• Title/Summary/Keyword: inhibiting activity

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The Effect of Fresh Paprika and Paprika powder dried by far-infrared ray on Inhibition of Lipid Oxidation in Lard Model System (돈지 모형계에서 생 파프리카와 원적외선 건조 파프리카 분말의 지질 산화 억제 효과 비교)

  • Park Jae-Hee;Kim Chang-Soon;Noh Sang-Kyu
    • Korean journal of food and cookery science
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    • v.21 no.4 s.88
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    • pp.475-481
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    • 2005
  • This study was conducted to determine the antioxidant activity of paprika in a lard model system. The effect of paprika (ground fresh paprika (FP) $3\%$, $50^{\circ}C$ far-infrared ray dried Paprika Powder (PP) $3\%$ and $5\%$) on the inhibition of lipid oxidation in lard was examined by pH, peroxide value (POV), thiobarbituric acid (TBA) value and fatty acid composition during 8 days of storage at $4^{\circ}C$. With paprika, POV and TBA values in lipid oxidation of lard were significantly lower than those of the control without paprika. Especially, in lard with FP $3\%$, there was hardly any change of lipid oxidation values such as POV, TBA values and destruction of unsaturated fatty acid inhibiting lipid oxidation. Heating of paprika during far-infrared ray drying decreased the inhibition effect on lipid oxidation in the lard model system probably due to loss of antioxidant substances, such as vitamin C, polyphenols and carotenoids including capsanthin, by heating. Therefore, FP containing a hish amount of antioxidant substance could be used as a good antioxidant in Pork Products containing large amounts of lard.

LC15-0133, a DPP IV Inhibitor: Efficacy in Various Animal Models (LC15-0133, DPP IV 저해제: 여러 동물 모델에서의 효능)

  • Yim, Hyeon-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2008.04a
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    • pp.5-20
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    • 2008
  • GLP-1-based drugs (GLP-1 analogues and DPP IV inhibitors) and incretin mimetics are currently one of the most exciting classes of agents for type II diabetes. GLP-1, a gut peptide, is an incretin that potentiates glucose-dependent insulin release from the pancreas, slows GI-transit and stimulates the proliferation of beta-cells. DPP IV inhibitors act like incretins by inhibiting DPP IV which inactivates GLP-1. LC15-0133 is a competitive, reversible DPP IV inhibitor ($IC_{50}$ = 24 nM, Ki=0.247 nM) with excellent selectivity over other critical human proteases such as DPP II, DPP 8, elastase, trypsin. and urokinase. LC15-0133 showed long half-life and good bioavailability in rats and dogs. Inhibition of plasma DPP IV activity by LC15-0133 was kept more than 50% 24 hours after oral dosing in rats and dogs at 0.1 mg/kg and 0.02 mg/kg, respectively. The Minimum effective doses of LC15-0133 were 0.01 mg/kg for lowering blood glucose excursion during oral glucose tolerance test and 0.1 mg/kg for increasing glucose-induced GLP-1 response in C57BL/6 mice. Repeat oral administration of LC15-0133 for 1 month delayed the progression to diabetes and reduced HbA1c levels in a dose-dependent manner in Zucker Diabetic Fatty rats. In conclusion, LC15-0133 is a novel, potent, selective and orally active DPP IV inhibitor and showed an excellent blood glucose lowering effects in various animal models.

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Anticancer Activities of the Methanolic Extract from Lemon Leaves in Human Breast Cancer Stem Cells (인간 유방암 줄기세포에서 레몬잎 메탄올 추출물의 항암 효능)

