• Title/Summary/Keyword: in vivo activity

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The Effects of Vitex rotundifolia Linne fil. Extract on the Inflammatory and Allergic Reactions (만형자 추출물이 염증 및 알레르기 반응에 미치는 영향)

  • Yeon, Kyoung-Jin;Jung, Hyun-A;Roh, Seok-Seon
    • Journal of Haehwa Medicine
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    • v.22 no.1
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    • pp.145-170
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    • 2013
  • Objectives : This study was carried out to investigate the anti inflammatory and anti allergy effects of Vitex rotundifolia Linne fil. extract(VRE). Results : 1. In vitro test, VRE was used to determine the modulation of cytokine secretion, the activation of inflammatory and allergic factor and the inhibition of gene expression. The cell survival rate of Raw 264.7 and Jurkat T cells didn't decrease and accordingly cytotoxicity wasn't observed. In anti-allergic assay, the secretion of IL-2, TNF-${\alpha}$, IL-4, IL-5 and IFN-${\gamma}$ were suppressed on Jurkat T cells induced by dust mites. And the gene expression of COX-2 was suppressed in HMC-1 stimulated by calcium ionophore A23187. In anti-inflammatory assay, the gene expression of TNF-${\alpha}$, COX-2 were suppressed on LPS-activated Raw 264.7 cells. And the secretion of IL-6 and IL-8 were suppressed on EoL-1 cells induced by dust mites. P38 and ERK activation of MAPK decreased generally. VRE showed potent inhibitory activity of NO production. 2. In vivo test, we used NC/Nga mouse induced by atopic dermatitis to observe the effects of VRE on the weight, water and feed, blood test, weight of organs, total IgE and histological change of main organs. Quantity of water and feed were not changed, therefore it didn't affect the weight directly, and no change was observed in related main organs, thus maybe there is no organ toxicity by test substances. And the symptoms were decreased significantly, and the thickness of epithelial cell layer and the number of mast cells were inhibited significantly by the difference of dosage. The number of total complete blood cells and IgE in serum were not changed significantly. Conclusion : These results suggest that VRE has anti-inflammatory and anti-allergic effects. Therefore VRE could be used effectively on improvement or treatment of atopic dermatitis. However, further study is needed to prove which component of VRE indicates effective pharmacological action.

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.

Molecular Basis of Organospecific Carcinogensis by Chemical Carcinogens-Study with Breast Cancer Specific Carcinogens: DMBA as an Indirect-Acting carcinogen and NMU as a Direct-Acting cancinogen. (화학적 발암원의 조직 특이성 암유발기전 - DMBA와 NMU의 선택적 유암 발생기전을 중심으로 )

  • 박종영;김승원;박상철
    • Environmental Mutagens and Carcinogens
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    • v.9 no.1
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    • pp.1-12
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    • 1989
  • To study the selective organospecific carcinogenesis by the specific chemical carcinogens, the breast cancer induction model by oral administration of 7, 12-dimethylbenzanthracene (DMBA) or by intravenous injection of N-methylni-trosourea (NMU) on female rats was analyzed. In the present experiment, we compared the effexts of ages on the chemical mammary carcinogenesis by studying the metabolic system of the carcinogenic activation, detoxification or DNA damage and repair. The breast tumor incidence was significantly higher in the young rats of 50 days old than in those of one year old rats. As an index of organospecific DNA damage or repair, the in vivo covalent binding index(CBI) of the specific organs by the specific chemical carcinogens was monitored. And for the analysis of carcinogenic activation, the quantity of cytochrome P450`s was determined with the respective type-specific monoclonal antibody, while the detoxication capacity was deduced by the activity monitoring of glutathione S-transferase (GST) and peroxidase. The skin tissues of the mammary region had the highest CBI with both of DMBA and NMU at 50 days of age. And there were contrasting differences in the contents of carcinogenic activation and detoxication system: that is, the content of T.C.D.D.-inducible cytochrome P450 was high, while the activities of GST and peroxidase was low in the mammary skin tissues at tumor prevalent age. These results led us to conclude that the molecular organospecific carcinogenesis, as illustrated with mammary carcinoge-nesis by DMBA and NMU, is operated probably through the differential capacity of the target tissues in the high carcinogenic activation, low detoxication and the low DNA repair function.

