• Title/Summary/Keyword: inhibiting activity

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Protective Effect of Curcumin on Dextran Sulfate Sodium-Induced Ulcerative Colitis in Obese Mice (비만마우스에서 Dextran Sulfate Sodium 유도 궤양성 대장염에 대한 커큐민의 보호효과)

  • Park, Ho
    • Korean Journal of Clinical Laboratory Science
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    • v.54 no.1
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    • pp.9-14
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    • 2022
  • Ulcerative colitis is a disease that causes inflammation in the mucosal or submucosal layer of the colon. Previous studies have reported that obesity increases the prevalence of ulcerative colitis and aggravates the progression. This study was therefore undertaken to investigate whether curcumin inhibits the progression of ulcerative colitis caused by obesity. Mice were bred on a high-fat diet to induce obesity, and curcumin was administered with the high-fat diet to confirm the anti-inflammatory effect. To induce ulcerative colitis, dextran sulfate sodium (DSS) was administered orally, and clinical symptoms of colitis were subsequently observed. For histological evaluation of curcumin, the colon, liver and abdominal fat tissue samples were prepared and analyzed by hematoxylin and eosin (H&E) and Alcian blue-periodic acid-Schiff (PAS) staining. Our results confirm that consumption of curcumin resulted in decreasing the score of the disease activity index, and inhibited shortening of the colon length. In addition, inflammatory cell infiltration and mucosal damage were inhibited in the colon tissue of ulcerative colitis exacerbated by obesity. We further confirmed that exposure to curcumin significantly reduced the steatosis area of the liver and adipocytes of abdominal fat. In conclusion, we believe that curcumin can be applied as a therapeutic agent to treat ulcerative colitis, by inhibiting the progression of colitis caused by obesity.

Anti-inflammatory effects of the ethanol fraction of Spiraea prunifolia var. simpliciflora in RAW 264.7 cells (RAW 264.7 세포에서 조팝나무 에탄올 분획물의 항염 활성)

  • Suhr, Jinhyung;Lee, Hansol;Kim, Suhwan;Lee, Sung Jin;Bae, Eun Young;Ly, Sun Yung
    • Journal of Nutrition and Health
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    • v.55 no.1
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    • pp.59-69
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    • 2022
  • Purpose: Natural medicinal plant extracts have recently attracted attention as health beneficial foods and potential therapeutic agents for prevention of various diseases. This study was undertaken to measure the anti-inflammatory effect of the ethanol-water fraction obtained from the above-ground portion of Spiraea prunifolia var. simpliciflora, a wild-growing plant in Korea. The final fraction used in this study was the H2O-EtOH (40:60) fraction (SP60), which had the highest antioxidant activity, as determined in previous studies. Methods: The amounts of nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-6 and IL-1β production were measured in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells exposed to SP60. Western blot was performed to measure the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, and the activation of nuclear factor (NF)-κB. Results: SP60 exerted no cytotoxicity up to concentrations of 125 ㎍/mL. The levels of inflammatory cytokines, such as NO, TNF-α, IL-6, and IL-1β, were significantly decreased in LPS-stimulated RAW264.7 cells exposed to SP60. In addition, the expression levels of iNOS, COX-2, and phosphorylated p65 showed a concentration-dependent decrease subsequent to SP60 treatment. These results indicate that SP60 inhibits the LPS-induced production of inflammatory cytokines, iNOS, and COX-2, by inhibiting the activation of NF-κB, which is responsible for the expression of inflammatory mediators. Conclusion: The results presented in this study indicate that the H2O-EtOH (40:60) fraction (SP60) extracted from the above-ground portion of Spiraea prunifolia var. simpliciflora has the potential to be developed as a medicine or healthcare food and functional material possessing anti-inflammatory effects. However, it is necessary to first confirm the anti-inflammatory effects of SP60 in in vivo models.

