scholarly journals Antiskin Inflammatory Activity of Black Ginger (Kaempferia parviflora) through Antioxidative Activity

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Myung-hee Lee ◽  
Ah-Ram Han ◽  
Mi Jang ◽  
Hyo-Kyoung Choi ◽  
Sung-Young Lee ◽  
...  
Keyword(s):  
Uv Light ◽  
Critical Role ◽  
Mouse Skin ◽  
Dry Weight ◽  
Mapk Signaling ◽  
Inflammatory Activity ◽  
Kaempferia Parviflora ◽  
Cox 2 ◽  
Anti Inflammatory

Kaempferia parviflora (Krachaidum (KD)) is a traditional herbal medicine and has properties that are beneficial for human health. In the current study, we sought to investigate the anti-inflammatory properties of KD extract (KPE). In mouse skin tissue, UV light representing solar wavelengths (sUV) increased COX-2 expression, while treatment with KPE reduced this effect. The anti-inflammatory activity of KPE was confirmed in in vitro models. MAPK signaling pathways were activated by sUV irradiation, and this was also repressed in the presence of KPE treatment. It is assumed that the anti-inflammatory activity of KPE is caused by the antioxidative effect. Furthermore, we confirmed the critical role of oxidative stress in sUV-induced COX-2 expression. We analyzed the polyphenol composition of KPE. Of the polyphenols identified, gallic acid, apigenin, and tangeretin were identified as the major polyphenols (at 9.31 ± 1.27, 2.37 ± 0.14, and 2.15 ± 0.19 μg/mg dry weight, resp.). Collectively, these findings show that in the presence of sUV irradiation, KD has anti-inflammatory properties and antioxidative effects in the skin.

scholarly journals IN VITRO ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ALCHORNEA CORDIFOLIA (SCHUMACH AND THONN.) MULL. ARG. AND ANTROCARYON KLAINEANUM PIERRE EXTRACTS

2020 ◽  
pp. 129-135
Author(s):  
ROSETTE CHRISTELLE NDJIB ◽  
STEVE VALDI DJOVA ◽  
CHRISTELLE WAYOUE KOM ◽  
AGBOR GABRIEL AGBOR ◽  
AMINA MAMAT ◽  
...  
Keyword(s):  
Concentration Level ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Dry Weight ◽  
Inflammatory Activity ◽  
Phytochemical Screening ◽  
Reducing Activity ◽  
Anti Inflammatory ◽  
Β Carotene

Objective: This study aims to evaluate the in vitro antioxidant, anti-inflammatory activities of the aqueous and hydroethanolic extracts recipe of Alchornea cordifolia and Antrocaryon klaineanum. A preliminary phytochemical screening was carried out. Methods: The total phenols content was determined by the Folin Ciocalteu reagent method, while the antioxidant activity of both extracts was characterized by the 2-2diphenyl-1-picrilhidrazil (DPPH) and β-carotene assays. The anti-inflammatory activity of the extracts was evaluated as the inhibition of Bovine Serum Albumin (BSA) denaturation and antiproteinase activity. Results: The aqueous extracts of Alchornea cordifolia and Antrocaryon klaineanum contained more polyphenols [270 mg Ascorbic acid equivalent (AAE)/g dry weight (dw)] than the hydroethanolic recipe extract (262.41 mg AAE/g dw) at the same concentration level. On the other hand, the aqueous and hydroethanolic recipe extract had the same radical scavenging activity with the antiradical power of 0.851 and 0.830, respectively. Similarly, the recipe extract had the same reducing activity with reducing the power of 94.2±2.03 mg EAA/g dw and 97.4±4.16 mg EAA/g dw for the aqueous and hydroethanolic recipe extract of Alchornea cordifolia and Antrocaryon klaineanum respectively. For the anti-inflammatory activity it was observed that both extracts possess the same activity as Diclofenac® with an IC50 of 50.21 μg/ml. The phytochemical screening of the extracts revealed the presence of alkaloids, flavonoids, carbohydrates, phenols and tannins, which may account for their activities. Conclusion: The plant recipe extract studied possess antioxidant and anti-inflammatory potentials, which may be beneficiary to its consumers.

