scholarly journals Bioactivity-Guided Single-Step Isolation of Stachyspinoside from Sideritis congesta by Centrifugal Partition Chromatography

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Julian Osthoff ◽  
Christophe Carola ◽  
Andrew Salazar ◽  
Joerg von Hagen
Keyword(s):  
Aqueous Extract ◽  
Single Step ◽  
Partition Chromatography ◽  
Centrifugal Partition Chromatography ◽  
Inhibition Activity ◽  
Mediterranean Countries ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Fraction I

Sideritis congesta is a plant native to Mediterranean countries. Infusions of this plant are used to treat various diseases. The anti-inflammatory potential of Sideritis species is widely known. However, the anti-inflammatory potential of an aqueous extract of S. congesta has not been investigated yet. In this study, the phytochemical composition and anti-inflammatory potential of different fractions of an aqueous extract from S. congesta using bioactivity guided fractionation via centrifugal partition chromatography (CPC) were determined. A CPC single-step isolation of a flavonoid stachyspinoside 1 from S. congesta is reported. In addition, a CPC fractionation protocol of the crude aqueous extract was developed. Three aqueous fractions (I, II, and III) of S. congesta were obtained, and their anti-inflammatory potential was evaluated with respect to their ability to inhibit the activity of COX-2 and NF-κB in vitro. Fraction I showed the highest COX-2 inhibition activity (92.3% inhibition at 0.1%). Fraction III showed the highest NF-κB inhibition activity (99.9% at 0.1%) among the CPC produced fractions. The structures of 3 compounds of fraction III could be identified and were validated by HPLC-PDA, HRMS, and NMR spectroscopy. Finally, the phenol, saponin, and flavonoid contents were quantified in the most potent CPC fractions (I and III).

A single-step isolation by centrifugal partition chromatography of the potential anti-inflammatory glaucolide B from Lepidaploa chamissonis

2019 ◽  
Vol 1605 ◽  
pp. 460362 ◽  
Author(s):  
Layzon Antonio Lemos Da Silva ◽  
Louis P. Sandjo ◽  
Eduarda Fratoni ◽  
Yeo Jim Kinoshita Moon ◽  
Eduardo Monguilhott Dalmarco ◽  
...  
Keyword(s):  
Single Step ◽  
Partition Chromatography ◽  
Centrifugal Partition Chromatography ◽  
Anti Inflammatory

scholarly journals Phytochemical, Antioxidant and Anti-Inflammatory Effects of Extracts from Ampelocissus africana (Lour) Merr (Vitaceae) Rhizomes

2020 ◽  
pp. 8-18
Author(s):  
W. Leila Marie Esther Belem- Kabré ◽  
Noufou Ouédraogo ◽  
Adjaratou Compaoré- Coulibaly ◽  
Mariam Nebié- Traoré ◽  
Tata K. Traoré ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Antioxidant Activity ◽  
Aqueous Extract ◽  
Methanolic Extract ◽  
Total Phenolic ◽  
Antioxidant Power ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Aims: To determine the phytochemical composition and evaluate the antioxidant and anti-inflammatory properties of methanolic and aqueous extracts from Ampelocissus africana (Lour) Merr rhizomes. Study Design: Phytochemical content and screening, in vitro antioxidant and anti-inflammatory assays. Place and Duration of Study: Department of Traditional Pharmacopoeia and Pharmacy (MEPHATRA / PH) of the Institute for Research in Health Sciences (IRSS) and Laboratory of Applied Biochemistry and Chemistry (LABIOCA), University Joseph KI-ZERBO in Ouagadougou between April and August 2020. Methodology: The antioxidant activity of both extracts of the plant was assessed using DPPH radical scavenging, ABTS+ radical cation decolorization, ferric ion reduction and lipid peroxidation inhibition in rat liver assays. The anti-inflammatory activities in vitro were measured on the ability of the extract to inhibit the activity of enzymes such as 15-lipoxygenase, phospholipase A2 (PLA2) and cyclooxygenases (COX-1 and COX-2). Results: This study revealed that the total phenolic contents of the extracts varied from 471.79 ± 1.71 mg GAE/g to 173.88 ± 1.71 mg GAE/g for methanolic and aqueous extract respectively. The extracts were also rich in flavonoids and tannins. The methanolic extract possessed better antioxidant activity with an IC50 of 2.32 ± 0.18 µg/ml for the ABTS, 1.71 ± 0.05 µg/mL for the DPPH, a reducing power agent of 87.44 ± 0.5 mmol AAE /100 g and a percentage inhibition of lipid peroxidation of 52.21%. The methanolic and aqueous extract of A. africana has an inhibitory action on activity of lipoxygenase with IC50 values of 26.09 ± 1.83 μg/mL to 34.32 ± 1.60 μg/mL, respectively. The methanolic extract caused COX-1 inhibition of 36.07%, COX-2 inhibition of 38.31% and PLA2 inhibition of 26.9%. Conclusion: These results showed that the methanolic and aqueous extract from the rhizomes of Ampelocissus africana possessed antioxidant power, inhibitor effect against proinflammatory enzymes.

