• Title/Summary/Keyword: growth inhibition activity

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A Novel Pyrazolo[3,4-d]pyrimidine Induces Heme Oxygenase-1 and Exerts Anti-Inflammatory and Neuroprotective Effects

  • Lee, Ji Ae;Kwon, Young-Won;Kim, Hye Ri;Shin, Nari;Son, Hyo Jin;Cheong, Chan Seong;Kim, Dong Jin;Hwang, Onyou
    • Molecules and Cells
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    • v.45 no.3
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    • pp.134-147
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    • 2022
  • The anti-oxidant enzyme heme oxygenase-1 (HO-1) is known to exert anti-inflammatory effects. From a library of pyrazolo[3,4-d]pyrimidines, we identified a novel compound KKC080096 that upregulated HO-1 at the mRNA and protein levels in microglial BV-2 cells. KKC080096 exhibited anti-inflammatory effects via suppressing nitric oxide, interleukin1β (IL-1β), and iNOS production in lipopolysaccharide (LPS)-challenged cells. It inhibited the phosphorylation of IKK and MAP kinases (p38, JNK, ERK), which trigger inflammatory signaling, and whose activities are inhibited by HO-1. Further, KKC080096 upregulated anti-inflammatory marker (Arg1, YM1, CD206, IL-10, transforming growth factor-β [TGF-β]) expression. In 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridinetreated mice, KKC080096 lowered microglial activation, protected the nigral dopaminergic neurons, and nigral damage-associated motor deficits. Next, we elucidated the mechanisms by which KKC080096 upregulated HO-1. KKC080096 induced the phosphorylation of AMPK and its known upstream kinases LKB1 and CaMKKbeta, and pharmacological inhibition of AMPK activity reduced the effects of KKC080096 on HO-1 expression and LPS-induced NO generation, suggesting that KKC080096-induced HO-1 upregulation involves LKB1/AMPK and CaMKKbeta/AMPK pathway activation. Further, KKC080096 caused an increase in cellular Nrf2 level, bound to Keap1 (Nrf2 inhibitor protein) with high affinity, and blocked Keap1-Nrf2 interaction. This Nrf2 activation resulted in concurrent induction of HO-1 and other Nrf2-targeted antioxidant enzymes in BV-2 and in dopaminergic CATH.a cells. These results indicate that KKC080096 is a potential therapeutic for oxidative stress-and inflammation-related neurodegenerative disorders such as Parkinson's disease.

Influence of cell-wall degrading enzyme treatment and Saccharomyces cerevisiae fermentation on the antioxidant and antibacterial activities of green tea leaf (세포벽 분해 효소 처리 및 Saccharomyces cerevisiae 발효가 녹차 잎의 항산화 및 항균 활성에 미치는 영향)

  • Dong-Wook Lim;Ga-Yang Lee;Min-Jeong Jung;Byoung-Mok Kim;Joon-Young Jun
    • Food Science and Preservation
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    • v.30 no.6
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    • pp.1043-1055
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    • 2023
  • This study was conducted to suggest an extraction method for preparing the extract from green tea leaves that possess enhanced antioxidant and antibacterial activities. Different ethanol concentrations were tested to recover phenolics and flavonoids, and 50% ethanol was the best under heat treatment (121℃, 15 min). The ethanol extract exhibited excellent DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity and growth inhibition against B. cereus, B. licheniformis, S. aureus subsp. aureus, and A. hydrophila subsp. hydrophila. To enhance the antioxidant and antibacterial activities, cell-wall degrading enzymes (2.5% cellulose+2.5% pectinase, v/w dry sample) treatment and Saccharomyces cerevisiae fermentation were applied singly or in combination. The enzymatic treatment of green tea leaves notably increased extraction yield. However, the antioxidant and antibacterial activities of the extract were lower than those of the control (heat-treated 50% ethanol extract). In contrast, the yeast fermentation alone did not affect the yield, but enhanced antioxidant and antibacterial activities, contributing to the increase in the extract's total phenolic and flavonoid contents.

