scholarly journals Anti-inflammatory Strategies for Schizophrenia: A Review of Evidence for Therapeutic Applications and Drug Repurposing

2020 ◽  
Vol 18 (1) ◽  
pp. 10-24 ◽  
Author(s):  
Jonghee Hong ◽  
Minji Bang
Keyword(s):  
Drug Repurposing ◽  
Therapeutic Applications ◽  
Anti Inflammatory

Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page
Keyword(s):  
Inflammatory Diseases ◽  
Therapeutic Applications ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

scholarly journals Antimicrobial Activity of Non-steroidal Anti-inflammatory Drugs on Biofilm: Current Evidence and Potential for Drug Repurposing

2021 ◽  
Vol 12 ◽  
Author(s):  
Rodrigo Cuiabano Paes Leme ◽  
Raquel Bandeira da Silva
Keyword(s):  
Bacterial Species ◽  
Drug Repurposing ◽  
Current Evidence ◽  
Pharmacokinetic Studies ◽  
Bacterial Populations ◽  
Human Pharmacokinetic ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

It has been demonstrated that some non-steroidal anti-inflammatory drugs (NSAIDs), like acetylsalicylic acid, diclofenac, and ibuprofen, have anti-biofilm activity in concentrations found in human pharmacokinetic studies, which could fuel an interest in repurposing these well tolerated drugs as adjunctive therapies for biofilm-related infections. Here we sought to review the currently available data on the anti-biofilm activity of NSAIDs and its relevance in a clinical context. We performed a systematic literature review to identify the most commonly tested NSAIDs drugs in the last 5 years, the bacterial species that have demonstrated to be responsive to their actions, and the emergence of resistance to these molecules. We found that most studies investigating NSAIDs’ activity against biofilms were in vitro, and frequently tested non-clinical bacterial isolates, which may not adequately represent the bacterial populations that cause clinically-relevant biofilm-related infections. Furthermore, studies concerning NSAIDs and antibiotic resistance are scarce, with divergent outcomes. Although the potential to use NSAIDs to control biofilm-related infections seems to be an exciting avenue, there is a paucity of studies that tested these drugs using appropriate in vivo models of biofilm infections or in controlled human clinical trials to support their repurposing as anti-biofilm agents.

scholarly journals Reinforcing the Supply Chain of Umifenovir and Other Antiviral Drugs with Retrosynthetic Software

2021 ◽  
Author(s):  
Yingfu Lin ◽  
Zirong Zhang ◽  
Babak Mahjour ◽  
Di Wang ◽  
Rui Zhang ◽  
...  
Keyword(s):  
Supply Chain ◽  
Supply Chains ◽  
Raw Materials ◽  
Antiviral Drug ◽  
Drug Repurposing ◽  
Antiviral Drugs ◽  
Multiple Drug ◽  
General Strategy ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Abstract The global disruption caused by the 2020 coronavirus pandemic stressed the supply chain of many products, including pharmaceuticals. Multiple drug repurposing studies for COVID-19 are now underway. If a winning therapeutic emerges, it is unlikely that the existing inventory of the medicine, or even the chemical raw materials needed to synthesize it, will be available in the quantities required. We used retrosynthetic software to arrive at alternate chemical supply chains for the antiviral drug umifenovir, as well as eleven other antiviral and anti-inflammatory drugs. We have experimentally validated four routes to umifenovir and one route to bromhexine. In several instances, the software utilizes C–H functionalization logic, and one route to umifenovir employs functionalization of six C–H bonds. The general strategy we apply can be used to identify distinct starting materials, and relieve stress on existing supply chains.

scholarly journals Mycophenolate suppresses inflammation by inhibiting prostaglandin synthases: a study of molecular and experimental drug repurposing

PeerJ ◽  
2021 ◽  
Vol 9 ◽  
pp. e11360
Author(s):  
Fahad Al-Hizab ◽  
Mahmoud Kandeel
Keyword(s):  
Root Mean Square ◽  
Inflammatory Diseases ◽  
Drug Repurposing ◽  
Inflammatory Cells ◽  
Acid Synthesis ◽  
Mean Square ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Mycophenolate mofetil is an established anti-proliferative and immune-suppressive agent that minimizes the proliferation of inflammatory cells by interfering with nucleic acid synthesis. Herein, we report our discovery of the prostaglandin inhibiting properties of MMF, which offers new applications for the drug in the treatment of inflammatory diseases. The estimated values of IC50MMFCOX-1, IC50MMFCOX-2, and IC50MMF5-LOX were 5.53, 0.19, and 4.47 µM, respectively. In contrast, mycophenolic acid (MPA) showed slightly stronger inhibition: IC50MPACOX-1, IC50MPACOX-2, and IC50MPA5-LOX were 4.62, 0.14, and 4.49 µM, respectively. These results indicate that MMF and MPA are, respectively, 28.6 and 33 times more selective for cyclooxygenase-2 than for cyclooxygenase-1, which implies that MMF would have less impact on the gastric mucosa than most nonselective, nonsteroidal anti-inflammatory drugs. Furthermore, MMF provided dose-dependent relief of acute inflammation in the carrageenan-induced rat paw edema test, with results comparable to those of celecoxib and indomethacin. Molecular dynamics simulations indicated that the MMF bond with COX-2 was stable, as evidenced by a low root-mean-square deviation of atomic positions, complementary per-residue root-mean-square fluctuation, and 0–4 hydrogen bonds during the 50-ns simulation time. Therefore, MMF provides immune-suppressing, cyclooxygenase-inhibiting, and inflammation-relieving properties. Our results indicate that MMF can be 1) repositioned for inflammation treatment without the need for further expensive clinical trials, 2) used for local acute inflammations, and 3) used as a sparing agent for other steroid and non-steroid anti-inflammatory medications, especially in topical applications.

