Quercetin and its relative therapeutic potential against COVID-19: A retrospective review and prospective overview

2020 ◽  
Vol 20 ◽  
Author(s):  
Saiyad Bastaminejad ◽  
Salar Bakhtiyari
Keyword(s):  
Interleukin 6 ◽  
Retrospective Review ◽  
Therapeutic Potential ◽  
Symptomatic Treatment ◽  
Emerging Disease ◽  
Global Community ◽  
Major Threat ◽  
Main Challenge

: COVID-19 is an emerging disease that is a major threat to the global community. The main challenge in this disease is the lack of proper or proven medication. The drugs used to treat this disease are only for symptomatic treatment. Studies of other coronaviruses, such as SARS and MERS, suggest that quercetin has sufficient potential to treat COVID-19. Previous studies have shown that quercetin reduces the entry of the virus into the cell by blocking the ACE2 receptor, as well as reducing the level of interleukin-6 in SARS and MERS patients. Therefore, the aim of this review was to scrutinize the potential of quercetin as a drug in the treatment of COVID-19 from a molecular perspective.

Physicochemical Characterization and Antinociceptive Effect of β-cyclodextrin/Lippia pedunculosa Essential Oil in Mice

2018 ◽  
Vol 18 (9) ◽  
pp. 797-807 ◽  
Author(s):  
Paula dos Passos Menezes ◽  
Francielly de Oliveira Araujo ◽  
Tatianny Araujo Andrade ◽  
Igor Araujo Santos Trindade ◽  
Heitor Gomes de Araujo-Filho ◽  
...  
Keyword(s):  
Essential Oil ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Physicochemical Characterization ◽  
Good Tool ◽  
Main Challenge ◽  
Higher Temperature

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.

Understanding Bakanae: a major threat and an emerging disease of Basmati rice

2018 ◽  
Vol 72 (4) ◽  
pp. 599-605
Author(s):  
Anita Puyam ◽  
P. P. S. Pannu ◽  
Jaspal Kaur ◽  
Shikha Sethi ◽  
Kiranjot Kaur
Keyword(s):  
Emerging Disease ◽  
Basmati Rice ◽  
Major Threat

scholarly journals Therapeutic potential of ivermectin as add on treatment in COVID 19: A systematic review and meta-analysis

2020 ◽  
Vol 23 ◽  
pp. 462-469
Author(s):  
Biswa Mohan Padhy ◽  
Rashmi Ranjan Mohanty ◽  
Smita Das ◽  
Bikash Ranjan Meher
Keyword(s):  
Systematic Review ◽  
Therapeutic Potential ◽  
Meta Analysis ◽  
Random Effect ◽  
Random Effect Model ◽  
Symptomatic Treatment ◽  
Effect Model ◽  
Usual Therapy

The current management of COVID-19 is mostly limited to general supportive care and symptomatic treatment. Ivermectin is a broad-spectrum anti-parasitic drug used widely for the treatment of onchocerciasis and lymphatic filariasis. Apart from its anti-parasitic effect it also exhibits antiviral activity against a number of viruses both in vitro and in vivo. Hence, we conducted this systematic review and meta-analysis to assess the currently available data on the therapeutic potential of ivermectin for the treatment of COVID‐19 as add on therapy. A total of 629 patients were included in the 4 studies and all were COVID-19 RT-PCR positive. Among them, 397 patients received ivermectin along with usual therapy. The random effect model showed the overall pooled OR to be 0.53 (95%CI: 0.29 to0.96) for the primary outcome (all-cause mortality) which was statistically significant (P=0.04). Similarly, the random effect model revealed that adding ivermectin led to significant clinical improvement compared to usual therapy (OR=1.98, 95% CI: 1.11 to 3.53, P=0.02).  However, this should be inferred cautiously as the quality of evidence is very low. Currently, many clinical trials are on-going, and definitive evidence for repurposing this drug for COVID-19 patients will emerge only in the future.

Therapeutic potential of interleukin-6 antagonism in bipolar disorder

2011 ◽  
Vol 76 (1) ◽  
pp. 21-23 ◽  
Author(s):  
E. Brietzke ◽  
M. Scheinberg ◽  
B. Lafer
Keyword(s):  
Bipolar Disorder ◽  
Interleukin 6 ◽  
Therapeutic Potential

Microwell Geometry Modulates Interleukin-6 Secretion in Human Mesenchymal Stem Cells

MRS Advances ◽  
2017 ◽  
Vol 2 (47) ◽  
pp. 2561-2570
Author(s):  
Xun Xu ◽  
Weiwei Wang ◽  
Zhengdong Li ◽  
Karl Kratz ◽  
Nan Ma ◽  
...  
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Interleukin 6 ◽  
Therapeutic Potential ◽  
Chemical Properties ◽  
Human Mesenchymal Stem Cells ◽  
Secretion Profile ◽  
Highly Sensitive ◽  
Physical And Chemical ◽  
Cell Culture Substrate

