Small molecules in the treatment of COVID-19

Signal Transduction and Targeted Therapy, Год журнала: 2022, Номер 7(1)

Опубликована: Дек. 5, 2022

Abstract The outbreak of COVID-19 has become a global crisis, and brought severe disruptions to societies economies. Until now, effective therapeutics against are in high demand. Along with our improved understanding the structure, function, pathogenic process SARS-CoV-2, many small molecules potential anti-COVID-19 effects have been developed. So far, several antiviral strategies were explored. Besides directly inhibition viral proteins such as RdRp M pro , interference host enzymes including ACE2 proteases, blocking relevant immunoregulatory pathways represented by JAK/STAT, BTK, NF-κB, NLRP3 pathways, regarded feasible drug development. development treat achieved strategies, computer-aided lead compound design screening, natural product discovery, repurposing, combination therapy. Several representative remdesivir paxlovid proved or authorized emergency use countries. And candidates entered clinical-trial stage. Nevertheless, due epidemiological features variability issues it is necessary continue exploring novel COVID-19. This review discusses current findings for treatment. Moreover, their detailed mechanism action, chemical structures, preclinical clinical efficacies discussed.

Язык: Английский

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Pharmacological activities of esculin and esculetin: A review

Medicine, Год журнала: 2023, Номер 102(40), С. e35306 - e35306

Опубликована: Окт. 6, 2023

Esculin and esculetin are 2 widely studied coumarin components of Cortex Fraxini , which is a well-known herbal medicine with 2000-year history. In vivo in vitro studies have demonstrated that both variety pharmacological activities, including antioxidant, anti-tumor, anti-inflammatory, antibacterial, antidiabetic, immunomodulatory, anti-atherosclerotic, so on. Their underlying mechanisms action biological activities include scavenging free radicals, modulating the nuclear factor erythroid 2-related pathway, regulating cell cycle, inhibiting tumor proliferation migration, promoting mitochondrial pathway apoptosis, NF-κB MAPK signaling pathways, CD4 + T cells differentiation associated cytokine release, vascular smooth muscle cells, etc. This review aims to provide comprehensive information on esculin esculetin, noteworthy importance exploring therapeutic potential compounds.

Язык: Английский

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Cinnamomum verum extract inhibits NOX2/ROS and PKCδ/JNK/AP-1/NF-κB pathway-mediated inflammatory response in PMA-stimulated THP-1 monocytes

Phytomedicine, Год журнала: 2023, Номер 112, С. 154685 - 154685

Опубликована: Янв. 30, 2023

Cinnamomum verum J. Presl (Cinnamon) is widely used in the food and pharmaceutical industries. C. exhibits various biological activities. However, it unclear whether can inhibit NOX, a major source of ROS generation, exert anti-inflammatory antioxidant effects PMA-stimulated THP-1 cells.This study investigates cells.The MeOH extract was analyzed using UPLC-QTOF/MS. Anti-inflammatory were examined by DCF-DA staining, immunofluorescence RT-PCR, immunoblotting cells.C. its components, cinnamic acid coumarin, significantly attenuated expression IL-1β, IL-8, CCL5, COX-2 THP-1. decreased levels via NOX2 downregulation, as well ameliorated plasma membrane translocation PKCδ JNK phosphorylation. Besides, suppressed nuclear AP-1 NF-κB, which modulates diverse pro-inflammatory genes.C. effectively inhibits inflammation oxidative stress during monocyte-macrophage differentiation downregulates inflammatory mediators NOX2/ROS PKCδ/JNK/AP-1/NF-κB signaling.

Язык: Английский

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Essential oil from Cinnamomum cassia Presl bark regulates macrophage polarization and ameliorates lipopolysaccharide-induced acute lung injury through TLR4/MyD88/NF-κB pathway

Phytomedicine, Год журнала: 2024, Номер 129, С. 155651 - 155651

Опубликована: Апрель 17, 2024

Язык: Английский

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Phytochemical investigation and assessment of the anti-inflammatory activity of four Heracleum taxa growing in Turkey

Frontiers in Pharmacology, Год журнала: 2025, Номер 15

Опубликована: Янв. 6, 2025

Heracleum L. has been known as "hogweed" and used for inflammatory diseases, including fever, enteritis, bronchitis, many years worldwide. The genus is also prominently recognized its high content of coumarins, which are considered a significant group natural compounds their noteworthy anti-inflammatory properties. present study evaluated the activity dichloromethane methanolic extracts from H. paphlagonicum, sphondylium subsp. ternatum, elegans, cyclocarpum (100 mg/kg), have not previously investigated Inflammation models induced by carrageenan, prostaglandin E2, serotonin were employed to evaluate activity, using indomethacin (10 mg/kg) reference standard. Statistical differences between treatment control groups ANOVA with Student-Newman-Keuls post-hoc tests. Additionally, coumarin contents quantified mg/g high-performance liquid chromatography. roots displayed highest inhibition serotonin-induced hind paw edema, ranges 22.8%-36.9%, 5.4%-35.7%, 3.9%-17.9%, respectively, while 12.8%-44.3%, 2.7%-41.3%, 7.1%-30.6%, respectively. bergapten imperatorin quantities found in (0.49% 0.14%) elegans roots, had xanthotoxin level (0.06%). Angelicin was detected at concentrations 0.04%, 0.02%, correlation inhibitory observed elevated levels particularly imperatorin, suggests potential link concentration effects. our findings support traditional use this treating disorders. Further investigations necessary identify active elucidate mechanisms action these plants, potentially leading discovery novel therapeutic options inflammation.

