• Title/Summary/Keyword: molecular activities

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Discovery, semisynthesis, biological activities, and metabolism of ocotillol-type saponins

  • Liu, Juan;Xu, Yangrong;Yang, Jingjing;Wang, Wenzhi;Zhang, Jianqiang;Zhang, Renmei;Meng, Qingguo
    • Journal of Ginseng Research
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    • v.41 no.3
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    • pp.373-378
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    • 2017
  • Ocotillol-type saponins are one kind of tetracyclic triterpenoids, sharing a tetrahydrofuran ring. Natural ocotillol-type saponins have been discovered in Panax quinquefolius L., Panax japonicus, Hana mina, and Vietnamese ginseng. In recent years, the semisynthesis of 20(S/R)-ocotillol-type saponins has been reported. The biological activities of ocotillol-type saponins include neuroprotective effect, antimyocardial ischemia, antiinflammatory, antibacterial, and antitumor activities. Owing to their chemical structure, pharmacological actions, and the stereoselective activity on antimyocardial ischemia, ocotillol-type saponins are subjected to extensive consideration. In this review, we sum up the discovery, semisynthesis, biological activities, and metabolism of ocotillol-type saponins.

NMR Data of Flavone Derivatives and Their Anti-oxidative Activities

  • Park, Yeong-Hui;Lee, Yong-Uk;Kim, Ho-Jung;Lee, Young-Shim;Yoon, Young-Ah;Mun, Byeong-Ho;Jeong, Yu-Hun;An, Jung-Hun;Shim, Yhong-Hee;Lim, Yoong-Ho
    • Bulletin of the Korean Chemical Society
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    • v.27 no.10
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    • pp.1537-1541
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    • 2006
  • The $^1H$ and $^{13}C$ chemical shifts of eleven flavone derivatives were completely determined by basic 1D and 2D NMR experiments. Nineteen flavone derivatives including the above eleven derivatives were examined for anti-oxidative effects using the 1,1-diphenyl-2-picryl-hydrazyl assay and Caenorhabditis elegans. In order to understand the relationships between the structures of flavone derivatives and their anti-oxidative activities, a Comparative Molecular Field Analysis was performed.

Taxonomic Characterization, Evaluation of Toxigenicity, and Saccharification Capability of Aspergillus Section Flavi Isolates from Korean Traditional Wheat-Based Fermentation Starter Nuruk

  • Bal, Jyotiranjan;Yun, Suk-Hyun;Chun, Jeesun;Kim, Beom-Tae;Kim, Dae-Hyuk
    • Mycobiology
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    • v.44 no.3
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    • pp.155-161
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    • 2016
  • The most economically important species used in a wide range of fermentation industries throughout Asia belong to Aspergillus section Flavi, which are morphologically and phylogenetically indistinguishable, with a few being toxigenic and therefore a major concern. They are frequently isolated from Korean fermentation starters, such as nuruk and meju. The growing popularity of traditional Korean alcoholic beverages has led to a demand for their quality enhancement, therefore requiring selection of efficient non-toxigenic strains to assist effective fermentation. This study was performed to classify the most efficient strains of Aspergillus section Flavi isolated from various types of traditional wheat nuruk, based on a polyphasic approach involving molecular and biochemical evaluation. A total of 69 strains were isolated based on colony morphology and identified as Aspergillus oryzae/flavus based on internal transcribed spacer and calmodulin gene sequencing. Interestingly, none were toxigenic based on PCR amplification of intergenic regions of the aflatoxin cluster genes norB-cypA and the absence of aflatoxin in the culture supernatants by thin-layer chromatography analysis. Saccharification capability of the isolates, assessed through ${\alpha}-amylase$ and glucoamylase activities, revealed that two isolates, TNA24 and TNA15, showed the highest levels of activity. Although the degrees of variation in ${\alpha}-amylase$ and glucoamylase activities among the isolates were higher, there were only slight differences in acid protease activity among the isolates with two, TNA28 and TNA36, showing the highest activities. Furthermore, statistical analyses showed that ${\alpha}-amylase$ activity was positively correlated with glucoamylase activity (p < 0.001), and therefore screening for either was sufficient to predict the saccharifying capacity of the Aspergillus strain.

