scholarly journals Extract From Tetrastigma hemsleyanum Leaf Alleviates Pseudomonas aeruginosa Lung Infection: Network Pharmacology Analysis and Experimental Evidence

2021 ◽  
Vol 12 ◽  
Author(s):  
Tian-ling Lou ◽  
Tao Ji ◽  
Xin Peng ◽  
Wei-wei Ji ◽  
Li-xia Yuan ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Animal Experiments ◽  
Reduction Process ◽  
Network Pharmacology ◽  
Dependent Manner ◽  
Active Components ◽  
High Concentration ◽  
Tetrastigma Hemsleyanum ◽  
Anti Inflammatory ◽  
Functional Components

Tetrastigma hemsleyanum Diels & Gilg (T. hemsleyanum) has attracted much attention due to its ability on pneumonia, bronchitis, and immune-related diseases, while its functional components and underlying mechanism of action on pneumonia have not been fully elucidated. Herein, we used a systematic network pharmacology approach to explore the action mechanism of T. hemsleyanum leaf in the treatment of pneumonia. In this study, the results of network pharmacology demonstrated that there were 34 active components and 80 drug–disease targets in T. hemsleyanum leaf, which were strongly in connection with signal transduction, inflammatory response, and the oxidation–reduction process. Subsequently, a mouse model of pneumonia induced by Pseudomonas aeruginosa (P. aeruginosa) was established to validate the predicted results of network pharmacology. In the animal experiments, aqueous extract of T. hemsleyanum leaf (EFT) significantly attenuated the histopathological changes of lung tissue in P. aeruginosa–induced mice and reduced the number of bacterial colonies in BALFs by 96.84% (p < 0.01). Moreover, EFT treatment suppressed the increase of pro-inflammatory cytokines IL-17, IL-6, and TNF-α in lung tissues triggered by P. aeruginosa, which led to the increase of Th17 cells (p < 0.05). High concentration of EFT treatment (2.0 g/kg) obviously increased the anti-inflammatory cytokine levels, accompanied by the enhancement of Treg proportion in a dose-dependent manner and a notable reversal of transcription factor RORγt expression. These findings demonstrated that network pharmacology was a useful tool for TCM research, and the anti-inflammatory effect of EFT was achieved by maintaining Th17/Treg immune homeostasis and thereby suppressing the inflammatory immune response.

scholarly journals Study on the Sleep-Improvement Effects of Hemerocallis citrina Baroni in Drosophila melanogaster and Targeted Screening to Identify Its Active Components and Mechanism

Foods ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 883
Author(s):  
Yuxuan Liang ◽  
Riming Huang ◽  
Yongchun Chen ◽  
Jing Zhong ◽  
Jie Deng ◽  
...  
Keyword(s):  
Drosophila Melanogaster ◽  
High Resolution Mass Spectrometry ◽  
Sleep Time ◽  
Network Pharmacology ◽  
Dependent Manner ◽  
Bioactive Components ◽  
Active Components ◽  
Edible Plant ◽  
Hemerocallis Citrina ◽  
Ultrahigh Performance Liquid Chromatography

Hemerocallis citrina Baroni (HC) is an edible plant in Asia, and it has been traditionally used for sleep-improvement. However, the bioactive components and mechanism of HC in sleep-improvement are still unclear. In this study, the sleep-improvement effect of HC hydroalcoholic extract was investigated based on a caffeine-induced insomnia model in Drosophila melanogaster (D. melanogaster), and the ultrahigh-performance liquid chromatography coupled with electrospray ionization quadrupole Orbitrap high-resolution mass spectrometry (UHPLC-ESI-Orbitrap-MS) and network pharmacology strategy were further combined to screen systematically the active constituents and mechanism of HC in sleep-improvement. The results suggested HC effectively regulated the number of nighttime activities and total sleep time of D. melanogaster in a dose-dependent manner and positively regulated the sleep bouts and sleep duration of D. melanogaster. The target screening suggested that quercetin, luteolin, kaempferol, caffeic acid, and nicotinic acid were the main bioactive components of HC in sleep-improvements. Moreover, the core targets (Akt1, Cat, Ple, and Sod) affected by HC were verified by the expression of the mRNA of D. melanogaster. In summary, this study showed that HC could effectively regulate the sleep of D. melanogaster and further clarifies the multi-component and multi-target features of HC in sleep-improvement, which provides a new insight for the research and utilization of HC.

