• Title/Summary/Keyword: indole inhibition

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Phenolic Compounds from the Leaves of Stewartia pseudocamellia Maxim. and their Whitening Activities

  • Roh, Hyun Jung;Noh, Hye-Ji;Na, Chun Su;Kim, Chung Sub;Kim, Ki Hyun;Hong, Cheol Yi;Lee, Kang Ro
    • Biomolecules & Therapeutics
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    • v.23 no.3
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    • pp.283-289
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    • 2015
  • The half-dried leaves of Stewartia. pseudocamellia were extracted with hot water (SPE) and partitioned with n-hexane (SPEH), dichloromethane (SPED), and ethyl acetate (SPEE) successively. SPE and SPEE showed significant inhibitory effects against melanogenesis and tyrosinase activities. By bioassay-guided isolation, ten phenolic compounds were isolated by column chromatography from SPEE. The whitening effect of the isolated compounds from SPEE were tested for the inhibitory activities against melanogenesis using B16 melanoma cells, in vitro inhibition of tyrosinase, and L-3,4-dihydorxy-indole-2-carboxylic acid (L-DOPA) auto-oxidation assay. A cytotoxic activity assay was done to examine the cellular toxicity in Raw 264.7 macrophage cells. Of the compounds isolated, gallic acid and quercetin revealed significant inhibitory activities against melanogenesis compared to arbutin. In particular, quercetin exhibited similar inhibitory activities against tyrosinase and L-DOPA oxidation without cytotoxicity. These results suggested that SPE could be used as a potential source of natural skin-whitening material in cosmetics as well as in food products.

HQSAR Study of Microsomal Prostaglandin E2 Synthase (mPGES-1) Inhibitors

  • San Juan, Amor A.;Cho, Seung-Joo;Cho, Hoon
    • Bulletin of the Korean Chemical Society
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    • v.27 no.10
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    • pp.1531-1536
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    • 2006
  • Microsomal prostaglandin $E_2$ synthase (mPGES-1) is an enzyme that is associated with inflammation, pain, fever and cancer. Hologram quantitative structure activity relationship (HQSAR) was conducted on the series of MK-886 compounds acting as mPGES-1 inhibitors. A training set with 24 compounds was used to establish the HQSAR model. The best model was chosen based on the cross-validated correlation coefficient ($q^2$=0.884) and the correlation coefficient($r^2$=0.976). The model was utilized to predict the activity of the eight-test set of compounds giving the predictive $r^2$ value of 0.845. The descriptors of the model are based on fragment distinction (atoms, bond and connectivity) and fragment size (2-5 atoms). The atomic contribution maps generated from HQSAR were useful in identifying the important structural features responsible for the inhibitory activity of MK-886 inhibitors. Based on the generated model, the presence of hydrophobic biphenyl group seems to enhance inhibition of mPGES-1 that is in agreement with the previous experiments. In addition, it seems important for a halogen to be substituted to the biphenyl ring and for an acyl group to be attached to the indole moiety for enhanced activity.

Beneficial Effects of Fluorescent Pseudomonads on Seed Germination, Growth Promotion, and Suppression of Charcoal Rot in Groundnut (Arachis hypogea L.)

  • Shweta, Bhatia;Maheshwari, Dinesh Kumar;Dubey, Ramesh Chand;Arora, Daljit Singh;Bajpai, Vivek K.;Kang, Sun-Chul
    • Journal of Microbiology and Biotechnology
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    • v.18 no.9
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    • pp.1578-1583
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    • 2008
  • Rhizobacteria are used as inoculants to enhance crop yield and for biological control of fungal pathogens. Fluorescent pseudomonads isolated from the rhizosphere of groundnut showed suppression of the phytopathogen Macrophomina phaseolina that causes charcoal rot of groundnut, an economically important agroproduct. Two strains of fluorescent pseudomonads, designated as PS1 and PS2, were selected as a result of in vitro antifungal activity. After 5 days of incubation at $28{\pm}1^{\circ}C$, both PS1 and PS2 caused clear inhibition zones in dual cultures, restricting the growth of M. phaseolina by 71 % and 74%, respectively. Both the strains were capable of producing siderophores, indole acetic acid, and hydrocyanic acid, and causing phosphate solubilization under normal growth conditions. These strains, when used as inoculants in groundnut, enhanced germination up to 15% and 30% with subsequent increase in grain yield by 66% and 77%, respectively. Conversely, when the pathogen alone was tested 57% decrease in yield was recorded. Thus the studies revealed the potential of the two pseudomonads not only as biocontrol agents against M. phaseolina, but also as a good growth promoter for groundnut.

