• Title/Summary/Keyword: inhibitior

Search Result 10, Processing Time 0.021 seconds

Purification and Characterization of Aminoglycoside-Resistant inhibitior from methylotrophic Actinomycetes (Methanol 자화 방선균으로부터 Aminoglycoside 내성 저해물질의 정제 및 특성)

  • 김현수;신재욱
    • Microbiology and Biotechnology Letters
    • /
    • v.27 no.3
    • /
    • pp.215-222
    • /
    • 1999
  • Methylotrophic actinomycetes No. 155 produced an aminoglycoside antibiotics(AG)-resistant inhibitor. We have previously reported that the inhibitor shows strong inhibition to sisomicin-resistant strain. In order to understand the functions of inhibitor and sisomicin-resistance, characterizations and purification of inhibitor were investigated. Strain No. 155 was tentatively identified as Nocardiopsis sp. based on morphological and some physiological characteristics. In the antimicrobial activity test, the addition of inhibitor to sisomicin showed a reduction effect of MIC on the test strains such as Gram(+), Gram(-) bacteria and yeasts. The combination of the inhibitor and various antibiotics revealed synergistic against E. coli K-12 and B. subtilis PCI 219. The induced intracellular proteins from sisomicin-resistant strain exhibited the sisomicin inactivation by invitro test. And the induced intracellular proteins were inactivated by addition of the inhibitor. The inhibitor compound was purified by anion exchange chromatography(Dowex-1) and HPLC using Asahipak ES-502C column. The purified inhibitor compound was detected in a single peak(above 98.5% purity) through the HPLC analysis.

  • PDF

Inhibitors of Nitric Oxide Synthesis from Ginseng in Activated Macrophages (활성화한 RAW 264.7 세 포주에서 인삼 Polyacetylene류의 Nitric Oxide 생성저해)

  • 류재하;장세란
    • Journal of Ginseng Research
    • /
    • v.22 no.3
    • /
    • pp.181-187
    • /
    • 1998
  • Nitric Oxide (NO), derived from L-arginine, is produced by two types (constitutive and inducible) of nitric oxide synthase (NOS). The NO produced in large amounts by the inducible NOS is known to be responsible for the vasodilation and hypotension observed in septic shock. We have found three polyacetylene compounds which inhibited the production of NO in LPS-activated RAW 264.7 cells. Their structures were identified as panauynol, ginsenoyne A and PQ-6 by the spec- troscopic analysis (IC50 values were 32.3 $\mu$M, 2.3 $\mu$M, 1.5 $\mu$M, respectively). These polyacetylenes may be useful candidates for the development of new drug to treat endotoxemia and inflammation accompanied by the overproduction of NO.

  • PDF

Alterations in Dichloromethane-Induced Carboxyhemoglobin Elevation by Several Metabolic Modulators (이염화메탄에 의한 Carboxyhemogolbin 생성에 몇몇 대사활성조절제들이 미치는 영향)

  • 강경애;김영철
    • Toxicological Research
    • /
    • v.11 no.2
    • /
    • pp.273-277
    • /
    • 1995
  • Several metabolic modulators on the generation of carbon monoxide (CO)from dichloromethane (DCM) was examined in adult female rats. It has been known that DCM is converted to CO by cytochrome P-450 or to carbon dioxide $(CO_2)$ by glutathione-dependent metabolic reaction. In rats treated with DCM (3 mmol/kg, ip) only, the carboxyhemoglobin (COHb) level reached a peak of approximately 10% 2 or 3 hr following the treatment. Disulfiram (300 mg/kg, ip) or allylsulfide (200 mg/kg, po), both known as a selective inhibitior for cytochrome P-450 2E1, blocked the increase in COHb concentratlons almost completely suggesting that the metabolic conversion of DCM to CO is mediated by the activity of this specific type of isozyme. YH439 (125 or 250 mg/kg, po), a potential hepatoprotective agent, decreased the COHb elevation as well indicating that this chemical is a potent inhibitor for 2E1. In rats treated with pyrazine (200 mg/kg, ip) 18 hr prior to DCM the peak COHb concentration was decreased by approximately 3 or 4%. However, pretreatment of rats with pyrazine either 24 or 48 hr before DCM increased the peak COHb concentration significantly compared to the rats treated with DCM only. The results in the present study strongly suggest that the generation of CO from DCM depends on the 2E1 activity and that the pharmacological and/or toxicological action of YH439 or pyrazine in animals or human is associated with its effect on this isozyme.

