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1.
Molecules ; 27(16)2022 Aug 22.
Статья в английский | MEDLINE | ID: covidwho-2023940

Реферат

Tuberculosis (TB) caused by the bacterial pathogen Mycobacterium tuberculosis (Mtb) remains a threat to mankind, with over a billion of deaths in the last two centuries. Recent advancements in science have contributed to an understanding of Mtb pathogenesis and developed effective control tools, including effective drugs to control the global pandemic. However, the emergence of drug resistant Mtb strains has seriously affected the TB eradication program around the world. There is, therefore, an urgent need to develop new drugs for TB treatment, which has grown researchers' interest in small molecule-based drug designing and development. The small molecules-based treatments hold significant potential to overcome drug resistance and even provide opportunities for multimodal therapy. In this context, various natural and synthetic flavonoids were reported for the effective treatment of TB. In this review, we have summarized the recent advancement in the understanding of Mtb pathogenesis and the importance of both natural and synthetic flavonoids against Mtb infection studied using in vitro and in silico methods. We have also included flavonoids that are able to inhibit the growth of non-tubercular mycobacterial organisms. Hence, understanding the therapeutic properties of flavonoids can be useful for the future treatment of TB.


Тема - темы
Mycobacterium tuberculosis , Tuberculosis , Antitubercular Agents/pharmacology , Antitubercular Agents/therapeutic use , Drug Delivery Systems , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Tuberculosis/drug therapy , Tuberculosis/microbiology
2.
Molecules ; 27(10)2022 May 18.
Статья в английский | MEDLINE | ID: covidwho-1953750

Реферат

Voltage-gated potassium channels of the Kv1.3 type are considered a potential new molecular target in several pathologies, including some cancer disorders and COVID-19. Lipophilic non-toxic organic inhibitors of Kv1.3 channels, such as statins and flavonoids, may have clinical applications in supporting the therapy of some cancer diseases, such as breast, pancreas, and lung cancer; melanoma; or chronic lymphocytic leukemia. This study focuses on the influence of the co-application of statins-simvastatin (SIM) or mevastatin (MEV)-with flavonoids 8-prenylnaringenin (8-PN), 6-prenylnarigenin (6-PN), xanthohumol (XANT), acacetin (ACAC), or chrysin on the activity of Kv1.3 channels, viability, and the apoptosis of cancer cells in the human T cell line Jurkat. We showed that the inhibitory effect of co-application of the statins with flavonoids was significantly more potent than the effects exerted by each compound applied alone. Combinations of simvastatin with chrysin, as well as mevastatin with 8-prenylnaringenin, seem to be the most promising. We also found that these results correlate with an increased ability of the statin-flavonoid combination to reduce viability and induce apoptosis in cancer cells compared to single compounds. Our findings suggest that the co-application of statins and flavonoids at low concentrations may increase the effectiveness and safety of cancer therapy. Thus, the simultaneous application of statins and flavonoids may be a new and promising anticancer strategy.


Тема - темы
COVID-19 , Hydroxymethylglutaryl-CoA Reductase Inhibitors , Neoplasms , Apoptosis , Cell Line , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Hydroxymethylglutaryl-CoA Reductase Inhibitors/therapeutic use , Kv1.3 Potassium Channel/metabolism , Neoplasms/drug therapy , Simvastatin/pharmacology
3.
Infect Disord Drug Targets ; 22(5): 22-30, 2022.
Статья в английский | MEDLINE | ID: covidwho-1951886

Реферат

BACKGROUND: Flavonoid class phytochemicals are natural compounds present in different medicinal plants, vegetables and fruits. Ginkgo biloba contains significant amounts of bioflavonoid 'bilobetin'. Bilobetin is an active phytochemical used for the treatment of human health complications due to its medicinal properties and therapeutic benefit. The purpose of this work is to collect and reviewed scientific data on bilobetin from different literature sources; highlight their biological properties, pharmacological activities and analytical aspects. METHODS: Health beneficial aspects of bilobetin have been investigated in the present work through scientific data analysis. PubMed, Google Scholar, Google, Scopus, etc. have been searched in the present work in order to collect scientific information on bilobetin. Medicinal importance and therapeutic benefit of bilobetin has been searched in the present work through these databases of bilobetin. Detailed pharmacological activities of bilobetin have been reviewed in the present work through literature data analysis of various scientific research works. However, analytical data of bilobetin were also collected and reviewed in the present reaserch. RESULTS: Literature data analysis of bilobetin in the present work revealed the medicinal properties and therapeutic potential of bilobetin mainly due to its anti-fungal, anti-inflammatory, anti-oxidant, antihyperlipidemic, and anti-proliferative activities. Literature data analysis revealed the effectiveness of bilobetin on osteoporosis, glucose metabolism, adipocytes, SARS CoV-2, Influenza A virus and human thrombin. Scientific data also revealed the importance of different analytical techniques for the isolation, separation, identification, and quantification of bilobetin. CONCLUSION: Scientific data analysis revealed biological importance and pharmacological activities of bilobetin in the health sector.