Desmutagenic Effects of Extracts from Green Tea (녹차 추출물의 항돌연변이원성)

  • 오창경;오명철;김수현
    • Korean journal of food and cookery science
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    • v.16 no.5
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    • pp.390-393
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    • 2000
  • Desmutagenic effects of water-soluble and ethanol-soluble extracts of dried green tea toward the mutagenicity of 4-nitroquinoline-N-oxide(4-NQO) and 3-Amino-1,4-dimethyl-5H-pyrido[4,3-b]indole(Trp-P-1) in streptomycin-dependent SD510 strains of Salmonella typhimurium TA98 were investigated. Inhibition effects toward the mutagenicity of 4-NQO and Trp-P-1 of water-soluble and ethanol-soluble extracts from green tea were high as increase of concentration of extracts. Desmutagenic effects toward 4-NQO of water-soluble and ethanol-soluble extracts from green tea harvested in May and August were up to 93% in 1,000 $\mu\textrm{g}$ of extract/plate. Desmutagenic effects toward Trp-P-1 of ethanol-soluble extracts from green tea were 53.3∼92.1%, but the effects of water-soluble extracts decreased as increase of concentration of extracts.

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Inhibitory Effect of Rice Extract on the Chemically Induced Mutagenesis (쌀 추출물의 돌연변이 억제효과)

  • Chun, Hyang-Sook;Kim, In-Ho;Kim, Young-Jin;Kim, Kil-Hwan
    • Korean Journal of Food Science and Technology
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    • v.26 no.2
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    • pp.188-194
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    • 1994
  • The inhibitory effects of rice extract on mutagenicity induced by 3-amino-1,4-dimethyl-5H-pyrido [4,3-b]indole(Trp-P-1), 3-amino-1-methyl-5H-pyrido [4,3-b]indole(Trp-P-2), sodium azide(SA), 2-nitrofluorene(2NF), mitomycin C(MMC), aflatoxin $B_1(AFB_1)$ and 4-nitroquinoline oxide(4-NQO) were investigated using Salmonella typhimurium reversion assay, SOS chromotest and spore rec-assay. In Salmonella typhimurium reversion assay, methanol extract from brown rice (Illpumbyeo, Japonica variety) showed the highest inhibitory effect among other extracting solvent including hexane, chloroform and water. Methanol extract showed stronger inhibitory effect, above 85%, on indirect-acting mutagens(Trp-P-1, Trp-P-2 and $AFB_1$) than those on direct-acting mutagens(4-NQO, 2NF). In SOS chromotest, methanol extracts showed $77.6{\sim}88.9%$ effects on SOS function induced by Trp-P-1, Trp-P-2, $AFB_1$ and 4-NQO. In spore rec-assay, methanol extracts inhibited the mutagenicity induced by $AFB_1$ and MMC. As the concentration of methanol extract increased, inhibitory effect on mutagenicity increased but reached at steady state as inhibition rate of 90% when the concentration was above 5 mg/plate. In inhibitory effects of methanol extracts by various rice varieties, all of 11 varieties turned out to have inhibitory effect on mutagenicity. There was no significant difference (p>0.05) in inhibitory effect of methanol extracts between brown and white rice against Trp-P-1, but showed difference (p<0.05) against 4-NQO.

