• 제목/요약/키워드: Inhibition rate

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Screening of Marine Microbial Extracts for Tyrosine Phosphatase 1B Inhibitors

  • Sohn, Jae-Hak;Park, Sun Jung;Seo, Changon;Chun, Bokyung;Oh, Hyuncheol
    • 한국해양바이오학회지
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    • 제2권4호
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    • pp.230-233
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    • 2007
  • Protein tyrosine phosphatase 1B (PTP1B) acts as a negative regulator of insulin signaling, and selective inhibition of PTP1B has served as a potential drug target for the treatment of type 2 diabetes. As part of our searching for PTP1B inhibitors from natural products, the extracts of marine microorganisms were screened for the inhibitory effects on the activity of protein tyrosine phosphatase 1B (PTP1B). Among the tested 304 extracts, 29 extracts exhibited inhibition rate ranging 40.1 - 83.6 % against PTP1B at the concentration level of $30{\mu}g/mL$.

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Bulbocapnine이 PC12 세포중의 도파민 함량에 미치는 영향 (Effects of Bulbocapnine on Dopamine Content in PC12 Cells)

  • 신정수;이명구
    • 약학회지
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    • 제42권2호
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    • pp.170-174
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    • 1998
  • The effects of bulbocapnine, an aporphine isoquinoline alkaloid, on dopamine content in PC12 cells were investigated. Bulbocapnine decreased the dopamine content dose-dependentl y (39.2% inhibition at 2O${\mu}$M for 24 hr). The $IC_{50}$ value of bulbocapnine was 22.7${\mu}$M. Dopamine content was lowered at 6 hr after exposure to bulbocapnine. And then, the decreased dopamine level was almost maintained at 36 hr and recovered to the control level at about 60 hr. Tyrosine hydroxylase, the rate limiting enzyme in the catecholamine blosynthetic pathway, was also inhibited at 20${\mu}$M of bulbocapnine by 23.1% relative to control. We, therefore, hypothesized that the inhibition of tyrosine hydroxylase by bulbocapnine with a single treatment might be partially contributed to the decrease in dopamine content in PC12 cells.

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니트로페놀화합물의 호기성생물분해시 pH 영향에 관한 연구 (pH Effect on the Aerobic Biodegradation of Nitrophenolic Compound in SBR)

  • 조관형
    • 한국환경과학회지
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    • 제16권7호
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    • pp.779-784
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    • 2007
  • Dinitrophenol is preventing cells from making energy for growth and it has been suggested that pH may be important in mitigating effects of uncouplers. The effect of pH on toxicity of dinitrophenol at high concentration was investigated, over a pH range of 5.7 to 8.7. DNP inhibition was found to be strongly dependent on mixed liquor pH. The DNP degradation rate was highest in the pH range of 7.0 to 7.8; at pH 6.0 degradation of 0.41 mM dinitrophenol was significantly inhibited; at pH <5.7, dinitrophenol degradation was completely inhibited after approximately 25% of the dinitrophenol was degraded. However no significant effect of pH variation was seen on glucose uptake by the activated sludge mixed culture.

인삼 포리아세틸렌 화합물이 Lymphoid lukemia L1210의 고분자물질 합성에 미치는 영향 (Effect of Polyacetylene Compounds from Panax Ginseng on Macromolecule Synthesis of Lymphoid lukemia L1210)

  • 김영숙;김신일;한덕용
    • 약학회지
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    • 제32권2호
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    • pp.137-140
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    • 1988
  • To investigate polyacetylene compounds isolated from petroleum ether extract of panax ginseng effect on the macromolecule synthesis, lympoid lukemia L1210 cell was incubated with them at 4, 8, 12,16 hours. Panaxydol, panaxynol and panaxytriol as cytotoxic substances inhibited the synthesis of macromolecule such as DNA, RNA and protein. Panaxydol which had the most potent cytotoxicity among these three compounds showed the strongest inhibitory effect on DNA, RNA and protein synthesis. For DNA and RNA synthesis, panaxynol and panaxytriol decreased the rate of inhibition with the incubation time but panaxydol had a strongest inhibitory effect at 16 hour incubation time. Protein synthesis was markedly inhibited by all these polyacetylene compounds. It was obserbed that there is a relationship between cytotoxicities of polyacetylene compounds and the inhibition of macromolecule synthesis.

