• Title/Summary/Keyword: Beta cell-protection

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Action Mechanism of LB10522, a New Catechol-Substituted Cephalosporin (카테콜 치환체를 가진 세파로스포린계 항생제 LB10522의 작용기전)

  • Kim, Mu-Yong;Oh, Jeong-In;Paek, Kyoung-Sook;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.102-111
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    • 1996
  • LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.

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Effects of EGb 761 and Korean Red Ginseng on Melanogenesis in B16F10 Melanoma Cells and Protection Against UVB Irradiation in Murine Skin

  • Han, Seon-Kyu;Choi, Wook-Hee;Ann, Hyoung-Soo;Ahn, Ryoung-Me;Yi, Seh-Yoon
    • Molecular & Cellular Toxicology
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    • v.4 no.1
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    • pp.85-91
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    • 2008
  • These days there is a constant possibility of exposure to UV radiation which can cause abnormal production of melanin and result in skin disease such as hyperpigmentation and melanoma. Many materials were investigated for skin whitening and protection against UV radiation. In this study, we assessed the melanogenesis inhibitory activities of Korean Red Ginseng (KRG, Ginseng Radix Rubra) and Ginkgo (EGb 761 Ginkgo Biloba) in an attempt to develop a new skin whitening agent derived from natural products. B16F10 melanoma cells were treated for 48 hr with KRG and EGb 761. The inhibitory effect on melanogenesis was measured and related cytokines and proteins expression were also investigated by RT-PCR and Western blotting. In addition, we also assessed the effects of these substances on the skin of C57BL/6 mice. Cell growth, melanin content and tyrosinase activity were inhibited effectively in B16F10 melanoma cells treated with KRG and EGb 761. Moreover, tyrosinase mRNA expression was inhibited clearly and melanogenesis related proteins (MRPs) containing tyrosinase, TRP1 and TRP2 were also reduced by KRG and EGb761, while cytokines such as IL-$1{\beta}$ and IL-6 were induced. In the case of UV irradiated mice, we observed induction of cytokine mRNA levels and reduction of MRPs mRNA expression. In addition, a decrease in pigmentation from treatment with KRG and EGb 761 on the skin of mice was observed. These results indicate that KRG and EGb 761 inhibit melanogenesis in B16F10 cells and have display protective activities against UVB. Therefore, we suggest that KRG and EGb 761 are good candidates to be used as whitening agents and UVB protectors for the skin.

Quantitative Changes of Plant Defense Enzymes in Biocontrol of Pepper (Capsicium annuum L.) Late Blight by Antagonistic Bacillus subtilis HJ927

  • LEE HYUN-JIN;PARK KEUN-HYUNG;SHIM JAE-HAN;PARK RO-DONG;KIM YONG-WOONG;CHO JEUNG-YONG;HWANGBO HOON;KIM YOUNG-CHEOL;CHA GYU-SUK;KRISHNAN HARI B.;KIM KIL-YONG
    • Journal of Microbiology and Biotechnology
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    • v.15 no.5
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    • pp.1073-1079
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    • 2005
  • To investigate plant protection, pathogenesis-related (PR) proteins and plant defense enzymes related to cell wall lignification were studied in pepper plants inoculated with antagonistic Bacillus subtilis HJ927 and pathogenic strain Phytophthora capsici. Phytophthora blight disease was reduced by $53\%$ in pepper roots when preinoculated with B. subtilis HJ927 against P. capsici. The activities of PR proteins (chitinase and ${\beta}$-1,3,-glucanase) and defense-related enzymes (peroxidase, polyphenoloxidase, and phenylalanine ammonia lyase) decreased in roots of B. subtilis+P capsid-treated plants, but increased in leaves with time. The decrease and increase were much greater in P. capsici-treated plants than in B. subtilis HJ927+P capsici-treated plants, although P. capsici-treated plants had more severe damage. Therefore, changes of enzyme activities do not seem to be directly related to plant protection. We suggest that the change of these enzymes in pathogen-treated plants may be related to plant response rather than to resistance against pathogen attacks.