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In vitro Evaluation of Biological Activities of Wa-song (Orostachys japonicus A. Berger) and Korean Traditional Plants Mixture (와송과 한약재 복합물의 in vitro 생리활성 평가)

  • Lee, Soo-Jung;Shin, Jung-Hye;Kang, Jae-Ran;Hwang, Cho-Rong;Sung, Nak-Ju
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.3
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    • pp.295-301
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    • 2012
  • This study was carried out to determine the biological activities of Wa-song (Orostachys japonicus) hot water extracts. Four types of extract samples were prepared, including Wa-song, traditional plants mixture [PM; mixture of Baekbokryung (Poria cocos), Changchul (Atractylodis rhizoma), and Sa-in (Amomum xanthoides)], and two different ratio composites of these (mixture of PM and Wa-song extract, 1:1 (v/v); PMO-1 and 1:3 (v/v); PMO-3). Their biological activities were measured using various in vitro assays. Total phenolic and flavonoid contents of PM were higher compared to those of Wa-song, and those of PMO-1 were higher than those of PMO-3. Further, PMO-1 contained higher ABTS and DPPH radical scavenging, reducing power, and nitrite scavenging activities than PMO-3. On the contrary, PMO-3 contained higher tyrosinase and inhibitory activities of MCF-7 and HT-29 cancer cells than PMO-1. According to the results, biological activities of PMOs were significantly higher than those of Wa-song extract and PM in in vitro assays. Therefore, we expect that PMOs could show higher biological activities than Wa-song extract alone in vivo.

Levosulpiride, (S)-(-)-5-Aminosulfonyl-N-[(1-ethyl-2-pyrrolidinyl) methyl]-2-methoxybenzamide, enhances the transduction efficiency of PEP-1-ribosomal protein S3 in vitro and in vivo

  • Ahn, Eun-Hee;Kim, Dae-Won;Kim, Duk-Soo;Woo, Su-Jung;Kim, Hye-Ri;Kim, Joon;Lim, Soon-Sung;Kang, Tae-Cheon;Kim, Dong-Joon;Suk, Ki-Tae;Park, Jin-Seu;Luo, Qiuxiang;Eum, Won-Sik;Hwang, Hyun-Sook;Choi, Soo-Young
    • BMB Reports
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    • v.44 no.5
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    • pp.329-334
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    • 2011
  • Many proteins with poor transduction efficiency were reported to be delivered to cells by fusion with protein transduction domains (PTDs). In this study, we investigated the effect of levosulpiride on the transduction of PEP-1 ribosomal protein S3 (PEP-1-rpS3), and examined its influence on the stimulation of the therapeutic properties of PEP-1-rpS3. PEP-1-rpS3 transduction into HaCaT human keratinocytes and mouse skin was stimulated by levosulpiride in a manner that did not directly affect the cell viability. Following 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice, levosulpiride alone was ineffective in reducing TPA-induced edema and in inhibiting the elevated productions of inflammatory mediators and cytokines, such as cyclooxygenase-2, inducible nitric oxide synthase, interleukin-6 and -1${\beta}$, and tumor necrosis factor-${\alpha}$. Anti-inflammatory activity by PEP-1-rpS3 + levosulpiride was significantly more potent than by PEP-1-rpS3 alone. These results suggest that levosulpiride may be useful for enhancing the therapeutic effect of PEP-1-rpS3 against various inflammatory diseases.

Protective Activities of Lactobacillus casei YIT 9018 against Salmonella enteritidis KU101 and Characteristics of 16S-23S rRNA Intergenic Spacer Region Sequence (Lactobacillus spp의 Salmonella enteritidis KU 101에 대한 보호 효과와 L. casei YIT 9018의 16S-23S rRNA Intergenic Spacer Region 염기배열 특성)

  • Sung, Bae-Jin;Ho, Yoon-Yung
    • Journal of Animal Science and Technology
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    • v.45 no.3
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    • pp.473-482
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    • 2003
  • In vivo protective and in vitro inhibitory activities of Lactobacillus casei YIT 9018. against typical enteritis causing Salmonella enteritidis KU101 and IgA level after challenge have been determined. In order to identify the strains of lactobacilli the sequences of 16S-23S rRNA intergenic spacer region were determined. All the test strains of Lactobacillus spp. inhibited Salmonella enteritidis, the intensity varied depending upon the species of lactobacilli. Effects on the survival rate of the mouse after challenge with Salmonella enteritidis KU101 on feeding Lactobacillus spp. have shown the highest survival rate in L. helveticus CU 631 followed by L. casei YIT 9018 and L. johnsonii C-4 and the lowest in control mice. The higher level of total Ig A concentration in the intestinal fluid of lactobacilli fed mice than control mice was observed. The sequences of 16S-23S rRNA intergenic spacer region of seven strains of Lactobacillus casei could be utilized as a strain identification, those sequences showed some degree of difference in homology.