scholarly journals Anti-Inflammatory Activity of the Active Compounds of Sanguisorbae Radix In Macrophages and in Vivo Toxicity Evaluation in Zebrafish

Cosmetics ◽  
2019 ◽  
Vol 6 (4) ◽  
pp. 68
Author(s):  
Young-Ah Jang ◽  
Yong Hur ◽  
Jin-Tae Lee
Keyword(s):  
Target Genes ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Active Components ◽  
Necrosis Factor Alpha ◽  
In Vivo Toxicity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Sanguisorbae Radix

Sanguisorbae Radix (SR) is the root of the Sanguisorba officinalis L., a plant native to Asian countries and used in traditional medicine. We isolated the active components of SR and investigated their anti-inflammatory potential. Quercetin (QC), (+)-catechin (CC), and gallic acid (GA) were isolated from acetone extracts of SR. To elucidate the molecular mechanism by which these compounds suppress inflammation, we analyzed the transcriptional up-regulation of inflammatory mediators, such as nuclear factor-kappa B (NF-κB) and its target genes, inducible NOS (iNOS), and cyclooxygenase (COX)-2, in lipopolysaccharide (LPS)-stimulated macrophage RAW264.7 cells. Notably, QC, CC, and GA were found to inhibit the production of nitric oxide, tumor necrosis factor-alpha, and prostaglandin in a dose-dependent manner. Western blot results indicate that the compounds decreased the expression of iNOS and COX-2 proteins. Furthermore, the compounds decreased phosphorylation of IKK, IκB, ERK, p-38, and JNK proteins in LPS-induced cells. The results support the notion that QC, CC, and GA can potently inhibit the inflammatory response, with QC showing the highest anti-inflammatory activity. In in vivo toxicity studies in zebrafish (Danio rerio), QC showed no toxicity up to 25 μg/mL. Therefore, QC has non-toxic potential as a skin anti-inflammatory biomaterial.

The Pharmacological and Pathological Studies on Taiwan Folk Medicine (VII): The Anti-inflammatory Effect of Echinops grjiisii

1992 ◽  
Vol 20 (02) ◽  
pp. 127-134 ◽  
Author(s):  
Chun-Ching Lin ◽  
Cheng-hung Lin ◽  
Hui-Fen Chiu ◽  
Min-Fu Hu
Keyword(s):  
Methanolic Extract ◽  
Folk Medicine ◽  
Animal Experiments ◽  
Active Principle ◽  
Chloroform Fraction ◽  
Protective Effects ◽  
Active Components ◽  
Crude Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The hepatotoxic-protective effects of "San-fang-feng" (the root of E. grijisii) and "Lou-lu" (the root of E. latifolius) on CCl 4 induced hepatotoxicity have been proposed in our previous paper (Lin et al, 1990). The anti-inflammatory effects of these two crude drugs were investigated in this experiment. The results indicated that both of them displayed pronounced anti-inflammatory activities against carrageenan-induced edema. Furthermore, in order to isolated the main active components of E. grijisii, fractions obtained from the methanolic extract of E. grijisii were investigated in mice for their 24-h LD 50 and 95% confidence limits, which could be used as a guiding for further animal experiments. Our findings demonstrated that n-hexane (100,300 mg/kg), chloroform (30,100,300 mg/kg) and ethyl acetate (30,100, 300 mg/kg) fractions could markedly inhibit the carrageenan-induced inflammation, and the main active principle was found to be concentrated in the chloroform fraction, which possessed significant inhibitory activities even more than does indomethacin.

scholarly journals Mechanism Underlying the Anxiolytic Effect of Cinnamomum Camphora Chvar. Borneol Essential Oil Revealed by Network Pharmacology

2021 ◽  
Author(s):  
Shanshan Xiao ◽  
Hang Yu ◽  
Yunfei Xie ◽  
Yahui Guo ◽  
Jiajia Fan ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anxiety Disorder ◽  
Central Area ◽  
Anxiolytic Effect ◽  
Network Pharmacology ◽  
Dependent Manner ◽  
Ppi Network ◽  
Active Components ◽  
Network Analyses ◽  
Dose Dependent

