• Title/Summary/Keyword: Inhibiting activity

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Effect of a Mixture of Centella asiatica and Rosamarinus officinalis Leaf Extracts on Delayed Cortisol-induced Keratinocyte Migration (병풀과 로즈마리 잎 추출 혼합물의 코티솔로 유도된 각질형성세포 이동지연에 미치는 영향)

  • WonTae Jo;Miji Yeom;ShinHwan Cho;Eunae Cho;Deokhoon Park;Eunsun Jung
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.50 no.2
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    • pp.111-118
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    • 2024
  • A key component of wound healing is epithelialization, which involves the proliferation and migration of epidermal keratinocytes surrounding the wound. Increasing cortisol, a stress hormone, is known to slow the healing process by inhibiting cell proliferation and migration. This study aims to develop an ingredient that can promote delayed wound healing by cortisol through a combination of Centella asiatica (C. asiatica), known for its excellent wound healing effect, and Rosamarinus officinalis (R. officinalis) leaf known for their antipsychotic effect. R. officinalis leaf extract was found to inhibit the activity of 11β-HSD1, an enzyme involved in the production of cortisol. A combination of C. asiatica and R. officinalis leaf extracts (AlfaCalm) was found to enhance cortisol induced delayed keratinocyte migration to a greater extent than C. asiatica extract. AlfaCalm enhanced the expression of CDC42 and the formation of filopodia, which are crucial for the relaxation of the actin skeleton. These results suggest that AlfaCalm can be used as an effective wound healing material in stress condition.

Effect of Adefovir Dipivoxil on the Inhibition of Osteogenic Differentiation of Mesenchymal Stem Cells and Osteoblasts (아데포비어가 중간엽 줄기세포와 조골세포의 골형성 분화 억제에 미치는 영향)

  • Ho PARK
    • Korean Journal of Clinical Laboratory Science
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    • v.55 no.4
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    • pp.284-290
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    • 2023
  • Adefovir dipivoxil (ADV) is used for the treatment of hepatitis and acquired immunodeficiency syndrome, but long-term use can cause osteoporosis. In this study, the effect of ADV on the osteocyte maturation process was evaluated at the level of undifferentiated cells using mesenchymal stem cells (MSCs) and osteoblasts (MG63). First, MSCs and MG63 cells were treated with ADV at different concentrations, and then a Cell Counting Kit-8 analysis was performed to determine the effect on the proliferation of each cell. Additionally, crystal violet and Hoechst staining were performed for the morphological analysis of each cell and nucleus. To determine the cause of cell hypertrophy, the transforming growth factor-beta (TGF-β) expression was investigated, and alkaline phosphatase (ALP) staining and activity were measured to determine the degree of differentiation of the MSCs and MG63 cells into mature osteocytes. The results confirmed that the ADV increases the expression of TGF-β in MSCs and MG63 cells, causing cellular and nuclear hypertrophy, and can cause osteoporosis by inhibiting cell proliferation and affecting the differentiation of mature osteocytes. Therefore, it is believed that these results can be used as a basis for understanding the adverse effects of ADV at a cytological level in basic medicine and clinical research.

Integration of virtual screening and proteomics reveals potential targets and pathways for ginsenoside Rg1 against myocardial ischemia