Isolation and Selection of Antagonistic Microbes for Biological Control of Zoysiagrass Large Patch Disease (한국잔디 갈색퍼짐병의 생물학적 방제를 위한 길항미생물의 분리 및 선발)

  • Ma, Ki-Yoon;Kwark, Soo Nyeon;Lee, Geung-Joo
    • Horticultural Science & Technology
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    • v.31 no.6
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    • pp.657-665
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    • 2013
  • A large patch disease caused by Rhizoctonia solani AG2-2 (IV) is a serious problem in Korean lawngrass (Zoysia japonica) sites including golf courses and sports fields in Korea. Antagonistic microorganisms against R. solani AG2-2 (IV) were isolated from various forest and crop soil sources in Southern Korea. Among the 61 isolates, I-009, FRIN-001-1, and YPIN-022 strains showing dramatic inhibition of the mycelial growth of R. solani AG2-2 (IV) in the pairing culture were selected as the most potential antagonistic microorganisms for this study. Based on the 16s RNA sequence comparison, I-009 and FRIN-001-1 isolates were identified as Bacillus spp., while YPIN-022 isolate belongs to the genus Pseudomonas. The greater inhibition (clear) zone between two edges of the selected and pathogenic microbes ranged from 11 to 15 mm in three selections, but the others averaged to 7 mm out of 30 mm distance. In another antifungal test using culture filtrate, those three isolates represented a range of 51.7 to 63.5% suppression potential. The selected isolates also inhibited significantly the stem-segment colonization by R. solani AG2-2 (IV) in vivo test by 28.1%, 43.0%, and 23.7% when inoculated with I-009, FRIN-001-1, and YPIN-022, respectively. The highest antagonistic activity for the large patch disease was demonstrated by the isolate FRIN-001-1, which will be useful for developing a bio-pesticide against Rhizoctonia.

β-lapachone-Induced Apoptosis of Human Gastric Carcinoma AGS Cells Is Caspase-Dependent and Regulated by the PI3K/Akt Pathway

  • Yu, Hai Yang;Kim, Sung Ok;Jin, Cheng-Yun;Kim, Gi-Young;Kim, Wun-Jae;Yoo, Young Hyun;Choi, Yung Hyun
    • Biomolecules & Therapeutics
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    • v.22 no.3
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    • pp.184-192
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    • 2014
  • ${\beta}$-lapachone is a naturally occurring quinone that selectively induces apoptotic cell death in a variety of human cancer cells in vitro and in vivo; however, its mechanism of action needs to be further elaborated. In this study, we investigated the effects of ${\beta}$-lapachone on the induction of apoptosis in human gastric carcinoma AGS cells. ${\beta}$-lapachone significantly inhibited cellular proliferation, and some typical apoptotic characteristics such as chromatin condensation and an increase in the population of sub-G1 hypodiploid cells were observed in ${\beta}$-lapachone-treated AGS cells. Treatment with ${\beta}$-lapachone caused mitochondrial transmembrane potential dissipation, stimulated the mitochondria-mediated intrinsic apoptotic pathway, as indicated by caspase-9 activation, cytochrome c release, Bcl-2 downregulation and Bax upregulation, as well as death receptor-mediated extrinsic apoptotic pathway, as indicated by activation of caspase-8 and truncation of Bid. This process was accompanied by activation of caspase-3 and concomitant with cleavage of poly(ADP-ribose) polymerase. The general caspase inhibitor, z-VAD-fmk, significantly abolished ${\beta}$-lapachone-induced cell death and inhibited growth. Further analysis demonstrated that the induction of apoptosis by ${\beta}$-lapachone was accompanied by inactivation of the phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway. The PI3K inhibitor LY29004 significantly increased ${\beta}$-lapachone-induced apoptosis and growth inhibition. Taken together, these findings indicate that the apoptotic activity of ${\beta}$-lapachone is probably regulated by a caspase-dependent cascade through activation of both intrinsic and extrinsic signaling pathways, and that inhibition of the PI3K/Akt signaling may contribute to ${\beta}$-lapachone-mediated AGS cell growth inhibition and apoptosis induction.