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Correlative Changes between Photosynthetic Activities and Chlorophyll Fluorescence in Wheat Chloroplasts Exposed to High Temperature

  • Young-Nam Hong
    • Journal of Plant Biology
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    • 제37권1호
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    • pp.37-42
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    • 1994
  • Correlative changes between photosynthetic O2 exchange rates and room temperature Chl fluorescence were investigated in wheat (Triticum aestivum L.) chloroplasts treated with high temperature for 5 min. With increasing treatment temperature, photosynthetic O2 evolution rate mediated by PSII was decreased, showing 50% inhibition at 38$^{\circ}C$ (I50). But PSI activity measured by O2 uptake rates was stimulated as a function of increasing temperature. Dark level fluorescence (Fo)-temperature (T) analysis showed that fluorescence rising temperature (Tr), critical temperature (Tc), and peak temperature (Tp) was 38, 43, and 52$^{\circ}C$, respectively. Quenching analysis of Chl fluorescence showed that both the oxidized fraction of plastoquinone (qQ) and degree of thylakoid membrane energization (qNP) increased up to 4$0^{\circ}C$ and then declined dramatically. These results suggest that Tr is correlated with temperature showing a 50% of inhibition of photosynthesis and under mild high temperature stress, qNP is worth regarding as indicator for heat-induced damage of photosynthesis.

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Characterization of BTX-degrading bacteria and identification of substrate interactions during their degradation

  • Oh, Young-Sook;Choi, Sung-Chan
    • Journal of Microbiology
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    • 제35권3호
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    • pp.193-199
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    • 1997
  • From several industrial wastewaters, 14 bacterial strains which degrade benzene, toluene, o-xylene, m-xylene, or p-xylene (BTX) were obtained. These strains were characterized as to their species composition and the substrate range, kinetic parameters and the substrate interactions were investigated. Although BTX components have a similar chemical structure, isolated strains showed different substrate ranges and kinetic parameters. None of the strains could degrade all of BTX components and most of them showed an inhibition (Haldane) kinetics on BTX, BTX mixtures were removed under inhibitory substrate interactions with variation in the intensity of inhibition. For a complete degradation of BTX, a defined mixed culture containing three different types of patyways was constructed and all of the BTX components were simultaneously degraded with the totla removal rate of 225.69 mg/g biomass/h Judging from the results, the obtained mixed culture seems to be useful for the treatment of BTX-contaminated wastewater or groundwater as well as for the removal of BTX from the contaminated air stream.

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Antifungal Activity of an Endophytic Fungus Aspergillus versicolor DYSJ3 from Aphanamixis grandifolia Blume against Colletotrichum musae

  • Li, Xiaoyu;Wu, Yateng;Liu, Zhiqiang
    • Mycobiology
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    • 제49권5호
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    • pp.498-506
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    • 2021
  • An endophytic fungus strain DYSJ3 was isolated from a stem of Aphanamixis grandifolia Blume, which was identified as Aspergillus versicolor based on the morphological characteristics, internal transcribed spacer (ITS) and calmodulin gene sequences analyses. A. versicolor DYSJ3 exhibited strong antagonistic activity against Colletotrichum musae, C. gloeosporioides and Fusarium oxysporum f. sp. cubense with the inhibition rates of 61.9, 51.2 and 55.3% respectively. The antifungal metabolites mainly existed in the mycelium of A. versicolor DYSJ3, and its mycelial crude extract (CE) had broad-spectrum antifungal activities against plant pathogenic fungi. The CE had a good thermal stability, and the inhibition rate of 100 mg/mL CE against C. musae was above 70.0% after disposing at 120 ℃ for 1 h. Five secondary metabolites were isolated from the CE and identified as averufanin, ergosterol peroxide, versicolorin B, averythrin and sterigmatocystin. Activity evaluation showed versicolorin B exhibited inhibitory effects on the mycelial growth and conidial germination of C. musae, and sterigmatocystin had a weak inhibitory effect on the mycelial growth of C. musae.

Adenosine Modulate the Oocyte Developmental Competence by Exposing Stages and Synthetic Blocking during In Vitro Maturation

  • Cheon, Yong-Pil
    • 한국발생생물학회지:발생과생식
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    • 제20권2호
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    • pp.127-133
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    • 2016
  • Purine metabolism is known factor for nuclear maturation of oocytes through both follicle cells and oocyte itself. However, it is largely unknown the roles of purine metabolism in the oocyte competence for fertilization and early development. In this study, the effects of adenosine in oocyte competence for development were examined using adenosine and its synthetic inhibitors. Adenosine treatment from GV intact stage for 18 hr (fGV) caused of decrease the fertilization rate but of increase the cleavage rate compared from the other stage treatment groups. Hadacidin did not effect on fertilization rate but increased cleavage rate without stage specificity. Adenosine did not block the effects of hadacidin with the exception of fGV group. Inhibition of purine synthetic pathways the fertilization rate was decreased in the fGV and fGVB groups but increased in the fMII group. Exogenous adenosine caused of decrease fertilization rate in the fGVB group but increase in the fMII group. Cleavage rate was dramatically increased in the adenosine treatment with synthetic inhibitors. It means that the metabolism of purine has stage specific effects on fertilization and cleavage. Exogenous adenosine had only can improve oocyte developmental competence when it treated at GV intact stage. On the other hand, endogenous synthesis in all maturation stage cause of increase the cleavage rate without effects on fertilization. These data suggest that adenosine at GV stage as a paracrine fashion and inhibitions of endogenous adenosine in all stage improve oocyte developmental competence.