Differential Effects of Tautomycetin and Its Derivatives on Protein Phosphatase Inhibition, Immunosuppressive Function and Antitumor Activity

  • Niu, Mingshan;Sun, Yan;Liu, Bo;Tang, Li;Qiu, Rongguo
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.2
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    • pp.145-151
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    • 2012
  • In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

Deletion of GBG1/AYR1 Alters Cell Wall Biogenesis in Saccharomyces cerevisiae

  • Ahn, Ki-Woong;Kim, Sung-Woo;Kang, Hyung-Gyoo;Kim, Ki-Hyun;Park, Yun-Hee;Choi, Won-Ja;Park, Hee-Moon
    • Mycobiology
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    • v.38 no.2
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    • pp.102-107
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    • 2010
  • We identified a gene for $\beta$-1,3-glucan synthesis (GBG1), a nonessential gene whose disruption alters cell wall synthesis enzyme activities and cell wall composition. This gene was cloned by functional complementation of defects in $\beta$-1,3-glucan synthase activity of the the previously isolated Saccharomyces cerevisiae mutant LP0353, which displays a number of cell wall defects at restrictive temperature. Disruption of the GBG1 gene did not affect cell viability or growth rate, but did cause alterations in cell wall synthesis enzyme activities: reduction of $\beta$-1,3-glucan synthase and chitin synthase III activities as well as increased chitin synthase I and II activities. GBG1 disruption also showed altered cell wall composition as well as susceptibility toward cell wall inhibitors such as Zymolyase, Calcofluor white, and Nikkomycin Z. These results indicate that GBG1 plays a role in cell wall biogenesis in S. cerevisiae.

Cytotoxic Activities of Amentoflavone against Human Breast and Cervical Cancers are Mediated by Increasing of PTEN Expression Levels due to Peroxisome Proliferator-Activated Receptor γ Activation

  • Lee, Eun-Jung;Shin, So-Young;Lee, Jee-Young;Lee, So-Jung;Kim, Jin-Kyoung;Yoon, Do-Young;Woo, Eun-Rhan;Kim, Yang-Mee
    • Bulletin of the Korean Chemical Society
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    • v.33 no.7
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    • pp.2219-2223
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    • 2012
  • Human peroxisome proliferator-activated receptor gamma ($hPPAR{\gamma}$) has been implicated in numerous pathologies, including obesity, diabetes, and cancer. Previously, we verified that amentoflavone is an activator of $hPPAR{\gamma}$ and probed the molecular basis of its action. In this study, we investigated the mechanism of action of amentoflavone in cancer cells and demonstrated that amentoflavone showed strong cytotoxicity against MCF-7 and HeLa cancer cell lines. We showed that $hPPAR{\gamma}$ expression in MCF-7 and HeLa cells is specifically stimulated by amentoflavone, and suggested that amentoflavone-induced cytotoxic activities are mediated by activation of $hPPAR{\gamma}$ in these two cancer cell lines. Moreover, amentoflavone increased PTEN levels in these two cancer cell lines, indicating that the cytotoxic activities of amentoflavone are mediated by increasing of PTEN expression levels due to $hPPAR{\gamma}$ activation.

Antifungal Activities Against Plasmodiophora brassicae Causing Club Root

  • Kim, Bum-Joon;Choi, Gyung-Ja;Cho, Kwang-Yun;Yang, Hee-Jung;Shin, Choon-Shik;Lee, Chul-Hoon;Lim, Yoong-Ho
    • Journal of Microbiology and Biotechnology
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    • v.12 no.6
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    • pp.1022-1025
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    • 2002
  • Club root is one of the major diseases that occur in crucifers. It is caused by Plasmodiophora brassicae. In order to discover microbial biopesticides against P. brassicae, forty-eight Streptomyces isolated from soil were screened. Among these, three strains showed excellent pesticidal activities. We report results on in vivo screening with fermentation broths of these strains and identification of the strain taxa.

Molecular Cloning and Expression of Genes Related to Antifungal Activities from Enterobacter sp. B54 Antagonistic to Phytophthora capsici

  • YOON, SANG-HONG
    • Journal of Microbiology and Biotechnology
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    • v.9 no.3
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    • pp.352-357
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    • 1999
  • Enterobacter sp. B54 inhibited growth of the fungus Phytophthora capsici on potato dextrose agar (PDA). Three mutants with antifungal activities (denoted M54-47, M54-113, and M54-329) which were lost or increased, through Pl::Tn5 lac mutagenesis, were used to isolate genes responsible for fungal inhibition on PDA. Two clones were selected from the partially EcoR1-digested genomic library of the wild-type strain by probing with genomic flanking sequences of each mutant. We have isolated a 20-kb EcoR1 genomic DNA fragment from this strain that contains genes involved in hyphal growth inhibition of P. capsici on PDA. Subcloning and expression analysis of the above DNA fragment identified a 8-kb region which was necessary for antifungal activities. A 8-kb HindⅢDNA fragment covers three genomic loci inserted by Tn5 lac in each mutant. This suggested that all genes which are related to antifungal activities might be clustered in simple forms of at least 5-8 kb sizes.

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Synthesis and Anti-HIV Activity of Sulfonated Amino Ribofuranans

  • Kang, Byoung-Won
    • Archives of Pharmacal Research
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    • v.26 no.6
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    • pp.441-445
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    • 2003
  • New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.