scholarly journals Antioxidant and Anti-inflammatory Compounds in Nutmeg (Myristica Fragrans) Pericarp as Determined by in vitro Assays

2015 ◽  
Vol 10 (8) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Chuan-Rui Zhang ◽  
Ettannil Jayashree ◽  
Paramasivam Suresh Kumar ◽  
Muraleedharan G. Nair
Keyword(s):  
In Vitro Assays ◽  
Bioactive Components ◽  
Methanolic Extracts ◽  
Myristica Fragrans ◽  
Food And Beverage ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Nutmeg, Myristica fragrans, is known for its culinary and medicinal values. The nutmeg pericarp, abundant during the production of the seed, is also used in food and beverage preparations. In this study, the pericarp of M. fragrans was evaluated for its bioactive components using in vitro antioxidant and anti-inflammatory assays. The hexane, ethyl acetate and methanolic extracts inhibited lipid peroxidation (LPO) by 82.5, 70.1 and 73.2%, and cyclooxygenase enzymes COX-1 by 44, 44 and 42% and COX-2 by 47, 41 and 36%, respectively, at 100 μg/mL. The bioassay-guided purifications of extracts yielded 20 compounds belonged to neolignans (0.13%), phenylpropanoids (0.28%), phenolic aldehyde (0.35%), triterpenoids (0.06%), triglycerides (0.20%), sugars (10.2%) and steroids (0.49%). Pure isolates 1–5 inhibited LPO by 70–99% and 3–12 inhibited COX-1 and -2 enzymes by 37–49%. This is the first report on the bioassay-guided characterization of constituents in nutmeg pericarp. Our results support the medicinal claims of nutmeg pericarp.

scholarly journals Anti- inflammatory effect of Prunus tomentosa Thunb total flavones in LPS-induced RAW264.7 cells

2019 ◽  
Vol 17 (1) ◽  
pp. 685-693
Author(s):  
Chen Xi ◽  
Liu Yuanyuan ◽  
Zhao Dongshuang ◽  
Fan Ziwei ◽  
Cao Shuang ◽  
...  
Keyword(s):  
Significant Inhibition ◽  
Raw264.7 Cells ◽  
Supernatant Fraction ◽  
Treatment Of Diabetes ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
The Impact ◽  
Cox 1 ◽  
Inflammatory Effect

AbstractIn this research, we investigated possible anti-inflammatory roles of Prunus tomentosa Thunb Total Flavones (PTTTF) in LPS-induced RAW264.7 cells. PTTTF (4μg/ml and 40μg/ml) was applied to RAW264.7 cells induced with 1μg/ml LPS to test the impact of these flavones on neutrophil phagocytosis in vitro. Levels of prostaglandin E2 (PGE2) and two pro-inflammatory interleukin cytokines (i.e. IL-6 and IL-1β) in the supernatant fraction were tested via Enzyme-linked immunosorbent assays (ELISA). Expression of cyclooxygenases COX-1 and COX-2 was detected via RT-PCR. Superoxide dismutase (SOD) content was determined with a spectrophotometric assay (Micromethod). The results revealed that PTTTF at doses higher than 4μg/ml reduces the content of IL-6, IL-1β and PGE2 (P < 0.05), and elevates the activity of SOD in LPS-induced RAW264.7 cells significantly (P < 0.05). PTTTF at 40μg/ml showed no significant effect on the expression of COX-1(P>0.05) but resulted in a significant inhibition of COX-2 in LPS-induced RAW264.7 cells (P<0.05). In summary, PTTTF had a substantial potential anti-inflammatory effect through the alteration of the synthesis of some cytokines and other mediators of the process of inflammation. Novelty statement - Prunus tomentosa Thunb Total Flavones (PTTTF) have known roles in the treatment of diabetes, but here we show that they are also potential anti-inflammatory agents. Our results show that PTTTF exhibited anti-inflammatory effects through altering the synthesis of some cytokines and other mediators of the inflammatory process.

scholarly journals Studies in 3,4-diaryl-1,2,5-oxadiazoles and their N-oxides: Search for better COX-2 inhibitors

2007 ◽  
Vol 57 (1) ◽  
pp. 13-30 ◽  
Author(s):  
Mange Yadav ◽  
Shrikant Shirude ◽  
Devendra Puntambekar ◽  
Pinkal Patel ◽  
Hetal Prajapati ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Docking Studies ◽  
Inflammatory Activity ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Cox 1