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Study on Pandoraea sp. BCNU 315 Isolated from Soil (토양으로부터 분리한 Pandoraea sp. BCNU 315 에 관한 연구)

  • Kim, Seon-A;Choi, Hye-Jung;Woo, Seung-Hee;Hwang, Min-Jung;Park, Mi-Ran;Kim, Dong-Wan;Moon, Ja-Young;Joo, Woo-Hong
    • Journal of Life Science
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    • v.18 no.2
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    • pp.255-263
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    • 2008
  • Bacteria that antagonize plant pathogenic fungi were isolated from the sediment soil at the Ansan industrial estate. One isolate of them showed growth inhibition of Rhizoctonia solani, Botrytis cenerea, and Fusarium oxysporum. This strain was identified as Pandoraea sp. based on phenotypic and phylogenetic characteristics and termed Pandoraea sp. BCNU 315. Tryptone as nitrogen source and sucrose as carbon source were found to be most effective for the microbial growth. In addition, the optimum temperature and pH for microbial growth were $30^{\circ}C$ and pH 7.0, respectively. The substances generated from Pandoraea sp. BCNU 315 were purified and analyzed by column chromatography, HPLC, GC-MS and NMR. As a result, one compound was determined to be indole, another compound was predicted as cyclopentadecaheptene. Detailed structural clarification of the all of the rest six compounds from Pandoraea sp. BCNU 315 has to be accompanied in the further studies.

The Effect of 12-O-Tetradecanoylphorbol-13-acetate-induced COX-2 Expression by 3,3'-Diindolylmethane (DIM) on Human Mammary Epithelial Cells (3,3'-Diindolylmethane(DIM)이 Human Mammary Epithelial Cell에서 12-O-tetradecanoylphorbol-13-acetate에 의해 유도된 COX-2 발현에 미치는 영향)

  • Park, So Young;Shim, Jae-Hoon;Kim, Jong-Dae;YoonPark, Jung Han
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.12
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    • pp.1701-1707
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    • 2012
  • 3,3'-Diindolylmethane (DIM) is a major in vivo derivative of the putative anticancer agent indole-3-carbinol, which is present in cruciferous vegetables and has been reported to have anti-carcinogenic properties. An abnorrmally elevated level of cyclooxygenase-2 (COX-2) has been implicated in the pathogenesis of carcinogenesis. To investigate the mechanism by which DIM exhibits anti-carcinogenic effects, we investigated the effects of DIM on COX-2 expression in MCF-10A human mammary epithelial cells treated with the tumor promoter 12-O-tetradecanoylphorbol 13-acetate (TPA). DIM inhibited TPA-induced COX-2 expression and suppressed the synthesis of prostaglandin $E_2$, one of the major products of COX-2. Nuclear factor-kappa B ($NF-{\kappa}B$) is a transcription factor known to play a role in regulation of COX-2 expression. Treatment of MCF-10A cells with TPA increased nuclear translocation of phospho-p65, with the maximal levels being reached at 1 hour, while DIM inhibited the TPA-induced nuclear translocation of phospho-p65. Overall, we demonstrated that DIM suppresses phorbol ester-induced $PGE_2$ production and COX-2 expression in MCF-10A cells. The reduction in COX-2 levels by DIM maybe mediated through inhibition of $NF-{\kappa}B$ signaling.

Antifungal Activity and Plant Growth Promotion by Rhizobacteria Inhibiting Growth of Plant Pathogenic Fungi (식물병원성 진균을 억제하는 근권세균의 항진균능과 식물생장촉진능)

  • Jung, Taeck-Kyung;Kim, Ji-Hyun;Song, Hong-Gyu
    • Korean Journal of Microbiology
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    • v.48 no.1
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    • pp.16-21
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    • 2012
  • Since many pesticides cause various health and environmental problems, alternative measures to replace them are needed, and the bacteria producing the antifungal substances can be one of them. In this study, several rhizobacteria were isolated and their antifungal activities against some important plant pathogenic fungi were examined. Pseudomonas otitidis TK1 and Paenibacillus peoriae RhAn32 inhibited the growth of Fusarium oxysporum f. sp. niveum and F. oxysporum f. sp. lycopersici by 49.8% and 45.6%, and 45.1% and 48.3%, respectively compared to those of the control. P. peoriae RhAn32 also decreased the growth of F. oxysporum f. sp. raphani by 37.5%. This growth inhibition might be due to the production of antifungal substances, such as siderophore, hydrogen cyanide and chitinase, which were produced by these rhizobacteria. P. otitidis TK1 also produced plant growth hormones indole acetic acid and indole butyric acid at $293.41{\mu}g/mg$ protein and $418.53{\mu}g/mg$ protein, respectively. When P. otitidis TK1 and B. cereus TK2 were inoculated together with F. oxysporum f. sp. lycopersici to the 4 weeks grown tomato seedlings and incubated additional 8 weeks, the stem lengths of tomato increased up to 45.7% and 55.3% and root lengths were raised to 64.9% and 60.8%, respectively than those of the control group. The wet weights increased by 118% and 182%, respectively compared to the control group.