Abstract Background: Anxiety disorder, the most common mental health issue, can cause palpitations, fear, and compulsive behavior, and can severely endanger human health. Most drugs to treat anxiety disorder can cause a variety of side effects, therefore, it is important to seek natural and safe complementary and alternative therapies.Methods: The open field (OF), elevated plus maze (EPM), and light-dark box (LDB) tests were used to confirm the anxiolytic effect of BEO in mice. Further, we constructed a component-target-signaling pathway network and a protein-protein interaction (PPI) network for the regulation of anxiety by BEO through pharmacological network analyses, and performed Gene Ontology (GO) enrichment analyses of BEO targets, and analyzed the active components and targets of BEO through molecular docking.Results: In the OF test, BEO significantly prolonged the time spent by the mice in the central area (p < 0.05), in a dose dependent manner (r = 0.9992), and also significantly increased the number of central area entries (p < 0.01). In the EPM test, BEO significantly increased the time spent in the open arms (p < 0.01) and the number of entries into the open arms (p < 0.01) in a dose-dependent manner (r = 0.9733, r = 0.9669). In the LDB tests, BEO significantly increased the light area duration (p < 0.05) and the transition number (p < 0.01) in a dose-dependent manner (r = 0.9166, r = 0.9572), thus confirming its anxiolytic effect. Network pharmacology results showed that 33 active components in BEO acted on 54 targets, mainly through modulation of neuroactive ligand-receptor interactions, G-protein coupled receptor signaling pathways, and RNA polymerase II transcription factor activity. PPI network analysis identified 48 key proteins, including estrogen receptor 1 (ESR1), androgen receptor (AR), and mitogen-activated protein kinase 8 (MAPK8). Molecular docking results showed that the main active components of BEO are borneol, β-caryophyllene, α-cadinol, limonene, and α- selinene, which act on the key targets CNR2, ADRA2B, and ADORA2A.Conclusion: Our results indicated that BEO has multi-component, multi-target, and multi-pathway characteristics, thus providing a theoretical basis for further research on the mechanism of action of BEO as a potential anxiolytic agent.

scholarly journals Ruanjian Sanjie Decoction Induces Apoptosis in Triple-negative Breast Cancer Cells by Downregulating cIAP1/2 and XIAP

2020 ◽  
Author(s):  
Xiumei Zhao ◽  
Tongxing Wang ◽  
Qiang Jia ◽  
Luyao Wang ◽  
Cheng Tan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Lines ◽  
Network Pharmacology ◽  
Therapeutic Effects ◽  
Dependent Manner ◽  
Active Components ◽  
The Core

Abstract Background: Traditional Chinese medicine (TCM) comprises a unique theoretical system developed over thousands of years. The previous study reported that Ruanjian Sanjie (RJSJ) exerts anti-tumor effects by inducing cell apoptosis. However, the mechanism is not clear. Methods: In this study, we investigated the possible mechanism by the strategy of combining network pharmacology analysis with experiment (in vitro and in vivo). First, four kinds of breast cancer cell lines were used to conduct proliferation, apoptosis and cell cycle analysis. Secondly, to study pathophysiological processes of breast cancer at the molecular network level, we for the first time constructed an “integrated apoptosis module network of breast cancer” by assembling the regulatory relationships of canonical apoptosis signaling pathways. Through the strategy of combining network analysis and experiments, we analyzed the main mechanism of RJSJ in breast cancer and screened out the core genes. We further studied the inhibitory effect of RJSJ combined with carboplatin (CBP) in vivo. Finally, the synergistic effect of RJSJ and CBP were analyzed and the potential active components in RJSJ were predicted.Results: This study demonstrated that RJSJ could significantly inhibit breast cancer cell proliferation and induce apoptosis in a concentration-dependent manner. The primary mechanism of RJSJ in the treatment of breast cancer was pro-apoptotic. The core apoptosis genes regulated by RJSJ were cIAP1/2 and XIAP. We also found that RJSJ in combination with CBP tended to synergistically induce apoptosis, which might mainly be achieved through the regulation of multiple targets and pathways. Alexandrin (BX05, XKC02, SCG01), baicalin (BX22), guanosine (BX32), arjunglucoside I (XKC10) etc. were predicted as potential active components.Conclusions: These findings provide the rationale for exploring the therapeutic effects of RJSJ against breast cancer and providing a bridge for the combined use of Chinese and Western medicine.

