scholarly journals Hypoglycemic and Anti-Inflammatory Effects of Triterpene Glycoside Fractions from Aeculus hippocastanum Seeds

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3784
Author(s):  
Avez Sharipov ◽  
Khurshid Tursunov ◽  
Sunnatullo Fazliev ◽  
Bahtigul Azimova ◽  
Jamoliddin Razzokov
Keyword(s):  
Triterpene Glycoside ◽  
Biomedical Applications ◽  
Chemical Compounds ◽  
Chemical Components ◽  
Horse Chestnut ◽  
Pharmaceutical Drugs ◽  
Triterpene Saponins ◽  
In Vivo Experiments ◽  
Anti Inflammatory

Horse chestnut (Aesculus hippocastanum L.)-derived drugs have shown their potential in biomedical applications. The seed of A. hippocastanum contains various kinds of chemical compounds including phenolics, flavonoids, coumarins, and triterpene saponins. Here, we investigated the chemical components in A. hippocastanum L. grown in Uzbekistan, which has not yet been studied in detail. We identified 30 kinds of triterpene saponins in an extract of A. hippocastanum L. Classifying extracted saponins into eight fractions, we next studied the hypoglycemic and the anti-inflammatory activities of escin and its derivatives through in vivo experiments. We came by data indicating the highest (SF-1 and SF-2) and the lowest (SF-5 and SF-8) antidiabetic and anti-inflammatory effects of those eight fractions. These results imply the prospective use of A. hippocastanum L. grown in Uzbekistan in the production of pharmaceutical drugs to treat diabetes and inflammation.

scholarly journals TAK1/AP-1-Targeted Anti-Inflammatory Effects of Barringtonia augusta Methanol Extract

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3053
Author(s):  
Anh Thu Ha ◽  
Mi-Yeon Kim ◽  
Jae Youl Cho
Keyword(s):  
Mouse Model ◽  
Methanol Extract ◽  
Folk Medicine ◽  
Activator Protein 1 ◽  
Western Blot Assay ◽  
In Vivo Experiments ◽  
Chemokine Ligand ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Barringtonia augusta methanol extract (Ba-ME) is a folk medicine found in the wetlands of Thailand that acts through an anti-inflammatory mechanism that is not understood fully. Here, we examine how the methanol extract of Barringtonia augusta (B. augusta) can suppress the activator protein 1 (AP-1) signaling pathway and study the activities of Ba-ME in the lipopolysaccharide (LPS)-treated RAW264.7 macrophage cell line and an LPS-induced peritonitis mouse model. Non-toxic concentrations of Ba-ME downregulated the mRNA expression of cytokines, such as cyclooxygenase and chemokine ligand 12, in LPS-stimulated RAW264.7 cells. Transfection experiments with the AP-1-Luc construct, HEK293T cells, and luciferase assays were used to assess whether Ba-ME suppressed the AP-1 functional activation. A Western blot assay confirmed that C-Jun N-terminal kinase is a direct pharmacological target of Ba-ME action. The anti-inflammatory effect of Ba-ME, which functions by β-activated kinase 1 (TAK1) inhibition, was confirmed by using an overexpression strategy and a cellular thermal shift assay. In vivo experiments in a mouse model of LPS-induced peritonitis showed the anti-inflammatory effect of Ba-ME on LPS-stimulated macrophages and acute inflammatory mouse models. We conclude that Ba-ME is a promising anti-inflammatory drug targeting TAK1 in the AP-1 pathway.

scholarly journals Shepherd’s Purse Polyphenols Exert Its Anti-Inflammatory and Antioxidative Effects Associated with Suppressing MAPK and NF-κB Pathways and Heme Oxygenase-1 Activation

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Jinming Peng ◽  
Tianyong Hu ◽  
Jin Li ◽  
Jing Du ◽  
Kerui Zhu ◽  
...  
Keyword(s):  
Heme Oxygenase ◽  
Chemical Constituents ◽  
Chemical Compounds ◽  
Heme Oxygenase 1 ◽  
Mice Model ◽  
Traditional Herbal Medicine ◽  
Raw 264.7 Macrophages ◽  
Antioxidative Effects ◽  
Anti Inflammatory

