• Title/Summary/Keyword: inhibitory index

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Plasma Cholesterol-Lowering Effects of Cinnamomi cortex Extract as an Inhibitor of Pancreatic Cholesterol Esterase (췌장 콜레스테롤 에스터레이즈 저해제로서의 계피 추출물레 혈중 콜레스테롤 농도에 미치는 영향)

  • 김희숙;최종원;허영미;류성호;서판길
    • Journal of Life Science
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    • v.12 no.1
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    • pp.106-112
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    • 2002
  • Ethanol extract of Cinnamomi cortex inhibited potently cholesterol esterase activity in vitro. Chloroform fraction of ethanol extract showed the stronger inhibitory effect than other solvent fractions - ethylacetate fraction, butanol fraction, and aqueous fraction. The chloroform fraction of Cinnamomi cortex was studied as a candidator of plasma cholesterol-lowering material using high cholesterol-fed rats. In high cholesterol-fed rats, the diet with chloroform fraction of 150 mg/kg lowered not only plasma neutral lipids contents 25.1% but also plasma total cholesterol level 49.6% than only high cholesterol diet. Plasma HDL-cholesterol level in Cinnamomi cortex chloroform fraction-fed rats was recovered as those level of normal rats. LD$_{50}$ of Cinnamomi chloroform extract was calculated as 1,300 mg/kg.

PIV measurement and numerical investigation on flow characteristics of simulated fast reactor fuel subassembly

  • Zhang, Cheng;Ju, Haoran;Zhang, Dalin;Wu, Shuijin;Xu, Yijun;Wu, Yingwei;Qiu, Suizheng;Su, G.H.
    • Nuclear Engineering and Technology
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    • v.52 no.5
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    • pp.897-907
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    • 2020
  • The flow characteristics of reactor fuel assembly always intrigue the designers and the experimentalists among the myriad phenomena that occur simultaneously in a nuclear core. In this work, the visual experimental method has been developed on the basis of refraction index matching (RIM) and particle image velocimetry (PIV) techniques to investigate the detailed flow characteristics in China fast reactor fuel subassembly. A 7-rod bundle of simulated fuel subassembly was fabricated for fine examination of flow characteristics in different subchannels. The experiments were performed at condition of Re=6500 (axial bulk velocity 1.6 m/s) and the fluid medium was maintained at 30℃ and 1.0 bar during operation. As for results, axial and lateral flow features were observed. It is shown that the spiral wire has an inhibitory effect on axial flow and significant intensity of lateral flow mixing effect is induced by the wire. The root mean square (RMS) of lateral velocity fluctuation was acquired after data processing, which indicates the strong turbulence characteristics in different flow subchannels.

A Novel Niosomal Combination of Selenium Coupled with Glucantime against Leishmania tropica

  • Mostafavi, Mahshid;Khazaeli, Payam;Sharifi, Iraj;Farajzadeh, Saeedeh;Sharifi, Hamid;Keyhani, Alireza;Parizi, Maryam Hakimi;Kakooei, Sina
    • Parasites, Hosts and Diseases
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    • v.57 no.1
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    • pp.1-8
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    • 2019
  • There is no effective treatment modality available against different forms of leishmaniasis. Therefore, the aim of this study was to improve the penetration and efficacy of selenium and glucantime coupled with niosomes and compared them with their simple forms alone on in vitro susceptibility assays. In this study, the niosomal formulations of selenium and in combination with glucantime were prepared. The size and morphology of the niosomal formulations were characterized and the effectivity of the new formulation was also evaluated using in vitro MTT assay, intra-macrophage model, and gene expression profile. From the results obtained, no cytotoxicity effect was observed for niosomal and simple forms of drugs, as alone or in combination. Niosomal formulations of the drugs significantly showed more inhibitory effects ($P{\leq}0.001$) than the simple drugs when the selectivity index was considered. The gene expression levels of Interleukin (IL-10) significantly decreased, while the level of IL-12 and metacaspase significantly increased ($P{\leq}0.001$). The results of the present study showed that selenium plus glucantime niosome possess a potent anti-leishmanial effect and enhanced their lethal activity as evidenced by the in vitro experiments.