Язык: Английский

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Characterization and In-vitro Release of Coumarin from Folic Acid-Conjugated Mesoporous Silica for Targeted Cancer Therapy

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141502 - 141502

Опубликована: Янв. 1, 2025

Язык: Английский

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Zebrafish as a Suitable Model for Utilizing the Bioactivity of Coumarins and Coumarin-Based Compounds

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(4), С. 1444 - 1444

Опубликована: Фев. 8, 2025

The aim of this review is to summarize the current knowledge on use coumarin-derived compounds in zebrafish (Danio rerio) model. Coumarins, a class naturally occurring with diverse biological activities, including such as coumarin, angelicin, and warfarin, have attracted considerable attention study potential therapeutic agents for cancer, central nervous system disorders, infectious diseases. capabilities coumarins active led synthesizing various derivatives their own properties. While variety certainly promising, it also cumbersome due large amount research needed find most optimal compounds. model offers unique advantages studies, high genetic physiological homology mammals, optical transparency embryos, rapid developmental processes, facilitating assessment compound toxicity underlying mechanisms action. This provides an in-depth analysis chemical properties coumarins, activity, results previous studies evaluating efficacy these assays. allows holistic coumarin derivatives, offering valuable insights advancing drug discovery development.

Язык: Английский

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Umbelliferone and Its Synthetic Derivatives as Suitable Molecules for the Development of Agents with Biological Activities: A Review of Their Pharmacological and Therapeutic Potential

Pharmaceuticals, Год журнала: 2023, Номер 16(12), С. 1732 - 1732

Опубликована: Дек. 15, 2023

Umbelliferone (UMB), known as 7-hydroxycoumarin, hydrangine, or skimmetine, is a naturally occurring coumarin in the plant kingdom, mainly from Umbelliferae family that possesses wide variety of pharmacological properties. In addition, use nanoparticles containing umbelliferone may improve anti-inflammatory anticancer therapy. Also, its derivatives are endowed with great potential for therapeutic applications due to their broad spectrum biological activities such anti-inflammatory, antioxidant, neuroprotective, antipsychotic, antiepileptic, antidiabetic, antimicrobial, antiviral, and antiproliferative effects. Moreover, 7-hydroxycoumarin ligands have been implemented develop 7-hydroxycoumarin-based metal complexes improved activity. Besides applications, analogues designed fluorescent probes detection biologically important species, enzymes, lysosomes, endosomes, monitoring cell processes protein functions well various diseases caused by an excess hydrogen peroxide. Furthermore, 7-hydroxy-based chemosensors serve highly selective tool Al3+ Hg2+ systems. This review devoted summary research on synthetic terms pharmaceutical properties, especially those reported literature during period 2017-2023. Future presented.

Язык: Английский

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Coumarins and flavones from Ficus erecta and their anti-inflammatory activity

Journal of Ethnopharmacology, Год журнала: 2024, Номер 333, С. 118472 - 118472

Опубликована: Июнь 19, 2024

Ficus erecta, a traditional Chinese She Ethnomedicine, has been historically utilized to treat various inflammatory conditions such as arthritis, nephritis, and osteoporosis. However, the underlying mechanisms accounting for its anti-inflammatory activity, well active components, largely remain elusive. The purpose of this research was investigate chemical constituents F. erecta that contribute effects. Coumarins flavones were obtained from 95% EtOH extract using virous column chromatography reversed-phase semipreparative HPLC. structures new compounds elucidated by extensive analysis spectroscopic methods, including HRESIMS, 1D 2D NMR spectra, CD experiments. Cultured macrophage RAW264.7 cells MTT cell viability assay, Griess reagent method, ELISA, Western blot experiments employed evaluate activity related mechanism. Four (1–4) eleven previously identified (5–16) coumarins, together with one (17) six known (18–23) isolated whole plant erecta. Compounds 7 17 significantly reduced nitric oxide (NO) prostaglandin E2 (PGE2) production without cytotoxic Furthermore, proinflammatory cytokines tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 in concentration-dependent manner. indicated suppressed expression iNOS, COX-2, p-IκBα LPS-stimulated cells. current phytochemical investigations revealed coumarins represent primary exhibit potent properties, linked inhibition NF-κB activation preventing degradation IκBα phosphorylation. These may serve promising candidates treating or certain diseases.

Язык: Английский

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Wool Fabric with an Improved Durable Biological Resistance Using a Coumarin Derivative

ACS Applied Bio Materials, Год журнала: 2025, Номер unknown

Опубликована: Янв. 15, 2025

Wool is the most widely used proteinic natural fiber in clothing industry by virtue of its versatile properties. Unfortunately, wool, as a fiber, more susceptible to attack microorganisms and moths, which may cause harm human health. That why antimicrobial mothproof finishing textiles prime importance textile industry. Herein, wool fabric was treated with synthesized 6-aminocoumarin adopting pad-dry-cure technique or without cross-linker. The evaluated for activity against Staphylococcus aureus Escherichia coli. also tested moth-proofing performance Tineola Bisselliella through assessing weight loss. Various analyses were conducted assign alteration structure fibers, viz., urea-bisulfite solubility, carboxylic content, Fourier transform infrared spectroscopy, X-ray diffraction pattern (XRD). Scanning electron microscopy displayed surface before after treatment. Some physical mechanical properties assessed. Results revealed that showed bacterial resistance Gram +ve −ve bacteria, addition improved moth larvae deterioration fabric's inherent

Язык: Английский

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