Shepherd’s purse (Capsella bursa-pastoris (L.) Medik.), a wild herb as a traditional herbal medicine, has been proved with multiple healthy benefits. In this study, the chemical constituents of shepherd’s purse were identified by UPLC-QTOF-MS/MS. The antioxidative and anti-inflammatory potential of shepherd’s purse extract (SPE) were also investigated applying lipopolysaccharide- (LPS-) induced inflammation in RAW 264.7 macrophages and a carrageenan-induced mice paw edema model. Twenty-four chemical compounds were identified mainly including phenolic acids and flavonoids. The data also indicated SPE inhibited the productions of NO, PGE2, TNF-α, and IL-6 stimulated with LPS. In addition, SPE inhibited the increase of reactive oxygen species (ROS) and upregulated the expression of heme oxygenase-1 (HO-1). We further found that SPE inhibited the phosphorylation of P38 MAPK and activation of NF-κB. In vivo mice model also indicated that SPE showed strong antioxidative and anti-inflammatory activity.

scholarly journals Multi-dimensional computational pipeline for large-scale deep screening of compound effect assessment: an in silico case study on ageing-related compounds

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Vipul Gupta ◽  
Alina Crudu ◽  
Yukiko Matsuoka ◽  
Samik Ghosh ◽  
Roger Rozot ◽  
...  
Keyword(s):  
Large Scale ◽  
Network Effects ◽  
Chemical Compounds ◽  
Structural Similarity ◽  
Computational Pipeline ◽  
In Vivo Experiments ◽  
Cell Vitality ◽  
Alternative Means ◽  
Related Compounds

AbstractDesigning alternative approaches to efficiently screen chemicals on the efficacy landscape is a challenging yet indispensable task in the current compound profiling methods. Particularly, increasing regulatory restrictions underscore the need to develop advanced computational pipelines for efficacy assessment of chemical compounds as alternative means to reduce and/or replace in vivo experiments. Here, we present an innovative computational pipeline for large-scale assessment of chemical compounds by analysing and clustering chemical compounds on the basis of multiple dimensions—structural similarity, binding profiles and their network effects across pathways and molecular interaction maps—to generate testable hypotheses on the pharmacological landscapes as well as identify potential mechanisms of efficacy on phenomenological processes. Further, we elucidate the application of the pipeline on a screen of anti-ageing-related compounds to cluster the candidates based on their structure, docking profile and network effects on fundamental metabolic/molecular pathways associated with the cell vitality, highlighting emergent insights on compounds activities based on the multi-dimensional deep screen pipeline.

Differences in Chemical Component and Anticancer Activity of Green and Ripe Forsythiae Fructus

2017 ◽  
Vol 45 (07) ◽  
pp. 1513-1536 ◽  
Author(s):  
Jiaolin Bao ◽  
Ren-Bo Ding ◽  
Yeer Liang ◽  
Fang Liu ◽  
Kai Wang ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Principal Component ◽  
Chemical Compounds ◽  
Clinical Applications ◽  
Chemical Components ◽  
Aqueous Extracts ◽  
Clear Separation ◽  
Marker Compounds

Forsythiae Fructus, Lianqiao in Chinese, is one of the most fundamental herbs in Traditional Chinese Medicine. Both green Forsythia (GF) and ripe Forsythia (RF) are referred to Forsythiae Fructus in medicinal applications. In most cases, they are used without distinction. In this study, a metabolomics approach was performed to compare componential differences of two Forsythiae Fructus aqueous extracts subtypes. Principal component analysis (PCA) score plots from the UPLC-MS data showed clear separation between the two subtypes, indicating there are significant differences in the chemical components between GF and RF. Meanwhile, the anticancer activity of them was also compared. GF exhibited much stronger antitumor activity than RF against B16-F10 murine melanoma both in vitro and in vivo. 15 chemical compounds were identified as specific markers for distinguishing GF and RF. Among these marker compounds, forsythoside I, forsythoside A, forsythoside E and pinoresinol were demonstrated to be key important active compounds that account for the different anticancer efficacies of GF and RF. Our data suggest that GF and RF should be distinctively used in clinical applications, particularly in the anticancer formulas, in which GF should be preferentially prescribed.