Effects of adenosine receptor agonist on the rocuronium-induced neuromuscular block and sugammadex-induced recovery

  • Kim, Yong Beom;Lee, Sangseok;Choi, Hey Ran;In, Junyong;Chang, Young Jin;Kim, Ha Jung;Ro, Young Jin;Yang, Hong-Seuk
    • Korean Journal of Anesthesiology
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    • v.71 no.6
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    • pp.476-482
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    • 2018
  • Background: Several types of receptors are found at neuromuscular presynaptic membranes. Presynaptic inhibitory $A_1$ and facilitatory $A_{2A}$ receptors mediate different modulatory functions on acetylcholine release. This study investigated whether adenosine $A_1$ receptor agonist contributes to the first twitch tension (T1) of train-of-four (TOF) stimulation depression and TOF fade during rocuronium-induced neuromuscular blockade, and sugammadex-induced recovery. Methods: Phrenic nerve-diaphragm tissues were obtained from 30 adult Sprague-Dawley rats. Each tissue specimen was randomly allocated to either control group or 2-chloroadenosine (CADO, $10{\mu}M$) group. One hour of reaction time was allowed before initiating main experimental data collection. Loading and boost doses of rocuronium were sequentially administered until > 95% depression of the T1 was achieved. After confirming that there was no T1 twitch tension response, 15 min of resting time was allowed, after which sugammadex was administered. Recovery profiles (T1, TOF ratio [TOFR], and recovery index) were collected for 1 h and compared between groups. Results: There were statistically significant differences on amount of rocuronium (actually used during experiment), TOFR changes during concentration-response of rocuronium (P = 0.04), and recovery profiles (P < 0.01) of CADO group comparing with the control group. However, at the initial phase of this experiment, dose-response of rocuronium in each group demonstrated no statistically significant differences (P = 0.12). Conclusions: The adenosine $A_1$ receptor agonist (CADO) influenced the TOFR and the recovery profile. After activating adenosine receptor, sugammadex-induced recovery from rocuronium-induced neuromuscular block was delayed.

Combination of berberine and ciprofloxacin reduces multi-resistant Salmonella strain biofilm formation by depressing mRNA expressions of luxS, rpoE, and ompR

  • Shi, Chenxi;Li, Minmin;Muhammad, Ishfaq;Ma, Xin;Chang, Yicong;Li, Rui;Li, Changwen;He, Jingshan;Liu, Fangping
    • Journal of Veterinary Science
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    • v.19 no.6
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    • pp.808-816
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    • 2018
  • Bacterial biofilms have been demonstrated to be closely related to clinical infections and contribute to drug resistance. Berberine, which is the main component of Coptis chinensis, has been reported to have efficient antibacterial activity. This study aimed to investigate the potential effect of a combination of berberine with ciprofloxacin (CIP) to inhibit Salmonella biofilm formation and its effect on expressions of related genes (rpoE, luxS, and ompR). The fractional inhibitory concentration (FIC) index of the combination of berberine with CIP is 0.75 showing a synergistic antibacterial effect. The biofilm's adhesion rate and growth curve showed that the multi-resistant Salmonella strain had the potential to form a biofilm relative to that of strain CVCC528, and the antibiofilm effects were in a dose-dependent manner. Biofilm microstructures were rarely observed at $1/2{\times}MIC/FIC$ concentrations (MIC, minimal inhibition concentration), and the combination had a stronger antibiofilm effect than each of the antimicrobial agents used alone at $1/4{\times}FIC$ concentration. LuxS, rpoE, and ompR mRNA expressions were significantly repressed (p< 0.01) at $1/2{\times}MIC/FIC$ concentrations, and the berberine and CIP combination repressed mRNA expressions more strongly at the $1/4{\times}FIC$ concentration. The results indicate that the combination of berberine and CIP has a synergistic effect and is effective in inhibiting Salmonella biofilm formation via repression of luxS, rpoE, and ompR mRNA expressions.