Studies in 3,4-diaryl-1,2,5-oxadiazoles and theirN-oxides: Search for better COX-2 inhibitorsA series of 3,4-diaryl-1,2,5-oxadiazoles and 3,4-diaryl-1,2,5-oxadiazoleN-oxides were prepared and evaluated for COX-2 and COX-1 binding affinityin vitroand for anti-inflammatory activity by the rat paw edema method.p-Methoxy (p-OMe) substituted compounds 9, 21, 34, 41, 42 showed COX-2 enzyme inhibition higher than that showed by compounds with other substituents. 3,4-Di(4-methoxyphenyl)-1,2,5-oxadiazoleN-oxide (42) showed COX-2 enzyme inhibition of 54% at 22 μmol L-1and COX-1 enzyme inhibition of 44% at 88 μmol L-1concentrations, but showed very lowin vivoanti-inflammatory activity. Its deoxygenated derivative (21) showed lower COX-2 enzyme inhibition (26% at 22 μmol L-1) and higher COX-1 enzyme inhibition (53% at 88 μmol L-1) but, markedin vivoanti-inflammatory activity (71% at 25 mg kg-1)vs.celecoxib (48% at 12.5 mg kg-1). Molecular modeling (docking) studies showed that the methoxy group is positioned in the vicinity of COX-2 secondary pocket and it also participates in hydrogen bonding interactions in the COX-2 active site. These preliminary studies suggest thatp-methoxy (p-OMe) group in one of benzene rings may give potentially active leads in this series of oxadiazole/N-oxides.

scholarly journals Anti-Arthritic and Anti-Inflammatory Potential of Spondias mangifera Extract Fractions: An In Silico, In Vitro and In Vivo Approach

Plants ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 825
Author(s):  
Mohammad Khalid ◽  
Mohammed H. Alqarni ◽  
Ambreen Shoaib ◽  
Muhammad Arif ◽  
Ahmed I. Foudah ◽  
...  
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Arthritis Score ◽  
Beneficial Effects ◽  
Tnf Α ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

The fruits of Spondias mangifera (S. mangifera) have traditionally been used for the management of rheumatism in the northeast region of India. The present study explores the probable anti-arthritis and anti-inflammatory potential of S. mangifera fruit extract’s ethanolic fraction (EtoH-F). To support this study, we first approached the parameters in silico by means of the active constituents of the plant (beta amyrin, beta sitosterol, oleonolic acid and co-crystallised ligands, i.e., SPD-304) via molecular docking on COX-1, COX-2 and TNF-α. Thereafter, the absorption, distribution, metabolism, excretion and toxicity properties were also determined, and finally experimental activity was performed in vitro and in vivo. The in vitro activities of the plant extract fractions were evaluated by means of parameters like 1,1-Diphenyl-2- picrylhydrazyl (DPPH), free radical-reducing potential, albumin denaturation, and protease inhibitory activity. The in vivo activity was evaluated using parameters like COX, TNF-α and IL-6 inhibition assay and arthritis score in Freund Adjuvant (CFA) models at a dose of 400 mg/kg b.w. per day of different fractions (hexane, chloroform, alcoholic). The molecular docking assay was performed on COX-1, COX-2 and TNF-α. The results of in vitro studies showed concentration-dependent reduction in albumin denaturation, protease inhibitors and scavenging activity at 500 µg/mL. Administration of the S. mangifera alcoholic fraction at the abovementioned dose resulted in a significant reduction (p < 0.01) in arthritis score, paw diameters, TNF-α, IL-6 as compared to diseased animals. The docking results showed that residues show a critical binding affinity with TNF-α and act as the TNF-α antagonist. The alcoholic fraction of S. mangifera extract possesses beneficial effects on rheumatoid arthritis as well as anti-inflammatory potential, and can further can be used as a possible agent for novel target-based therapies for the management of arthritis.

Synthesis of new hexahydropyrimido[1,2-a]azepine derivatives bearing functionalized aryl and heterocyclic moieties as anti-inflammatory agents

2021 ◽  
Author(s):  
Hassanein H Hassanein ◽  
Doaa E Abdel Rahman ◽  
Marwa A Fouad ◽  
Rehab F Ahmed
Keyword(s):  
Molecular Docking ◽  
Binding Sites ◽  
Docking Study ◽  
In Vivo Studies ◽  
Molecular Docking Study ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

New hexahydropyrimido[1,2- a]azepine derivatives bearing functionalized aryl and heterocyclic moieties were synthesized as anti-inflammatory agents with better safety profiles. All synthesized compounds were assessed in vitro for their COX-1 and COX-2 inhibition activities. The most selective compounds, 2f, 5 and 6, were further evaluated for their in vivo anti-inflammatory activity and PGE2 inhibitory activity. To rationalize their selectivity, molecular docking within COX-1 and COX-2 binding sites was performed. Their physicochemical properties and drug-like nature profile were also calculated. The good activity and selectivity of compounds 2f, 5 and 6 were rationalized using a molecular docking study and supported by in vivo studies. These promising findings are encouraging for performing future investigations of these derivatives.

