Anti-COVID-19, Anti-Inflammatory, and Anti-Osteoarthritis Activities of Sesamin from Sesamum indicum L. DOI Creative Commons

Shu‐Ming Huang,

Cheng-Yang Hsieh, Jasmine U. Ting

и другие.

Bioengineering, Год журнала: 2023, Номер 10(11), С. 1263 - 1263

Опубликована: Окт. 30, 2023

During the COVID-19 (coronavirus disease 2019) outbreak, many people were infected, and symptoms may persist for several weeks or months recovering patients. This is also known as "long COVID" includes such fatigue, joint pain, muscle et cetera. The virus trigger hyper-inflammation associated with cytokine levels in body. can inflammation joints, which lead to osteoarthritis (OA), while long-term damage other problems. According studies, sesame has potent anti-inflammatory properties due its major constituent, sesamin. study examined sesamin's anti-inflammatory, anti-osteoarthritis, anti-COVID-19 effects. Moreover, vivo vitro assays used determine activity against RAW264.7 SW1353 cell lines. Sesamin had a dose-dependent effect (20 mg/kg) monoiodoacetic acid (MIA)-induced rat model. reduced paw swelling discomfort. In addition, findings indicated that sesamin suppressed expression of iNOS (inducible nitric oxide synthase) COX-2 (cyclooxygenase-2) line within concentration range 6.25-50 μM. Furthermore, suppressive on MMP (matrix metalloproteinase) chondrocytes same To examine anti-viral activity, an silico analysis was performed evaluate binding affinity SARS-CoV-2 RdRp (severe acute respiratory syndrome coronavirus 2 RNA-dependent RNA polymerase) human ACE2 (angiotensin-converting enzyme 2). Compared controls, exhibited strong affinities towards ACE2. higher target protein. suggests shows potential anti-SARS-CoV-2 drug development.

Язык: Английский

Small molecules in the treatment of COVID-19 DOI Creative Commons
Sibei Lei, Xiaohua Chen, Jieping Wu

и другие.

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

Процитировано

82
Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry DOI Creative Commons
Zilun Li,

Meixiu Peng,

Pin Chen

и другие.

Cell Metabolism, Год журнала: 2022, Номер 34(3), С. 424 - 440.e7

Опубликована: Фев. 11, 2022

Язык: Английский

Процитировано

46
Host Cell Targets for Unconventional Antivirals against RNA Viruses DOI Creative Commons
Vicky C. Roa-Linares, Manuela Escudero-Flórez, Miguel Vicente‐Manzanares

и другие.

Viruses, Год журнала: 2023, Номер 15(3), С. 776 - 776

Опубликована: Март 17, 2023

The recent COVID-19 crisis has highlighted the importance of RNA-based viruses. most prominent members this group are SARS-CoV-2 (coronavirus), HIV (human immunodeficiency virus), EBOV (Ebola DENV (dengue HCV (hepatitis C ZIKV (Zika CHIKV (chikungunya and influenza A virus. With exception retroviruses which produce reverse transcriptase, majority RNA viruses encode RNA-dependent polymerases do not include molecular proofreading tools, underlying high mutation capacity these as they multiply in host cells. Together with their ability to manipulate immune system different ways, frequency poses a challenge develop effective durable vaccination and/or treatments. Consequently, use antiviral targeting agents, while an important part therapeutic strategy against infection, may lead selection drug-resistant variants. crucial role cell replicative processing machinery is essential for cycle driven attention potential drugs directed alternatives treat viral infections. In review, we discuss small molecules effects that target cellular factors steps infectious many We emphasize repurposing FDA-approved broad-spectrum activity. Finally, postulate ferruginol analog (18-(phthalimide-2-yl) ferruginol) host-targeted antiviral.

Язык: Английский

Процитировано

18
Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors DOI

Aijia Wu,

Kunyu Shi,

Jiaxing Wang

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 263, С. 115923 - 115923

Опубликована: Окт. 31, 2023

Язык: Английский

Процитировано

17
Inhibitory effect of lactoferrin-coated zinc nanoparticles on SARS-CoV-2 replication and entry along with improvement of lung fibrosis induced in adult male albino rats DOI Open Access
Esmail M. El‐Fakharany, Hamada El‐Gendi, Yousra A. El‐Maradny

и другие.

International Journal of Biological Macromolecules, Год журнала: 2023, Номер 245, С. 125552 - 125552

Опубликована: Июнь 24, 2023

Язык: Английский

Процитировано

13
Potency of Xanthone Derivatives from Garcinia mangostana L. for COVID-19 Treatment through Angiotensin-Converting Enzyme 2 and Main Protease Blockade: A Computational Study DOI Creative Commons
Cecep Suhandi,

Siti Sarah Alfathonah,

Aliya Nur Hasanah

и другие.

