scholarly journals Study on the Bioassay of Anti-Inflammatory Effects of Fuke Qianjin Capsule Based on COX-2 Inhibiting Activity

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Run-ran Ma ◽  
Xiao-juan Yang ◽  
Ying Huang ◽  
Shuai-shuai Chen ◽  
Xiao-he Xiao ◽  
...  
Keyword(s):  
Quality Control ◽  
High Performance ◽  
Linear Regression Analysis ◽  
Parallel Line ◽  
Multiple Linear Regression Analysis ◽  
Positive Control ◽  
Bioassay Method ◽  
Cox 2 ◽  
Anti Inflammatory

Fuke Qianjin Capsule (FKQJ) is a common TCM compound formula in the treatment of gynecological inflammation-related diseases. This study intends to explore and establish a bioassay method to further improve its quality control. The bioassay method for the determination of anti-inflammatory biopotency was established based on its inhibitory activity on recombinant human cyclooxygenase-2 (COX-2), an active target of FKQJ in the treatment of female pelvic inflammatory disease. We firstly established chemical fingerprint of 20 batches of FKQJ by ultra-high-performance liquid chromatography to identify the components and analyze the chemical similarities. The similarity within different batches of FKQJ was relatively high. The values of similarity of the 19 batches were between 0.973 and 0.995, while one batch’s similarity value was 0.813. Celecoxib, a selective inhibitor of COX-2, was chosen as the positive control drug in COX-2 activity assay to establish an anti-inflammatory biopotency detection method based on parallel line test of qualitative response. The methodological investigation showed that the method possessed good repeatability and precision. Secondly, the anti-inflammatory biopotency of 20 batches of FKQJ for inhibiting COX-2 was determined. The results showed that the biopotency of different batches of FKQJ ranged from 676 U/μg to 1310 U/μg, with average value of 918 U/μg and RSD of 16.7%. Based on multiple linear regression analysis, we found that three contents were highly correlated with the anti-inflammatory biopotency, while chlorogenic acid was validated of the strongest anti-inflammatory activity in vitro. Compared with chemical detection, bioassay can better reflect the quality fluctuation of different batches of products and correlate the known pharmacodynamic targets. The supplement of the bioassay method based on chemical evaluation is helpful to improve the quality control ability of Chinese patent medicine and ensure its clinical efficacy is stable and controllable.

scholarly journals Structure-Hepatoprotective Activity Relationship Study of Iridoids

2020 ◽  
Vol 5 (3) ◽  
pp. 108-118
Author(s):  
Durbek Usmanov ◽  
Bakhtiyor Rasulev ◽  
Vladimir Syrov ◽  
Ugiloy Yusupova ◽  
Nurmurod Ramazonov
Keyword(s):  
High Performance ◽  
Statistical Significance ◽  
Linear Regression Analysis ◽  
Predictive Ability ◽  
Multiple Linear Regression Analysis ◽  
Hepatoprotective Activity ◽  
Activity Relationship ◽  
Quantum Chemical Descriptors ◽  
Qsar Analysis

Iridoids, the largest class of monoterpenoids, are widespread group of substances present in various plant organisms. This study is devoted to investigation of the hepatoprotective activity of a series of iridoid compounds with application of a quantitative structure-activity relationship (QSAR) analysis. The investigated activity was based on in vitro experimental data, where iridoids' effects on CCl4-induced hepatocytes' damage were obtained. The QSAR analysis was carried out using a combination of genetic algorithm for variable selection and multiple linear regression analysis. A set of calculated descriptors was used for modeling, including quantum-chemical descriptors. Several high-performance models were developed and the best model describing the hepatoprotective activity of iridoids is proposed. The model obtained in this study shows not only a statistical significance, but also excellent predictive ability. The obtained model can be used to estimate the hepatoprotective activity of new substituted iridoids.

scholarly journals Potential Antioxidant and Anti-Inflammatory Function of Gynura procumbens Polyphenols Ligand

