Cordycepin and its nucleoside analogs for the treatment of systemic COVID-19 infection

Coronaviruses ◽  
2021 ◽  
Vol 02 ◽  
Author(s):  
Chellapandi P ◽  
Saranya S
Keyword(s):  
Nucleoside Analogs ◽  
Drug Candidate ◽  
Rnase L ◽  
Structural Genomic ◽  
Human Rnase ◽  
Medicinal Fungi ◽  
Anti Inflammatory ◽  
The Individual ◽  
Human Viruses ◽  
Anti Inflammation

: Coronavirus disease (COVID-19) pandemic is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a new coronavirus isolated from Wuhan, China. It is a global health emergency, and there is no effective antiviral therapeutics available to date. Continuous structural genomic insights of SARS-CoV-2 proteins provide a warranty for the development of rational-based antivirals. Nevertheless, a structure-based drug candidate with multiple therapeutic actions would be a practical choice of medication in the treatment of severe COVID-19 patients. Cordycepin from medicinal fungi (Cordyceps spp.) and its nucleoside analogs targeting viral RNA-dependent RNA polymerase and human RNase L have potent antiviral activity against various human viruses with additional immunomodulatory and anti-inflammatory effects. Anti-inflammation treatment is of pivotal importance and should be timely tailored to the individual patient along with antivirals. Our perspective on the combined antiviral and anti-inflammatory effects of cordycepin and its analogs suggests them as new therapeutics in the treatment of systemic COVID-19 infection.

Anti-Inflammatory Properties of Plant Derived Natural Products – A Systematic Review

2019 ◽  
Vol 26 (24) ◽  
pp. 4506-4536 ◽  
Author(s):  
Iris E. Allijn ◽  
René P. Brinkhuis ◽  
Gert Storm ◽  
Raymond M. Schiffelers
Keyword(s):  
Systematic Review ◽  
Natural Products ◽  
Positive Control ◽  
Therapeutic Effects ◽  
Reference Compound ◽  
Individual Molecular Species ◽  
The Past ◽  
Anti Inflammatory ◽  
The Individual ◽  
Natural Medicines

Traditionally, natural medicines have been administered as plant extracts, which are composed of a mixture of molecules. The individual molecular species in this mixture may or may not contribute to the overall medicinal effects and some may even oppose the beneficial activity of others. To better control therapeutic effects, studies that characterized specific molecules and describe their individual activity that have been performed over the past decades. These studies appear to underline that natural products are particularly effective as antioxidants and anti-inflammatory agents. In this systematic review we aimed to identify potent anti-inflammatory natural products and relate their efficacy to their chemical structure and physicochemical properties. To identify these compounds, we performed a comprehensive literature search to find those studies, in which a dose-response description and a positive control reference compound was used to benchmark the observed activity. Of the analyzed papers, 7% of initially selected studies met these requirements and were subjected to further analysis. This analysis revealed that most selected natural products indeed appeared to possess anti-inflammatory activities, in particular anti-oxidative properties. In addition, 14% of the natural products outperformed the remaining natural products in all tested assays and are attractive candidates as new anti-inflammatory agents.

Activation of human RNase L by 5’-C-phosphonate-modified oligoadenylates

2014 ◽  
Author(s):  
Magdalena Petrová ◽  
Miloš Buděšínský ◽  
Eva Zborníková ◽  
Natalia Panova ◽  
Pavel Novák ◽  
...  
Keyword(s):  
Rnase L ◽  
Human Rnase

scholarly journals The Antimicrobial and Anti-Inflammatory Effects of Silver Nanoparticles Synthesised from Cotyledon orbiculata Aqueous Extract

Nanomaterials ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 1343
Author(s):  
Caroline Tyavambiza ◽  
Abdulrahman Mohammed Elbagory ◽  
Abram Madimabe Madiehe ◽  
Mervin Meyer ◽  
Samantha Meyer
Keyword(s):  
Staphylococcus Aureus ◽  
Silver Nanoparticles ◽  
Metallic Nanoparticles ◽  
Methicillin Resistance ◽  
Antimicrobial Activities ◽  
Transmission Electron ◽  
Anti Inflammatory ◽  
Anti Inflammation ◽  
Important Medicinal Plant ◽  
Pro Inflammatory Cytokines