  • Moon, Jeong Yong;Nguyen, Linh Thi Thao;Hyun, Ho Bong;Osman, Ahmed;Cho, Minwhan;Han, Suyeong;Lee, Dong-Sun;Ahn, Kwang Seok
    • Journal of Applied Biological Chemistry
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    • v.58 no.3
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    • pp.219-226
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    • 2015
  • The anticancer activity of a methanolic extract from lemon leaves (MLL) was assessed in MCF-7-SC human breast cancer stem cells. MLL induced apoptosis in MCF-7-SC, as evidenced by increased apoptotic body formation, sub-G1 cell population, annexin V-positive cells, Bax/Bcl-2 ratio, as well as proteolytic activation of caspase-9 and caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein. Concomitantly, MLL induced the formation of acidic vesicular organelles, increased LC3-II accumulation, and reduced the activation of Akt, mTOR, and p70S6K, suggesting that MLL initiates an autophagic progression in MCF-7-SC via the Akt/mTOR pathway. Epithelial-mesenchymal transition (EMT), a critical step in the acquisition of the metastatic state, is an attractive target for therapeutic interventions directed against tumor metastasis. At low concentrations, MLL induced anti-metastatic effects on MCF-7-SC by inhibiting the EMT process. Exposure to MLL also led to an increase in the epithelial marker E-cadherin, but decreased protein levels of the mesenchymal markers Snail and Slug. Collectively, this study provides evidence that lemon leaves possess cytotoxicity and anti-metastatic properties. Therefore, MLL may prove to be beneficial as a medicinal plant for alternative novel anticancer drugs and nutraceutical products.

Isolation and Structure Identification of Antifungal Substance from Aspergillus terreus (Aspergillus terreus로부터 항진균성 물질의 분리 및 구조분석)

  • Kim, Keun-Ki;Park, Ki-Hun;Moon, Suk-Sik;Kang, Kyu-Young
    • Applied Biological Chemistry
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    • v.40 no.6
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    • pp.593-596
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    • 1997
  • In the course of search antagonistic fungi from soil in green house, four kind of fungi (AF1, AF2, AF3, AF4) were isolated, which have activities against Phytophthora capsici, Botrytis cinera, Rhizoctonia solani, Pythium ultimum and Fusarium oxysporum. The AF2 was identified according to the morphological description of Aspergillus terreus. This antagonistic fungus inhibiting various plant pathogens was effective to reduce disease incidence of cucumber seedlings caused by mixed inoculum of Rhizoctonia solani, Pythium ultimum and Fusarium oxysporum. Antifungal compound I was isolated and purified by fresh chromatography from A. terreus. The $^1H$ and $^{13}C$ assignment of compound I was achieved from two-dimensional $^1H-^1H\;COSY$, HMQC, HMBC with the add of homonuclear and heteronuclear double resonance experiment. The compound I was identified butyrolactone I (${\alpha}$-oxo-${\beta}$-(p-hydroxyphenyl)-${\gamma}$-(p-hydroxy-m-3,3-dimethyl-allylbenzyl)-${\gamma}$-methoxycarbonyl-${\gamma}$-butyrolactone, $C_{24}H_{24}O_7$, M.W.=424).

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Effects of Caffeine and Dietary Fat on Mouse Mammary Development (Caffeine과 지방급여가 생쥐의 유선발달에 미치는 효과)

  • Lee, Seung-Yop;Yuh, In-Suh
    • Korean Journal of Animal Reproduction
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    • v.25 no.4
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    • pp.349-357
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    • 2001
  • This study was conducted to examine the effect of caffeine and three dietary levels of fat, i.e., 0%, 5% and 20% on mammary gland development. Mice were assigned to three groups (dietary levels 0%, 5%, 20% fat), and treated caffeine of half within the each group. Caffeine-treated mice with 0% or 20% fat levels significantly increased 4$^{th}$ mammary gland development in comparison with that of no caffeine -treated mice (P<0.05). Caffeine-treated mice significantly increased DNA contents of 4$^{th}$ mammary gland in comparison with that of no caffeine-treated mice (P<0.05), and DNA contents of mammary gland increased as fat levels increased within caffeine-treated or no caffeine-treated group. nteraction effect was shown between caffeine and 20% fat diet, [(20% fat+caffeine) - (20% fat + no caffeine) vs (0% fat + caffeine) - (0% fat + no caffeine)](P<0.01). Conclusively, caffeine significantly increased mouse mammary gland development possibly by inhibiting phosphodiesterase activity, and dietary fat supplements increased mammary gland development as the fat content of the diet increased from 0 to 20%. The stimulatory effect of caffeine in mammary development interacted with high level of fat diet.