scholarly journals Chemical Characterization and Anti-Inflammatory Activity of Phytoconstituents from Swertia alata

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1109
Author(s):  
Sakshi Bajaj ◽  
Shivkanya Fuloria ◽  
Vetriselvan Subramaniyan ◽  
Dhanalekshmi Unnikrishnan Meenakshi ◽  
Sharad Wakode ◽  
...  
Keyword(s):  
Ethanolic Extract ◽  
Attenuated Total Reflection ◽  
Inflammatory Activity ◽  
Inhibition Activity ◽  
Ulcerogenic Activity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Swertia alata C.B Clarke (Gentianaceae) is a well-reported plant in the traditional system of medicine. The present study was intended to isolate the phytoconstituents from the ethanolic extract of the aerial parts of S. alata; and evaluate for in vitro COX-1/COX-2 inhibition activity, in vivo anti-inflammatory and ulcerogenic activity. Phytoisolation involved partitioning of S. alata ethanolic extract into petroleum ether and chloroform soluble fractions using silica gel-based column chromatography. The isolation afforded two phytoisolates, namely oleanolic acid (SA-1) and 3-hydroxylup-12-(13)-ene-17-carboxylic acid (SA-4). Phytoisolates structures were established by melting point, ultraviolet (UV), attenuated total reflection-Fourier-transform infrared (ATR-FTIR), nuclear magnetic resonance (1H-NMR, 13C-NMR and HMBC) and mass spectrometry. Phytoisolates were further evaluated for in vitro cyclooxygenase (COX-1/COX-2) inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity. The study revealed SA-4 (COX-1/COX-2 inhibition activity of 104/61.68 µM with % inhibition of 61.36) to be more effective than SA-1 (COX-1/COX-2 inhibition activity of 128.4/87.25 µM, with % inhibition of 47.72). SA-1 and SA-4, when subjected to ulcerogenic study, exhibited significant gastric tolerance. The current study reports chromatographic isolation and spectrometric characterization of SA-1 and SA-4. The present study concludes that compound SA-4 possess significant anti-inflammatory activity and less irritant property over gastric mucosa with no significant ulcerogenicity in comparison to indomethacin.

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 Oriental Hornet (Vespa orientalis) Larval Extracts Induce Antiproliferative, Antioxidant, Anti-Inflammatory, and Anti-Migratory Effects on MCF7 Cells

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3303
Author(s):  
Amina M. G. Zedan ◽  
Mohamed I. Sakran ◽  
Omar Bahattab ◽  
Yousef M. Hawsawi ◽  
Osama Al-Amer ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Aqueous Extract ◽  
Antioxidant Activities ◽  
Individual Treatment ◽  
Alcoholic Extract ◽  
Anticancer Effect ◽  
Mcf7 Cells ◽  
Vespa Orientalis ◽  
Anti Inflammatory

The use of insects as a feasible and useful natural product resource is a novel and promising option in alternative medicine. Several components from insects and their larvae have been found to inhibit molecular pathways in different stages of cancer. This study aimed to analyze the effect of aqueous and alcoholic extracts of Vespa orientalis larvae on breast cancer MCF7 cells and investigate the underlying mechanisms. Our results showed that individual treatment with 5% aqueous or alcoholic larval extract inhibited MCF7 proliferation but had no cytotoxic effect on normal Vero cells. The anticancer effect was mediated through (1) induction of apoptosis, as indicated by increased expression of apoptotic genes (Bax, caspase3, and p53) and decreased expression of the anti-apoptotic gene Bcl2; (2) suppression of intracellular reactive oxygen species; (3) elevation of antioxidant enzymes (CAT, SOD, and GPx) and upregulation of the antioxidant regulator Nrf2 and its downstream target HO-1; (4) inhibition of migration as revealed by in vitro wound healing assay and downregulation of the migration-related gene MMP9 and upregulation of the anti-migratory gene TIMP1; and (5) downregulation of inflammation-related genes (NFκB and IL8). The aqueous extract exhibited the best anticancer effect with higher antioxidant activities but lower anti-inflammatory properties than the alcoholic extract. HPLC analysis revealed the presence of several flavonoids and phenolic compounds with highest concentrations for resveratrol and naringenin in aqueous extract and rosmarinic acid in alcoholic extract. This is the first report to explain the intracellular pathway by which flavonoids and phenolic compounds-rich extracts of Vespa orientalis larvae could induce MCF7 cell viability loss through the initiation of apoptosis, activation of antioxidants, and inhibition of migration and inflammation. Therefore, these extracts could be used as adjuvants for anticancer drugs and as antioxidant and anti-inflammatory agents.