  • Rongfang Xie;Chenlu Li;Chenhui Zhong;Zuan Lin;Shaoguang Li;Bing Chen;Youjia Wu;Fen Hu;Peiying Shi;Hong Yao
    • Journal of Ginseng Research
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    • v.48 no.4
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    • pp.395-404
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    • 2024
  • Background: Ginsenoside Rg1 (Rg1) is one of the main active components in Chinese medicines, Panax ginseng and Panax notoginseng. Research has shown that Rg1 has a protective effect on the cardiovascular system, including anti-myocardial ischemia-reperfusion injury, anti-apoptosis, and promotion of myocardial angiogenesis, suggesting it a potential cardiovascular agent. However, the protective mechanism involved is still not fully understood. Methods: Based on network pharmacology, ligand-based protein docking, proteomics, Western blot, protein recombination and spectroscopic analysis (UV-Vis and fluorescence spectra) techniques, potential targets and pathways for Rg1 against myocardial ischemia (MI) were screened and explored. Results: An important target set containing 19 proteins was constructed. Two target proteins with more favorable binding activity for Rg1 against MI were further identified by molecular docking, including mitogen-activated protein kinase 1 (MAPK1) and adenosine kinase (ADK). Meanwhile, Rg1 intervention on H9c2 cells injured by H2O2 showed an inhibitory oxidative phosphorylation (OXPHOS) pathway. The inhibition of Rg1 on MAPK1 and OXPHOS pathway was confirmed by Western blot assay. By protein recombination and spectroscopic analysis, the binding reaction between ADK and Rg1 was also evaluated. Conclusion: Rg1 can effectively alleviate cardiomyocytes oxidative stress injury via targeting MAPK1 and ADK, and inhibiting oxidative phosphorylation (OXPHOS) pathway. The present study provides scientific basis for the clinical application of the natural active ingredient, Rg1, and also gives rise to a methodological reference to the searching of action targets and pathways of other natural active ingredients.

Effects of Chamaeneron angustifolia Extract on Lipid Metabolism and Differentiation of 3T3-L1 Preadipocyte (Chamaeneron angustifolia 추출물이 3T3-L1 Preadipocyte의 지방대사 및 분화에 미치는 영향)

  • Seul Bi Lee;Moon-Yeol Choi;Mi Hyung Kim;So-Young Kim;Mi Ryeo Kim
    • The Korea Journal of Herbology
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    • v.39 no.4
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    • pp.29-35
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    • 2024
  • Objectives : Obesity is an imbalance between energy intake and consumption due to overeating and lack of exercise, and if it persists, it increases non-infectious diseases such as high blood pressure, diabetes, and hyperlipidemia. In this study, we tried to investigate the possibility of using Chamaeneron angustifolia (CA) as a material for anti-obesity by confirming the effect of inhibiting lipid differentiation. Methods : We measured the effects of CA extract on oil-red-o staining, cell cytotoxicity evaluation activity using 3T3-L1 cells. Additionally, we assessed fat decomposition and metabolism-related protein expression through Western blot analysis. Results : In this study, the anti-obesity effects of CA extract were experimentally assessed. Results showed significant inhibition of adipocyte differentiation and accumulation at concentrations of 0.05, 0.1, and 0.2 mg/ml of oil-red-o staining, with reductions of 80% or more. CA notably increased the phosphorylation of AMPK protein expression compared to the control group across all concentrations. Additionally, phosphorylation of ACC significantly increased at a concentration of 0.2 mg/ml compared to the control. PPAR-γ, which regulates adipogenesis, exhibited a significant decrease compared to the control, while protein expression of CPT-1, involved in fatty acid oxidation, showed a concentration-dependent increase across all groups. Therefore, CA extract demonstrates potential as a functional material for anti-obesity by increasing the expression of proteins related to fat decomposition and synthesis while decreasing others. Conclusions : These results suggest that CA may also be useful as an anti-obesity functional substance.

Cell proliferation inhibition effects of epigallocatechin-3-gallate in TREK2-channel overexpressing cell line (TREK2-채널 과발현 세포주에서 에피갈로카테킨-3-갈레이트의 세포 증식 억제 효과)