scholarly journals Biocompatible N-acetyl-nanoconstruct alleviates lipopolysaccharide-induced acute lung injury in vivo

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Seongchan Kim ◽  
Shin Young Kim ◽  
Seung Joon Rho ◽  
Seung Hoon Kim ◽  
So Hyang Song ◽  
...  
Keyword(s):  
Acute Lung Injury ◽  
Lung Injury ◽  
Inflammatory Responses ◽  
Therapeutic Potential ◽  
Intratracheal Instillation ◽  
Sprague Dawley ◽  
In Vivo Experiments ◽  
Anti Inflammatory

AbstractOxidative stress plays important roles in inflammatory responses during acute lung injury (ALI). Recently, nanoconstruct (Nano)-based drug-delivery systems have shown promise in many models of inflammation. In this study, we evaluated the anti-inflammatory effects of N-acetylcysteine (NAC) loaded in a biocompatible Nano using a rat model of ALI. We synthesized a Nano with a good NAC-releasing capacity using porous silica Nano, which was used to produce Nano/NAC complexes. For in vivo experiments, Sprague–Dawley rats were intraperitoneally administered NAC or Nano/NAC 30 min after intratracheal instillation of lipopolysaccharide. After 6 h, bronchoalveolar lavage fluids and lung tissues were collected. The anti-oxidative effect of the Nano/NAC complex was confirmed by demonstrating reduced levels of reactive oxygen species after treatment with the Nano/NAC in vitro. In vivo experiments also showed that the Nano/NAC treatment may protect against LPS‐induced ALI thorough anti‐oxidative and anti‐inflammatory effects, which may be attributed to the inactivation of the NF‐κB and MAPK pathways. In addition, the effects of Nano/NAC treatment were shown to be superior to those of NAC alone. We suggest the therapeutic potential of Nano/NAC treatment as an anti‐inflammatory agent against ALI. Furthermore, our study can provide basic data for developing nanotechnology-based pharmacotherapeutics for ALI.

scholarly journals Chemical Composition of Melaleuca Cajuputi Powell

2019 ◽  
Vol 9 (1) ◽  
pp. 3479-3483 ◽  
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Chemical Compound ◽  
Steam Distillation ◽  
Chemical Compounds ◽  
Chemical Components ◽  
Melaleuca Cajuputi ◽  
Anti Inflammatory

Essential oil extracted from Melaleucagenus has been widely used worldwidefor many purposes. Most of the its has been reported as the source of phytochemical compound where mostly have anti-inflammatory, antiulcer, antioxidant, antimicrobial and insecticide properties. Thus, three objectives that have been highlighted in this study are (1) to extract essential oil (cajuput oil) from fresh leaves of MelaleucacajuputiPowell using simple steam distillation,(2) to determine the chemical components of MelaleucacajuputPowell essential oil using GCMS and (3) to compare the chemical compound and its percentage with the previous study.Results found that there were 41 chemical compounds that have been identified. The chemical compounds were monoterpenes such as α-terpinolene, α-pinene, sabinene, 4-terpineol and γ-terpinene. The highest chemical compounds found were caryophyllene (20.16%), α-terpinolene (17.0%),α-humulene (11.91%), βelemene (7.62%) and γ-terpinene (5.62%). In previous research, 1,8-cineole chemical compound was foundhowever, in this study a different chemical compound found, it was caryophyllene, this is due to different geographic area.As a conclusion, most of the compounds found was aromatic, antibacterial andinsecticide properties.