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 EVALUATION OF IN VITRO ANTI-INFLAMMATORY AND ANTIMICROBIAL ACTIVITY OF AQUEOUS AND METHANOLIC SEED EXTRACTS OF CITRULLUS LANATUS

2017 ◽  
Vol 9 (5) ◽  
pp. 29
Author(s):  
Iswariya S. ◽  
Uma T. S.
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Aqueous Extract ◽  
Seed Extract ◽  
Inflammatory Activity ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Anti Inflammatory ◽  
Seed Extracts

Objective: The present study was designed to identify the bioactive phytochemicals and its antibacterial and in vitro anti-inflammatory potential of aqueous and methanolic seed extract of Citrullus lanatus.Methods: The phytochemical screening of both the aqueous and methanolic seed extract was carried out qualitatively to identify the major Phyto-constituents present in the extracts. The antimicrobial activity of the extracts was evaluated against six pathogenic bacterial strains by agar well diffusion method and the Minimum inhibitory concentration (MIC) was determined by broth dilution method. In vitro anti-inflammatory activity of C. lanatus seed extracts was evaluated by using human red blood cell (HRBC) membrane stabilization and inhibition of albumin denaturation method.Results: The results of the study indicated that both the extracts of the seed having antimicrobial activity, while the methanolic extract showed more significant activity against the tested organism than aqueous extract. Methanol extract had the lowest MIC of 1.562 mg/ml against Escherichia coli, Staphylococcus aureus, Klebsiella pneumonia, Pseudomonas aeruginosa and Bacillus subtilis, whereas in aqueous extract was highly sensitive to Bacillus subtilis, E. coli and Klebsiella pneumonia with MIC of 3.125 and 6.25 mg/ml, respectively. Methanolic extracts exerted comparative higher anti-inflammatory activity than aqueous extract.Conclusion: Present study provides a firm evidence to support that the synergistic effect of C. lanatus seed extracts having potent anti-inflammatory and antimicrobial property, which might serve as an effective drug for various microbial infections and inflammatory disorders.

2,5-disubstituted-4-thiazolidinones: Synthesis, anti-inflammatory, free radical scavenging potentials and structural insights through molecular docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh
Keyword(s):  
Free Radicals ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Assay Method ◽  
Acidic Group ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory

: The present work reports synthesis and screening of fifteen 2,5-disubstituted-4-thiazolidinones with different substitutions of varied arylidene groups at imino. The structures of the compounds were confirmed by spectral characterization. The compounds were subjected to in vivo anti-inflammatory and in vitro antioxidant activities. The derivatives possessed remarkable activities quite close to standard drugs used. Unlike conventional non-selective NSAIDs, the synthesized compounds did not contain any acidic group, thereby ensuring a complete cure from ulcers. To further substantiate the claim for safer derivatives, the active compounds were docked against the cyclooxygenase (COX)-2 enzyme. It was found that 4-fluorophenylimino substituent at 2- position and 3-nitro moiety on a 5-benzylidene nucleus of the 4-thiazolidinone derivative fitted in the COX-2 binding pocket. The compounds exhibited remarkable activity in scavenging free radicals, as depicted by the DPPH assay method. The structure-activity relationship was also established in the present work with respect to the nature and position of the substituents. The active compounds were evaluated for drug-like nature under Lipinski’s rule of five, and the toxicity behaviour of active compounds was predicted using ADMETlab software. The compounds have the potential to target degenerative disorders associated with inflammation and the generation of free radicals.

scholarly journals Design, Synthesis and Comprehensive Investigations of Pyrrolo[3,4-d]pyridazinone-Based 1,3,4-Oxadiazole as New Class of Selective COX-2 Inhibitors

2020 ◽  
Vol 21 (24) ◽  
pp. 9623
Author(s):  
Łukasz Szczukowski ◽  
Edward Krzyżak ◽  
Adrianna Zborowska ◽  
Patrycja Zając ◽  
Katarzyna Potyrak ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
One Pot ◽  
Design Synthesis ◽  
Biological Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Dna Strand ◽  
Cox 2 Inhibitors

The long-term use of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) in treatment of different chronic inflammatory disorders is strongly restricted by their serious gastrointestinal adverse effects. Therefore, there is still an urgent need to search for new, safe, and efficient anti-inflammatory agents. Previously, we have reported the Mannich base-type derivatives of pyrrolo[3,4-d]pyridazinone which strongly inhibit cyclooxygenase, have better affinity to COX-2 isoenzyme and exert promising anti-oxidant activity. These findings encouraged us to perform further optimization of that structure. Herein, we present the design, synthesis, molecular docking, spectroscopic, and biological studies of novel pyrrolo[3,4-d]pyridazinone derivatives bearing 4-aryl-1-(1-oxoethyl)piperazine pharmacophore 5a,b–6a,b. The new compounds were obtained via convenient, efficient, one-pot synthesis. According to in vitro evaluations, novel molecules exert no cytotoxicity and act as selective COX-2 inhibitors. These findings stay in good correlation with molecular modeling results, which additionally showed that investigated compounds take a position in the active site of COX-2 very similar to Meloxicam. Moreover, all derivatives reduce the increased level of reactive oxygen and nitrogen species and prevent DNA strand breaks caused by oxidative stress. Finally, performed spectroscopic and molecular docking studies demonstrated that new compound interactions with bovine serum albumin (BSA) are moderate, formation of complexes is in one-to-one ratio, and binding site II (subdomain IIIA) is favorable.

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