수종 지혈 한약물이 Cytochrome P450 3A4 활성에 미치는 영향 (Influence of Five Herbal Medicines on Cytochrome P450 3A4 Drug-Metabolizing Enzymes in Human Liver Microsomes)

  • 황진우;고재언;고호연;최유경;박종형;전찬용
    • 대한한방내과학회지
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    • 제29권4호
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    • pp.846-855
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    • 2008
  • Objects : The aim of this study was to investigate the influence of five herbal medicines on cytochrome P450 3A4 drug-metabolizing enzymes in human liver microsomes. Methods : To use human liver microsomes, an extract of five herbal medicines, which are Artemisia princeps Pampan, Sophora jeponica Linne, Panax notoginseng F. H. Chen, Lithospermum Erythrorhizon Sieb., and Cirsium maackii Maxim, which together are called Jihyulyak(止血藥, drugs for arresting bleeding, hemostatics), was co-incubated and measured for relative enzyme activity in incubation condition compared to ketoconazole, a representative inhibitor of CYP 3A4. Results : We showed that all five of the traditional herbal medicines had no inhibition effect of CYP 3A4 at 10, 20, 30, 40, and $50{\mu}g/ml$ doses in human liver microsomes, although Sophora japonica Linne(SJL) showed a little inhibition at about 81% inhibition rate of control. However, this result is not enough to prove that SJL has a CYP 3A4 inhibition effect. Moreover, we can't make sure that those rates had significant induction effect on CYP 3A4. Conclusions : The result of this study could support that those herbal medicines are safer than chemical drugs, even if this is the basic step to prove that result.

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Tumor Inhibition Effects and Mechanisms of Angelica sinensis and Sophorae flavescentis ait Decoction Combined with Cisplatin in Xenograft Mice

  • Yan, De-Qi;Liu, Yong-Qi;Li, Ying-Dong;Li, Dou;Cheng, Xiao-Li;Wu, Zhi-Wei
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권11호
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    • pp.4609-4615
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    • 2014
  • Background: To investigate tumor inhibition effects and mechanisms of Angelica sinensis and Sophorae flavescentis ait decoction (ASSF) combined with diamine-dichloroplatinum (DDP). Materials and Methods: Bodyweight, tumor inhibition rate and q value were calculated for single ASSF or ASSF combined with DDP on H22 carcinoma xenograft KM mice. Biochemical methods for serum LDH, AST, ALT, and AKP, ELISA method for serum HIF-$1{\alpha}$, pathological assessemnt of thymus, immunohistochemistry detection of tumor tissue caspase3 and mutant p53 protein, and qRT-PCR detection of bax/ bcl-2 mRNA were applied. Results: Compared with DDP control group, the bodyweight increased in ASSF-DDP group (p<0.01). Tumor inhibition rates for DDP, ASSF, ASSF-DDP were 62.7%. 43.7% and 71.0% respectively, with a q value of 0.90. Compared with other groups, thymus of DDP control group had obvious pathological injury (p<0.01), serum LDH, AST, ALT, AKP increased significantly in DDP control group (p<0.01), while serum HIF-$1{\alpha}$ was increased in the model control group. Compared with this latter, the expression of mutant p53 protein and bcl-2 mRNA were decreased in all treatment groups (p<0.01), but there were no statistical difference between DDP control p and ASSF-DDP groups. The expression of caspase3 protein and bax mRNA was increased in all treatment groups, with statistical differences between the DDP and ASSF-DDP groups (p<0.01). Conclusions: ASSF can inhibit bodyweight decrease caused by DDP, can inhibit tumor growth synergistically with DDP mainly through increasing serum HIF-$1{\alpha}$ and pro-apoptotic molecules such as caspase 3 and bax, rather than through decreasing anti-apoptotic mutant p53 and bcl-2. ASSF can reduce DDP toxicity due to decreasing the release of LDH, AST, ALT, AKP into blood and enhancing thymus protection.