  • Kim, Yangmi;Kim, Kyung-Ah
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.17 no.3
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    • pp.127-135
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    • 2016
  • Two-pore domain potassium (K2P) channels are the targets of physiological stimuli, such as intracellular pH, bioactive lipids, and neurotransmitters, and they set the resting membrane potential. Some types of K2P channels play a critical role in both apoptosis and tumoriogenesis. Among the K2P channels, no antagonists of the TREK2 channel have been reported. The aim of the present study was to determine if the TREK2 channel is blocked and whether cell proliferation is influenced by flavonoids in the TREK2 overexpressing HEK293 cells (HEKT2). The electrophysiological current was recorded using single channel patch clamp techniques and cell proliferation was measured using a XTT assay. The electrophysiological results showed that the TREK2 channel activity was reduced to $91.5{\pm}13.1%$ (n=5) and $82.2{\pm}13.7%$ (n=5) by flavonoids, such as epigallocatechin-3-gallate (EGCG) and quercetin in HEKT2 cells, respectively. In contrast, the EGCG analogue, epicatechin (EC), had no significant inhibitory effects on the TREK2 single channel activity. In addition, cell proliferation was reduced to $69.4{\pm}14.0%$ (n=4) by ECGG in the HEKT2 cells. From these results, EGCG and quercetin represent the first known TREK2 channel inhibitors and only EGCG reduced HEKT2 cell proliferation. This suggests that the flavonoids may work primarily by inhibiting the TREK2 channel, leading to a change in the resting membrane potential, and triggering the initiation of a change in intracellular signaling for cell proliferation. TREK2 channel may, at least in part, contribute to cell proliferation.

Antimicrobial Activity of Medicinal Herbs against Salmonella gallinarum and Staphylococcus epidermidis (Salmonella gallinarum와 Staphylococcus epidermidis 균주에 대한 한약재의 항균 활성)

  • Choi, I.;Chang, H.S.
    • Korean Journal of Poultry Science
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    • v.36 no.3
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    • pp.231-238
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    • 2009
  • The present study was conducted to investigate the antimicrobial activities of extracts from approximately 40 different traditional Korean medicinal herbs against S. gallinarum and S. epidermidis. The extracts from Schizandra chinensis Baill., Melia azedarach Linn$\acute{e}$, Caesalpinia sappan Linn$\acute{e}$. and Rhus javanica Linn$\acute{e}$. exhibited high antimicrobial activities against S. gallinarum, whereas the extracts from Melia azedarach Linn$\acute{e}$ and Rhus javanica Linn$\acute{e}$. exhibited high antimicrobial growth for S. epidermidis. Minimum inhibitory concentrations (MIC) of Melia azedarach Linn$\acute{e}$, Caesalpinia sappan Linn$\acute{e}$. and Rhus javanica Linn$\acute{e}$. for S. gallinarum were 1.2 mg/mL, whereas MIC of exracts from Rhus javanica Linn$\acute{e}$. extract for S. epidermidis were 0.6 mg/mL. Heat treatment of the extracts from Schizandra chinensis Baill. and Rhus javanica Linn$\acute{e}$. caused a significant reduction in antimicrobial activities against S. gallinarum. but didn't affect antimicrobial activities against S. edidermidis. Alkaline treatment of the extracts from Schizandra chinensis Baill. caused a significant reduction in antimicrobial activities against S. gallinarum, while similar treatment of the extracts from Rhus javanica Linn$\acute{e}$. caused a significant increase in antimicrobial activities against S. edidermidis. Since extracts from Rhus javanica Linn$\acute{e}$. and Caesalpinia sappan Linn$\acute{e}$. exhibited the highest antimicrobial activities, these extracts at the concentrations of 100, 300 or 500 ppm were added and then bacterial growth-inhibiting activities for S. gallinarum and S. epidermidis by these two extracts were further examined. Optical density at 620 nm ($OD_{620}$) after 24 hours incubation in the absence of Rhus javanica Linn$\acute{e}$. extract ranged from 0.30 to 0.45 compared with $OD_{620}$ value ranging from 0.06 to 0.18 in the presence of 100, 300 or 500 ppm of the extract, indicating that growth of all bacteria was significantly inhibited within 24 hours by the addition of at least 100 ppm of Rhus javanica Linn$\acute{e}$ extract. Value of $OD_{620}$ after 24 hours incubation in the absence of Caesalpinia sappan Linn$\acute{e}$. extract ranged from 0.30 to 0.55 compared with $OD_{620}$ value ranging from 0.05 to 0.15 in the presence of 300 or 500 ppm of the extract, indicating that growth of all bacteria was also significantly inhibited within 24 hours by the addition of at least 300 ppm of Caesalpinia sappan Linn$\acute{e}$. extract. In conclusion, these findings suggest that extracts from Rhus javanica Linn$\acute{e}$. and Caesalpinia sappan Linn$\acute{e}$. may play important roles in antimicrobial activities against S. gallinarum and S. epidermidis.