Quality Preservation of Shredded Carrots Stored in UV LED Packaging System (자외선 LED 포장용기 시스템에 의한 포장절단당근의 품질보존)

  • Kim, Nam Yong;Lee, Dong Sun;An, Duck Soon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.1
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    • pp.135-140
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    • 2014
  • Pre-storage ultra-violet (UV) light treatment on fresh produce is known to inactivate the contaminated microorganisms, activate the defense system, and delay ripening extending the shelf life. As UV light emitting diode (LED) becomes available at a relatively low price, continuous or intermittent UV treatment during chilled storage is possible in a container or package. This study attempted an in situ UV LED treatment on fresh produce stored under a refrigerated container in order to see its potential in the fresh produce storage and further optimize its application conditions. The effect of in-container UV LED irradiation on the quality preservation of shredded carrots was investigated in the air and modified atmosphere (MA) conditions. Two sets of experiment with Escherichia coli inoculation and with natural microbial flora in the air (two 30 minute on-off cycles of 1 $diode/dm^2$ per day at a location above 2 cm) showed a clear and significant effect of the UV LED irradiation on the suppression of microbial growth: 280 nm was the most effective by maintaining a lower microbial count by at least 0.5 log (CFU/g) throughout the 6 day storage period. The carotenoids content of shredded carrots subjected to UV LED treatment at 365 and 405 nm in the air was higher than that of the control shredded carrots. In MA condition of $O_2$ of 1.2~4.3% and $CO_2$ of 8.4~10.6% being indifferent with LED wavelengths, 280 nm UV LED irradiation was also effective in inhibiting the microbial growth. While there was no observed difference in the carotenoids content between untreated and UV LED-treated shredded carrots in MA, UV LED irradiation at 365 and 405 nm was slightly better in DPPH radical scavenging activity. The use of UV LED in storage container or package seems to give the benefits of preserving the microbial and nutritional qualities of minimally processed fruits and vegetables.

Isolation of Strain for the Preparation of the Fermented Antler and Its Physiological Activities (발효녹용의 균주 선별 및 발효녹용의 생리활성)

  • Kim, Min-Kyung;Jung, Eun-Young;Lee, Hyun-Sun;Shin, Kwang-Soon;Kim, Yoo-Kyung;Ra, Kyung-Soo;Park, Chul-Soo;Woo, Moon-Jea;Lee, Sang-Hun;Kim, Jin-Soo;Suh, Hyung-Joo
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.9
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    • pp.1237-1242
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    • 2009
  • This study was conducted to isolate strain for the preparation of fermented antler (Cervus cornu parvum) and evaluate its physiological activities. The growth degrees of twenty-one samples from Bacillus sp., Lactobacillius sp. and mushroom strain on antler extract agar were evaluated in this study, and Bacillus subtilis KH-15, SCB-3, Cordyceps militaris, Phellinus linteus, Inonotus obliquus 26136, and Inonotus obliquus 26147 were selected. The fermented antler extract by C. militaris had relatively higher contents of total sugar (1619.3 ${\mu}g$/mL), uronic acid (302.0 ${\mu}g$/mL), sulfated-glycosaminoglycan (S-GAGs) (119.9 ${\mu}g$/mL) and sialic acid (21.6 ${\mu}g$/mL) than any other extracts. The anti-complementary activities of all fermented antler extracts were higher than non-fermented antler extract, and among these samples, fermented antler extract by C. militaris showed the highest anti-complementary activity (inhibition of 50% total complement hemolysis, $ITCH_{50}$; 50.1% at 1,000 ${\mu}g$/mL). The ability of fermented antler extract by B. subtilis KH-15 to scavenge 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical ($IC_{50}$; 4.97 mg/mL) was significantly the highest (p<0.05), whereas the extract from I. obliquus exerted significantly (p<0.05) high 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity ($IC_{50}$; 16.98 mg/mL) among all samples. The results of this study suggest that physiological effects including immuno-modulating and antioxidant activities of the antler may be increased through fermentation process.