Cotyledon orbiculata, commonly known as pig’s ear, is an important medicinal plant of South Africa. It is used in traditional medicine to treat many ailments, including skin eruptions, abscesses, inflammation, boils and acne. Many plants have been used to synthesize metallic nanoparticles, particularly silver nanoparticles (AgNPs). However, the synthesis of AgNPs from C. orbiculata has never been reported before. The aim of this study was to synthesize AgNPs using C. orbiculata and evaluate their antimicrobial and immunomodulatory properties. AgNPs were synthesized and characterized using Ultraviolet-Visible Spectroscopy (UV-Vis), Dynamic Light Scattering (DLS) and High-Resolution Transmission Electron Microscopy (HR-TEM). The antimicrobial activities of the nanoparticles against skin pathogens (Staphylococcus aureus, Staphylococcus epidermidis, Methicillin Resistance Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans) as well as their effects on cytokine production in macrophages (differentiated from THP-1 cells) were evaluated. The AgNPs from C. orbiculata exhibited antimicrobial activity, with the highest activity observed against P. aeruginosa (5 µg/mL). The AgNPs also showed anti-inflammatory activity by inhibiting the secretion of pro-inflammatory cytokines (TNF-alpha, IL-6 and IL-1 beta) in lipopolysaccharide-treated macrophages. This concludes that the AgNPs produced from C. orbiculata possess antimicrobial and anti-inflammation properties.

scholarly journals BAM15, a Mitochondrial Uncoupling Agent, Attenuates Inflammation in the LPS Injection Mouse Model: An Adjunctive Anti-Inflammation on Macrophages and Hepatocytes

2021 ◽  
pp. 1-17
Author(s):  
Cong Phi Dang ◽  
Jiraphorn Issara-Amphorn ◽  
Awirut Charoensappakit ◽  
Kanyarat Udompornpitak ◽  
Thansita Bhunyakarnjanarat ◽  
...  
Keyword(s):  
Atp Depletion ◽  
Organ Injury ◽  
Flux Analysis ◽  
Energy Status ◽  
Mitochondrial Uncoupling ◽  
Inflammatory Monocytes ◽  
Tnf Α ◽  
Cell Energy ◽  
Anti Inflammatory ◽  
Anti Inflammation

Controlof immune responses through the immunometabolism interference is interesting for sepsis treatment. Then, expression of immunometabolism-associated genes and BAM15, a mitochondrial uncoupling agent, was explored in a proinflammatory model using lipopolysaccharide (LPS) injection. Accordingly, the decreased expression of mitochondrial uncoupling proteins was demonstrated by transcriptomic analysis on metabolism-associated genes in macrophages (RAW246.7) and by polymerase chain reaction in LPS-stimulated RAW246.7 and hepatocytes (Hepa 1–6). Pretreatment with BAM15 at 24 h prior to LPS in macrophages attenuated supernatant inflammatory cytokines (IL-6, TNF-α, and IL-10), downregulated genes of proinflammatory M1 polarization (iNOS and IL-1β), upregulated anti-inflammatory M2 polarization (Arg1 and FIZZ), and decreased cell energy status (extracellular flux analysis and ATP production). Likewise, BAM15 decreased expression of proinflammatory genes (IL-6, TNF-α, IL-10, and iNOS) and reduced cell energy in hepatocytes. In LPS-administered mice, BAM15 attenuated serum cytokines, organ injury (liver enzymes and serum creatinine), and tissue cytokines (livers and kidneys), in part, through the enhanced phosphorylated αAMPK, a sensor of ATP depletion with anti-inflammatory property, in the liver, and reduced inflammatory monocytes/macrophages (Ly6C +ve, CD11b +ve) in the liver as detected by Western blot and flow cytometry, respectively. In conclusion, a proof of concept for inflammation attenuation of BAM15 through metabolic interference-induced anti-inflammation on macrophages and hepatocytes was demonstrated as a new strategy of anti-inflammation in sepsis.

scholarly journals Phytochemical Analysis, Pharmacological and Safety Evaluations of Halophytic Plant, Salsola cyclophylla