Antibacterial activity of florfenicol composite nanogels against Staphylococcus aureus small colony variants

  • Liu, Jinhuan;Ju, Mujie;Wu, Yifei;Leng, Nannan;Algharib, Samah Attia;Luo, Wanhe
    • Journal of Veterinary Science
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    • v.23 no.5
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    • pp.78.1-78.13
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    • 2022
  • Background: Florfenicol might be ineffective for treating Staphylococcus aureus small colony variants (SCVs) mastitis. Objectives: In this study, florfenicol-loaded chitosan (CS)-sodium tripolyphosphate (TPP) composite nanogels were prepared to allow targeted delivery to SCV infected sites. Methods: The formulation screening, the characteristics, in vitro release, antibacterial activity, therapeutic efficacy, and biosafety of the florfenicol composite nanogels were studied. Results: The optimized formulation was obtained when the CS and TPP were 10 and 5 mg/mL, respectively. The encapsulation efficiency, loading capacity, size, polydispersity index, and zeta potential of the optimized florfenicol composite nanogels were 87.3% ± 2.7%, 5.8% ± 1.4%, 280.3 ± 1.5 nm, 0.15 ± 0.03, and 36.3 ± 1.4 mv, respectively. Optical and scanning electron microscopy showed that spherical particles with a relatively uniform distribution and drugs might be incorporated in cross-linked polymeric networks. The in vitro release study showed that the florfenicol composite nanogels exhibited a biphasic pattern with the sustained release of 72.2% ± 1.8% at 48 h in pH 5.5 phosphate-buffered saline. The minimal inhibitory concentrations of commercial florfenicol solution and florfenicol composite nanogels against SCVs were 1 and 0.25 ㎍/mL, respectively. The time-killing curves and live-dead bacterial staining showed that the florfenicol composite nanogels were concentration-dependent. Furthermore, the florfenicol composite nanogels displayed good therapeutic efficacy against SCVs mastitis. Biological safety studies showed that the florfenicol composite nanogels might be a biocompatible preparation because of their non-toxic effects on the renal tissue and liver. Conclusions: Florfenicol composite nanogels might improve the treatment of SCV infections.

Characteristics and Comparison of Antimicrobial Resistance Patterns of Escherichia coli Isolated from Fish Farms in the South Coast of Korea in 2018-2019 (2018-2019년 남해안 어류양식장에서 분리한 대장균(Escherichia coli)의 항생제 내성 특성 및 비교)

  • Kunbawui Park;Yeoun Joong Jung;Hong Sik Yu;Mi Ra Jo;Yeon Gyeom Jeong;Kwang Tae Son;Jong Soo Mok
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.56 no.2
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    • pp.188-195
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    • 2023
  • Antimicrobial resistance patterns of Escherichia coli strains isolated from 30 seawater samples and 30 Korean rockfish Sebastes schlegelii collected from fish farms off the South Coast of Korea in 2018-2019, were investigated. The isolated E. coli (154 strains) showed the highest antimicrobial resistance to tetracycline (44.8%) followed by chloramphenicol (38.3%), streptomycin (37.6%), and trimethoprim/sulfamethoxazole (35.7%). The antimicrobial resistance rate was higher in E. coli strains isolated from Korean rockfish than those from seawater. Multiple antibiotic resistance (MAR) against at least three antimicrobials (MAR index: ≥0.2) was observed in 35.6% and 79.2% of the seawater and Korean rockfish isolates, respectively. In conclusion, continuous monitoring is required to identify changes in antimicrobial resistance and their correlations in the aquatic environment and products.

Mixture of Corni Fructus and Schisandrae Fructus improves testosterone-induced benign prostatic hyperplasia through regulating 5α-reductase 2 and androgen receptor