Effect of Indole-3-Carbinol on Inhibition of MMP Activity via MAPK Signaling Pathway in Human Prostate Cancer Cell Line, PC3 Cells (인돌이 인체 전립선암세포 PC3 Cell 전이 관련 Matrix Metalloproteinases (MMPs) 활성과 발현에 미치는 영향)

  • Kim, Sung-Ok
    • Journal of Nutrition and Health
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    • v.41 no.3
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    • pp.224-231
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    • 2008
  • We examined the effect of indole-3-carbinol (I3C, $C_9H_9NO$), an autolysis product of a glucosinolate and a glucobrassicin in vegetables, on MMP-2, -9 activities and TIMP-l and -2 inductions via microtubule-associated protein kinase (MAPK) signaling pathway in prostate cancer cell line, PC3 cells. Our results indicated that I3C inhibited cell growth of PC3 cells in dose (0,50, 100 ,${\mu}M$) and time (0,24,48 and 72 h) dependent manners. Using gelatin zymography for MMP activity, we demonstrated that I3C significantly decrease MMP-2 and -9 activities in PC3 cells. We also observed that I3C decreased the proteins and mRNA levels of MMP-2 and -9 in PC3 cells as well. Inversely, expressions of TIMP-l and -2 protein and mRNA in PC3 cells were increased by I3C in a dose dependent manner. In another experiment, we showed that I3C inhibited PC3 cells invasiveness by using marigel invasion assay and we also found that I3C suppressed MMP transcriptional activity by MAPK signaling pathways. Taken together, our results suggest that I3C may contribute to the potential beneficial food component to prevent the cancer metastasis in prostate cancer cells. (KoreanJNutr2008; 41(3): 224~23I)

Effects of Ethylene Precursor, Auxin and Methyl Jasmonate on the Aerenchyma Formation in the Primary Root of Maize (Zea mays) (옥수수(Zea mays) 원뿌리의 통기조직 발달에 미치는 에틸렌 전구체, 옥신, 메틸자스몬산의 효과)

  • Ho, Jongyoon;Maeng, Sohyun;Park, Woong June
    • Journal of Life Science
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    • v.25 no.1
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    • pp.37-43
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    • 2015
  • We have investigated the effects of the ethylene precursor 1-aminocyclopropane-1-carboxylic acid (ACC), indole-3-acetic acid (IAA) and methyl jasmonate (MeJA) on the development of aerenchyma in the primary root of maize (Zea mays). Because plant hormones affected the longitudinal organization of the primary root, we need an indicator to direct the positions for comparison between control and hormone-treated roots. Therefore, the zones of the maize primary root were categorized as PR25, PR50 and PR75, where each value indicates the relative position between the root tip (PR0) and the base (PR100). Aerenchyma was not observed at PR25 and PR50 and rarely found at PR75 in the cortex of control roots. The aerenchymal area at PR75 increased in the presence of the ethylene precursor ACC or a natural auxin IAA. On the other hand, MeJA differentially acted on non-submerged and submerged roots. Exogenously applied MeJA suppressed the aerenchyma formation in non-submerged roots. When the primary root was submerged, aerenchymal area expanded prominently. The submergence-induced aerenchyma formation was amplified with MeJA. Lateral root primordia have been known to inhibit aerenchymal death of surrounding cells. All the three hormones stimulating aerenchyma formation as described above did not restore the inhibition caused by lateral root primordia, suggesting that the inhibitory step regulated by lateral root primordia can be located after hormonal signaling steps.