Protective Effects of Medicinal Herbal Mixture (HME) through Akt/FoxO3 Signal Regulation in Oxidative Damaged C2C12 Myotubes (C2C12 myotube의 산화적 손상에 대한 혼합 한약재 추출물(HME)의 Akt/FoxO3 신호 조절을 통한 보호 효과)

  • Kim, So Young;Choi, Moon-Yeol;Lee, Un Tak;Choo, Sung Tae;Kim, Mi Ryeo
    • The Korea Journal of Herbology
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    • v.37 no.4
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    • pp.31-38
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    • 2022
  • Objectives : In this study, we investigated the synergistic protective effects of medicinal herbal mixture (HME) including Mori Ramulus (MR), Acanthopanacis Cortex (AC), Eucommiae Cortex (EC), and Black soybean (BS) in C2C12 cells, mouse myoblasts. Methods : Effects of HME on cell viability of C2C12 myoblasts were monitored by MTT assay. Anti-atrophic activity of HME was determined in myoblasts and myotubes under oxidative stress by H2O2. C2C12 myoblasts were differentiated into myotubes in a medium containing 2% horse serum for 6 days. After that, we measured that expression of MyoD and myogenine, the myogenic regulatory factors, to identify the mechanism of inhibiting muscle atophy after HME treatment. In addition, suppression of phosphorylation of Akt, FoxO3a and MARF-1, transcription factors of degradation proteins were analyzed via western blotting. Results : As a result of MTT, HME there was no show cytotoxicity up to a concentration of 1 mg/ml. The cytoprotective effects on oxidative stressed myoblast and myotube was better in HME extract than those of MR, AC, EU, and BS, respectively. HME treatment in Myotube induced by oxidative stress after H2O2 treatment increased Myo D, Myogenine activation, and Akt, FoxO3a phosphorylation and decreased expression of MuRF-1. As the results, HME has synergistic effects on protection against proteolysis of C2C12 myotubes through activation of the Akt signaling pathway under oxidative stress. Conclusions : These results suggest that HME may also be useful as a preventing and treating material for skeletal muscle atrophy caused by age-related diseases.

In Vitro Antibacterial Effects of the Chimeric Peptides from Chicken and Pig Antimicrobial Peptide NK-Lysin (닭과 돼지의 항균펩타이드 NK-Lysin으로부터 조합된 펩타이드의 In Vitro 항균효과)

  • Hong, Yeojin;Lee, Gi Yong;Yang, Soo-Jin;Lillehoj, Hyun Soon;Hong, Yeong Ho
    • Korean Journal of Poultry Science
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    • v.49 no.2
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    • pp.69-77
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    • 2022
  • Antimicrobial peptides (AMPs) play an important role in innate immunity against pathogenic infections. AMPs exterminate pathogenic bacteria by disrupting cell membranes or inhibiting intracellular molecules. NK-2, first identified in pigs and derived from NK-lysin, has antimicrobial effects against bacteria and parasites. In this study, chimeric peptides (cpNK) of chicken and pig NK-2 and cpNK-derived peptides (cpNK-a1 and cpNK-a2) were synthesized, and their antimicrobial effects against various pathogenic bacteria such as Escherichia coli, Salmonella spp., Listeria monocytogenes, Staphylococcus aureus, and methicillin-resistant Staphylococcus aureus (MRSA) were investigated. The structure of chimeric peptides from chicken and pig NK-2, cpNK, include α-helix like NK-2 and peptide net charge was +9 like porcine NK-2. The cpNK peptide showed powerful bactericidal effects against most bacterial species, including MRSA, especially against gram-negative bacteria. Furthermore, cpNK-derived short peptides, cpNK-a1 and a2 also showed bactericidal activity, but the effects were weaker than those of cpNK. Therefore, we conclude that cpNK- and cpNK-derived short peptides have the potential to be used as antibiotic alternatives.