In vitro anti-inflammatory activity of carvacrol: Inhibitory effect on COX-2 catalyzed prostaglandin E2 biosynthesisb

2009 ◽  
Vol 32 (1) ◽  
pp. 75-78 ◽  
Author(s):  
Premysl Landa ◽  
Ladislav Kokoska ◽  
Marie Pribylova ◽  
Tomas Vanek ◽  
Petr Marsik
Keyword(s):  
Prostaglandin E2 ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
Cox 2 ◽  
Anti Inflammatory

scholarly journals 18α-Glycyrrhetinic acid monoglucuronide as an anti-inflammatory agent through suppression of the NF-κB and MAPK signaling pathway

MedChemComm ◽  
2017 ◽  
Vol 8 (7) ◽  
pp. 1498-1504 ◽  
Author(s):  
Bo Li ◽  
Yongan Yang ◽  
Liuzeng Chen ◽  
Shichao Chen ◽  
Jing Zhang ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Mapk Signaling ◽  
Mapk Signaling Pathway ◽  
Glycyrrhetinic Acid ◽  
Inflammatory Activity ◽  
Inflammatory Agent ◽  
Cox 2 ◽  
Anti Inflammatory

18α-GAMG exhibited strong anti-inflammatory activity through inhibiting the expression of iNOS, COX-2, and MAPKs, as well as activation of NF-κB.

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.

Bacopamonnieri (L.) exerts anti-inflammatory effects on cells of the innate immune system in vitro

2014 ◽  
Vol 5 (3) ◽  
pp. 517-520 ◽  
Author(s):  
Roderick Williams ◽  
Gerald Münch ◽  
Erika Gyengesi ◽  
Louise Bennett
Keyword(s):  
Immune System ◽  
Acute Pain ◽  
Innate Immune System ◽  
Selective Inhibition ◽  
Innate Immune ◽  
Inflammatory Activity ◽  
Consequent Reduction ◽  
Cox 2 ◽  
Anti Inflammatory

Bacopa monnieri(L., BM) is a traditional Ayurvedic medicinal herb recognised for its efficacy in relieving acute pain and inflammation, as related to selective inhibition of cyclo-oxygenase-2 (COX-2) enzyme and consequent reduction in COX-2-mediated prostanoid mediators. Anti-inflammatory activity of BM might also account for its benefits in cognition.

scholarly journals Preliminary Assessment of the Anti-Inflammatory Activity of New Structural Honokiol Analogs with a 4′-O-(2-fluoroethyl) Moiety and the Potential of Their 18F-Labeled Derivatives for Neuroinflammation Imaging

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6630
Author(s):  
Daria D. Vaulina ◽  
Kira I. Stosman ◽  
Konstantin V. Sivak ◽  
Andrey G. Aleksandrov ◽  
Nikolai B. Viktorov ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Inflammatory Activity ◽  
Preliminary Evaluation ◽  
Moderate Increase ◽  
Biodistribution Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
The Brain