Antioxidative and Antimicrobial Activities of Eriobotrya japonica Lindl. Leaf Extracts (비파 잎 추출물의 항산화 및 항균활성)

  • Lee, Kyoung-In;Kim, Sun-Min
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.3
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    • pp.267-273
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    • 2009
  • Antioxidative, antimicrobial activities and Raw 264.7 cell viability as cytotoxicity of various solvent extracts from leaf of Eriobotrya japonica Lindl. dried by different methods were investigated for processing as functional ingredient. In DPPH radical scavenging activity, RLE (80% EtOH extract of raw leaf) and FLE (80% EtOH extract of freeze-dried leaf) exhibited strong scavenging effect on $300{\mu}M$ DPPH radical solution (1.71 mg/mL and 2.11 mg/mL for RLE $SC_{50}$ and FLE $SC_{50}$). Also in nitric oxide scavenging activity, RLE and FLE showed strong activities (83.9% and 82.2% in 5 mg/mL sample concentration). Total phenolic compound contents of each extracts were found to be $73.7{\sim}215.4$ mg/g and RLE was showed the highest phenolic compound content. Also, total flavonoid contents were found to be $24.85{\sim}110.3$ mg/g and RLE was showed the highest flavonoid content. In antimicrobial activity, RLE was showed higher growth inhibition effect against all microbial strains. RLE, RLW (hot water extract of raw leaf), and FLW (hot water extract of freeze-dried leaf) exhibited strong antimicrobial activities against MRSA and S. aureus. In measurement of cytotoxicity by MTT assay, Raw 264.7 cell viabilities of 80% EtOH extracts showed better effect than water extracts. Especially viability of RLE was found be over 100% in every tested sample concentration.

Effect of Aceton Extract from Styela Clava on Oxidative DNA Damage and Anticancer Activity (미더덕 아세톤 추출물이 산화적 DNA 손상억제 및 암세포 독성에 미치는 영향)

  • Seo, Bo-Young;Jung, Eun-Sil;Kim, Ju-Young;Park, Hae-Ryong;Lee, Seung-Cheol;Park, Eun-Ju
    • Applied Biological Chemistry
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    • v.49 no.3
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    • pp.227-232
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    • 2006
  • Styela clava (also called as rough sea squirt or leathery tunicate) is regarded as native to the northwest Pacific region including Korea and widely distributed in parts of northwestern Europe, North America and Australia. To evaluate Styela clava as a potential bioactive agent, the antioxidant activity of aceton extracts from Styela clava (whole, substance and tunic) was tested by measuring inhibitory effect of $H_2O_2$ induced DNA damage using comet assay. Also, anticancer activity on human colon cancer cell (HT-29) was investigated by MTT reduction assay. The $200\;{\mu}M$ $H_2O_2$ induced DNA damage was inhibited with Styela clava aceton extract in dose dependent manner in human leukocytes. The maximum inhibition was by 62.8, 62.1 and 78.3% at the concentration of $50\;{\mu}g/ml$ of whole, substance and tunic extracts, respectively. The aceton extracts from S. clava were also found to inhibit the growth of human colon cancer cell. The cell proliferation rates decreased to 26.9, 30.6 and 12.0% at the concentration of $500\;{\mu}g/ml$ of whole, substance and tunic extracts, respectively. These results support that aceton extracts from S. clava may be a potential candidate as a possible antimutagenic and chemotherapeutic agent.

