceus) in Culture Farm Influenced by Heated Effluent Water from a Power Plant in Summer (여름철 온배수 수역에 인접한 양식장 넙치(Paralichthys olivaceus)의 혈액 성상)

  • Chang, Young-Jin;Hur, Jun-Wook;Chin, Pyung
    • Journal of Aquaculture
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    • 제15권4호
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    • pp.267-273
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    • 2002
  • Effect of heated water from a power plant in summer on hematological characteristics of flounder (Paralichthys olivaceus) were investigated. Hematocrit level fluctuated between 15.7 and 16.3% in control farm, but it significantly increased to 17.7% in the high-WT farm. The corresponding values for hemoglobin concentration were 9.9~18.0 $g/㎗$ for the control farm and 6.2~19.4 $g/㎗$ for the exposed farm. The plasma cortisol remained between 0.6 and 2.8 ng/$ml$ in the former but significantly decreased 317.1 to 3.3 ng/$ml$ in the later. The plasma glucose also decreased from 36.5~46.0 to 23.5~36.5 mg/$dl$. Plasma osmolality decreased from 551.5~597.0 to 391.0~466.5 mOsm/kg.

Replacement of ITO for efficient organic polymer solar cells (ITO를 대체한 고효율 유기박막 태양전지)

  • Kim, Jae Ryoung;Park, Jin Uk;Lee, Bohyun;Lee, Pyo;Lee, Jong-Cheol;Moon, Sang-Jin
    • 한국신재생에너지학회:학술대회논문집
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    • 한국신재생에너지학회 2010년도 춘계학술대회 초록집
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    • pp.69.1-69.1
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    • 2010
  • We have fabricated organic photovoltaic cells (OPVs) with highly conductive poly 3,4-ethylenedioxythiophene : poly styrenesulfonate (PEDOT:PSS) layer as an anode without using transparent conducting oxide (TCO), which has been modified by adding some organic solvents like sorbitol (So), dimethyl sulfoxide (DMSO), N-methyl-pyrrolidone (NMP), dimethylformamide (DMF), and ethylene glycol (EG). The conductivity of PEDOT:PSS film modified with each additive was enhanced by three orders of magnitude. According to atomic force microscopy (AFM) study, conductivity enhancement might be related to better connections between the conducting PEDOT chains. TCO-free solar cells with modified PEDOT:PSS layer and the active layer composed of poly(3-hexylthiophene) (P3HT) and phenyl [6,6] C61 butyric acid methyl ester (PCBM) exhibited a comparable device performance to indium tin oxide (ITO) based organic solar cells. The power conversion efficiency (PCE) of the organic solar cells incorporating DMSO, So + DMSO and EG modified PEDOT:PSS layer reached 3.51, 3.64 and 3.77%, respectively, under illumination of AM 1.5 (100mW/$cm^2$).

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Changes of splenocyte $IFN-{\gamma}$ mRNA synthesis in rats infected with Paragonimus westermani

  • Cho, Jun-Kyong;KWon, Hye-Soo;Joo, Kyoung-Hwan;Lee, Joon-Sang;Cho, Sung-Weon
    • Parasites, Hosts and Diseases
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    • 제37권4호
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    • pp.285-287
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    • 1999
  • Changes in the expression level of splenocyte $IFN-{\gamma}$mRNA of Sprague-Dawley (SD) rats infected with Paragonimus westermani were analyzed by competitive reverse transcription-polymerase chain reaction (RT-PCR) followed by southern blot. The template RNA was extracted from the splenocytes of rats infected with 20 metacercariae of P. westermani. The products of competitive RT-PCR were subjected to southern blot and enhanced chemiluminescence (ECL), and analyzed with a densitometer. In comparison with that of uninfected control rat splenocytes (value of 1), the levels of mRNA expression of $IFN-{\gamma}$had changed to 0.747 at 1 week post infection (PI), 0.00175 at 2 week PI, 0.0217 at 3 week PI, 0.194 at 4 week PI and then to 0.537 at 5 week PI. The level at 7 week PI had returned to 1.25, comparable with that of uninfected rats. These results show that, when infected with p. westermani, the levels of $IFN-{\gamma}$ mRNA of SD rat splenocytes were remarkably reduced by more than 500 times at 2 week PI and restored to normal level at 7 week PI.