2021 ◽  
Vol 22 (16) ◽  
pp. 8716
Author(s):  
Hun Hwan Kim ◽  
Sang Eun Ha ◽  
Preethi Vetrivel ◽  
Pritam Bhagwan Bhosale ◽  
Seong Min Kim ◽  
...  
Keyword(s):  
Binding Affinity ◽  
High Performance ◽  
Kynurenic Acid ◽  
Screening Methods ◽  
Bioactive Ingredients ◽  
Pharmaceutical Industries ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The antioxidant and anti-inflammatory potentials of polyphenols contained in Gynura procumbens (GP) extract were systematically analyzed. Polyphenols in GP were analyzed for nine peaks using high-performance liquid chromatography (HPLC) combined with mass spectrometry (MS), and quantitatively determined through each standard. A total of nine polyphenolic compounds were identified in the samples and their MS data were tabulated. To determine the potential of bioactive ingredients targeting DPPH and COX-2, we analyzed them by ultrafiltration combined with LC. The results identified the major compounds exhibiting binding affinity for DPPH and COX-2. Caffeic acid, kynurenic acid, and chlorogenic acid showed excellent binding affinity to DPPH and COX-2, suggesting that they can be considered as major active compounds. Additionally, the anti-inflammatory effect of GP was confirmed in vitro. This study will not only be used to provide basic data for the application of GP to the food and pharmaceutical industries, but will also provide information on effective screening methods for other medicinal plants.

scholarly journals Phytochemical Analysis, Anti-inflammatory, and Antioxidant Activities of Dendropanax dentiger Roots

2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Li Yang ◽  
Yiwei Fang ◽  
Ronghua Liu ◽  
Junwei He
Keyword(s):  
High Performance ◽  
Cyclic Peptide ◽  
Antioxidant Activities ◽  
Inflammatory Diseases ◽  
Phytochemical Analysis ◽  
Chemical Compositions ◽  
Biological Functions ◽  
Cox 2 ◽  
Anti Inflammatory

Dendropanax dentiger root is a traditional medicinal plant in China and used to treat inflammatory diseases for centuries, but its phytochemical profiling and biological functions are still unknown. Thus, a rapid, efficient, and precise method based on ultra high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS/MS) was applied to rapidly analyse the phytochemical profiling of D. dentiger with anti-inflammatory and antioxidant activities in vitro. As a result, a total of 78 chemical compositions, including 15 phenylpropanoids, 15 alkaloids, 14 flavonoids, 14 fatty acids, 7 phenols, 4 steroids, 4 cyclic peptides, 3 terpenoids, and 2 others, were identified or tentatively characterized in the roots of D. dentiger. Moreover, alkaloid and cyclic peptide were reported from D. dentiger for the first time. In addition, the ethanol crude extract of D. dentiger roots exhibited remarkable anti-inflammatory activity against cyclooxygenase- (COX-) 2 inhibitory and antioxidant activities in vitro. This study is the first to explore the phytochemical analysis and COX-2 inhibitory activity of D. dentiger. This study can provide important phytochemical profiles and biological functions for the application of D. dentiger roots as a new source of natural COX-2 inhibitors and antioxidants in pharmaceutical industry.

scholarly journals Bone Marrow Mesenchymal Stromal Cells on Silk Fibroin Scaffolds to Attenuate Polymicrobial Sepsis Induced by Cecal Ligation and Puncture

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1433
Author(s):  
Ok-Hyeon Kim ◽  
Jun-Hyung Park ◽  
Jong-In Son ◽  
Ok-Ja Yoon ◽  
Hyun-Jung Lee
Keyword(s):  
Bone Marrow ◽  
Cecal Ligation ◽  
Biological Properties ◽  
Pge2 Production ◽  
Polymicrobial Sepsis ◽  
Control Surface ◽  
Related Factors ◽  
Cox 2 ◽  
Anti Inflammatory

Suitable scaffolds with appropriate mechanical and biological properties can improve mesenchymal stromal cell (MSC) therapy. Because silk fibroins (SFs) are biocompatible materials, they were electrospun and applied as scaffolds for MSC therapy. Consequently, interferon (IFN)-primed human bone marrow MSCs on SF nanofibers were administered into a polymicrobial sepsis murine model. The IL-6 level gradually decreased from 40 ng/mL at 6 h after sepsis to 35 ng/mL at 24 h after sepsis. The IL-6 level was significantly low as 5 ng/mL in primed MSCs on SF nanofibers, and 15 ng/mL in primed MSCs on the control surface. In contrast to the acute response, inflammation-related factors, including HO-1 and COX-2 in chronic liver tissue, were effectively inhibited by MSCs on both SF nanofibers and the control surface at the 5-day mark after sepsis. An in vitro study indicated that the anti-inflammatory function of MSCs on SF nanofibers was mediated through enhanced COX-2-PGE2 production, as indomethacin completely abrogated PGE2 production and decreased the survival rate of septic mice. Thus, SF nanofiber scaffolds potentiated the anti-inflammatory and immunomodulatory functions of MSCs, and were beneficial as a culture platform for the cell therapy of inflammatory disorders.