scholarly journals The Acne-treatment Potential of Cinnamomum Camphora Chvar. Borneol Essential Oil in Vitro and in Vivo

2021 ◽  
Author(s):  
Shanshan Xiao ◽  
Hang Yu ◽  
Yunfei Xie ◽  
Yahui Guo ◽  
Jiajia Fan ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Inflammatory Mediators ◽  
Staphylococcus Epidermidis ◽  
Network Pharmacology ◽  
Dependent Manner ◽  
Tnf Α ◽  
Rabbit Ear ◽  
Inflammatory Skin ◽  
Anti Inflammatory

Abstract Background: Acne is one of the most common chronic inflammatory skin diseases, abnormal proliferation of keratinocytes can block the hair follicle sebaceous glands result in the formation of acne. Most drugs to treat acne can cause a variety of side effects, therefore, it is important to seek natural and safe complementary and alternative therapies.Methods: The inhibitory effects of BEO were determined on the proliferation of human keratinocyte (HaCaT) cells induced by heat-inactivated Staphylococcus epidermidis and release of the inflammatory mediators. Further, a component-target-signal pathway for BEO’s effects on acne was constructed through network pharmacology and the mechanism of BEO action was studied in vivo through the rabbit ear acne model.Results: BEO inhibited both cell proliferation, induced by heat-inactivated Staphylococcus epidermidis (p < 0.0001), and release of the inflammatory mediators TNF-α (p < 0.0001) and IL-1β (p < 0.05) in a dose-dependent manner (r = -0.9952, -0.9492), in a HaCaT cell-model of acne. A network pharmacology analysis of the chemical components of BEO characterized these effects as multi-component, multi-target and multi-pathway. All targets were mainly associated with metabolic pathways, the toll-like receptor signaling pathway and the NF-κB signaling pathway. BEO also reduced the severity of acne lesions, induced by intracutaneous injection of S. epidermidis in a rabbit ear acne model. The expression of inflammatory mediators and key signaling pathway components, including TLR2, AKT, P13K, NF-κB, TNF-α, IL-1β in rabbit ear, and TNF-α and IL-1 β in serum, were down-regulated (p < 0.05), indicating that BEO acts by inhibiting the pro-inflammatory TLR2/PI3K-AKT/NF-κB signaling pathway.Conclusion: The current results showed that BEO has clear potential for development into a natural and safe anti-inflammatory skin preparation, which is an effective alternative to conventional treatments containing antibiotics and synthetic anti-inflammatory agents.

scholarly journals Polyphenols from Salix tetrasperma Impair Virulence and Inhibit Quorum Sensing of Pseudomonas aeruginosa

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1341 ◽  
Author(s):  
Islam Mostafa ◽  
Hisham A. Abbas ◽  
Mohamed L. Ashour ◽  
Abdelaziz Yasri ◽  
Assem M. El-Shazly ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Quorum Sensing ◽  
Secondary Metabolites ◽  
Bacterial Resistance ◽  
Stem Bark ◽  
Dependent Manner ◽  
Active Components ◽  
Quorum Sensing Inhibitors ◽  
Bacterial Quorum Sensing ◽  
Bacterial Quorum

Bacterial resistance represents one of the emerging obstacles in plants, animals, and humans that impairs treatment with antibacterial agents. Targeting of the bacterial quorum sensing system is one of the strategies to overcome this problem. Recently, research has been focused on natural and food components which can function as quorum sensing inhibitors. In this study, a methanol extract from Salix tetrasperma stem bark was phytochemically profiled by LC-MS analysis. This resulted in the identification of 38 secondary metabolites with (epi)catechin-(epi)catechin, epicatechin, tremulacin, salicortin, and trichocarposide as the major constituents. The extracts of both stem bark and the previously profiled flower of S. tetrasperma were tested for anti-quorum sensing activity in a common and widely distributed pathogen Pseudomonas aeruginosa. The natural products inhibited swimming and swarming motilities, as well as proteolytic and hemolytic activities in a dose-dependent manner. Molecular docking of the constituents from both extracts against the quorum sensing controlling systems Lasl/LasR, rhll/rhlR, and PQS/MvfR showed that epicatechin, (epi)catechin-(epi)catechin, p-hydroxy benzoyl galloyl glucose, p-hydroxy benzoyl protocatechuic acid glucose, and caffeoylmalic acid could be the main active components. This study supports the importance of secondary metabolites, especially polyphenols, as quorum sensing inhibitors.