Molecules, Год журнала: 2023, Номер 28(13), С. 5187 - 5187

Опубликована: Июль 4, 2023

ACE2 and Mpro in the pathology of SARS-CoV-2 show great potential developing COVID-19 drugs as therapeutic targets, due to their roles "gate" viral entry reproduction. Of many compounds for inhibition, α-mangostin is a promising candidate. Unfortunately, secondary metabolite with anti-SARS-CoV-2 activity hindered its low solubility water. Other xanthone isolates, which also possess core structure like α-mangostin, are predicted be alternatives treatment, addressing drug-likeness α-mangostin. This study aims assess derivative pericarp mangosteen (Garcinia mangostana L.) through computational study. The was conducted screening using molecular docking study, prediction Lipinski's rule five filtration, pharmacokinetic toxicity evaluate safety profile, dynamic stability formed interactions. research results showed that there were 11 high inhibit 12 Mpro. However, only garcinone B, addition being indicated active, possesses drug-likeness, pharmacokinetic, profile suitable. exhibited proper interaction between B Therefore, isolate compound, has further treatment an inhibitor.

Язык: Английский

Процитировано

13
Molecular Analysis of SARS-CoV-2 Spike Protein-Induced Endothelial Cell Permeability and vWF Secretion DOI Open Access

Yuexi Guo,

Venkateswarlu Kanamarlapudi

International Journal of Molecular Sciences, Год журнала: 2023, Номер 24(6), С. 5664 - 5664

Опубликована: Март 16, 2023

Coronavirus disease COVID-19, which is caused by severe acute respiratory syndrome coronavirus SARS-CoV-2, has become a worldwide pandemic in recent years. In addition to being disease, COVID-19 'vascular disease' since it causes leaky vascular barrier and increases blood clotting elevating von Willebrand factor (vWF) levels the blood. this study, we analyzed vitro how SARS-CoV-2 spike protein S1 induces endothelial cell (EC) permeability its vWF secretion, underlying molecular mechanism for it. We showed that receptor-binding domain (RBD) sufficient induce vWF-secretion through angiotensin-converting enzyme (ACE)2 an ADP-ribosylation (ARF)6 activation-dependent manner. However, mutants, including those South African Californian variants of did not affect induced EC secretion. addition, have identified signaling cascade downstream ACE2 protein-induced secretion using pharmacological inhibitors. The knowledge gained from study could be useful developing novel drugs or repurposing existing treating infections particularly strains respond poorly vaccines.

Язык: Английский

Процитировано

12
Characterization of passive microfluidic mixer with a three-dimensional zig-zag channel for cryo-EM sampling DOI
Byungjin Lee, MinJoong Kim,

Seoyeon Oh

и другие.

Chemical Engineering Science, Год журнала: 2023, Номер 281, С. 119161 - 119161

Опубликована: Авг. 7, 2023

Язык: Английский

Процитировано

12
Identifying Exifone as a Dual-Target Agent Targeting Both SARS-CoV-2 3CL Protease and the ACE2/S-RBD Interaction Among Clinical Polyphenolic Compounds DOI Open Access
Jiani Lu, Yan Tang, Hongtao Li

и другие.

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(5), С. 2243 - 2243

Опубликована: Март 2, 2025

The ongoing emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants has led to resistance against multiple disease 2019 (COVID-19) vaccines and therapeutic medications, making the development effective therapeutics SARS-CoV-2 a high priority. Studies have shown that bioactive polyphenols, particularly those with triphenol groups, can effectively inhibit activity 3-chymotrypsin-like protease (3CLpro). However, structural instability polyphenols necessitates further research. To address this, we conducted literature review identify compounds are either approved or currently undergoing clinical trials, assessing their potential 3CLpro. Exifone benserazide hydrochloride were identified as inhibitors 3CLpro among these compounds, using fluorescence resonance energy transfer (FRET)-based assay. Benserazide was confirmed covalent binder through time-dependent inhibition kinetic analysis, its binding mode elucidated by molecular docking. Notably, exifone not only inhibited but also blocked interaction between host cell receptor angiotensin-converting enzyme (ACE2) spike protein domain (S-RBD), surface plasmon (SPR) flow cytometry. Additionally, demonstrated antiviral various SARS-CoV-2-S pseudovirus variants. In conclusion, discovery underscores in developing conserved for coronaviruses, offering new strategies rapid drugs both current future pandemics.

Язык: Английский

Процитировано

0
Anti-Fungal Drug Anidulafungin Inhibits SARS-CoV-2 Spike-Induced Syncytia Formation by Targeting ACE2-Spike Protein Interaction DOI Creative Commons
Shahzaib Ahamad, Hashim Ali, Ilaria Secco

и другие.

Frontiers in Genetics, Год журнала: 2022, Номер 13

Опубликована: Март 25, 2022

Drug repositioning continues to be the most effective, practicable possibility treat COVID-19 patients. The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus enters target cells by binding ACE2 receptor

Язык: Английский

Процитировано

18