ABSTRACTThe therapeutic effect of mesenchymal stem cells (MSCs) has been investigated in various clinical applications, in which their functional benefits are mainly attributed to the secretion of soluble factors. The enhancement of their therapeutic potential by physical and chemical properties of cell culture substrate is a safe and effective strategy, since they are highly sensitive to their microenvironment such as the elasticity and surface topography. In this study, we demonstrated that the geometry of polymeric substrate regulated the interleukin-6 (IL-6) secretion of human adipose derived MSCs. Polystyrene substrates comprising arrays of square-shaped (S50) or round-shaped (R50) microwells (side length or diameter of 50 μm and depth of 10 μm) were prepared by injection molding. Cellular apoptototic rate of MSCs was not affected by the microwell geometry, while the upregulated secretion of IL-6 and the enhancement of nuclear transcription factor STAT3 were detected in MSCs seeded on S50 substrate. The geometry-dependent modulatory effect was highly associated with ROCK signaling cascade. The inhibition of ROCK abolished the disparity in IL-6 secretion. These findings highlight the possibility to steer the secretion profile of stem cells via microwell geometry in combination with the manipulation of ROCK signaling pathway.

scholarly journals Broad Kinase Inhibition Mitigates Early Neuronal Dysfunction in Tauopathy

2021 ◽  
Vol 22 (3) ◽  
pp. 1186 ◽  
Author(s):  
Shon A. Koren ◽  
Matthew J. Hamm ◽  
Ryan Cloyd ◽  
Sarah N. Fontaine ◽  
Emad Chishti ◽  
...  
Keyword(s):  
Quantitative Proteomics ◽  
Molecular Mechanisms ◽  
Kinase Inhibitor ◽  
Therapeutic Potential ◽  
Early Stage ◽  
Symptomatic Treatment ◽  
Cognitive Outcomes ◽  
Proteomics Data ◽  
Progressive Neurodegeneration ◽  
Cellular Dysfunction

Tauopathies are a group of more than twenty known disorders that involve progressive neurodegeneration, cognitive decline and pathological tau accumulation. Current therapeutic strategies provide only limited, late-stage symptomatic treatment. This is partly due to lack of understanding of the molecular mechanisms linking tau and cellular dysfunction, especially during the early stages of disease progression. In this study, we treated early stage tau transgenic mice with a multi-target kinase inhibitor to identify novel substrates that contribute to cognitive impairment and exhibit therapeutic potential. Drug treatment significantly ameliorated brain atrophy and cognitive function as determined by behavioral testing and a sensitive imaging technique called manganese-enhanced magnetic resonance imaging (MEMRI) with quantitative R1 mapping. Surprisingly, these benefits occurred despite unchanged hyperphosphorylated tau levels. To elucidate the mechanism behind these improved cognitive outcomes, we performed quantitative proteomics to determine the altered protein network during this early stage in tauopathy and compare this model with the human Alzheimer’s disease (AD) proteome. We identified a cluster of preserved pathways shared with human tauopathy with striking potential for broad multi-target kinase intervention. We further report high confidence candidate proteins as novel therapeutically relevant targets for the treatment of tauopathy. Proteomics data are available via ProteomeXchange with identifier PXD023562.

The therapeutic potential of interleukin-6 hyperagonists and antagonists

1997 ◽  
Vol 6 (3) ◽  
pp. 237-266 ◽  
Author(s):  
Kari-Josef Kallen ◽  
Karl-Hermann Meyer zum Büschenfelde ◽  
Stefan Rose-John
Keyword(s):  
Interleukin 6 ◽  
Therapeutic Potential

scholarly journals Identification of Mutations Conferring Tryptanthrin Resistance to Mycobacterium smegmatis

Antibiotics ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 6
Author(s):  
Svetlana G. Frolova ◽  
Ksenia M. Klimina ◽  
Ravinder Kumar ◽  
Aleksey A. Vatlin ◽  
Deepak B. Salunke ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Transcriptional Regulator ◽  
Test System ◽  
Comparative Genomic ◽  
Promising Alternative ◽  
Main Challenge

Tuberculosis (TB), caused by Mycobacterium tuberculosis, is a global burden, responsible for over 1 million deaths annually. The emergence and spread of drug-resistant M. tuberculosis strains (MDR-, XDR- and TDR-TB) is the main challenge in global TB-control, requiring the development of novel drugs acting on new biotargets, thus able to overcome the drug-resistance. Tryptanthrin is a natural alkaloid, with great therapeutic potential due to its simple way of synthesis and wide spectrum of biological activities including high bactericidal activity on both drug-susceptible and MDR M. tuberculosis strains. InhA was suggested as the target of tryptanthrins by in silico modeling, making it a promising alternative to isoniazid, able to overcome drug resistance provided by katG mutations. However, neither the mechanism of action of tryptanthrin nor the mechanism of resistance to tryptanthrins was ever confirmed in vitro. We show that the MmpS5-MmpL5 efflux system is able to provide resistance to tryptanthrins using an in-house test-system. Comparative genomic analysis of spontaneous tryptanthrin-resistant M. smegmatis mutants showed that mutations in MSMEG_1963 (EmbR transcriptional regulator) lead to a high-level resistance, while those in MSMEG_5597 (TetR transcriptional regulator) to a low-level one. Mutations in an MFS transporter gene (MSMEG_4427) were also observed, which might be involved in providing a basal level of tryptanthrins-resistance.

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