Anti-obesity Activities of Cirsium setidens Nakai Ethanolic Extract (고려엉겅퀴 주정 추출물을 함유하는 임상시험제품의 항비만 활성 평가)

  • Cho, Bong-Yeon;Choi, Sun-Il;Choi, Seung-Hyun;Sim, Wan-Sup;Xionggao, Han;Ra, Moon-Jin;Kim, Sun-Young;Kang, Il-Jun;Han, Kyoung-Chan;Lee, Ok-Hwan
    • Journal of Food Hygiene and Safety
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    • v.33 no.5
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    • pp.389-398
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    • 2018
  • The purpose of this study was to evaluate anti-obesity activity of Cirsium setidens Nakai test material (CNTM) in 3T3-L1 adipocytes and obese C57BL/6J mice fed with a high-fat diet using various obesity-related in vitro experiments. During adipocyte differentiation, CNTM significantly inhibited lipid accumulation and ROS production compared to controls. To evaluate whether CNTM could exert glycerol release effects on mature 3T3-L1 adipocytes, we treated cells with various concentrations of CNTM for 1 h. Treatment of mature adipocytes with $160-320{\mu}g/mL$ of CNTM increased the release of glycerol, but not in a significant dose-dependent manner. Anti-adipogenic and anti-lipogenic effects of CNTM seemed to be mediated by the inhibition of $PPAR{\gamma}$ and $C/EBP{\alpha}$. Moreover, CNTM stimulated fatty acid oxidation in an AMPK-dependent manner. CNTM-treated groups of C57BL/6J mice showed reduced body weights and adipose tissue weight with improving serum lipid profiles and adiponectin protein expression in obese C57BL/6J mice fed with a high-fat diet. These results suggest that CNTM might have anti-obesity effect on adipogenesis and lipid metabolism in vitro and in vivo. This presents the possibility of developing a treatment for obesity using nontoxic natural resources.

Anti-osteoarthritis Effects on Fruit Extract of Litsea japonica (까마귀쪽나무 열매 추출물의 골관절염 억제 효과)

  • Yoon, Weon-Jong;Song, Sang Mok;Ham, Young-Min;Oh, Dae-Ju;Ko, Chang-Sik;Yoon, Sun-A;Lee, Yong-Bum;Park, Dae Won;Jeong, Yong Joon;Kwon, Jung Eun;Cho, Young-Mi;Cho, Ju-Hyun;Kim, Chang-Sook;Kang, Se Chan
    • Korean Journal of Plant Resources
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    • v.28 no.5
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    • pp.591-599
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    • 2015
  • Osteoarthritis (OA) is a degenerative disease characterized by the progressive degradation of joint cartilage and is accompanied by secondary inflammation of synovial membranes. The purpose of this study describes a preliminary evaluation of the anti-inflammatory activity on test material of Litsea japonica. fruit (LJTM) Also, this study was to evaluate the effects of LJTM on the joint cartilage of rat with OA induced by monosodium iodoacetate (MIA). To study for anti-inflammatory agents effectively, we first examined the inhibitory effect of the LJTM on the production of pro-inflammatory factors and cytokines stimulated with lipopolysaccharide. We identified anti-nociceptive effects of the LJTM by using in vivo peripheral and central nervous pain models. In addition, the aim of this study was to evaluate the effects on mRNA expression of MMP-2, -3, -7, -9, -13, TIMP-1 and –2 in cartilage of OA. In the LJTM inhibited production of pro-inflammatory mediators (NO and PGE2) and pro-inflammatory cytokines (TNF-α and IL-6). In cartilage, Expression of MMPs and TIMPs mRNA was suppressed in LJTM treatment group than in the control group. This study suggests that LJTM are potential candidates as anti-inflammation and anti-osteoarthritis agents (painkillers) for the treatment of OA.