scholarly journals Comparative Study Regarding the Properties of Methylene Blue and Proflavine and Their Optimal Concentrations for In Vitro and In Vivo Applications

Diagnostics ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 223 ◽  
Author(s):  
Maria-Eliza Nedu ◽  
Mihaela Tertis ◽  
Cecilia Cristea ◽  
Alexandru Valentin Georgescu
Keyword(s):  
Methylene Blue ◽  
Fluorescent Dyes ◽  
Tissue Level ◽  
In Vivo Studies ◽  
Cell Nuclei ◽  
In Vivo Experiments ◽  
Bacteriostatic Agent ◽  
Anti Inflammatory

Methylene blue and proflavine are fluorescent dyes used to stain nucleic acid from the molecular level to the tissue level. Already clinically used for sentinel node mapping, detection of neuroendocrine tumors, methemoglobinemia, septic shock, ifosfamide-induced encephalopathy, and photodynamic inactivation of RNA viruses, the antimicrobial, anti-inflammatory, and antioxidant effect of methylene blue has been demonstrated in different in vitro and in vivo studies. Proflavine was used as a disinfectant and bacteriostatic agent against many gram-positive bacteria, as well as a urinary antiseptic involved in highlighting cell nuclei. At the tissue level, the anti-inflammatory effects of methylene blue protect against pulmonary, renal, cardiac, pancreatic, ischemic-reperfusion lesions, and fevers. First used for their antiseptic and antiviral activity, respectively, methylene blue and proflavine turned out to be excellent dyes for diagnostic and treatment purposes. In vitro and in vivo studies demonstrated that both dyes are efficient as perfusion and tissue tracers and permitted to evaluate the minimal efficient concentration in different species, as well as their pharmacokinetics and toxicity. This review aims to identify the optimal concentrations of methylene blue and proflavine that can be used for in vivo experiments to highlight the vascularization of the skin in the case of a perforasome (both as a tissue tracer and in vascular mapping), as well as their effects on tissues. This review is intended to be a comparative and critical presentation of the possible applications of methylene blue (MB) and proflavine (PRO) in the surgical field, and the relevant biomedical findings from specialized literature to date are discussed as well.

Potential Papain-like Protease Inhibitors against COVID-19: A Comprehensive In Silico Based Review

2021 ◽  
Vol 25 ◽  
Author(s):  
Neetu Agrawal ◽  
Shilpi Pathak ◽  
Ahsas Goyal
Keyword(s):  
In Silico ◽  
Chemical Compounds ◽  
Potential Candidate ◽  
In Vivo Experiments ◽  
Drug Databases ◽  
In Silico Studies ◽  
Approved Drugs ◽  
Fda Approved Drugs

: The entire world has been in a battle against the COVID-19 pandemic since its first appearance in December 2019. Thus researchers are desperately working to find an effective and safe therapeutic agent for its treatment. The multifunctional coronavirus enzyme papain-like protease (PLpro) is a potential target for drug discovery to combat the ongoing pandemic responsible for cleavage of the polypeptide, deISGylation, and suppression of host immune response. The present review collates the in silico studies performed on various FDA-approved drugs, chemical compounds, and phytochemicals from various drug databases and represents the compounds possessing the potential to inhibit PLpro. Thus this review can provide quick access to a potential candidate to medicinal chemists to perform in vitro and in vivo experiments who are thriving to find the effective agents for the treatment of COVID-19.

PPARγ Regulates the Anti-Inflammatory Effects of Carbon Monoxide on Macrophages: A Gene Profiling Study.

