scholarly journals New 1,4-Dienonesteroids from the Octocoral Dendronephthya sp.

Marine Drugs ◽  
2019 ◽  
Vol 17 (9) ◽  
pp. 530 ◽  
Author(s):  
Thanh-Hao Huynh ◽  
Pei-Chin Chen ◽  
San-Nan Yang ◽  
Feng-Yu Lin ◽  
Tung-Pin Su ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Spectroscopic Methods ◽  
Inos Protein ◽  
Macrophage Cells ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage

Two new steroids, dendronesterones D (1) and E (2), featuring with 1,4-dienone moiety, along with three known steroids, methyl 3-oxochola-4,22-diene-24-oate (3), 5α,8α-epidioxy-24(S)- methylcholesta-6,22-dien-3β-ol (4), and 5α,8α-epidioxy-24(S)-methylcholesta-6,9(11),22-trien-3β-ol (5), were isolated from an octocoral Dendronephthya sp. The structures of steroids 1 and 2 were elucidated by using spectroscopic methods and steroid 1 was found to exhibit significant in vitro anti-inflammatory activity in lipopolysaccharides (LPS)-induced RAW264.7 macrophage cells by inhibiting the expression of the iNOS protein.

scholarly journals Phenanthrenes in Chinese Yam Peel Exhibit Anti-inflammatory Activity, as Shown by Strong in Vitro Cyclooxygenase Enzyme Inhibition

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Qian Li ◽  
Chuan-Rui Zhang ◽  
Amila A. Dissanayake ◽  
Qun-yu Gao ◽  
Muraleedharan G. Nair
Keyword(s):  
Food Item ◽  
Inflammatory Activity ◽  
Spectroscopic Methods ◽  
Over The Counter ◽  
Chinese Yam ◽  
Inflammatory Drugs ◽  
In Vitro Bioassays ◽  
Anti Inflammatory ◽  
Cox 1

Chinese yam ( Dioscorea opposita), peeled or whole, is a popular food item that is considered to be healthy. Often, the yam is peeled before cooking. However, it is also consumed with peel. Therefore, in this study, the peel of this yam was extracted sequentially with n-hexane, ethyl acetate and methanol, and studied for its health-benefits, using in vitro bioassays. Bioactivity-guided purifications of extracts of the peel afforded phenanthrenes (1-4), as characterized by spectroscopic methods. Phenanthrene 1 is a novel analogue. The extracts and isolates were tested for anti-inflammatory activity using cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. All phenanthrenes isolated from the yam peel showed higher inhibition of COX enzymes than the over-the-counter nonsteroidal anti-inflammatory drugs (NSAIDs) aspirin, ibuprofen and naproxen.

scholarly journals Pentoxifylline Can Reduce the Inflammation Caused by LPS after Inhibiting Autophagy in RAW264.7 Macrophage Cells

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Danping Ruan ◽  
Sinan Deng ◽  
Zhonglong Liu ◽  
Jie He
Keyword(s):  
Phosphodiesterase Inhibitor ◽  
Inflammatory Factors ◽  
Signal Pathways ◽  
Ampk Signaling ◽  
Macrophage Cells ◽  
Raw264.7 Macrophages ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage ◽  
In Cells

Pentoxifylline (PTX), as a methylxanthine derivative and nonspecific phosphodiesterase inhibitor, has the characteristics of anti-inflammatory and partial inflammatory process inhibition. However, the regulatory effect of PTX on inflammatory cytokines is unclear. Autophagy can regulate the activation of inflammasomes and then inhibit inflammation as previously described. Our study attempts to explore the relationship between autophagy and PTX-mediated regulation of inflammasome suppression. Macrophage-like RAW264.7 cells were studied as the in vitro macrophage model. We investigated the anti-inflammatory effect caused by PTX with time and dose response against the LPS-induced inflammatory factors (TNF-α, IL-1β). Western blot detected the levels of autophagy-related proteins Beclin-1 and LC3, as well as the signal pathways of AMPK and p-AMPK. Fluorescence microscope and transmission electron microscope were used to observe the autophagy bodies in cells influenced by PTX. The autophagy in cells inhibited by PTX exhibited dose- and time-dependent effects, and PTX alleviated LPS-induced inflammation caused by retarded autophagy. Furthermore, in RAW264.7 macrophage cells, our data indicated that AMPK signaling perhaps functioned importantly in repressed autophagy. In addition, in RAW264.7 macrophages, our data suggested that AMPK signaling might play an important role in inhibiting autophagy during the process of PTX ameliorating LPS-mediated inflammation.

scholarly journals Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives

2020 ◽  
Vol 67 (4) ◽  
pp. 1139-1147
Author(s):  
Fatih Tok ◽  
Bedia Koçyiğit-Kaymakçıoğlu
Keyword(s):  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Spectroscopic Methods ◽  
Design Synthesis ◽  
Reference Drug ◽  
Ic50 Values ◽  
Adme Properties ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 μM) and their IC50 values were in the range of 0.68 and 4.45 μM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski’s and Veber’s rules.

