05 / Anti-inflammatory functionalized membrane for periodontal regeneration: in vivo evaluation in periodontitis-induced mouse model

Selenium (Se) as an essential micronutrient that has implications in human diseases, including inflammatory bowel disease (IBD), especially with respect to Se deficiencies. Recently, selenium nanoparticles (SeNPs) have attracted significant...

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TAK1/AP-1-Targeted Anti-Inflammatory Effects of Barringtonia augusta Methanol Extract

Molecules ◽

10.3390/molecules26103053 ◽

2021 ◽

Vol 26 (10) ◽

pp. 3053

Author(s):

Anh Thu Ha ◽

Mi-Yeon Kim ◽

Jae Youl Cho

Keyword(s):

Mouse Model ◽

Methanol Extract ◽

Folk Medicine ◽

Activator Protein 1 ◽

Western Blot Assay ◽

In Vivo Experiments ◽

Chemokine Ligand ◽

Anti Inflammatory ◽

Inflammatory Effect

Barringtonia augusta methanol extract (Ba-ME) is a folk medicine found in the wetlands of Thailand that acts through an anti-inflammatory mechanism that is not understood fully. Here, we examine how the methanol extract of Barringtonia augusta (B. augusta) can suppress the activator protein 1 (AP-1) signaling pathway and study the activities of Ba-ME in the lipopolysaccharide (LPS)-treated RAW264.7 macrophage cell line and an LPS-induced peritonitis mouse model. Non-toxic concentrations of Ba-ME downregulated the mRNA expression of cytokines, such as cyclooxygenase and chemokine ligand 12, in LPS-stimulated RAW264.7 cells. Transfection experiments with the AP-1-Luc construct, HEK293T cells, and luciferase assays were used to assess whether Ba-ME suppressed the AP-1 functional activation. A Western blot assay confirmed that C-Jun N-terminal kinase is a direct pharmacological target of Ba-ME action. The anti-inflammatory effect of Ba-ME, which functions by β-activated kinase 1 (TAK1) inhibition, was confirmed by using an overexpression strategy and a cellular thermal shift assay. In vivo experiments in a mouse model of LPS-induced peritonitis showed the anti-inflammatory effect of Ba-ME on LPS-stimulated macrophages and acute inflammatory mouse models. We conclude that Ba-ME is a promising anti-inflammatory drug targeting TAK1 in the AP-1 pathway.

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Ketorolac-dextran conjugates: Synthesis, in vitro and in vivo evaluation

Acta Pharmaceutica ◽

10.2478/v10007-007-0035-3 ◽

2007 ◽

Vol 57 (4) ◽

pp. 441-450 ◽

Cited By ~ 12

Author(s):

Savita Vyas ◽

Piyush Trivedi ◽

Subhash Chaturvedi

Keyword(s):

Human Plasma ◽

Parent Drug ◽

Aqueous Solubility ◽

Spectrophotometric Analysis ◽

In Vivo Evaluation ◽

Gastrointestinal Side Effects ◽

Molecular Masses ◽

Anti Inflammatory

Ketorolac-dextran conjugates: Synthesis,in vitroandin vivoevaluationKetorolac is a non-steroidal anti-inflammatory drug. Dextran conjugates of ketorolac (KD) were synthesized and characterized to improve ketorolac aqueous solubility and reduce gastrointestinal side effects. An N-acylimidazole derivative of ketorolac (KAI) was condensed with a model carrier polymer, dextran of different molecular masses (40000, 60000, 110000 and 200000). IR spectral data confirmed formation of ester bonding. Ketorolac contents were evaluated by UV-spectrophotometric analysis. The molecular mass was determined by measuring viscosity using the Mark-Howink-Sakurada equation. Invitrohydrolysis studies were performed in aqueous buffers (pH 1.2, 7.4, 9) and in 80% (V/V) human plasma (pH 7.4). At pH 9, a higher rate of ketorolac release from KD was observed as compared to aqueous buffer of pH 7.4 and 80% human plasma (pH 7.4), following first-order kinetics.In vivobiological screening in mice and rats indicated that conjugates retained analgesic and anti-inflammatory activities with significantly reduced ulcerogenicity compared to the parent drug.