Shalf Life Enhancement of Minimally Processed Fruits and Vegetables

  • Kim, Dong-Man
    • Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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    • 1993.12a
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    • pp.6-9
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    • 1993
  • According to changes in population, economic conditions, life-stile and eating habits, the frui ts and vegetables market wi 11 be shi fted from processed (i. e. , canned) to fresh. Undressed fresh produce, consisting of washed, disinfected and peeled fruits and vegetables that either sliced or grated, are currently increased in demand by retail and institutional market which use them as salad components or in ready-to use foods, Main attributes of minimally processed fruits and vegetables are convenience and fresh-like quality. Minimally processed Products readily deteriorate in quality, especially color and texture, as a result of endogeneous enzyme enhanced respiration and microorganisms which lead to reduced shelf Iife. According to changes in population, economic conditions, life-stile and eating habits, the frui ts and vegetables market wi 11 be shi fted from processed (i. e. , canned) to fresh. Undressed fresh produce, consisting of washed, disinfected and peeled fruits and vegetables that either sliced or grated, are currently increased in demand by retail and institutional market which use them as salad components or in ready-to use foods, Main attributes of minimally processed fruits and vegetables are convenience and fresh-like quality. Minimally processed Products readily deteriorate in quality, especially color and texture, as a result of endogeneous enzyme enhanced respiration and microorganisms which lead to reduced shelf Iife. Thus. to prevent these undesirable changes , val'ious techniques such as controlled atmosphere (CA) storage, modified atmosphere OIA) storage, including vacuum packaging have been receiving considerable attention, Although milch research has been done to find optimal conditions for whole intact frui ts and vegetables, only limi ted information is avai lable on fresh cut. and other minimally processed products. 81 iced frui ts exhibi t increas~d ethylene production and respiration compal'ed to whole f, 'uits during distribution in response to tissue damage. As a result, accelerated senescence and enzymatic browning OCCUI', Recent l'esearch on minimally processed fl'uits and vegetables has mainly focused on methods to inhibit browning, due to ban on use of sulfur dioxide, In order to retard or prevent these physiological changes, val'ious al ternatives, reducing agents. acidulants, chelating agents and inol'ganic sal ts have been evaluated for use on fresh cut fl'ui ts. Al though some agents were effective replacement for sulfur dioxide. consum$\textregistered$I'S demandless use of chemical on such products. Shel~ life of minimally processed products has been extended by inhibition of metabolic reactions associated with loss of quality and by inhibition of aerobic spoilage caused by wide variety of microorganisms. Appl ication of ~I.-\ packaging, including vacuum packaging, retards the rate of respiration, prevents growth of aerobic spoilage organisms, inhibits oxidation and color deterioration. Tissue softening is another major problem in minimally processed products because enzymes re 1 a ted to ce 11 wa 11 degrada t i on are not inactivated. Various treatments have been investigated for retardation of the softening of sliced products. Some studies have concentrated on the application of an active packaging system with ~I, l. packaging and calcium infi 1 tration as possible measures to retain firmness of processed products. In my opinion, one important step for production of minimally processed frui ts wi th favorabl e color of cut surface and firm texture is the selection of better cultivar. As the view, changing tendency of fresh color by apple cultivars and relationship between the tendency and PPO activity will be discussed in the seminar. In addition to the topic, research result on quality enhancement of fresh apple slices by heat shock treatment will be introduced.

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Apoptosis Induction of Human Breast Carcinoma Cells by Ethyl Alcohol Extract of Hizikia fusiforme (Apoptosis 유도에 의한 톳 ethyl alcohol 추출물의 인체 유방암세포 증식 억제)

  • Jung, Sun-Hwa;Hwang, Won-Deuk;Nam, Taek-Jeong;Choi, Yung-Hyun
    • Journal of Life Science
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    • v.19 no.11
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    • pp.1581-1590
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    • 2009
  • Hizikia fusiforme is a kind of brown edible seaweed that mainly grows in the temperate seaside areas of the northwest pacific, including Korea, Japan and China, and has been widely used as a health food for hundreds of years. Recently, H. fusiforme has been known to exert pharmacological activities including antioxidant, antimutagenic and anticoagulant activities. However, the molecular mechanisms of H. fusiforme in malignant cells have not been clearly elucidated yet. In this study, the effects of ethyl alcohol extract of H. fusiforme (EAHF) on the anti-proliferative effects of MDA-MB-231 and MCF-7 human breast cancer cells were investigated. EAHF treatment resulted in a concentration-dependent growth inhibition by including apoptosis in MDA-MB-231 cells and G1 phase arrest in MCF-7 cells, which could be proved by MTT assay, DAPI staining, agarose gel electrophoresis and flow cytometry analysis. In MDA-MB-231 cells, the increase in apoptosis induced by EAHF treatment correlated with up-regulation of pro-apoptotic Bax expression. EAHF treatment induced the proteolytic activation of caspase-3 and caspase-9, and a concomitant inhibition of poly (ADP-ribose) polymerase, $\beta$-catenin, phospholipase-${\gamma}1$ protein and DNA fragmentation factor 45/inhibitor of caspase-activated DNase. Taken together, these findings provide important new insights into the possible molecular mechanisms of the anti-cancer activity of H. fusiforme.