The protective effect of Areca Semen and Toosendan Fructus mixture in a chronic model of reflux esophagitis (빈랑자와 천련자 복합물의 만성 역류성 식도염에서 보호 효과)

  • Shin, Mi-Rae;Lee, Jin A;Kim, Min Ju;An, Hyo-Jin;Roh, Seong-Soo
    • The Korea Journal of Herbology
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    • v.35 no.1
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    • pp.57-68
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    • 2020
  • Objective : The aim of present study was to clarify the effect of Areca Semen and Toosendan Fructus Mixture (AT-mix) on chronic reflux esophagitis (CRE) in rats. Methods : The antioxidant activity of AT-mix was measured through DPPH and ABTS radical scavenging activities in vitro. CRE was induced in SD rats (5 weeks, male) by ligating the border forestomach and granular portion with 2-0 silk and the duodenum near the pyloric portion was covered with 2-mm wide piece of 18-Fr Nélaton catheter. And then rats were treated AT-mix 200 mg/kg one daily for 14 days. The anti-oxidant and inflammatory protein levels were evaluated using western blotting. Results : Gross lesion of esophageal mucosa after AT-mix treatment showed a superior enhancement compared with that of CRE control rats. AT-mix treatment strongly reduced both DPPH and ABTS radical scavenging activities (DPPH, IC50 8.15±0.14 ㎍/mL; ABTS, IC50 24.69±0.03 ㎍/mL, repspectively). Levels of the NADPH oxidase subunit including NOX4 and p22phox increased in CRE control rats. Otherwise, AT-mix treatment significantly reduced. The activation of Nuclear factor-erythroid 2-related factor 2 (Nrf2) led to significantly the up-regulation of HO-1. The inhibition of IκBα phosphorylation led to NF-κB inactivation. Subsequently, NF-κB inactivation significantly induced the decrease of COX-2, iNOS, TNF-α, and IL-6 protein expressions. Conclusion : Taken together, these results suggest that AT-mix treatment can attenuate the esophageal mucosal ulcer though inhibiting NF-κB pathway and enhancing Nrf2/HO-1 pathway. Thus, the additional mechanism study about AT-mix would need for the development as a safe herbal therapy for CRE.

Research Trends on the Therapeutic Potential of Cordycepin, an Active Ingredient of the Insect Fungus Cordyceps spp., for the Prevention of Sarcopenia (동충하초(Cordyceps spp.)의 유효 생리활성 성분인 cordycepin의 근감소증 예방에 대한 연구 동향)

  • Kim, Sung Ok;Choi, Yung Hyun
    • Journal of Life Science
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    • v.32 no.6
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    • pp.482-490
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    • 2022
  • Sarcopenia, a geriatric and multifactorial syndrome characterized by progressive systemic skeletal muscle disorder, may be associated with many comorbidities. Sarcopenia caused by a decrease in muscle mass and muscle strength is accompanied by the aggravation of various pathological conditions, and as life expectancy increases, its prevalence will continue to increase in the future. During the aging process, chronic oxidative stress and increased inflammatory responses act as major contributors to skeletal muscle loss. In addition, disruption of autophagy and apoptosis signals associated with dysfunction of mitochondria, which are essential for energy metabolism, accelerates the loss of muscle proteins. The pharmacological effect of cordycepin, a major physiologically active substance in the genus Cordyceps, which has been widely used for the prevention and treatment of various diseases for a long time, is directly related to its antioxidant and anti-inflammatory actions. In this review, we present the correlation between apoptosis, autophagy, protein catabolism, and satellite cell activity important for muscle regeneration using cordycepin for the prevention and treatment of sarcopenia. Although there have been few studies so far on the use of cordycepin for sarcopenia, previous studies suggest that cordycepin may contribute to inhibiting the age-related weakening of mitochondrial function and blocking the breakdown of muscle proteins. In addition, the protective effect of cordycepin on muscle cell damage is considered to be closely related to its antioxidant and anti-inflammatory activities. Therefore, it is considered that more continuous basic research is needed, focusing on the molecular biological mechanism of cordycepin, which is involved in the anti-aging of muscle cells.