scholarly journals Hydrolase-treated royal jelly attenuates LPS-induced inflammation and IgE-antigen-mediated allergic reaction

2020 ◽  
Vol 10 (3) ◽  
pp. 127
Author(s):  
Worrapanit Chansuwan ◽  
Matthawan Khamhae ◽  
Nualpun Sirinupong
Keyword(s):  
Allergic Reaction ◽  
Royal Jelly ◽  
Inflammatory Activity ◽  
Severe Allergic Reaction ◽  
Degree Of Hydrolysis ◽  
No Production ◽  
Human Beings ◽  
Macrophage Cells ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage

Background: Royal jelly (RJ) is one of the most effectual and beneficial remedies for human beings and currently utilized in many sectors, ranging from the pharmaceutical and food industries to cosmetic and manufacturing sectors due to RJ possessing many bio-therapeutical activities including anti-tumor, antimicrobial and antioxidant activities, vasodilative and hypotensive activities, as well as growth-stimulating, infection-preventing, anti-hypercholesterolemic and anti-inflammatory activities. However, some reports showing direct consumption of RJ can lead to severe allergic reaction and has been linked with acute asthma, dermatitis, and life-threatening anaphylaxis. Thus, this research purposes to explore the potential anti-inflammatory and anti-allergic activities of hydrolyzed RJ as a function of enzyme and the extent of hydrolysis.Methods: RJ was enzymatically hydrolyzed with three commercial enzymes (AlcalaseÒ, FlavourzymeÒ and ProtamexÒ). Anti-inflammatory activity of the hydrolysates was measured by their inhibitory effect on nitric oxide (NO) production of lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Anti-allergy was determined from the ability of the hydrolysates to inhibit b-hexsosaminidase (b-HEX) release from RBL-2H3 mast cells. Cytotoxicity was also investigated in both RAW264.7 macrophage cells and RBL-2H3 mast cells.Results: The electrophoretic profiles indicated that AlcalaseÒ and FlavourzymeÒ hydrolysates did not show the presence of proteins causing allergic reaction after 60 mins of hydrolysis while these allergens disappeared from ProtamexÒ hydrolysate at the hydrolysis time of 240 min. It was observed that hydrolyzed RJ showed no toxicity on RAW264.7 and RBL-2H3 cells. With the progression of hydrolysis, IC50 values of NO production inhibition significantly decreased while degree of hydrolysis (DH) was increased in all hydrolyzed samples (p < 0.05). Results of b-HEX release inhibition were found in the same fashion. FlavourzymeÒ hydrolysate at the 240 min time point effectively mitigated the oxidative stress and protected DNA in a dose dependent manner.Conclusions: RJ hydrolysates from FlavourzymeÒ resulted in peptides with anti-inflammatory activity as determined by the inhibition of NO production in LPS-stimulated RAW264.7 macrophage cells and anti-allergic property as measured by the suppression of degranulation of sensitized RBL-2H3 cells. Anti-inflammatory effect may be due to their anti-oxidative capability. Inhibition of b-HEX release may be due to their membrane-stabilizing effects or/and blockade of IgE antibody binding to its receptors.Keywords: anti-inflammation, enzymatic hydrolysate, royal jelly, anti-allergy

scholarly journals 99mTc-labeled TSPO ligand CB86 targeting macrophages for rheumatoid arthritis SPECT imaging and preliminary evaluation of anti-inflammatory effect

2019 ◽  
Author(s):  
Peng Liu ◽  
Rongshui Yang ◽  
Fu Su ◽  
Zhenyu Hou ◽  
Wentao Dong ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Radiochemical Purity ◽  
Spect Imaging ◽  
Translocator Protein ◽  
Raw264.7 Cells ◽  
Macrophage Cells ◽  
Translocator Protein 18 Kda ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage