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Inhibitory Effects of Rehmannia glutinosa Liboschitz on Endothelial Cell Proliferation

  • Lee, Sung-Jin;Lee, Hak-Kyo
    • Korean Journal of Medicinal Crop Science
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    • 제15권5호
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    • pp.311-314
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    • 2007
  • Vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) are the most important angiogenic molecules associated with tumor-induced neovascularization. This study was carried out to investigate inhibitory effect of extracts from root of Rehmannia glutinosa LIBOSCHITZ (Rehmannia Radix and Rehmannia Radix Preparata) on endothelial cell proliferation. The methanol extracts from the medicinal herb were fractionated into n-hexane, ethyl acetate, n-butanol and aqueous fractions. Among the four fractions, the n-butanol fraction from R. Radix on exhibited highly effective inhibition (${\approx}79%$ inhibition) on the binding of KDR/Flk-1-Fc to immobilized $VEGF_{165}$ and then ethyl acetate fraction from R. Radix (${\approx}45%$ inhibition) at the concentration of $100\;{\mu}g/ml$. The n-butanol fraction efficiently blocked the VEGF- and bFGF-induced HUVEC proliferation in a dose-dependent manner, but did not affect the growth of HT1080 human fibrosarcoma cells. The n-butanol fraction more efficiently blocked the binding of KDR/Flk-1-Fc to immobilized $VEGF_{165}$ and VEGF- and bFGF-induced human umbilical vein endothelial cell proliferation than the fraction from R. Radix Preparata. Our results suggest that Rehmannia Radix may be used as a candidate for developing anti-angiogenic agent.

Heavy Metal Ion Detection in Living Cell Using Fluorescent Chemosensor (형광화학센서를 이용한 살아있는 세포 내에서의 중금속이온검출)

  • Kwon, Pil-Seung;Kim, Jin-Kyung;Kim, Jong-Wan
    • Journal of the Korean Chemical Society
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    • 제54권4호
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    • pp.451-459
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    • 2010
  • The fluorescence detection of intracellular metal ions are high interest in the fields of organic molecular chemistry and cellular biology. This study was purposed to detection for mercury and zinc in the cell using fluorescent chemosensor (FS). FS exhibits a weak fluorescence, but emits strong fluorescence upon Zn$^{2+}$ complexation. The increased fluorescence of the 2FS/Zn$^{2+}$ can be quenched completely by addition of only 1 equiv of Hg$^{2+}$ with the formation of complex FS-Hg$^{2+}$. Four cell lines (LLC-MK2, Hela, HT29 and AMC-HN3) were used for fluorescence imaging by confocal microscope. The cell viability MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was evaluated after cell treatment of FS, Zn$^{2+}$, FS-Zn$^{2+}$, Hg$^{2+}$ on LLC-MK2 cell line. The cytotoxicity of FS was showed to viability over 80%. This study has shown that FS can be detected for selective imaging of Zn$^{2+}$ and Hg$^{2+}$ in living cells.

Screening of Biological Activities of Ethanol Extracts from Fermented Gastrodia elata Blume (발효 천마 에탄올 추출물의 생리활성 검정)

  • Kim, Mi Hyun
    • The Korean Journal of Food And Nutrition
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    • 제27권5호
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    • pp.837-844
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    • 2014
  • This study was carried out to analyze the differences in p-hydroxylbenzyl alcohol (HBA) content, antitumor and anti-obesity activities and tyrosinase inhibitory activity between non-fermented G. elata (NFGP) and fermented G. elata powder. The HBA content, which is an index-component of G. elata decreased from 1.58 mg/g before fermentation to 1.07, 0.32, and 0.13 mg/g after the $1^{st}$ fermentation ($1^{st}$ FGP), $2^{nd}$ fermentation ($2^{nd}$ FGP) and $3^{rd}$ fermentation ($3^{rd}$ FGP), respectively. The anti-proliferation effects on the cell lines HT29 and AGS were significantly higher for the fermented G. elata than the NFGP. The antitumor activity was also increased in a fermentation number-dependent manner. During adipocyte differentiation, the ethanol extract of the $3^{rd}$ FGP inhibited lipid accumulation in 3T3-L1 cells significantly better than NFGP and the $1^{st}$ FGP, treated at the concentration of $10{\mu}g/mL$. The tyrosinase inhibitory activity of the $2^{nd}$ FGP at $600{\mu}g/mL$ over was higher than that of kojic acid. At the concentration of $1,000{\mu}g/mL$, the tyrosinase inhibitory activity was increased in a fermentation number-dependent manner. From these results, the fermented G. elata, especially the $3^{rd}$ FGP, is expected to be good candidate for the development of functional food and agents with antitumor, anti-obesity, and tyrosinase inhibitory potential.