Chemical characterization and anti-inflammatory activity of phytoconstituents from Swertia alata

2020 ◽  
Author(s):  
sakshi bajaj ◽  
Sharad Wakode ◽  
Avneet Kaur ◽  
Himangini Bansal ◽  
Satish Manchanda ◽  
...  
Keyword(s):  
Multiple Bond ◽  
Attenuated Total Reflection ◽  
Antiulcer Activity ◽  
Traditional System ◽  
Ulcerogenic Activity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Abstract Background: Swertia alata C.B Clarke (Gentianaceae) is well reported in Indian Traditional system of medicine and plant was known for its febrifuge, tonic, laxative and antimalarial properties.Objective: To isolate the phytoconstituents from the plant species S alata (Gentianaceae) and to study in vitro COX-1/COX-2, in vivo anti-inflammatory and ulcerogenic activity.Material and methods: With intent to explore newer phytoconstituents, the ethanolic extract of aerial parts of S. alata was partitioned into petroleum ether and chloroform soluble fractions. The isolation of phytoconstituents was performed using silica gel base column chromatography, afforded two phytoisolates (one new and one known) characterized as oleanolic acid (SA-1) and 3-hydroxylup-12-(13)-ene-17-carboxylic acid (SA-4). The structures of the isolated compounds were established based on melting point (MP), Ultraviolet (UV), Attenuated total reflection-Fourier-transform infrared spectroscopy (ATR-FTIR), 1D (1H NMR & 13C NMR) 2D Heteronuclear Multiple Bond Correlation (HMBC) Nuclear magnetic resonance (NMR) and Mass spectrometry. Pharmacological screening was performed to evaluate in vitro Cyclooxygenase (COX-1 /COX-2) inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity.Results: Among the compounds, SA-4 (COX-1: COX-2 :: 104 : 61.68 µM, % inhibition = 61.36) found to be more effective than SA-1(COX-1:COX-2:: 128.4:87.25 µM, % inhibition = 47.72) Ulcerogenic study was also performed on the isolated compounds (SA-1 and SA-4) and found to possess significant gastric tolerance than indomethacin. Conclusion: Ayurvedic knowledge supported by modern science is necessary to isolate, characterize, and standardize the active constituents from herbal sources for anti-inflammatory and antiulcer activity.

scholarly journals Selective COX-2 Inhibitory Properties of Dihydrostilbenes from Liquorice Leaves–In Vitro Assays and Structure/Activity Relationship Study

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901 ◽  
Author(s):  
Domenico Trombetta ◽  
Salvatore V. Giofrè ◽  
Antonio Tomaino ◽  
Roberto Raciti ◽  
Antonella Saija ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Docking Study ◽  
In Vitro Assays ◽  
Molecular Docking Study ◽  
Pge2 Release ◽  
Human Therapy ◽  
Glycyrrhiza Glabra L ◽  
Cox 2 ◽  
Cox 1

Three dihydrostilbenes belonging to the polyphenol pool characterized in the leaves of Sicilian liquorice ( Glycyrrhiza glabra L.) have been tested for their antioxidant and anti-inflammatory activity. The three dihydrostilbenes (PA-82, GA-23, DO-07) were in vitro tested to evaluate their capability to scavenge the stable radical 1,1-diphenyl-2-picrylhydrazyl (DPPH), and to decrease thromboxane B2 (TxB2) and prostaglandin E2 (PGE2) release in human whole blood samples. On the basis of the observed capability of these compounds to affect the cell COX-1/COX-2 pathway, a molecular docking study was carried out in order to understand in detail the ability of these compounds to bind to COX-1 and COX-2. The results show that the liquorice dihydrostilbenes are preferred ligands for COX-2 rather than for COX-1, providing a good rational for the observed selectivity in ex vivo experiments. Therefore, they appear to be good candidates for employment in human therapy against inflammation-related pathological conditions.

scholarly journals Antiinflammatory Potential and Fatty Acid Content of Lipophilic Leaf Extracts of Four Staphylea L. Species

2009 ◽  
Vol 4 (4) ◽  
pp. 1934578X0900400
Author(s):  
Lubica Lacikova ◽  
Eva-Maria Pferschy-Wenzig ◽  
Irena Masterova ◽  
Daniel Grancai ◽  
Rudolf Bauer
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Acid Content ◽  
Unsaturated Fatty Acids ◽  
Fatty Acid Content ◽  
In Vitro Assays ◽  
Leaf Extracts ◽  
Cox 2 ◽  
Cox 1