20 (S)-ginsenoside Rh2 inhibits colorectal cancer cell growth by suppressing the Axl signaling pathway in vitro and in vivo

  • Zhang, Haibo;Yi, Jun-Koo;Huang, Hai;Park, Sijun;Kwon, Wookbong;Kim, Eungyung;Jang, Soyoung;Kim, Si-Yong;Choi, Seong-kyoon;Yoon, Duhak;Kim, Sung-Hyun;Liu, Kangdong;Dong, Zigang;Ryoo, Zae Young;Kim, Myoung Ok
    • Journal of Ginseng Research
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    • v.46 no.3
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    • pp.396-407
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    • 2022
  • Background: Colorectal cancer (CRC) has a high morbidity and mortality worldwide. 20 (S)-ginsenoside Rh2 (G-Rh2) is a natural compound extracted from ginseng, which exhibits anticancer effects in many cancer types. In this study, we demonstrated the effect and underlying molecular mechanism of G-Rh2 in CRC cells in vitro and in vivo. Methods: Cell proliferation, migration, invasion, apoptosis, cell cycle, and western blot assays were performed to evaluate the effect of G-Rh2 on CRC cells. In vitro pull-down assay was used to verify the interaction between G-Rh2 and Axl. Transfection and infection experiments were used to explore the function of Axl in CRC cells. CRC xenograft models were used to further investigate the effect of Axl knockdown and G-Rh2 on tumor growth in vivo. Results: G-Rh2 significantly inhibited proliferation, migration, and invasion, and induced apoptosis and G0/G1 phase cell cycle arrest in CRC cell lines. G-Rh2 directly binds to Axl and inhibits the Axl signaling pathway in CRC cells. Knockdown of Axl suppressed the growth, migration and invasion ability of CRC cells in vitro and xenograft tumor growth in vivo, whereas overexpression of Axl promoted the growth, migration, and invasion ability of CRC cells. Moreover, G-Rh2 significantly suppressed CRC xenograft tumor growth by inhibiting Axl signaling with no obvious toxicity to nude mice. Conclusion: Our results indicate that G-Rh2 exerts anticancer activity in vitro and in vivo by suppressing the Axl signaling pathway. G-Rh2 is a promising candidate for CRC prevention and treatment.

Volatile Components of Essential Oils from Spices and It's Inhibitory Effects against Biofilm Formed by Food Poisoning Bacteria (향신료 정유의 휘발성 성분 및 식중독 세균에 의해 형성된 biofilm 억제 효과)

  • Kim, Hyeong-Eun;Kim, Yong-Suk
    • Journal of Food Hygiene and Safety
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    • v.37 no.4
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    • pp.285-295
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    • 2022
  • The ability of volatile components of essential oils (EO) from cinnamon, clove, and lemongrass to inhibit biofilms formed on polyethylene and stainless steel by six types of food poisoning bacteria was investigated. The main components of cinnamon EO were identified as cinnamaldehyde (38.30%), linalool (9.61%), β-caryophyllene (8.90%), and 1,3,4-eugenol (8.19%). 1,3,4-Eugenol (61.84%) was the dominant component of clove EO. The major component of lemongrass EO was citral. Citral is a natural mixture of two isomeric acyclic monoterpene aldehydes: geranial (trans-citral, 19.11%) and neral (cis-citral, 19.23%). Among these major compounds, cinnamaldehyde, linalool, eugenol, and citral exhibited comparatively strong antimicrobial activity in the disc diffusion assay. Treatments with 0.1% eugenol and citral were highly effective on biofilm inhibition on both tested surfaces. Cinnamaldehyde (0.1%) was effective against biofilm formation by Listeria monocytogenes ATCC 19112 and Staphylococcus aureus KCCM 11812. These results suggested the potential of cinnamaldehyde, eugenol, and citral treatments in inhibiting the formation of biofilms by food poisoning bacteria.

Virtual Screening and Testing of GSK-3 Inhibitors Using Human SH-SY5Y Cells Expressing Tau Folding Reporter and Mouse Hippocampal Primary Culture under Tau Cytotoxicity