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Hot Water Extract of Scutellaria baicalensis Inhibits Migration, Invasion and Tube Formation in a Human Umbilical Vein Endothelial Cell Model and a Rat Aortic Ring Sprouting Model (혈관내피세포와 흰쥐 대동맥 미세혈관 발아 모델을 이용한 황금 열수추출물의 세포의 이동, 침투 및 관형성 억제 연구)

  • Kim, Eok-Cheon;Bae, Kiho;Kim, Han Sung;Yoo, Yeong-Min;Gelinsky, Michael;Kim, Tack-Joong
    • Journal of Life Science
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    • v.26 no.1
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    • pp.91-100
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    • 2016
  • Angiogenesis is essential for the pathophysiological processes of embryogenesis, tissue growth, diabetic retinopathy, psoriasis, wound healing, rheumatoid arthritis, cardiovascular diseases, and tumor growth. Inhibition of angiogenesis represents an attractive therapeutic approach for the treatment of angiogenic diseases such as cancer. However, uncontrolled angiogenesis is also necessary for tumor development and metastasis. Inhibition of vascular endothelial growth factor (VEGF) signaling, a critical factor in the induction of angiogenesis, cause robust and rapid changes in blood vessels of tumors and therefore VEGF constitutes a target for such anti-angiogenic therapy. Recently, since natural compounds pose significantly less risk of deleterious side effects than synthetic compounds, a great many natural resources have been assessed for useful substance for anti-angiogenic treatment. Here we evaluated the anti-angiogenic effects of a hot water extract of Scutellaria baicalensis (SBHWE) using in vitro assays and ex vivo animal experiments. Our results show that SBHWE dose-dependently abrogated vascular endothelial responses by inhibiting VEGF-stimulated migration and invasion as well as tube formation in a human umbilical vein endothelial cell (HUVEC) model, without cytotoxicity, as determined by a cell viability assay. Further study revealed that SBHWE prevented VEGF-induced neo-vascularization in a rat aortic ring sprouting model. Taken together, our findings reveal an anti-angiogenic activity of Scutellaria baicalensis and suggest that SBHWE is a novel candidate inhibitor of VEGF-induced angiogenesis.

The Effects and Mechanisms of Glycolic Acid on the UV-induced Skin Cell Proliferation (UV에 대한 Glycolic Acid의 피부세포증식 기전연구 및 억제효과)

  • Hong, Jin-Tae;Lee, Hwa-Jeong;Lee, Chung-Woo;Ahn, Kwang-Soo;Yun, Yeo-Pyo;Pyo, Heung-Bae;Cho, Chan-Hwi;Hong, Ki-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.3 s.52
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    • pp.219-236
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    • 2005
  • Glycolic acid, an alpha-hydroxy acid derived from fruit and milk sugars, has been commonly used as a cosmetic ingredient since it was known to have photo-protective, anti-inflammatory effects, and anti-oxidant effect in UV-irradiated skin. However, little has been know about the functional role of glycolic acid on UV-induced skin cell proliferation. It was previously found that glycolic acid inhibited UV-induced skin tumor development in hairless mouse. As a possible mechanism of glycolic acid on the UV-induced skin tumor development, the ability of glycolic acid to inhibit the UVB-induced cell growth and possible mechanisms were investigated. Glycolic acid treatment attenuated the UV-induced cell proliferation and apoptotic cell death in the skin. In vitro study, glycolic acid inhibited the UVB-induced cell growth and apoptotic death through inhibiting caspase-3 activity. These results suggest that glycolic acid may exert the Inhibitory effect on the UVB-induced skin tumor development by regulating cell growth and apoptotic cell death.