The effect of antagonists produced by Paenibacillus polymyxa CK-1 on the growth of Trichoderma sp. (Paenibacillus polymyxa CK-1이 생산한 길항물질이 Trichoderma sp. 생육에 미치는 영향)

  • Lee, Sang-Won;Choi, Jin-Sang;Kim, Chul-Ho
    • Journal of Mushroom
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    • v.12 no.3
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    • pp.201-208
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    • 2014
  • The separation of the bacteria inhibiting Trichoderma sp. mold, the strain causing blue mold disease that occurs frequently when cultivating mushroom while carrying out the efficient fermentation of mushroom medium, from the growth was done. In about 200 strains isolated primarily from fungus garden samples, 6 strains were secondly isolated, which had fast growth rates and a clear zone on the plate medium of SM, AM, and CM. Among the 6 strains isolated, the C-1 strain showed high enzymatic activity of cellulase, amylase, and protease, and strong antibacterial activity for the T. virens and T. harzianum, selected finally. The selected C-1 strain was identified as Paenibacillus polymyxaby the result of the identification by Bergey's Manual of Systematic Bacteriology and the analysis of the nucleotide sequence of 16S rRNA, and named as P. polymyxa CK-1. In reviewing the growth conditions of the P. polymyxa CK-1 strain, the optimum cultivation temperature was $45^{\circ}C$, and the optimum pH for growth was in the range of 6.0~7.0. Appropriate incubation time of P. polymyxa CK-1 for the growth inhibition of the fungus T. virens and T. harzianum was 22 to 36 hours. And the fungal growth was not observed, even when leaving two molds inoculated on each petri dishes, which were treated with 24 hour culture solution of P. polymyxa CK-1 strain for 10 days. As a result of studying the thermal stability of the antagonists produced by the P. polymyxa CK-1 strain, no mycelial growth of the two fungi was observed in the test group treated for 20 minutes at $60^{\circ}C$ and $100^{\circ}C$, but mycelial growth was slightly observed in the test group treated for 20 minutes at $121^{\circ}C$. As aresult of reviewing the impact of the P. polymyxa CK-1 culture medium on mushroom mycelial growth, it showed no effect on a variety of mushroom mycelial growth including enoki mushroom and shiitake mushroom.

Cholinesterase Activities in Blood and Nervous Tissues of Rats following Intraperitoneal Repetitive Injection of Parathion (Parathion의 복강내 반복투여로 인한 Rat의 혈액 및 신경조직내 Cholinesterase 활성변화)

  • Do, Jae Cheul;Mo, Ki Chul;Kim, Young Hong;Huh, Rhin Sou
    • Current Research on Agriculture and Life Sciences
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    • v.6
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    • pp.171-180
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    • 1988
  • Parathion is widely used in agriculture, but it is highly toxic and now clear that parathion behaves like a cholinergic drug by inhibiting the enzyme cholinesterase. In order to know the effect of toxicity and cholinesterase activity in rats injected repeatedly with parathion, cholinesterase activity in plasma, whole brain and spinal cord, and the subacute toxicity after repetitive intraperitoneal injection of parathion 20 times every 3 days were investigated. The results obtained were summerized as follows ; $LD_{50}$ value of parathion given intraperitoneally to rats was 10.5mg/kg(95% confidence limits, 6.6-16.8mg/kg). In subacute toxicity test of parathion injected intraperitoneally, mortality of parathion-pretreated rats(B : 57%, C : 83%) were increased in comparison with the control(50%). Cholinesterase activities in plasma of parathion-pretreated rats(B : 0.47 U/ml, C : 0.36 U/ml, AA : 0.31 U/ml, B : 0.26 U/ml, CC : 0.17 U/ml) were significantly decreased in comparison with the control(0.58 U/ml). Cholinesterase activities in spinal cord of parathion-pretreated rats(B : 1.87 U/g, C : 1.29 U/g, AA : 1.27 U/g, BB : 0.71 U/g, CC : 0.25 U/g) were decreased in comparison with the control(2.48 U/g). Cholinesterase activities in whole brain of parathion-pretreated rats(B : 2.52 U/g, C : 1.32 U/g, AA : 2.48 U/g, BB : 1.08 U/g, CC : 0.51 U/g) were significantly inhibited in comparison with the control(4.67 U/g). However, there were no differences in the urea nitrogen and creatinine concentrations between parathion-pretreated rats and control.

