scholarly journals Scarlet Flax Linum grandiflorum (L.) In Vitro Cultures as a New Source of Antioxidant and Anti-Inflammatory Lignans

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4511
Author(s):  
Bushra Asad ◽  
Taimoor Khan ◽  
Faiza Zareen Gul ◽  
Muhammad Asad Ullah ◽  
Samantha Drouet ◽  
...  
Keyword(s):  
Callus Cultures ◽  
In Vitro Cultures ◽  
Naphthalene Acetic Acid ◽  
Efficient Production ◽  
Cotyledon Explants ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Linum Grandiflorum ◽  
Cox 1

In vitro cultures of scarlet flax (Linum grandiflorum L.), an important ornamental flax, have been established as a new possible valuable resource of lignans and neolignans for antioxidant and anti-inflammatory applications. The callogenic potential at different concentrations of α-naphthalene acetic acid (NAA) and thidiazuron (TDZ), alone or in combinations, was evaluated using both L. grandiflorum hypocotyl and cotyledon explants. A higher callus induction frequency was observed on NAA than TDZ, especially for hypocotyl explants, with a maximum frequency (i.e., 95.2%) on 1.0 mg/L of NAA. The presence of NAA (1.0 mg/L) in conjunction with TDZ tended to increase the frequency of callogenesis relative to TDZ alone, but never reached the values observed with NAA alone, thereby indicating the lack of synergy between these two plant growth regulators (PGRs). Similarly, in terms of biomass, NAA was more effective than TDZ, with a maximum accumulation of biomass registered for medium supplemented with 1.0 mg/L of NAA using hypocotyls as initial explants (DW: 13.1 g). However, for biomass, a synergy between the two PGRs was observed, particularly for cotyledon-derived explants and for the lowest concentrations of TDZ. The influence of these two PGRs on callogenesis and biomass is discussed. The HPLC analysis confirmed the presence of lignans (secoisolariciresinol (SECO) and lariciresinol (LARI) and neolignan (dehydrodiconiferyl alcohol [DCA]) naturally accumulated in their glycoside forms. Furthermore, the antioxidant activities performed for both hypocotyl- and cotyledon-derived cultures were also found maximal (DPPH: 89.5%, FRAP 866: µM TEAC, ABTS: 456 µM TEAC) in hypocotyl-derived callus cultures as compared with callus obtained from cotyledon explants. Moreover, the anti-inflammatory activities revealed high inhibition (COX-1: 47.4% and COX-2: 51.1%) for extract of hypocotyl-derived callus cultures at 2.5 mg/L TDZ. The anti-inflammatory action against COX-1 and COX-2 was supported by the IC50 values. This report provides a viable approach for enhanced biomass accumulation and efficient production of (neo)lignans in L. grandiflorum callus cultures.

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 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.

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 Identification of Active Compounds From Yi Nationality Herbal Formula Wosi Influencing COX-2 and VCAM-1 Signaling

2020 ◽  
Vol 11 ◽  
Author(s):  
Ji-Zhong Zhang ◽  
Xiao-Yi Chen ◽  
You-Jiao Wu ◽  
Li-Min Li ◽  
Li Huang ◽  
...  
Keyword(s):  
Uric Acid ◽  
Oleanolic Acid ◽  
Glucuronic Acid ◽  
Folk Medicine ◽  
Herbal Formula ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

The Yi nationality herbal formula Wosi is used in China as a folk medicine to treat arthritis and related diseases. Despite its widespread use, the active ingredients, and pharmacological mechanisms are not performed. This is the first time to identify the active compounds from Wosi with the aim at providing the potential effect of Wosi and exploring its underlying anti-inflammatory mechanism in monosodium urate crystals (MSU)-induced arthritis rats. In this study, anti-hyperuricemia effect was assessed by reducing the serum uric acid levels and increasing uric acid excretion in the urine for the hyperuricemia rat model. Wosi significantly suppressed the degree of joint swelling and improved the symptoms of inflammation induced by MSU crystals. The inhibition of IL-2, IL-1β, IFN-γ, and IL-6 secretion and IL-10 increase in the serum were also observed. This study also focuses on the screening of the main compounds from Wosi against cyclooxygenase for anti-inflammatory properties using molecular docking. The result showed 3-O-[α-L-pyran rhamnose(1-3)-β-D-pyran glucuronic acid]- oleanolic acid, 3-O-(β-D-pyran glucuronic acid)-oleanolic acid-28-O-β-D-pyran glucoside, and 3-O-[α-L-pyran rhamnose(1-3)-β-D-pyran glucuronic acid]-oleanolic acid-28-O-β-D-pyran glucoside with a higher binding affinity for COX-2 than COX-1 which indicated relatively higher interaction than COX-1. The preferential selectivity toward inhibiting COX-2 enzyme over COX-1 of three compounds from Wosi were evaluated using in-vitro cyclooxygenases 1 and 2 (COX-1/2) inhibition assays. Meanwhile, the down-regulated protein expression of COX-2 and VCAM-1 in synovial tissue sections from ankle joints of experiments rats were confirmed by immunohistochemistry analysis after the Wosi treatment. In conclusion, three oleanolic acid glycosides were implied as mainly efficient compounds in Yi nationality herbal formula Wosi for arthritis therapy via selectively influencing COX-2 and VCAM-1 signaling.

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