Forsythiae Fructus Induces VEGF Production via p38 MAPK Activation in Human Keratinocytes (각질형성세포에서 p38 MAPK 활성을 통한 연교의 VEGF 생성 효과)

  • Kim, Mi-Sun;Choi, Yun Ho;Park, Sun Gyoo;Lee, Cheon Koo;Lee, Sang Hwa
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.4
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    • pp.329-336
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    • 2016
  • Cutaneous microvasculature plays a critical role in age-associated skin changes. A considerable reduction of number and size of vessels has been observed in the upper dermis of elderly skin. Forsythiae fructus (FF), the dried fruit of plant Forsythia suspensa (F. suspensa), has been traditionally used as an herbal medicine to treat inflammatory diseases and bacterial diseases. However, its regulatory effect on angiogenic responses has not been elucidated in skin. Therefore, we analyzed secretory profiles upon treatment of FF extract using array designed to detect angiogenesis-associated mediators in human keratinocytes. Because keratinocyte-derived VEGF (vascular endothelial growth factor) has been regarded as a potent factor for new microvasculature under the epidermis, we further investigated the effect of FF extract on VEGF production. We observed that the VEGF expression of mRNA and protein level was increased by about 2 folds in a dose-dependent manner after FF extract treatment. In signaling experiments, FF extract induced rapid p38 MAPK activation within 5 min, and the activation was totally abrogated by pretreatment with a p38 MAPK specific inhibitor. The FF-induced VEGF upregulation was also significantly attenuated by a p38 MAPK inhibition. Taken together, FF extract induces VEGF production via p38 MAPK activation in human epidermal keratinocytes. These novel findings suggest that FF is useful as a potential agent with pro-angiogenic activity and may help to improve age-dependent reduction of the microvasculature in aged skin or to heal skin wound.

Identification of Growth Inhibitory Substance on Food-borne Microorganisms from Commiphora molmol Engl. and Its Application to Food Products (몰약(Commiphora molmol Engl.)의 식중독 미생물 증식 억제 물질의 구조동정 및 식품적용)

  • Han, Ji-Sook;Shin, Dong-Hwa;Baek, Nam-In
    • Korean Journal of Food Science and Technology
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    • v.33 no.4
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    • pp.401-408
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    • 2001
  • The ethanol extract and n-hexane fraction of Commiphora molmol Engl. showed minimum inhibitory concentration of 50 ppm and 25 ppm, respectively, on 5 strains of Listeria monocytogenes at $32^{\circ}C$. The purified substance, C3-3-2 fraction, was isolated by silica gel column and preparative thin layer chromatography from n-hexane fraction of Commiphora molmol Engl. The C3-3-2 fraction showed a strong bactericidal activity on 5 strains of L. monocytogenes at the concentration of 10 ppm in tryptic soy broth medium. At that concentration, the viable count was reduced $5{\sim}6$ log cycle from initial cell number. The n-hexane fraction of Commiphora molmol Engl. showed strong growth inhibition at the concentration of 25 ppm on Bacillus cereus and Staphylococcus aureus, at 50 ppm in broth on Salmonella enteritidis, and at 500 ppm on Vibrio parahaemolyticus. The purified antimicrobial substance, the C3-3-2 fraction, was identified as m-nonylphenol by on the basis of the $^1H-,\;^{13}C-NMR$ and EI/MS data. For the application test, the C3-3-2 fraction which was purely isolated from Commiphora molmol Engl. at 100 ppm were applied to minced Alaska pollack and ground beef at $32^{\circ}C$ and $5^{\circ}C$. The antimicrobial substances did not reduce L. monocytogenes ATCC 19113 at $32^{\circ}C$, while they reduced L. monocytogenes ATCC 19113 in viable number at $5^{\circ}C$. However, the antimicrobial effect of C3-3-2 fraction in food system was lower than that of broth condition.

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