  • Hyun Hwangbo;Min Yeong Kim;Seon Yeong Ji ;Beom Su Park;TaeHee Kim;Seonhye Yoon;Hyunjin Kim;Sung Yeon Kim ;Haeun Jung;Taeiung Kim;Hyesook Lee;Gi-Young Kim;Yung Hyun Choi
    • Nutrition Research and Practice
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    • v.17 no.1
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    • pp.32-47
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    • 2023
  • BACKGROUND/OBJECTIVES: Benign prostatic hyperplasia (BPH) characterized by an enlarged prostate gland is common in elderly men. Corni Fructus (CF) and Schisandrae Fructus (SF) are known to have various pharmacological effects, including antioxidant and anti-inflammatory activities. In this study, we evaluated the inhibitory efficacy of CF, SF, and their mixture (MIX) on the development of BPH using an in vivo model of testosterone-induced BPH. MATERIALS/METHODS: Six-week-old male Sprague-Dawley rats were randomly divided into seven groups. To induce BPH, testosterone propionate (TP) was injected to rats except for those in the control group. Finasteride, saw palmetto (SP), CF, SF, and MIX were orally administered along with TP injection. At the end of treatment, histological changes in the prostate and the level of various biomarkers related to BPH were evaluated. RESULTS: Our results showed that BPH induced by TP led to prostate weight and histological changes. Treatment with MIX effectively improved TP-induced BPH by reducing prostate index, lumen area, epithelial thickness, and expression of BPH biomarkers such as 5α-reductase type 2, prostate-specific antigen, androgen receptor, and proliferating cell nuclear antigen compared to treatment with CF or SF alone. Moreover, MIX further reduced levels of elevated serum testosterone, dihydrotestosterone, and prostate-specific antigen in BPH compared to the SP, a positive control. BPH was also improved more by MIX than by CF or SF alone. CONCLUSIONS: Based on the results, MIX is a potential natural therapeutic candidate for BPH by regulating 5α-reductase and AR signaling pathway.

Enhanced antibacterial activity of tilmicosin against Staphylococcus aureus small colony variants by chitosan oligosaccharide-sodium carboxymethyl cellulose composite nanogels

  • Luo, Wanhe;Liu, Jinhuan;Zhang, Shanling;Song, Wei;Algharib, Samah Attia;Chen, Wei
    • Journal of Veterinary Science
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    • v.23 no.1
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    • pp.1.1-1.11
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    • 2022
  • Background: The poor bioadhesion capacity of tilmicosin resulting in treatment failure for Staphylococcus aureus small colony variants (SASCVs) mastitis. Objectives: This study aimed to increase the bioadhesion capacity of tilmicosin for the SASCVs strain and improve the antibacterial effect of tilmicosin against cow mastitis caused by the SASCVs strain. Methods: Tilmicosin-loaded chitosan oligosaccharide (COS)-sodium carboxymethyl cellulose (CMC) composite nanogels were formulated by an electrostatic interaction between COS (positive charge) and CMC (negative charge) using sodium tripolyphosphate (TPP) (ionic crosslinkers). The formation mechanism, structural characteristics, bioadhesion, and antibacterial activity of tilmicosin composite nanogels were studied systematically. Results: The optimized formulation was comprised of 50 mg/mL (COS), 32 mg/mL (CMC), and 0.25 mg/mL (TPP). The size, encapsulation efficiency, loading capacity, polydispersity index, and zeta potential of the optimized tilmicosin composite nanogels were 357.4 ± 2.6 nm, 65.4 ± 0.4%, 21.9 ± 0.4%, 0.11 ± 0.01, and -37.1 ± 0.4 mV, respectively; the sedimentation rate was one. Scanning electron microscopy showed that tilmicosin might be incorporated in nano-sized crosslinked polymeric networks. Moreover, adhesive studies suggested that tilmicosin composite nanogels could enhance the bioadhesion capacity of tilmicosin for the SASCVs strain. The inhibition zone of native tilmicosin, tilmicosin standard, and tilmicosin composite nanogels were 2.13 ± 0.07, 3.35 ± 0.11, and 1.46 ± 0.04 cm, respectively. The minimum inhibitory concentration of native tilmicosin, tilmicosin standard, and tilmicosin composite nanogels against the SASCVs strain were 2, 1, and 1 ㎍/mL, respectively. The in vitro time-killing curves showed that the tilmicosin composite nanogels increased the antibacterial activity against the SASCVs strain. Conclusions: This study provides a potential strategy for developing tilmicosin composite nanogels to treat cow mastitis caused by the SASCVs strain.

3-Phenethyl-2-phenylquinazolin-4(3H)-one isolated from marine-derived Acremonium sp. CNQ-049 as a dual- functional inhibitor of monoamine oxidases-B and butyrylcholinesterase

  • Jong Min Oh;Prima F. Hillman;Sang-Jip Nam;Hoon Kim
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.165-170
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    • 2023
  • Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC50 value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC50 value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.