Тема - темы
Biflavonoids , COVID-19 , Plants, Medicinal , Anti-Inflammatory Agents , Antioxidants/pharmacology , Antioxidants/therapeutic use , Biflavonoids/pharmacology , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Phytochemicals/pharmacology , Phytotherapy , Plant Extracts/pharmacology , Plants, Medicinal/chemistry
4.
Molecules ; 27(9)2022 May 02.
Статья в английский | MEDLINE | ID: covidwho-1875712

Реферат

Hydroxylated polyphenols, also called flavonoids, are richly present in vegetables, fruits, cereals, nuts, herbs, seeds, stems, and flowers of numerous plants. They possess numerous medicinal properties such as antioxidant, anti-cancer, anti-microbial, neuroprotective, and anti-inflammation. Studies show that flavonoids activate antioxidant pathways that render an anti-inflammatory effect. They inhibit the secretions of enzymes such as lysozymes and ß-glucuronidase and inhibit the secretion of arachidonic acid, which reduces inflammatory reactions. Flavonoids such as quercetin, genistein, apigenin, kaempferol, and epigallocatechin 3-gallate modulate the expression and activation of a cytokine such as interleukin-1beta (IL-1ß), Tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8); regulate the gene expression of many pro-inflammatory molecules such s nuclear factor kappa-light chain enhancer of activated B cells (NF-κB), activator protein-1 (AP-1), intercellular adhesion molecule-1 (ICAM), vascular cell adhesion molecule-1 (VCAM), and E-selectins; and also inhibits inducible nitric oxide (NO) synthase, cyclooxygenase-2, and lipoxygenase, which are pro-inflammatory enzymes. Understanding the anti-inflammatory action of flavonoids provides better treatment options, including coronavirus disease 2019 (COVID-19)-induced inflammation, inflammatory bowel disease, obstructive pulmonary disorder, arthritis, Alzheimer's disease, cardiovascular disease, atherosclerosis, and cancer. This review highlights the sources, biochemical activities, and role of flavonoids in enhancing human health.


Тема - темы
COVID-19 , Flavonoids , Anti-Inflammatory Agents/adverse effects , Antioxidants/adverse effects , Flavonoids/chemistry , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Inflammation/drug therapy , NF-kappa B/metabolism , Tumor Necrosis Factor-alpha/pharmacology
5.
Curr Drug Targets ; 23(4): 420-436, 2022.
Статья в английский | MEDLINE | ID: covidwho-1799012

Реферат

Chrysin (a flavonoid) has shown various promising pharmacological activities viz. anticancer, anti-diabetic, immune-modulation, antidepressant, and anti-asthmatic. Additionally, it exhibited potential protective effects against various toxins on different organs like the liver, brain, kidney, and heart. A multitude of studies have been conducted to explore the possible targets for its possible mechanism of action. However, its therapeutic applications have been limited due to its poor oral bioavailability. The major reason for its poor bioavailability is its extensive first-pass metabolism. A critical review of the pharmacological properties of chrysin and its associated molecular targets has not been discussed as yet comprehensively. Therefore, the emphasis of the present work is to provide an in-depth understanding of molecular targets accountable for the pharmacological actions of chrysin. Moreover, a schematic diagram was made for the first time to represent the comprehensive pharmacokinetic properties of chrysin, which helps to understand the biopharmaceutical aspect for its successful delivery. An in-depth understanding of the biopharmaceutical properties of chrysin will help in adopting a suitable formulation approach to overcome poor oral bioavailability. Additionally, it facilitates to study the possible pharmacokinetic interactions of chrysin with other drugs. Hence, we found that chrysin is a miraculous natural agent with myriad therapeutic properties, and its benefit can be exploited with an in-depth understanding of molecular targets, pharmacological actions, and biopharmaceutical attributes.