Blood ◽  
2004 ◽  
Vol 104 (11) ◽  
pp. 3445-3445
Author(s):  
Martin Bilban ◽  
Sherrie L. Otterbein ◽  
Emeka Ifedigbo ◽  
Keiji Enjyoji ◽  
Anny Usheva ◽  
...  
Keyword(s):  
Carbon Monoxide ◽  
Inflammatory Response ◽  
Acute Phase Proteins ◽  
Expression Patterns ◽  
Endotoxic Shock ◽  
Gene Profiling ◽  
In Vivo Experiments ◽  
Anti Inflammatory

Abstract Carbon monoxide (CO) at low concentrations has generated recent interest due to its ability to modulate the inflammatory response associated with chronic graft rejection, vascular injury and septic shock. Both in vivo and in vitro CO can inhibit the expression of pro-inflammatory genes such as TNFα in macrophages while simultaneously increasing the expression of the anti-inflammatory cytokine IL-10. The mechanisms by which this occurs are still unclear. To better understand the mechanisms underlying the effects of CO, we employed the Affymetrix GeneChip technology to evaluate the time-dependent expression patterns of >12,000 genes in macrophages stimulated with bacterial endotoxin (LPS) in the presence or absence of a low concentration of CO previously demonstrated to evoke an anti-inflammatory response. We were particularly interested whether CO would, by itself, modulate in a specific manner the expression of proteins that might explain the anti-inflammatory effects observed following subsequent administration of endotoxin. RAW 264.7 murine macrophages were grown to 75% confluency and then exposed to CO (250 ppm) for 3 hr prior to administration of LPS (10 ng/ml). At 0, 15, 30, 60, 120 and 240 min thereafter, total RNA was isolated by standard methods and the RNA was then labeled and hybridized to U74Av2 GeneChips. Of >12,000 genes assessed, 116 of 270 that were LPS-responsive were affected by CO treatment. CO inhibited the majority of LPS-induced pro-inflammatory cytokines and acute phase proteins including expression of early growth response-1 (Egr-1), a transcription factor that serves as a central intermediary regulating many genes. Egr-1 was nearly completely inhibited by CO as was Egr-1-dependent expression of tissue factor (TF) and PAI-1. Treatment of cells with CO alone led to a rapid early increase in PPARγ, the expression of which was essential for the anti-inflammatory effects of CO. Inhibition of PPARγ using the selective chemical inhibitor GW9662 reversed the CO inhibitory effects on LPS-induced Egr-1 and TF expression. Correlative in vivo experiments in mice showed that CO pre-treatment blocked endotoxin-induced Egr-1 expression and decreased markers of lung inflammmation the effects of which were also lost with inhibition of PPARγ. Our analyses of gene expression patterns has led to the first molecular understanding of how treatment with CO, in this case by inducing PPARγ, blocks the pro-inflammatory response. These experiments provide novel insights into the mechanisms and pathophysiology of endotoxic shock and identify cellular targets by which CO mediates these cytoprotective effects.

scholarly journals The Anti-Inflammatory Activity of HMGB1 A Box Is Enhanced When Fused with C-Terminal Acidic Tail

2010 ◽  
Vol 2010 ◽  
pp. 1-6 ◽  
Author(s):  
Wei Gong ◽  
Yingru Zheng ◽  
Fan Chao ◽  
Yuan Li ◽  
Zhizhen Xu ◽  
...  
Keyword(s):  
Fusion Proteins ◽  
Inflammatory Diseases ◽  
Inflammatory Activity ◽  
In Vivo Experiments ◽  
Specific Antagonist ◽  
Proinflammatory Activity ◽  
Anti Inflammatory ◽  
Inflammatory Effect

HMGB1, composed of the A box, B box, and C tail domains, is a critical proinflammatory cytokine involved in diverse inflammatory diseases. The B box mediates proinflammatory activity, while the A box alone acts as a specific antagonist of HMGB1. The C tail contributes to the spatial structure of A box and regulates HMGB1 DNA binding specificity. It is unknown whether the C tail can enhance the anti-inflammatory effect of A box. In this study, we generated fusion proteins consisting of the A box and C tail, in which the B box was deleted and the A box and C tail were linked either directly or by the flexible linker sequence(Gly4Ser)3. In vitro and in vivo experiments showed that the two fusion proteins had a higher anti-inflammatory activity compared to the A box alone. This suggests that the fused C tail enhances the anti-inflammatory effect of the A box.

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