scholarly journals Ingol and Ingenol-Type Diterpenes from Euphorbia trigona Miller with Keratinocyte Inhibitory Activity

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1206
Author(s):  
Reham Hammadi ◽  
Norbert Kúsz ◽  
Csilla Zsuzsanna Dávid ◽  
Zoltán Behány ◽  
László Papp ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
High Performance ◽  
Skin Condition ◽  
Positive Control ◽  
Active Species ◽  
The European Union ◽  
Ingenol Mebutate

Ingenol mebutate, isolated from Euphorbia peplus, is an ingenane-type diterpenoid, primarily used for the topical treatment of actinic keratosis, a premalignant skin condition. The aim of our work was to investigate other Euphorbia species to find structurally similar diterpenes that can be used as alternatives to ingenol mebutate. Pharmacological investigation of Euphorbia candelabrum, Euphorbia cotinifolia, Euphorbia ramipressa, and Euphorbia trigona revealed the potent keratinocyte (HPV-Ker cell line) inhibitory activity of these spurge species. From the methanolic extract of the aerial parts of Euphorbia trigona Miller, the most active species, five ingol (1–5) and four ingenane-type diterpenoids (6–9) were isolated by various chromatographic separation techniques, including open column chromatography, vacuum liquid chromatography, thin-layer chromatography, and high-performance liquid chromatography. The structures of the compounds were determined by NMR spectroscopic analysis and by comparison of the assignations with the literature data. The cytotoxic activity of the compounds against keratinocytes was tested in vitro by using ingenol mebutate as a positive control. Among the isolated compounds, two ingenane derivatives (6 and 7) exhibited remarkably stronger cytotoxic activity (IC50 values 0.39 μM and 0.32 μM, respectively) on keratinocytes than ingenol mebutate (IC50 value 0.84 μM). These compounds could serve as starting materials for further investigations to find alternatives to Picato® (with active substance ingenol mebutate), which was withdrawn from marketing authorization in the European Union.

Anti-inflammatory Effects ofScoparia dulcisL. and Betulinic Acid

2011 ◽  
Vol 39 (05) ◽  
pp. 943-956 ◽  
Author(s):  
Jen-Chieh Tsai ◽  
Wen-Huang Peng ◽  
Tai-Hui Chiu ◽  
Shang-Chih Lai ◽  
Chao-Ying Lee
Keyword(s):  
Betulinic Acid ◽  
High Performance ◽  
Ethanol Extract ◽  
Paw Edema ◽  
Scoparia Dulcis ◽  
Inflammatory Mechanism ◽  
Tnf Α ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analytical Result

The aims of this study intended to investigate the anti-inflammatory activity of the 70% ethanol extract from Scoparia dulcis (SDE) and betulinic acid on λ-carrageenan-induced paw edema in mice. The anti-inflammatory mechanism of SDE and betulinic acid was examined by detecting the levels of cyclooxygenase-2 (COX-2), nitric oxide (NO), tumor necrosis factor (TNF-α), interleukin-1β (IL-1β) and malondialdehyde (MDA) in the edema paw tissue and the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione reductase (GRd) in the liver. The betulinic acid content in SDE was detected by high performance liquid chromatography (HPLC). In the anti-inflammatory model, the results showed that SDE (0.5 and 1.0 g/kg) and betulinic acid (20 and 40 mg/kg) reduced the paw edema at 3, 4 and 5 h after λ-carrageenan administration. Moreover, SDE and betulinic acid affected the levels of COX-2, NO, TNF-α and IL1-β in the λ-carrageenan-induced edema paws. The activities of SOD, GPx and GRd in the liver tissue were increased and the MDA levels in the edema paws were decreased. It is suggested that SDE and betulinic acid possessed anti-inflammatory activities and the anti-inflammatory mechanisms appear to be related to the reduction of the levels of COX-2, NO, TNF-α and IL1-β in inflamed tissues, as well as the inhibition of MDA level via increasing the activities of SOD, GPx and GRd. The analytical result showed that the content of betulinic acid in SDE was 6.25 mg/g extract.