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2384
Author(s):  
Hamdoon A. Mohammed ◽  
Mohsen S. Al-Omar ◽  
Salman A. A. Mohammed ◽  
Ahmad H. Alhowail ◽  
Hussein M. Eldeeb ◽  
...  
Keyword(s):  
Ethanolic Extract ◽  
Phytochemical Analysis ◽  
High Concentration ◽  
Halophytic Plant ◽  
Anti Oxidant ◽  
Aqueous Ethanolic Extract ◽  
Phytochemical Constituents ◽  
Anti Inflammatory ◽  
Dpph Scavenging ◽  
Anti Inflammation

Salsola cyclophylla, an edible halophyte, is traditionally used for inflammation and pain. To confirm the claimed anti-inflammatory and analgesic properties, a detailed study on respective pharmacological actions was undertaken. The activities are contemplated to arise from its phytoconstituents. The LC-MS analysis of S. cyclophylla 95% aqueous-ethanolic extract revealed the presence of 52 compounds belonging to phenols, flavonoids, coumarins, and aliphatics class. A high concentration of Mn, Fe, and Zn was detected by atomic absorption spectroscopic analysis. The ethyl acetate extract showed the highest flavonoid contents (5.94 ± 0.04 mg/g, Quercetin Equivalents) and Fe2+-chelation (52%) potential with DPPH radicals-quenching IC50 at 1.35 ± 0.16 mg/mL, while the aqueous ethanolic extract exhibited maximum phenolics contents (136.08 ± 0.12 mg/g, gallic acid equivalents) with DPPH scavenging potential at IC50 0.615 ± 0.06 mg/mL. Aqueous ethanolic extract and standard quercetin DPPH radicals scavenging’s were equal potent at 10 mg/mL concentrations. The aqueous ethanolic extract showed highest analgesic effect with pain reduction rates 89.86% (p = 0.03), 87.50% (p < 0.01), and 99.66% (p = 0.0004) after 60, 90, and 120 min, respectively. Additionally, aqueous ethanolic extract exhibited the highest anti-inflammation capacity at 41.07% (p < 0.0001), 34.51% (p < 0.0001), and 24.82% (p < 0.0001) after 2, 3, and 6 h of extract’s administration, respectively. The phytochemical constituents, significant anti-oxidant potential, remarkable analgesic, and anti-inflammatory bioactivities of extracts supported the traditionally claimed anti-inflammatory and analgesic plant activities.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

2017 ◽  
Vol 9 (6) ◽  
pp. 145
Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp
Keyword(s):  
Acetic Acid ◽  
Protective Effect ◽  
Vascular Permeability ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
The Individual

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.

scholarly journals Gratophyllum Pictum (L.) Griff Extract as Anti-Inflammatory on Wistar Rat with Experimental Hemorrhoids. Study on serum IL-6, COX-2, TNF-alpha and total leucocytes in anal tissue.

2020 ◽  
Author(s):  
Sigit Adi Prasetyo ◽  
Ignatius Riwanto ◽  
Edi Dharmana ◽  
Neni Susilaningsih ◽  
Yan Wisnu Prajoko ◽  
...  
Keyword(s):  
Leucocyte Count ◽  
Wistar Rat ◽  
Tnf Alpha ◽  
Croton Oil ◽  
Post Test ◽  
Physiologic Saline ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Anti Inflammation ◽  
Better Than

The author would like to study the effects of ethanol Graptophyllum pictum (L.) Griff extract (EGPE) as anti-inflammation on wistar with experimental hemorrhoids. RCT post-test only design were done on 28 wistar, that were allocated into four groups. The 2nd , 3rd and 4th group were induced with 6% croton oil into anus for three days, the 1st group was not induced. On the 4th day, 1st and 2nd group were given physiologic saline, 3rd and 4th group was given EGPE 100 mg and 300 mg/ kg bw respectively. At the 9th day, before termination, blood was aspirated from retro-ocular region for examination of serum IL-6, COX-2 and TNF-alpha using ELISA method, and SGOT, SGPT, urea and creatinine level. Anus was removed and prepared for microscopic examination to count the leucocyte under 400 HPF. Induction of 6% croton oil was significantly increased TNF-alpha, IL-6, COX-2 and leucocyte count. Treatment with EGPE dose 100 mg and 300 mg/ kg bw significantly reduce TNF-alpha, IL-6, COX-2 and leucocyte count, dose 100 mg was even better than 300 mg except for leucocyte count. SGOT, SGPT, blood urea and creatinine were not significantly different among groups. In conclusion, the EGPE 100 mg and 300 mg have anti-inflammatory effects in hemorrhoids wistar, which can suppress IL-6, COX-2, TNF-alpha, and total leucocytes. The EGPE dose 100 mg is better than dose 300 mg. EGPE save for kidney and liver.