scholarly journals Anti-Inflammatory Effects ofSiegesbeckia orientalisEthanol Extract inIn VitroandIn VivoModels

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Yong-Han Hong ◽  
Li-Wen Weng ◽  
Chi-Chang Chang ◽  
Hsia-Fen Hsu ◽  
Chao-Ping Wang ◽  
...  
Keyword(s):  
Inflammatory Mediators ◽  
Inflammatory Responses ◽  
Animal Experiments ◽  
Ethanol Extract ◽  
Raw264.7 Cells ◽  
Control Group ◽  
Dependent Manner ◽  
Anti Inflammatory

This study aims to investigate the anti-inflammatory responses and mechanisms ofSiegesbeckia orientalisethanol extract (SOE). In cell culture experiments, RAW264.7 cells were pretreated with SOE and stimulated with lipopolysaccharide (LPS) for inflammatory mediators assay. In animal experiments, mice were tube-fed with SOE for 1 week, and s.c. injected withλ-carrageenan or i.p. injected with LPS to simulate inflammation. The degree of paw edema was assessed, and cytokine profile in sera and mouse survival were recorded. Data showed that SOE significantly reduced NO, IL-6, and TNF-α production in LPS-stimulated RAW264.7 cells.In vivostudies demonstrated that mice supplemented with 32 mg SOE/kg BW/day significantly lowered sera IL-6 level and resulted a higher survival rate compared to the control group (P=0.019). Furthermore, SOE inhibited LPS-induced NF-κB activation by blocking the degradation of IκB-α. The SOE also reduced significantly the phosphorylation of ERK1/2, p38, and JNK in a dose-dependent manner. In summary, thein vitroandin vivoevidence indicate that SOE can attenuate acute inflammation by inhibiting inflammatory mediators via suppression of MAPKs- and NF-κB-dependent pathways.

scholarly journals Antibiofilm activity of aminopropanol derivatives against Pseudomonas aeruginosa

2018 ◽  
pp. 93-100
Author(s):  
D. M. Dudikova ◽  
Z. S. Suvorova ◽  
V. V. Nedashkivska ◽  
A. O. Sharova ◽  
M. L. Dronova ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Biofilm Formation ◽  
Antimicrobial Agents ◽  
Bacterial Biofilm ◽  
Antibiofilm Activity ◽  
Dependent Manner ◽  
Inhibition Activity ◽  
Chronic Infections ◽  
High Concentration ◽  
Biofilm Inhibition

Bacterial biofilm, particularly formed by Pseudomonas aeruginosa, are a cause of severe chronic infectious diseases. Bacteria within a biofilm are phenotypically more resistant to antibiotics and the macroorganism immune system, making it an important virulence factor for many microbes. The aminopropanol derivatives with adamantyl (KVM-97) and N-alkylaryl radicals (KVM-194, KVM-204, KVM-261, and KVM-262) were used as study object. The aim of this study was to investigate the antibiofilm activity of compounds on biofilm formation and on mature biofilm of P. aeruginosa. The effects of the aminopropanol derivatives on the biofilm mass were evaluated by using crystal violet assay. Ciprofloxacin, meropenem, ceftazidime, gentamicin were used as reference substances. Reported results demonstrate that all compounds displayed antibiofilm activity at the tested concentrations. Remarkable reduction in biofilm formation of P. aeruginosa was found after treatment with KVM-97, KVM-261 and KVM-262 in high concentration (5× MIC), biofilm inhibition activity were 84.3%, 90.5% and 83.3% respectively. After a treatment with KVM-204 at 250 μg/ml (5× MIC) 76.6% of the preformed 24-hr biofilms were destroyed. Furthermore, compounds KVM-97, KVM-194, and KVM-261 in both concentrations showed potent antibiofilm activity against the P. aeruginosa, inhibition activity values being between 56.7 and 65.7%. All tested compounds in dose-dependent manner exhibited pronounced inhibition activity against mature 5-days P. аeruginosa biofilm. It was also observed that tested compounds show high antibiofilm activity in comparison to reference antimicrobials. The aminopropanol derivatives may provide templates for a new group of antimicrobial agents and potential future therapeutics for treating chronic infections.

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