Effects of Egg Shell Membrane Hydrolysates on UVB-radiation-induced Wrinkle Formation in SKH-1 Hairless Mice

  • Yoo, Jin Hee;Kim, Jong Keun;Yang, Hee Jin;Park, Ki Moon
    • Food Science of Animal Resources
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    • v.35 no.1
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    • pp.58-70
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    • 2015
  • This study was conducted to examine the effect of egg shell membrane hydrolysates (ESMH) on wrinkle, UV, and moisture protection for cosmetic use. ESMH were fragmented as whole ESMH (before fractioning), Fraction I (> 10 kDa), Fraction II (3-10 kDa), and Fraction III (< 3 kDa). In order to test whether fractionated ESMH can be used for functional cosmetic materials, we examined not only the level of hyaluronic acid and collagen production, but also the MMP-1 activity using a HaCaT and CCD-986Sk cell line. Our study treated each sample of fractionated ESMH with different concentrations (0.01, 0.1, 1 mg/mL). In our in vivo research, we used hairless mice that had been exposed to UV-B to induce wrinkles for 7 wk, then applied Fraction I to the treatment group for 5 wk and then tested skin thickness, minimum erythema dose and moisture content. In addition, Fraction I was high in collagen and HA biosynthesis and it was better than TGF-${\beta}$ in improving of the skin. When TNF-${\alpha}$ caused MMP-1 activity in the CCD-986Sk cells, the whole ESMH and Fraction I proved to be effective in hindering the induction of collagenase depending on the concentration, and also showed outstanding effects in the suppression of skin aging. We found that the treatment group mice's UV-B radiation-induced skin damage was largely mitigated compared to that of the non-treatment group mice. Thus, we have concluded that EMSH helps to mitigate UV-B radiation-induced wrinkles, collagen, HA, MMP-1 activity and can be used for functional cosmetic materials.

Antioxidants and Anti-inflammatory Effects of Fermented Houttuynia cordata Thunb and Scoria Mixture Extract

  • Lee, Sung-Gyu;Kang, Sangmoon;Lee, Kee-Young;Park, Kwang-Lyul;Kang, Hyun
    • Biomedical Science Letters
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    • v.23 no.4
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    • pp.355-361
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    • 2017
  • In this study, antioxidant and anti-inflammatory of fermented Houttuynia cordata Thunb and scoria mixture extract were investigated in vitro. Radical-scavenging activities of the ethanol extracts were examined by using ${\alpha},{\alpha}$-diphenyl-${\beta}$-picrylhydrazyl (DPPH) and 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid (ABTS)) radicals assay. Consequently, we confirmed that fermented Houttuynia cordata Thunb and scoria mixture extract dependent removed DPPH and ABTS radical. Also, to confirm anti-inflammatory activity of ethanol extract, we treated fermented Houttuynia cordata Thunb and scoria mixture extract on BV-2 cell with LPS. The result showed that fermented Houttuynia cordata Thunb and scoria mixture extract concentration-dependent inhibited NO production. Therefore, fermented Houttuynia cordata Thunb and scoria mixture extract showed inhibition radical oxygen activities and inflammatory and have available for a pharmacological composition on neuritis-protection and treatment.

PROTECTION EFFECT OF GINSENG EXTRACT AGAINST APOPTOTIC CELL DEATH INDUCED BY 2,2,5,5-TETRACHLOROBIPHENYL IN NEURONAL SK-N-MC CELLS

  • Lee, Ji-Young;Kim, Jae-Won;Song, Ji-Eun;Kim, Soo-Jung;Chung, Weon-Gu;Kim, Yong-Hoon;Lee, Bo-Ram;Kim, Jin-Hee;Choi, Young-Keun;Joo, Woo-Hong;Cho, Yong-Kweon;Moon, Ja-Young
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.112-112
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    • 2001
  • Oxidative stress plays an important role in the pathological process of neurodegenerative diseases. Polychlorinated biphenyls (PCBs) are ubiquitous environmental contaminants, some of which may be neurotoxic. Our previous studies showed that 2,2',5,5'-TetracWorobiphenyl (PCB 52) induced apoptotic death in human neuronal SK-N-MC cells, which was demonstrated on gel electrophoresis by visualization of the proteolytic cleavages of $\beta$-catenin and poly (ADP-ribose) polymerase (PARP) and of the production of characteristic ladder patterns of DNA fragmentation.