Neolignans honokiol and 4′-O-methylhonokiol (MH) and their derivatives have pronounced anti-inflammatory activity, as evidenced by numerous pharmacological studies. Literature data suggested that cyclooxygenase type 2 (COX-2) may be a target for these compounds in vitro and in vivo. Recent studies of [11C]MPbP (4′-[11С]methoxy-5-propyl-1,1′-biphenyl-2-ol) biodistribution in LPS (lipopolysaccharide)-treated rats have confirmed the high potential of MH derivatives for imaging neuroinflammation. Here, we report the synthesis of four structural analogs of honokiol, of which 4′-(2-fluoroethoxy)-2-hydroxy-5-propyl-1, 1′-biphenyl (F-IV) was selected for labeling with fluorine-18 (T1/2 = 109.8 min) due to its high anti-inflammatory activity confirmed by enzyme immunoassays (EIA) and neuromorphological studies. The high inhibitory potency of F-IV to COX-2 and its moderate lipophilicity and chemical stability are favorable factors for the preliminary evaluation of the radioligand [18F]F-IV in a rodent model of neuroinflammation. [18F]F-IV was prepared with good radiochemical yield and high molar activity and radiochemical purity by 18F-fluoroethylation of the precursor with Boc-protecting group (15) with [18F]2-fluoro-1-bromoethane ([18F]FEB). Ex vivo biodistribution studies revealed a small to moderate increase in radioligand uptake in the brain and peripheral organs of LPS-induced rats compared to control animals. Pretreatment with celecoxib resulted in significant blocking of radioactivity uptake in the brain (pons and medulla), heart, lungs, and kidneys, indicating that [18F]F-IV is likely to specifically bind to COX-2 in a rat model of neuroinflammation. However, in comparison with [11C]MPbP, the new radioligand showed decreased brain uptake in LPS rats and high retention in the blood pool, which apparently could be explained by its high plasma protein binding. We believe that the structure of [18F]F-IV can be optimized by replacing the substituents in the biphenyl core to eliminate these disadvantages and develop new radioligands for imaging activated microglia.

scholarly journals Design and Synthesis of 2-Mercapto Benzoxazole coupled Benzyl Triazoles as Anti-inflammatory Agents Targeting COX-2 Enzyme

2020 ◽  
Vol 32 (12) ◽  
pp. 3209-3218
Author(s):  
K. Praveen Kumar ◽  
Y. Prashanthi ◽  
G. Rambabu ◽  
Md. Ataur Rahman ◽  
J.S. Yadav
Keyword(s):  
Chemical Space ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Anti Inflammatory

In this study, we report the design, synthesis and the biological evaluation of 19 analogues of 2-mercapto benzoxazole coupled benzyl triazoles (BOTs) based on analysis of the binding site and literature of chemical space. These BOTs were evaluated both in vitro and in vivo for their anti-inflammatory activity. Eleven compounds showed less than 10 μM in vitro COX-2 enzyme activities. The most potent analogue among the BOT analogues were BOT15, BOT3 and BOT19 with IC50 3.40 μM, 4.50 μM and 4.57 μM respectively against COX-2. The in vivo anti-inflammatory activity of two BOTs has significantly higher than that of standard drug, ibuprofen. 2-Mercapto benzoxazole coupled benzyl triazoles (BOTs) were also tested for their antioxidant capacity and proved to be an as active scavenger, better than ascorbic acid.

Design, Synthesis, Antioxidant, Anti-inflammatory Activity and Molecular Docking Studies of Novel 3,4,5-Trisubstituted-1,2,4-Triazole Derivatives Bearing Benzimidazole Moiety

2020 ◽  
Vol 17 ◽  
Author(s):  
Ramamurthy Katikireddy ◽  
Ramu Kakkerla ◽  
M.P.S. Murali Krishna ◽  
Gandamalla Durgaiah ◽  
Narasimha Reddy Yellu
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
Biological Data ◽  
Inflammatory Activity ◽  
Design Synthesis ◽  
Molecular Docking Studies ◽  
Cox 2 ◽  
Anti Inflammatory

: 5-(7-Methyl-2-propyl-1H-benzo[d]imidazol-5-yl)-4-phenyl-4H-1,2,4-triazole-3-thiols(6a-i) have been synthesized from key intermediate 7-methyl-2-propyl-1H-benzo[d]imidazole-5-carbohydrazide(3). The hydrazide was treated with different aryl isothiocyanatesto give corresponding thiosemicarbazone derivatives, which underwent cyclization in 4N sodium hydroxide to affordcorresponding title compound. All the compounds evaluated for their in vitro antioxidant and in vivo anti-inflammatory activity. From the results, compounds 6b and 6e have shown potential antioxidant and anti-inflammatory activity. The biological data was further supported by molecular docking studies, which revealed the binding pattern and the affinity of the molecules in the active site of COX-2.

Sign in / Sign up

Export Citation Format

Share Document