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Antioxidant Activities of Dianthus chinensis L. Extract and Its Inhibitory Activities against Nitric Oxide Production and Cancer Cell Growth and Adhesion (패랭이꽃 추출물의 항산화, Nitric Oxide 생성저해, 암세포 성장 및 부착 억제 활성)

  • Lee, Jungjae;Seo, Younggeo;Lee, Junho;Ju, Jihyeung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.1
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    • pp.44-51
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    • 2016
  • The aim of the study was to investigate the antioxidant content and activities of ethanol extract of the edible flower Dianthus chinensis L. (DCE) as well as its inhibitory activities against nitric oxide (NO) production in macrophages and growth and adhesion of human cancer cells. The total polyphenol, flavonoid, and carotenoid levels of DCE were 19.0 mg gallic acid equivalent/g, 65.7 mg quercetin equivalent/g, and $95.0{\mu}g/g$, respectively. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and ferric reducing antioxidant power of DCE at a concentration of $1,000{\mu}g/mL$ were 44% and 51%, respectively. In lipopolysaccharide-treated RAW 264.7 macrophages, treatment with DCE at concentrations of 500 and $1,000{\mu}g/mL$ resulted in significantly reduced NO levels (to 7~23% of the control). In H1299 human lung carcinoma cells and HCT116 human colorectal carcinoma cells, treatment with DCE at concentrations of 250, 500, and $1,000{\mu}g/mL$ resulted in dose-dependent growth inhibition. DCE was also effective in inhibiting adhesion of both H1299 cells (to 55% of the control at concentration of $1,000{\mu}g/mL$) and HCT116 (to 26~40% of the control at concentrations of 250, 500, and $1,000{\mu}g/mL$). These results suggest that DCE exerts antioxidant, anti-inflammatory, and anti-cancer activities in vitro.

Anti-inflammatory Activity of Extracts of Hovenia dulcis on Lipopolysaccharides-stimulated RAW264.7 Cells (LPS로 유도된 RAW264.7 대식세포에 대한 헛개나무(Hovenia dulcis) 추출물의 항염증 효과)

  • Woo, Hyun Sim;Lee, Sun Min;Heo, Jeong Doo;Lee, Min-Sung;Kim, Yeong-Su;Kim, Dae Wook
    • Korean Journal of Plant Resources
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    • v.31 no.5
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    • pp.466-477
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    • 2018
  • In this study, the anti-inflammatory activities of the extracts of different parts of Hovenia dulcis such as leaves, stems, and roots were investigated. Among them, the roots extract (RE) showed the most potent suppressive effect against pro-inflammatory mediators in LPS-stimulated mouse macrophage cells. RE induced dose-dependent reduction of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and concomitantly reduced the production of NO and $PGE_2$. Additionally, pre-treatment with RE significantly suppressed the production of inflammatory cytokines, such as tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$), interleukin $(IL)-1{\beta}$, and IL-6, as well as mRNA levels. Moreover, phosphorylation of mitogen-activated protein kinases (MAPKs) and nuclear translocation of nuclear factor-kappa B (NF-kB) were also strongly attenuated by RE in RAW264.7 cell. Furthermore, RE induced HO-1 expression through nuclear translocation of nuclear factor E2-related factor 2 (Nrf2) and increase HO-1 activity in RAW264.7 macrophages. Therefore, these results indicate that RE strongly inhibits LPS-induced inflammatory responses by blocking NF-kB activation, inhibiting MAPKs phosphorylation, and enhancing HO-1 expression in macrophages, suggesting that RE of H. dulicis and a major component, 27-O-protocatechuoylbetulinic acid could be applied as a valuable natural anti-inflammatory material.