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Future Prospects of the Development of Calcium Antagonists

  • Schwartz, Arnold
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.53-53
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    • 1993
  • In considering the mechanism of action of the calcium antagonists, it is important to realize that there are three distinct receptor types and that the new classification divides these three drugs as members of the dihydropyridine, phenylalkylamines and benzothiazipines, respectively. The World Health Organization as well as the International Union of Pharmacology and Cardiology have adopted this classification. Unlike every other class of drugs, such as the alpha and beta adrenergic blocking agents, diuretics, etc., the calcium antagonists need to be thought of as three distinct drug classes. The reason they share some, but not all of the pharmacological profile is that they all act at specific receptor domains present in one large protein of 165 daltons present in all excitable tissue. This protein along with several other subunits make up what is known as the voltage-dependent calcium channel (the so-called "L"type, L-VDCC). The mechanism of action of the three drugs involve first a specfic binding and then an inhibition of the movement of calcium into the cell Some of these drugs, such as diltiazem, may have other interesting intracellular effects perhaps associated with protection of the mitochondria during ischemic insults. The nature of the receptor is being explored by molecular genetic techniques, and we have recently cloned two of the major subunits; some of the data will be presented.

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Ganoderma Lucidum Pharmacopuncture for Teating Ethanol-induced Chronic Gastric Ulcers in Rats

  • Park, Jae-Heung;Jang, Kyung-Jun;Kim, Cheol-Hong;Kim, Jung-Hee;Kim, Young-Kyun;Yoon, Hyun-Min
    • Journal of Pharmacopuncture
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    • v.18 no.1
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    • pp.72-78
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    • 2015
  • Objectives: The stomach is a sensitive digestive organ that is susceptible to exogenous pathogens from the diet. In response to such pathogens, the stomach induces oxidative stress, which might be related to the development of both gastric organic disorders such as gastritis, gastric ulcers, and gastric cancer, and functional disorders such as functional dyspepsia. This study was accomplished to investigate the effect of Ganoderma lucidum pharmacopuncture (GLP) on chronic gastric ulcers in rats. Methods: The rats were divided into 4 groups of 8 animals each: the normal, the control, the normal saline (NP) and the GLP groups. In this study, the modified ethanol gastritis model was used. The rats were administrated 56% ethanol orally every other day. The dose of ethanol was 8 g/kg body weight. The normal group received the same amount of normal saline instead of ethanol. The NP and the GLP groups were treated with injection of saline and GLP respectively. The control group received no treatment. Two local acupoints CV12 (中脘) and ST36 (足三里) were used. All laboratory rats underwent treatment for 15 days. On last day, the rats were sacrificed and their stomachs were immediately excised. Results: Ulcers of the gastric mucosa appeared as elongated bands of hemorrhagic lesions parallel to the long axis of the stomach. In the NP and GLP groups, the injuries to the gastric mucosal injuries were not as severe as they were in the control group. Wound healings of the chronic gastric ulcers was promoted by using GLP and significant alterations of the indices in the gastric mucosa were observed. Such protection was demonstrated by gross appearance, histology and immunehistochemistry staining for Bcl-2-associated X (BAX), B-cell lymphoma 2 (Bcl-2) and Transforming growth factor-beta 1 (TGF-${\beta}1$). Conclusion: These results suggest that GLP at CV12 and ST36 can provide significant protection to the gastric mucosa against an ethanol induced chronic gastric ulcer.