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Antihyperuricemic, Anti-Inflammatory and Antihypertensive Effect of a Dry Extract from Solidago virgaurea L. (Asteraceae)

Scientia Pharmaceutica ◽

10.3390/scipharm89020027 ◽

2021 ◽

Vol 89 (2) ◽

pp. 27

Author(s):

Mircea Tămaş ◽

Oliviu Vostinaru ◽

Loredana Soran ◽

Ildiko Lung ◽

Ocsana Opris ◽

...

Keyword(s):

Blood Pressure ◽

Rat Model ◽

Antihypertensive Effect ◽

Chemical Constituents ◽

In Vivo Evaluation ◽

Dry Extract ◽

The Balkans ◽

Solidago Virgaurea ◽

Anti Inflammatory

Solidago virgaurea L. is a perennial plant used in European traditional medicine as a diuretic or a remedy for inflammatory conditions of the urinary tract but also for gout, especially in the Balkans. The present study was focused on a preclinical, in vivo evaluation of antihyperuricemic, anti-inflammatory, and antihypertensive effects of a dry extract from S. virgaurea L. (ESV). Colorimetric and HPLC–MS techniques were used to identify the main chemical constituents of ESV. Antihyperuricemic effect of ESV was assessed in a rat model of hyperuricemia induced by the administration of potassium oxonate. Antihypertensive effect of ESV was evaluated in hyperuricemic rats by monitoring systolic blood pressure with a non-invasive blood-pressure recording system. The anti-inflammatory effect of ESV was tested using a rat model of paw edema. The main chemical constituents of ESV were rutin and phenolic acids represented by chlorogenic and caffeic acid. ESV demonstrated significant antihyperuricemic effects in rats due to an uricosuric mechanism. Additionally, ESV reduced the progression of arterial hypertension in hyperuricemic rats and also showed anti-inflammatory properties slightly inferior to diclofenac. The results suggest that ESV could be a natural remedy for the treatment of gout and protection against endothelial dysfunction caused by hyperuricemia.

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472 Anti-inflammatory actions of phosphatidyl glycerol and its precursor glycerol in vitro and in an in vivo mouse model of psoriasis

Journal of Investigative Dermatology ◽

10.1016/j.jid.2017.02.491 ◽

2017 ◽

Vol 137 (5) ◽

pp. S81

Author(s):

V. Choudhary ◽

V. Custer ◽

I. Kaddour-Djebbar ◽

W.B. Bollag

Keyword(s):

Mouse Model ◽

Phosphatidyl Glycerol ◽

Anti Inflammatory

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Modulation of Glial Responses by Furanocembranolides: Leptolide Diminishes Microglial Inflammation in Vitro and Ameliorates Gliosis In Vivo in a Mouse Model of Obesity and Insulin Resistance

Marine Drugs ◽

10.3390/md18080378 ◽

2020 ◽

Vol 18 (8) ◽

pp. 378

Author(s):

Miriam Corraliza-Gómez ◽

Amalia B. Gallardo ◽

Ana R. Díaz-Marrero ◽

José M. de la Rosa ◽

Luis D’Croz ◽

...

Keyword(s):

Mouse Model ◽

Microglial Cells ◽

Obese Mouse ◽

Neurodegenerative Process ◽

Age Related ◽

Bv2 Cells ◽

Anti Inflammatory ◽

Inflammatory Molecules

Neurodegenerative diseases are age-related disorders caused by progressive neuronal death in different regions of the nervous system. Neuroinflammation, modulated by glial cells, is a crucial event during the neurodegenerative process; consequently, there is an urgency to find new therapeutic products with anti-glioinflammatory properties. Five new furanocembranolides (1−5), along with leptolide, were isolated from two different extracts of Leptogorgia sp., and compound 6 was obtained from chemical transformation of leptolide. Their structures were determined based on spectroscopic evidence. These seven furanocembranolides were screened in vitro by measuring their ability to modulate interleukin-1β (IL-1β) production by microglial BV2 cells after LPS (lipopolysaccharide) stimulation. Leptolide and compounds 3, 4 and 6 exhibited clear anti-inflammatory effects on microglial cells, while compound 2 presented a pro-inflammatory outcome. The in vitro results prompted us to assess anti-glioinflammatory effects of leptolide in vivo in a high-fat diet-induced obese mouse model. Interestingly, leptolide treatment ameliorated both microgliosis and astrogliosis in this animal model. Taken together, our results reveal a promising direct biological effect of furanocembranolides on microglial cells as bioactive anti-inflammatory molecules. Among them, leptolide provides us a feasible therapeutic approach to treat neuroinflammation concomitant with metabolic impairment.

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