Abstract Background and Objective TSPO (translocator protein, 18 kDa) is up-regulated in activated macrophages, and serves as an attractive target for macrophages molecular imaging. Previous studies showed that TSPO radiotracer can visualize arthritis via positron emission tomography (PET). Compared with PET, single photon emission computed tomography (SPECT) has several advantages, such as lower cost and commercial availability. The aim of the present study is to develop the 99mTc-labeled TSPO ligand CB86 as a novel SPECT probe for imaging of rheumatoid arthritis and preliminary evaluating the effectiveness of steroid anti-inflammatory therapy. Methods A novel TSPO ligand CB86 was linked to DTPAA and then labeled with 99mTc to obtain 99mTc-DTPA-CB86. The labeling efficiency, radiochemical purity, and stability were determined in vitro. In vitro cellular uptake, efflux and binding affinity of 99mTc-DTPA-CB86 to TSPO were performed on RAW264.7 macrophage cells. The distribution and SPECT studies were conducted on Freund’s Adjuvant-Induced Left Arthritis in rats after the injection of 99mTc-DTPA-CB86 with or without co-injection of unlabeled DTPA-CB86. Result The radiosynthesis of 99mTc-DTPA-CB86 was completed successfully with the labeling yields and radiochemical purity of 95.86 ± 2.45 % and 97.45 ± 0.69 %, respectively. 99mTc-DTPA-CB86 displayed good stability, which the radiochemical purity was more than > 90%, in the saline or mouse serum at 4 h. It also exhibited high specific TSPO binging in RAW264.7 macrophage cells in vitro. The highest uptake ratio was (36.45 ± 2.18) % at 3 h after incubation, and decreased significantly after adding excessive unlabeled DTPA-CB86. 99mTc-DTPA-CB86 bound to TSPO with low nanomolar affinity (IC50 =0.49 nM) in RAW264.7 cells. The cell efflux study showed that 99mTc-DTPA-CB86 has good cell retention by RAW264.7 cells, with only about 13.99 % (decreased from (33.31 ± 2.34) % to (19.32 ± 2.01) % of total input radioactivity) of 99mTc-DTPA-CB86 efflux observed during 4.5 h to 8 h incubation. Biodistribution studies showed the left inflammatory ankle uptake was 2.35±0.10 %ID/g, and the inflammatory ankle to muscle ratio was 3.01 ± 0.09 at 180 min after injection. Small animal SPET imaging studies revealed that 99mTc-DTPA-CB86 could clearly identify left inflammatory ankle with good contrast at 30-180 min after injection. Uptake of 99mTc-DTPA-CB86 in the inflammatory ankles could be largely blocked by an excess of unlabled DTPA-CB86. Furthermore, 99mTc-DTPA-CB86 accumulation in the left inflammatory ankles significantly decreased in RA rats treated with dexamethasone. Conclusion 99mTc-DTPA-CB86 can be readily synthesized, clearly visualized arthritis with low background and monitor therapy response of anti-inflammatory therapy, suggesting its potential as a novel promising molecular probe targeting TSPO for arthritic SPECT imaging. Key words TSPO (translocator protein, 18 kDa); Technetium radioisotope; SPECT imaging; Rheumatoid arthritis; Macrophages; Glucocorticoids.

Flavonolignan 2, 3-dehydroderivatives from Oenanthe javanica and their anti inflammatory activities

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Rong-Rui Wei ◽  
Qin-Ge Ma
Keyword(s):  
Data Analysis ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Macrophage Cells ◽  
Oenanthe Javanica ◽  
Anti Inflammatory ◽  
New Compounds ◽  
First Time ◽  
Raw264.7 Macrophage

Abstract Flavonolignans, for example, silymarin and silybin, have interesting biological activities. For the first time, three new flavonolignans named oenanthenoid A-C (1–3) and nine known flavonolignan derivatives (4–12) were isolated from Oenanthe javanica. Comprehensive spectroscopic data analysis and references were used to identify all of the compounds. The anti inflammatory activities of these isolates (1–12) on RAW264.7 macrophage cells were investigated. Three new compounds (1–3) demonstrated anti inflammatory activity with IC50 values ranging from 6.5 ± 0.6 to 14.7 ± 1.6 µM. Furthermore, two compounds (11 and 12) demonstrated moderate anti inflammatory activity, with IC50 values ranging from 24.1 ± 1.2 to 62.5 ± 1.9 µM.

scholarly journals Anti-Inflammatory Activity of the Wild Mushroom, Echinodontium tinctorium, in RAW264.7 Macrophage Cells and Mouse Microcirculation

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3509 ◽  
Author(s):  
Sumreen Javed ◽  
Wai Ming Li ◽  
Mehreen Zeb ◽  
Almas Yaqoob ◽  
Linda E. Tackaberry ◽  
...  
Keyword(s):  
British Columbia ◽  
Average Molecular Weight ◽  
Water Soluble ◽  
Size Exclusion ◽  
Inflammatory Activity ◽  
Modern World ◽  
Wild Mushroom ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage

The aim of this study was to investigate the anti-inflammatory activity of a previously un-studied wild mushroom, Echinodontium tinctorium, collected from the forests of north-central British Columbia. The lipopolysaccharide (LPS)-induced RAW264.7 macrophage model was used to study the in vitro anti-inflammatory activity. The crude alkaline extract demonstrated potent anti-inflammatory activity, and was further purified using a “bio-activity-guided-purification” approach. The size-exclusion and ion-exchange chromatography yielded a water-soluble anti-inflammatory polysaccharide (AIPetinc). AIPetinc has an average molecular weight of 5 kDa, and is a heteroglucan composed of mainly glucose (88.6%) with a small amount of galactose (4.0%), mannose (4.4%), fucose (0.7%), and xylose (2.3%). In in vivo settings, AIPetinc restored the histamine-induced inflammatory event in mouse gluteus maximus muscle, thus confirming its anti-inflammatory activity in an animal model. This study constitutes the first report on the bioactivity of Echinodontium tinctorium, and highlights the potential medicinal benefits of fungi from the wild forests of northern British Columbia. Furthermore, it also reiterates the need to explore natural resources for alternative treatment to modern world diseases.

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