scholarly journals Molecular Basis of the Therapeutical Potential of Clove (Syzygium aromaticum L.) and Clues to Its Anti-COVID-19 Utility

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1880
Author(s):  
Caterina Vicidomini ◽  
Valentina Roviello ◽  
Giovanni N. Roviello
Keyword(s):  
Potential Role ◽  
Folk Medicine ◽  
Drug Repurposing ◽  
Syzygium Aromaticum ◽  
Traditional Medicines ◽  
Antithrombotic Effects ◽  
Ancient Times ◽  
Anti Inflammatory ◽  
Problem Drug

The current COronaVIrus Disease 19 (COVID-19) pandemic caused by SARS-CoV-2 infection is enormously affecting the worldwide health and economy. In the wait for an effective global immunization, the development of a specific therapeutic protocol to treat COVID-19 patients is clearly necessary as a short-term solution of the problem. Drug repurposing and herbal medicine represent two of the most explored strategies for an anti-COVID-19 drug discovery. Clove (Syzygium aromaticum L.) is a well-known culinary spice that has been used for centuries in folk medicine in many disorders. Interestingly, traditional medicines have used clove since ancient times to treat respiratory ailments, whilst clove ingredients show antiviral and anti-inflammatory properties. Other interesting features are the clove antithrombotic, immunostimulatory, and antibacterial effects. Thus, in this review, we discuss the potential role of clove in the frame of anti-COVID-19 therapy, focusing on the antiviral, anti-inflammatory, and antithrombotic effects of clove and its molecular constituents described in the scientific literature.

scholarly journals 91 Overlapping effects of MI-R-21 inhibition and oral anti-fibrotic and anti-inflammatory drugs: rationale for drug repurposing to relieve ischemia/reperfusion injury

2020 ◽  
Vol 22 (Supplement_N) ◽  
pp. N83-N79
Author(s):  
Alberto Aimo ◽  
Oriol Iborra Egea ◽  
Michele Emdin ◽  
Antoni Bayes-Genis
Keyword(s):  
Target Genes ◽  
Cardiac Fibrosis ◽  
Ischemia Reperfusion Injury ◽  
Ischemia Reperfusion ◽  
Biological Significance ◽  
Drug Repurposing ◽  
Published Data ◽  
St Segment Elevation ◽  
Network Analyses ◽  
Anti Inflammatory

Abstract Aims Reperfusion strategies have reduced the mortality of ST-segment elevation myocardial infarction (STEMI), but ischemia/reperfusion (I/R) injury still represents an important issue, and the prevalence of heart failure (HF) after STEMI is raising. Intracoronary infusion of miR-21 inhibitors after reperfusion has been reported to reduce cardiac fibrosis and hypertrophy and improve cardiac function in pigs. Possible drawbacks of miR-21 inhibitors are their high costs and the need for intracoronary administration. Oral drugs with anti-fibrotic or anti-inflammatory actions could have similar effects on protein expression than miR-21 inhibition. We examined the 2 drugs approved for idiopathic pulmonary fibrosis (nintedanib and pirfenidone) and colchicine, which is being evaluated for the prevention of adverse ventricular remodelling after STEMI (NCT03156816). Methods and results We identified the regulatory profile of miR-21 (588 target genes). Only 99 of these interactions were supported by robust experimental data (i.e., information from reporter gene assays), and were then considered for further examination. The biological significance of these 99 targets was evaluated through over-representation analysis, and 13 genes were identified as potentially related to cardiovascular diseases. We retrieved all known targets and main downstream interactions of nintedanib, pirfenidone and colchicine (source: www.drugbank.ca). We cross-validated these datasets by using neural network analyses to search for protein-protein interactions, focusing on those shared by miR-21 inhibition and each one of the 3 drugs. Nintedanib and miR-21 inhibition shared many targets, which could indicate overlapping mechanisms of action. The proto-oncogene SRC, which participates in gene transcription, immune response, apoptosis and migration, emerged as the leading signaling effector. By blocking SRC expression and many downstream effectors of SRC, as well as platelet derived growth factor, nintedanib could decreased miR-21 expression. The molecular effects of nintedanib include an inhibition of inflammation, fibrosis and angiogenesis, and then ultimately a relief from I/R injury, in a similar fashion than anti-miR-21. Contrary to nintedanib, no overlap between the effects of pirfenidone and miR-21 inhibition was found. Conversely, colchicine seems to determine an indirect blockade of the important pro-inflammatory signaling pathway AKT/NFKB, similarly to miR-21 inhibition. Colchicine has also been proposed to inhibit SRC, but few published data are available. Conclusion miR-21 inhibition is emerging as a potential treatment for I/R cardiac injury, but its applicability in clinical practice is burdened by several limitations. Drug repurposing could aid this situation by mimicking the molecular activity of miR-21 inhibition. Through a bioinformatic approach, we found that nintedanib could exert beneficial effects similar to those reported for miR-21 inhibition, with a lower degree of overlap between the effects of colchicine and anti-miR-21. If confirmed by experimental evidence, nintedanib or colchicine could enter the stage of clinical trials to assess their efficacy as cardioprotective therapies in human patients with STEMI.

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