  • PDF

Effect of Cordycepin on the Cumulus Expansion and Meiotic Maturation of Mouse Cumulus-oocyte Complexes in Vitro (Cordycepin이 생쥐의 난구세포 분산과 난자의 성숙에 미치는 영향)

  • Lee, Gy-Soog
    • Clinical and Experimental Reproductive Medicine
    • /
    • v.13 no.2
    • /
    • pp.201-206
    • /
    • 1986
  • These experiments were conducted to know whether RNA syntheis is involved in the cumulus expansion and oocyte maturation of mouse cumulus-oocyte complexes in vitro. Mouse cumulus-oocyte complexes(COC's) were cultured in the presence of cordycepin, an inhibitior of RNA synthesis and its effect on the cumulus expansion and oocyte maturation were examined. The results were as follows. 1. Continuous presence of cordycepin in the medium(200${\mu}g/ml$) inhibited the HCG-induced cumulus cell expansion of mouse complexes. This inhibition was reversible. 2. When the COC'S were preincubated with different concentration of cordycepin plus HCG for 3 hours and then transferred to the plain medium, the HCG induced cumulus expansion was suppressed at $100{\mu}g/ml$ of cordycepin. 3. When the COC'S were cultured with cordycepin after HCG stimulation(3hrs), the cumulus expansion were not suppressed by cordycepin. 4. Oocyte meiotic maturation did not appear to be affected by cordycepin. The data presented here imply that RNA synthesis is involved in the cumulus expansion process and that mouse oocytes are more resistant to RNA synthesis inhibitor than cumulus cells.

  • PDF

Involvement of Nitric Oxide During In Vitro Fertilization and Early Embryonic Development in Mice

  • Kim, Bo-Hyun;Kim, Chang-Hong;Jung, Kyu-Young;Jeon, Byung-Hun;Ju, Eun-Jin;Choo, Young-Kug
    • Archives of Pharmacal Research
    • /
    • v.27 no.1
    • /
    • pp.86-93
    • /
    • 2004
  • Nitric oxide (NO) has emerged as an important intracellular and intercellular messenger, controlling many physiological processes and participating in the fertilization process via the autocrine and paracrine mechanisms. This study investigated whether nitric oxide synthase (NOS) inhibitior (L-NAME) and L-arginine could regulate in vitro fertilization and early embryonic development in mice. Mouse epididymal spermatozoa, oocytes, and embryos were incubated in mediums of variable conditions with and without L-NAME or L-arginine (0.5, 1, 5 and 10mM). Fertilization rate and early embryonic development were significantly inhibited by treating sperms or oocytes with L-NAME (93.8% vs 66.3%,92.1% vs 60.3%), but not with L-arginine. In contrast, fertilization rate and early embryonic development were conspicuously reduced when L-NAME or L-arginine was added to the culture media for embryos. Early embryonic development was inhibited by microinjection of L-NAME into the fertilized embryosin a dose-dependent manner, but only by high concentrations of L-arginine. These results suggest that a moderate amount of NO production is essential for fertilization and early embryo development in mice.

Protective Effects of Dohongsamul-tang on 2-deoxy-D-glucose Induced Autophagic Cell Death in C6 Glial Cells (도홍사물탕(挑紅四物湯)이 C6 신경교세포의 2-DG에 의한 오토파지성 세포사멸에 미치는 영향)

  • Shin, Hak-Soo;Lee, Seung-Geun;Moon, Byung-Soon
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.23 no.3
    • /
    • pp.581-589
    • /
    • 2009
  • The water extract of Dohongsamul-tang(DHSMT) has been traditionally used in treatment of ischemic heart and brain diseases in Oriental Medicine. However, little is known about the mechanism by which DHSMT protects C6 glial cells from glucose deprevation induced damages. Therefore, this study was designed to evaluate the protective effects of DHSMT on 2-deoxy-D-glucose induced autophagy of C6 glial cells. Autophagic phenotype is evaluated by fluorescence microscopy and flow cytometry with specific biological staining dyes, including monodansylcadaverine and acridine orange, as well as Western blot analysis with microtubule-associated protein 1 light chain 3(LC3) and Beclin-1. Treatment with 2-deoxy-D-glucose significantly resulted in a decrease of the viability of C6 glial cells and increase of the extracellular LDH release in a dose and time-dependent manner. However, pretreatment with DHSMT protected C6 glial cells from glucose deprivation with 2-deoxy-D-glucose. The author also observed the fact that autophagy phenotype occurred by 2-deoxy-D-glucose in C6 glial cells. Pretreatment with 3-MA, a pharmacological inhibitior of autophagy, abolished the formation of acidic vesicle organelle in C6 glial cells treated with 2-deoxy-D-glucose. However, pretreatment with DHSMT inhibited the formation of autophagic phenotypes, including formation of acidic vesicle organelle, and increase of the expression of LC-3 II Beclin-1 proteins in C6 glial cells treated with 2-deoxy-D-glucose. Taken together, these data suggest that DHSMT is able to protect C6 glial cells from glucose deprivation with marked inhibition of autophagy formation.