Change of Antioxidant Activities in Carrots (Daucus carota var. sativa) with Enzyme Treatment (효소처리 가공이 당근(Daucus carota var. sativa)의 항산화 활성 변화에 미치는 영향)

  • Yoo, Jin-Kyoun;Lee, Jin-Hee;Cho, Hyung-Yong;Kim, Jung-Gook
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.2
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    • pp.262-267
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    • 2013
  • The purpose of this research is to minimize the loss of nutrients in carrots (Daucus carota var. sativa). A protopectinase was used to enzymatically macerated and separate cells without damage. The enzyme modification group's collection rate was 81% (residue rate 19%), while the grinding process group's collection rate was 56% (residue rate 44%)-an over 20% of collection rate difference. Thus we predicted a big difference in transference number after the process and wastage. In comparing ingredient changes in the enzyme modification group versus the grinding process group, the content of ${\beta}$-carotene (the carrot's main ingredient) showed a change in protection factor (PF) ($2.2{\pm}0.2$ PF, $1.4{\pm}0.4$ PF, respectively), total polyphenol content ($89{\pm}3.42{\mu}g/g$, $64{\pm}4.16{\mu}g/g$, respectively), and total flavonoid content ($68{\pm}2.73{\mu}g/g$, $41{\pm}3.26{\mu}g/g$, respectively). Thus we confirmed that nutrient destruction, due to cell membrane preservation, occurred less often in the enzyme modification process than the mechanical grinding process group. We also measured DPPH radical scavenging activity, hydroxyl radical scavenging activity, and nitrite scavenging activity. DPPH radical scavenging activity was $87{\pm}0.29%$ and $74{\pm}1.56%$ in the enzymatic modification group compared to the mechanical grinding process group, respectively. Hydroxyl radical scavenging activity was $44{\pm}0.49%$ and $32{\pm}0.48%$ in the enzymatic modification group compared to the mechanical grinding process group, respectively. Nitrite scavenging activity was $59{\pm}0.53%$ and $46{\pm}0.62%$ in the enzymatic modification group compared to the mechanical grinding process group, respectively. Our results show that cell membrane preservation, via the protopectinase enzyme process, decreases the loss of nutrients and still preserves inherent antioxidants.

Protective Effects of Bifidobacterium bifidum Culture Supernatants and Intracellular Cell-Free Extracts on Human Dermal Fibroblasts against UV-B Irradiation (인간 진피섬유아세포에서 Bifidobacterium bifidum 배양액 및 추출액의 자외선B에 대한 보호 효능)

  • Gwon, Gi Yeong;Park, Gwi Gun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.46 no.7
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    • pp.801-808
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    • 2017
  • The present study investigated the protective effects of Bifidobacterium bifidum culture supernatants (BbSC) and intracellular cell-free extracts (BbICFE) on human dermal fibroblasts (HDFs) against ultraviolet-B (UV-B) irradiation. HDFs were treated with UV-B, UV-B+BbCS, and UV-B+BbICFE. Treatment of UV-B-irradiated HDFs with BbCS and BbICFE significantly increased cell viability compared to UV-B-irradiated HDFs. BbCS treatment reduced senescence in HDFs by approximately 40.0%. Moreover, sub-G1 phase was significantly reduced in BbCS- and BbICFE-treated HDFs (3.3% and 4.5%, respectively). The effect of UV-B on oxidative damage of HDFs was measured by dichlorofluorescin diacetate. Fluorescence intensity significantly increased in UV-B-irradiated HDFs. Inhibition of cellular reactive oxygen species in HDFs treated with 0.01% BbCS was the highest at 34.1%. Levels of p21 and p53 protein expression induced by UV-B irradiation were reduced by treatment with BbCS and BbICFE (47.0% and 35.6%, respectively). These results show that BbCS and BbICFE reduce UV-B-induced cellular senescence and apoptosis in HDFs. Thus, BbCS and BbICFE can be used as potential agents for protection of UV-B-induced skin cell damage.