  • Chih-Hsin Lin;Yu-Shao Hsieh;Ying-Chieh Sun;Wun-Han Huang;Shu-Ling Chen;Zheng-Kui Weng;Te-Hsien Lin;Yih-Ru Wu;Kuo-Hsuan Chang;Hei-Jen Huang;Guan-Chiun Lee;Hsiu Mei Hsieh-Li;Guey-Jen Lee-Chen
    • Biomolecules & Therapeutics
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    • v.31 no.1
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    • pp.127-138
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    • 2023
  • Glycogen synthase kinase-3β (GSK-3β) is an important serine/threonine kinase that implicates in multiple cellular processes and links with the neurodegenerative diseases including Alzheimer's disease (AD). In this study, structure-based virtual screening was performed to search database for compounds targeting GSK-3β from Enamine's screening collection. Of the top-ranked compounds, 7 primary hits underwent a luminescent kinase assay and a cell assay using human neuroblastoma SH-SY5Y cells expressing Tau repeat domain (TauRD) with pro-aggregant mutation ΔK280. In the kinase assay for these 7 compounds, residual GSK-3β activities ranged from 36.1% to 90.0% were detected at the IC50 of SB-216763. In the cell assay, only compounds VB-030 and VB-037 reduced Tau aggregation in SH-SY5Y cells expressing ΔK280 TauRD-DsRed folding reporter. In SH-SY5Y cells expressing ΔK280 TauRD, neither VB-030 nor VB-037 increased expression of GSK-3α Ser21 or GSK-3β Ser9. Among extracellular signal-regulated kinase (ERK), AKT serine/threonine kinase 1 (AKT), mitogen-activated protein kinase 14 (P38) and mitogenactivated protein kinase 8 (JNK) which modulate Tau phosphorylation, VB-037 attenuated active phosphorylation of P38 Thr180/ Tyr182, whereas VB-030 had no effect on the phosphorylation status of ERK, AKT, P38 or JNK. However, both VB-030 and VB-037 reduced endogenous Tau phosphorylation at Ser202, Thr231, Ser396 and Ser404 in neuronally differentiated SH-SY5Y expressing ΔK280 TauRD. In addition, VB-030 and VB-037 further improved neuronal survival and/or neurite length and branch in mouse hippocampal primary culture under Tau cytotoxicity. Overall, through inhibiting GSK-3β kinase activity and/or p-P38 (Thr180/Tyr182), both compounds may serve as promising candidates to reduce Tau aggregation/cytotoxicity for AD treatment.

Ficus vasculosa Wall. ex Miq. Inhibits the LPS-Induced Inflammation in RAW264.7 Macrophages

  • Ji-Won, Park;Jin-Mi, Park;Sangmi, Eum;Jung Hee, Kim;Jae Hoon, Oh;Jinseon, Choi;Tran The, Bach;Nguyen, Van Sinh;Sangho, Choi;Kyung-Seop, Ahn;Jae-Won, Lee
    • Microbiology and Biotechnology Letters
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    • v.50 no.4
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    • pp.574-583
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    • 2022
  • Ficus vasculosa Wall. ex Miq. (FV) has been used as a herbal medicine in Southeast Asia and its antioxidant activity has been shown in previous studies. However, it has not yet been elucidated whether FV exerts anti-inflammatory effects on activated-macrophages. Thus, we aimed to evaluate the ameliorative property of FV methanol extract (FM) on lipopolysaccharide (LPS)-induced inflammatory responses and the underlying molecular mechanisms in RAW264.7 macrophages. The experimental results indicated that FM decreased the production of inflammatory mediators (NO/PGE2) and the mRNA/protein expression of iNOS and COX-2 in LPS-stimulated RAW264.7 cells. FM also reduced the secretion of interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α and monocyte chemoattractant protein (MCP)-1 in LPS-stimulated RAW264.7 cells. Results also demonstrated that FM improved inflammatory response in LPS-stimulated A549 airway epithelial cells by inhibiting the production of cytokines, such as IL-1β, IL-6 and TNF-α. In addition, FM suppressed MAPK activation and NF-κB nuclear translocation induced by LPS. FM also upregulated the mRNA/protein expression levels of heme oxygenase-1 and the nuclear translocation of nuclear factor erythroid 2-related factor 2 in RAW264.7 cells. In an experimental animal model of LPS-induced acute lung injury, the increased levels of molecules in bronchoalveolar lavage (BAL) fluid were suppressed by FM administration. Collectively, it was founded that FM has anti-inflammatory properties on activated-macrophages by suppressing inflammatory molecules and regulating the activation of MAPK/NF-κB signaling.