scholarly journals Effectiveness of Pugun Tanoh Leaves Ethanol Extract (Curanga fel-terrae (Lour.) Merr) as an Anti-inflammation in Patients after Tooth Extraction at Dental and Mouth Hospital of Dentistry Faculty, Universitas Sumatera Utara

2020 ◽  
Vol 8 (D) ◽  
pp. 209-212
Author(s):  
Hendry Rusdy ◽  
Marianne Marianne ◽  
Baginda Mangatur Gurning
Keyword(s):  
Treatment Group ◽  
Mefenamic Acid ◽  
Tooth Extraction ◽  
Ethanol Extract ◽  
Control Group ◽  
Analog Scale ◽  
Chi Square ◽  
Chi Square Test ◽  
Anti Inflammatory ◽  
Anti Inflammation

BACKGROUND: Pugun Tanoh (Curanga fel-terrae (Lour.) Merr) is one of the medicinal plants. C. fel-terrae often used by the Karo tribe of Tiga Lingga Village, Kabupaten Dairi, Provinsi Sumatera Utara to treat diarrhea, asthma, cough, scabies, inflammation, bruising, and abdominal pain. Hence, it is necessary to examine the anti-inflammatory effects of Pugun Tanoh leaf extract. AIM: The present study aimed to determine the effectiveness of Pugun Tanoh leaves ethanol extract as an anti-inflammatory in patients after tooth extraction at Dental and Mouth Hospital of Dentistry Faculty, Universitas Sumatera Utara. METHODS: There were two research groups, namely the treatment group, which was given the extract plus amoxicillin 500 mg and mefenamic acid 500 mg as well as the control group who were only given amoxicillin 500 mg and mefenamic acid 500 mg without the extract. However, the instructions given to the patient are only required to take 500 mg of amoxicillin as an antibiotic, but for the 500 mg mefenamic acid drug, it is only instructed to drink it if there is pain that is felt by the patient. After the extracted teeth, the treatment group was given C. fel-terrae leaves ethanol extract 1.1 mg/kg on the tooth extraction socket using a 3 ml syringe then measurements were made on day 1 and day 2 after the extract was given using a visual analog scale (VAS) and through direct observation. Statistical analysis using the t-test independent and Chi-square test (significant p < 0.05). RESULTS: The treatment group did not have signs of inflammation both on the 1st and 2nd days after tooth extraction, while the control group had signs of inflammation both on the 1st day and the 2nd day after tooth extraction. In the treatment group, there were no patients who took the mefenamic acid drug while in the control group, it was found that all patients took mefenamic acid because they felt post-extraction pain. Statistical result are obtained with p = 0.00 (p < 0.05). CONCLUSION: C. fel-terrae leaves ethanol extract is effective to be used as an anti-inflammatory in patients after tooth extraction combined with amoxicillin 500 mg and mefenamic acid 500 mg.

scholarly journals SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0

2010 ◽  
Vol 4 (3) ◽  
pp. 180-185
Author(s):  
Enade Perdana Istyastono ◽  
Rr. Sri Untari Siwi S.M.P ◽  
Andreas Asdi Utama ◽  
Supardjan A.M
Keyword(s):  
Inflammatory Activity ◽  
Physiological Changes ◽  
Solubility In Water ◽  
Curcumin Analogues ◽  
Inflammatory Agent ◽  
Curcumin Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Living Tissues ◽  
Anti Inflammation

Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been  developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0).   Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

scholarly journals Synthesis of double-headed 2-5A-antisense chimeras and their ability to activate human RNase L

2003 ◽  
Vol 3 (1) ◽  
pp. 63-64 ◽  
Author(s):  
Y. Ueno ◽  
S. Okatani ◽  
Y. Yamada ◽  
Y. Kitade
Keyword(s):  
Rnase L ◽  
Human Rnase
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