scholarly journals Mesenchymal Stem Cells (MSCs) Coculture Protects [Ca2+]i Orchestrated Oxidant Mediated Damage in Differentiated Neurons In Vitro

Cells ◽  
2018 ◽  
Vol 7 (12) ◽  
pp. 250 ◽  
Author(s):  
Adel Alhazzani ◽  
Prasanna Rajagopalan ◽  
Zaher Albarqi ◽  
Anantharam Devaraj ◽  
Mohamed Hessian Mohamed ◽  
...  
Keyword(s):  
Cell Death ◽  
Transforming Growth Factor ◽  
Neuronal Cells ◽  
Neuronal Cell Death ◽  
Neuronal Cell ◽  
Apoptotic Cells ◽  
Sequence Of Events ◽  
Cox 2 ◽  
Anti Inflammatory

Cell-therapy modalities using mesenchymal stem (MSCs) in experimental strokes are being investigated due to the role of MSCs in neuroprotection and regeneration. It is necessary to know the sequence of events that occur during stress and how MSCs complement the rescue of neuronal cell death mediated by [Ca2+]i and reactive oxygen species (ROS). In the current study, SH-SY5Y-differentiated neuronal cells were subjected to in vitro cerebral ischemia-like stress and were experimentally rescued from cell death using an MSCs/neuronal cell coculture model. Neuronal cell death was characterized by the induction of proinflammatory tumor necrosis factor (TNF)-α, interleukin (IL)-1β and -12, up to 35-fold with corresponding downregulation of anti-inflammatory cytokine transforming growth factor (TGF)-β, IL-6 and -10 by approximately 1 to 7 fold. Increased intracellular calcium [Ca2+]i and ROS clearly reaffirmed oxidative stress-mediated apoptosis, while upregulation of nuclear factor NF-B and cyclo-oxygenase (COX)-2 expressions, along with ~41% accumulation of early and late phase apoptotic cells, confirmed ischemic stress-mediated cell death. Stressed neuronal cells were rescued from death when cocultured with MSCs via increased expression of anti-inflammatory cytokines (TGF-β, 17%; IL-6, 4%; and IL-10, 13%), significantly downregulated NF-B and proinflammatory COX-2 expression. Further accumulation of early and late apoptotic cells was diminished to 23%, while corresponding cell death decreased from 40% to 17%. Low superoxide dismutase 1 (SOD1) expression at the mRNA level was rescued by MSCs coculture, while no significant changes were observed with catalase (CAT) and glutathione peroxidase (GPx). Interestingly, increased serotonin release into the culture supernatant was proportionate to the elevated [Ca2+]i and corresponding ROS, which were later rescued by the MSCs coculture to near normalcy. Taken together, all of these results primarily support MSCs-mediated modulation of stressed neuronal cell survival in vitro.

scholarly journals Pengaruh Etos Kerja Terhadap Kinerja Karyawan PT. AE

2017 ◽  
Vol 3 (2) ◽  
pp. 150
Author(s):  
Andri Hadiansyah ◽  
Rini Purnamasari Yanwar
Keyword(s):  
High Performance ◽  
Work Ethic ◽  
Employee Performance ◽  
Linear Regression Analysis ◽  
Multiple Linear Regression Analysis ◽  
Positive Influence ◽  
Vital Role ◽  
Theoretical Test ◽  
High Work ◽  
Synergistic Relationship