Anti-Inflammatory and Anti-allergic Effects of Gnaphalium affine Extract (떡쑥 추출물의 항염증 및 항알러지 효과)

  • Roh, Kyung-Baeg;Lee, Jung-A;Park, Junho;Jung, Kwangseon;Jung, Eunsun;Park, Deokhoon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.43 no.2
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    • pp.103-114
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    • 2017
  • Gnaphalium affine D. DON (GA) has been used as a vegetable as well as a folk medicine in East Asia. The antioxidant and anti-complementary activity of GA extract (GAE) has also been reported. However, little is known about its anti-inflammatory and anti-allergic effect and mechanism of action. In this study, we evaluated the inhibitory effects of GAE on the production of inflammatory mediators such as NO, $PGE_2$, TLR4, eotaxin-1 and histamine. Our results suggest that GAE inhibits the production of NO and $PGE_2$ by inhibiting transcriptional activation via the involvement of iNOS and COX-2. The LPS-induced expression of Toll-like receptor 4 (TLR4) was also attenuated. In addition, GAE inhibited A23187-induced histamine release from MC/9 mast cells. It also inhibited the production of eotaxin-1 induced by IL-4. Collectively, these results suggest that GAE may have considerable potential as a cosmetic ingredient with anti-inflammatory and anti-allergic properties.

Anti-Inflammatory Effect of Biji (Soybean curd residue) on LPS-Stimulated RAW264.7 Cells (마우스 RAW264.7 세포에 대한 비지 추출물의 항염증 활성)

  • Park, Su Bin;Song, Hun Min;Kim, Ha Na;Park, Gwang Hun;Son, Ho-Jun;Um, Yurry;Park, Ji Ae;Jeong, Jin Boo
    • Korean Journal of Plant Resources
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    • v.31 no.2
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    • pp.117-123
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    • 2018
  • In this study, we evaluated anti-inflammatory effect of biji in LPS-stimulated RAW264.7 cells. Biji inhibited the generation of NO and $PGE_2$ through the suppression of iNOS and COX-2 expression. In addition, biji attenuated the expression of TNF-${\alpha}$ and IL-$1{\beta}$ induced by LPS. Biji blocked LPS-mediated $I{\kappa}B-{\alpha}$ degradation and subsequently inhibited p65 nucleus accumulation in RAW264.7 cells, which indicates that biji inhibits NF-${\kappa}B$ signaling. In addition, biji suppressed p38 phosphorylation induced by LPS. Our results suggests that biji may exert anti-inflammatory activity through blocking the generation of the inflammatory mediators such as NO, $PGE_2$, iNOS, COX-2, TNF-${\alpha}$ and IL-$1{\beta}$ via the inhibiting the activation of NF-${\kappa}B$ and p38. From these findings, biji has potential to be a candidate for the development of chemoprevention or therapeutic agents for inflammatory diseases.

Upregulation of miR-23b Enhances the Autologous Therapeutic Potential for Degenerative Arthritis by Targeting PRKACB in Synovial Fluid-Derived Mesenchymal Stem Cells from Patients

  • Ham, Onju;Lee, Chang Youn;Song, Byeong-Wook;Lee, Se-Yeon;Kim, Ran;Park, Jun-Hee;Lee, Jiyun;Seo, Hyang-Hee;Lee, Chae Yoon;Chung, Yong-An;Maeng, Lee-So;Lee, Min Young;Kim, Jongmin;Hwang, Jihwan;Woo, Dong Kyun;Chang, Woochul
    • Molecules and Cells
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    • v.37 no.6
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    • pp.449-456
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    • 2014
  • The use of synovial fluid-derived mesenchymal stem cells (SFMSCs) obtained from patients with degenerative arthropathy may serve as an alternative therapeutic strategy in osteoarthritis (OA) and rheumatoid arthritis (RA). For treatment of OA and RA patients, autologous transplantation of differentiated MSCs has several beneficial effects for cartilage regeneration including immunomodulatory activity. In this study, we induced chondrogenic differentiation of SFMSCs by inhibiting protein kinase A (PKA) with a small molecule and microRNA (miRNA). Chondrogenic differentiation was confirmed by PCR and immunocytochemistry using probes specific for aggrecan, the major cartilaginous proteoglycan gene. Absorbance of alcian blue stain to detect chondrogenic differentiation was increased in H-89 and/or miRNA-23b-transfected cells. Furthermore, expression of matrix metalloproteinase (MMP)-9 and MMP-2 was decreased in treated1 cells. Therefore, differentiation of SFMSCs into chondrocytes through inhibition of PKA signaling may be a therapeutic option for OA or RA patients.