Staphylea preparations are used in TCM and have been used by native Americans for a number of indications, such as rheumatism. Based on this knowledge, the anti-inflammatory activity of light petroleum extracts of leaves of Staphylea colchica Stev., S. elegans Zab., S. holocarpa Hemsl. and S. pinnata L. has been determined using in vitro assays for inhibition of cyclooxygenase (COX-1 and COX-2) and leukotriene B4 (LTB4) formation by lipoxygenase (5-LOX). All extracts inhibited COX-1 and COX-2, with S. holocarpa and S. elegans performing best. Inhibition of LTB4 formation was less pronounced. As unsaturated fatty acids are known to inhibit arachidonic acid metabolism in vitro, the fatty acid content was determined of the active extracts and set in correlation with their activity. Unsaturated fatty acids were found to contribute to the observed COX-2 and LTB4 formation inhibitory activity to a different extent.

scholarly journals In vitro Anti-inflammatory Activity of Ligustrum vulgare Extracts and Their Analytical Characterization

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Anna Macková ◽  
Pavel Mučaji ◽  
Ute Widowitz ◽  
Rudolf Bauer
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Neutrophil Granulocytes ◽  
Cyclooxygenase 1 ◽  
Ligustrum Vulgare ◽  
China And Japan ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Interest in the anti-inflammatory effects of Ligustrum vulgare L., which has been used traditionally in China and Japan prompted us to determine anti-inflammatory effects of the plant's compounds in leukocytes. The leaves of L. vulgare were used to prepare a decoction which was successively extracted with organic solvents (dichloromethane (DCM), n-butanol, ethyl acetate) using liquid-liquid partition. Extracts were tested for inhibition of LTB4, resp. PGE2 biosynthesis. Each extract was evaluated for its in vitro cyclooxygenase-1/2 (COX-1/2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes, as well as for their LTB4 formation inhibitory activity using an assay with activated human neutrophil granulocytes. All extracts reported inhibitory actions against COXs in comparison with the synthetic inhibitors NS-398 (IC50 = 2.6 μM) and indomethacin (IC50 = 0.9 μM). The dichloromethane extract of privet leaves showed a considerable inhibitory effect against COX-1 and COX-2 enzyme activity. The DCM extract revealed 2.7 times higher inhibitory activity against LTB4 formation in comparison with the known specific LT inhibitor zileuton (IC50 = 5.0 μM). Additionally, oleuropein and echinacoside were detected by HPLC-DAD and LC-MS in the Ligustrum vulgare leaves. Both compounds exhibited weak inhibitory activity on cyclooxygenases and leukotriene formation.

Design, Synthesis and Pharmacological Evaluation of Gastro- Protective Anti-inflammatory Analgesic Agents based on Dual Oxidative Stress / Cyclooxygenase Inhibition

2020 ◽  
Vol 19 (3) ◽  
pp. 268-290 ◽  
Author(s):  
Monika Gaba ◽  
Sarbjot Singh ◽  
Chander Mohan ◽  
Richa Dhingra ◽  
Monika Chauhan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Inhibitory Activity ◽  
Frap Assay ◽  
Anti Oxidant ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Cox 1

Background: Non-steroidal anti-inflammatory drugs (NSAIDs) derived local generation of reactive oxygen species (ROS) plays a crucial role in the formation of gastric ulceration. Objective: Therefore, anti-inflammatory analgesics with potent antioxidant activity could be a potential therapeutic strategy for the treatment of pain and inflammatory disorders without gastrointestinal (GI) side effects. Methods: In an effort to develop gastroprotective analgesic and anti-inflammatory agents, a series of 2-methylamino-substituted-1H-benzo[d] imidazol-1-yl) (phenyl) methanone derivatives were synthesized and evaluated in vitro for cyclooxygenase (COX) inhibition as well as anti-oxidant potential by the FRAP assay. The compounds with significant in vitro COX-1/COX-2 inhibitory activity and antioxidant activity were further screened in vivo for their anti-inflammatory and analgesic activities. Moreover, the ulcerogenic potential of test compounds was also studied. To gain insight into the plausible mode of interaction of compounds within the active sites of COX-1 and COX-2, molecular docking simulations were performed. Results: Among the various synthesized molecules, most of the compounds showed good cyclooxygenase inhibitory activity and efficient antioxidant activity in FRAP assay. After preliminary and indicative in vitro assays, three compounds exhibited most significant antiinflammatory and analgesic activity with better gastric tolerability during their in vivo evaluation. Ligand interaction studies indicated highest dock score -43.05 of 1,2- disubstituted benzimidazole derivatives in comparison to the reference ligand -30.70. Overall studies provided us (2-((4-methoxyphenylamino) methyl) -1h-benzo [d] imidazol- 1-yl) (phenyl) methanone as a lead with potent gastro-protective anti-inflammatory and analgesic activities that can be used for future research. Conclusion: From the above results, it can be concluded that designing of multifunctional molecules with COX-1/COX-2 inhibitory and anti-oxidant activities could hold a great promise for further development of GI-safer NSAIDs.

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