<p><em>Abstrak -<strong> </strong></em><strong>U</strong><strong>ntuk dapat mencapai hubungan yang sinergis, perusahaan harus dapat memperhatikan pola kinerja karyawannya.</strong><strong> </strong><strong>K</strong><strong>aryawan yang bermutu dan dapat menghasilkan kinerja yang tinggi adalah karyawan yang dibutuhkan oleh suatu organisasi. Peran yang sangat vital dalam mewujudkan prestasi kinerja seorang karyawan adalah dirinya sendiri. Bagaimana dia memiliki semangat dan etos kerja yang tinggi untuk dapat memberikan pengaruh positif pada lingkungannya. Karyawan yang memiliki pemikiran yang luhur mengenai pekerjaannya dapat bekerja dengan tulus. Suatu pandangan dan sikap terhadap kerja dikenal dengan istilah etos kerja. Penelitian ini bertujuan untuk melakukan uji teoritik mengenai pengaruh etos kerja terhadap kinerja karyawan PT. AE. Untuk menguji pengaruh variabel etos kerja terhadap kinerja karyawan digunakan analisis regresi linear berganda dengan menyebar 132 kuesioner pada karyawan PT. AE. Setelah dianalisis didapat hasil R square 0.724 dengan signifikansi</strong><strong> </strong><strong>(p&lt;0.05), yang berarti etos kerja memberikan pengaruh secara signifikan</strong><strong> </strong><strong>terhadap kinerja karyawan sebesar 72.4%.</strong><strong></strong></p><p><strong><em> </em></strong></p><p><strong><em>Kata Kunci</em></strong><em>: Etika Kerja, Performa Kerja </em></p><p> </p><p><em>Abstract - </em><strong>T</strong><strong>o be able to achieve a synergistic relationship, the company should be able to notice employee performance. Employees who are qualified and able to produce high performance is needed by the organization. A very vital role in realizing the achievement of the performance of an employee is himself. How does he have the spirit and high work ethic to be a positive influence on the environment. Employees who have lofty thoughts about the job can work sincerely. An outlook and attitude towards work is known as the work ethic. This study aims to perform a theoretical test on the effect of the work ethic on the performance of employees of PT. AE. To test the effect of variables on the</strong> <strong>performance of the employee's work ethic multiple linear regression analysis was used, by spread 132 questionnaires to employees of PT. AE. Having analyzed the results obtained R square 0.724 with 0.000 significance (p &lt;0.05), which means the work ethic significant influence on employee performance amounted to 72.4%. The dominant aspect of the work ethic that effect the performance is the view of work is trustworthy.</strong></p><p> </p><p><em><strong>Keywords:</strong> Work ethic, Employee performance</em></p>

Kynurenic Acid in Synovial Fluid and Serum of Patients with Rheumatoid Arthritis, Spondyloarthropathy, and Osteoarthritis

2013 ◽  
Vol 40 (6) ◽  
pp. 903-909 ◽  
Author(s):  
Jolanta Parada-Turska ◽  
Wojciech Zgrajka ◽  
Maria Majdan
Keyword(s):  
Rheumatoid Arthritis ◽  
Regression Analysis ◽  
Synovial Fluid ◽  
Blood Cell ◽  
Red Blood Cell ◽  
High Performance ◽  
Kynurenic Acid ◽  
Linear Regression Analysis ◽  
Cell Counts

Objective.Previously we demonstrated that kynurenic acid (KYNA), an endogenous metabolite of kynurenine, is present in the synovial fluid of patients with rheumatoid arthritis (RA). KYNA inhibits proliferation of synoviocytesin vitro. The goal of our study was to compare KYNA concentrations in synovial fluid and blood of patients with RA, inflammatory spondyloarthropathies (SpA), and osteoarthritis (OA).Methods.Serum and synovial fluid samples were obtained from 189 patients with RA, 56 patients with SpA, and 32 patients with OA. KYNA was separated using a high-performance liquid chromatography system and measured fluorometrically.Results.KYNA concentration in synovial fluid obtained from patients with RA and SpA was significantly lower than that in patients with OA (p < 0.05). The concentration of KYNA in serum of patients with RA, SpA, and OA did not differ among all groups studied. The positive correlation between KYNA content in synovial fluid and serum was found in patients with RA (p < 0.05). Univariate linear regression analysis demonstrated that fibrinogen was significantly associated with KYNA in synovial fluid (p < 0.05), and red blood cell counts, morning stiffness, and pain scores were significantly associated with KYNA level in serum (all p < 0.05). Multivariate regression analysis revealed correlation between the following independent variables: hemoglobin level, hematocrit, red blood cell count in conjunction with age and KYNA content in synovial fluid. A lack of correlation was observed between KYNA content in synovial fluid of patients with RA and other clinical and laboratory measures of disease activity.Conclusion.Our data show a local deficit of KYNA in inflammatory states.

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