Requirement for ERK Activity in Sodium Selenite-induced Apoptosis of Acute Promyelocytic Leukemia-derived NB4 Cells

  • Han, Bingshe;Wei, Wei;Hua, Fangyuan;Cao, Tingming;Dong, Hua;Yang, Tao;Yang, Yang;Pan, Huazhen;Xu, Caimin
    • BMB Reports
    • /
    • v.40 no.2
    • /
    • pp.196-204
    • /
    • 2007
  • Our previous study has shown that sodium selenite can cause apoptosis in acute promyelocytic leukemia-derived NB4 cells in a caspase-dependent manner, but the detailed mechanism is unknown. Here we demonstrate a requirement for extracellular signal-regulated protein kinase (ERK) in mediating sodium selenite -induced apoptosis in NB4 cell. Though no apparent elevation of ERK activity was observed during the apoptosis in NB4 cells caused by 20 μM sodium selenite treatment, PD98059 and U0126, specific chemical inhibitors of the MEK/ERK signaling pathway, were shown to strongly prevent the apoptosis process, while ERK activator TPA enhanced the process. It is also known that p38 MAPK inhibitor SB203580 and JNK inhibitor SP600125 had slight effects on apoptosis. Further study indicated that ERK exerted its proapoptotic effect only at the early stage of apoptosis and played an antiapoptotic role at the later stages. Taken together, our findings suggest that ERK plays an active role in mediating sodium seleniteinduced apoptosis in NB4 cells .

Browning and Its Inhibition in Fermentation of Rice-grape Wine (쌀.포도 혼합 발효주의 갈변특성 및 갈변저해방법)

  • Koo, Ha-Na;Yook, Cheol;Kim, Jae-Sik
    • Korean Journal of Food Science and Technology
    • /
    • v.38 no.4
    • /
    • pp.554-561
    • /
    • 2006
  • The objective of this study was to investigate the effects of browning inhibitors during fermentation and storage of rice-grape wine. Bentonite, polyvinylopolypyrrolidone (PVPP), and potassium metabisulfite were added to rice-grape wine during fermentation and storage in order to find an effective method of inhibiting browning. Total phenolics content, pH, amino acidity, hydroxymethylfurfural content, and absorbance at 420 nm were measured during storage to assess the effects of the different browning substrates. Potassium metabisulfite was the most effective browning inhibitior. Sensory evaluation also showed that rice-grape wine treated with potassium metabisulfite was highly Preferable in terms of color, taste, flavor, and overall quality.

Cardiovascular Biofunctional Activity and Antioxidant Activity of Gugija (Lycium chinensis Mill) Species and Its Hybrids (구기자 품종과 교배종의 부위별 심혈관관련 질환 예방 기능성 및 항산화 활성비교)

  • Park, Won-Jong;Lee, Bong-Chun;Lee, Ju-Chan;Lee, Eun-Na;Song, Jung-Eun;Lee, Dae-Hyung;Lee, Jong-Soo
    • Korean Journal of Medicinal Crop Science
    • /
    • v.15 no.6
    • /
    • pp.391-397
    • /
    • 2007
  • To develop new high valuable Gugija (Lycium chinensis), biofunctionalities of Gugija standard species and its hybrids were investigated and compared with each water extracts and methanol extracts from Lycii Fructus, Lycii Folium and buds and Lycii Cortex Radicis. Among various biofunctionalities of Gugija standard species, antioxidant activity was showed the highest in methanol extracts from buds of Cheongwoon species (93%) and antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity was 84.1% in the water extracts from Lycii Cortex Radicis of Cheongyang NO.7. Futhermore, methanol extracts from Lycii Cortex Radicis of Myungan A-2 hybrid showed 93.1% of antioxidant activity and 96.9% of ACE inhibitory activity was also showed in the methanol extracts from Lycii Fructus of DO148-72(A11) hybrid. However, fibrinolytic activity and anticholesteromia HMG-CoA reductase inhibitory activity were weak or not detected in almost of Gugija standard species and its hybrids. Therefore, we finally selected Cheongwoon Gugija standard species (buds) and Myungan A-2 hybrid (Lycii Cortex Radicis) as good antioxidant sources and also DO148-72 (A11) hybrid (Lycii Fructus) as excellent antihypertensive ACE inhibitior sources for manufacturing functional food product.