Тема - темы
Biological Products , Flavonoids , Biological Availability , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Pharmaceutical Preparations
6.
Curr Opin Pharmacol ; 64: 102231, 2022 06.
Статья в английский | MEDLINE | ID: covidwho-1797024

Реферат

Coronavirus disease (COVID-19) outbreak has caused unprecedented global disruption since 2020. Approximately 238 million people are affected worldwide where the elderly succumb to mortality. Post-COVID syndrome and its side effects have popped up with several health hazards, such as macular degeneration and vision loss. It thus necessitates better medical care and management of our dietary practices. Natural flavonoids have been included in traditional medicine and have also been used safely against COVID-19 and several other diseases. Kaempferol is an essential flavonoid that has been demonstrated to influence several vital cellular signaling pathways involved in apoptosis, angiogenesis, inflammation, and autophagy. In this review, we emphasize the plausible regulatory effects of Kaempferol on hallmarks of COVID-19 and macular degeneration.


Тема - темы
COVID-19 , Macular Degeneration , Retinal Diseases , Aged , COVID-19/drug therapy , Flavonoids/therapeutic use , Humans , Kaempferols/pharmacology , Kaempferols/therapeutic use , Macular Degeneration/drug therapy , Macular Degeneration/metabolism , Retina/metabolism , Retinal Diseases/drug therapy
7.
Phytother Res ; 36(5): 2042-2060, 2022 May.
Статья в английский | MEDLINE | ID: covidwho-1750432

Реферат

The high incidence of post-covid symptoms in humans confirms the need for effective treatment. Due to long-term complications across several disciplines, special treatment programs emerge for affected patients, emphasizing multidisciplinary care. For these reasons, we decided to look at current knowledge about possible long-term complications of COVID-19 disease and then present the effect of flavonoids, which could help alleviate or eliminate complications in humans after overcoming the COVID-19 infection. Based on articles published from 2003 to 2021, we summarize the flavonoids-based molecular mechanisms associated with the post-COVID-19 syndrome and simultaneously provide a complex view regarding their prophylactic and therapeutic potential. Review clearly sorts out the outcome of post-COVID-19 syndrome according particular body systems. The conclusion is that flavonoids play an important role in prevention of many diseases. We suggest that flavonoids as critical nutritional supplements, are suitable for the alleviation and shortening of the period associated with the post-COVID-19 syndrome. The most promising flavonoid with noteworthy therapeutic and prophylactic effect appears to be quercetin.


Тема - темы
COVID-19 , COVID-19/complications , COVID-19/drug therapy , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , SARS-CoV-2
8.
Front Public Health ; 10: 814669, 2022.
Статья в английский | MEDLINE | ID: covidwho-1731868

Реферат

BACKGROUND: This meta-analysis aimed to investigate the efficacy and safety of flavonoids in treating viral acute respiratory tract infections (ARTIs). METHODS: Randomized controlled trials (RCTs) were entered into meta-analyses performed separately for each indication. Efficacy analyses were based on changes in disease-specific symptom scores. Safety was analyzed based on the pooled data from all eligible trials, by comparing the incidence of adverse events between flavonoids and the control. RESULTS: In this study, thirty RCTs (n = 5,166) were included. In common cold, results showed that the flavonoids group decreased total cold intensity score (CIS), the sum of sum of symptom intensity differences (SSID) of CIS, and duration of inability to work vs. the control group. In influenza, the flavonoids group improved the visual analog scores for symptoms. In COVID-19, the flavonoids group decreased the time taken for alleviation of symptoms, time taken for SARS-CoV-2 RT-PCR clearance, the RT-PCR positive subjects at day 7, time to achievement of the normal status of symptoms, patients needed oxygen, patients hospitalized and requiring mechanical ventilation, patients in ICU, days of hospitalization, and mortality vs. the control group. In acute non-streptococcal tonsillopharyngitis, the flavonoids group decreased the tonsillitis severity score (TSS) on day 7. In acute rhinosinusitis, the flavonoids group decreased the sinusitis severity score (SSS) on day 7, days off work, and duration of illness. In acute bronchitis, the flavonoids group decreased the bronchitis severity score (BSS) on day 7, days off work, and duration of illness. In bronchial pneumonia, the flavonoids group decreased the time to symptoms disappearance, the level of interleukin-6 (IL-6), interleukin-8 (IL-8), and tumor necrosis factor-α (TNF-α). In upper respiratory tract infections, the flavonoids group decreased total CIS on day 7 and increased the improvement rate of symptoms. Furthermore, the results of the incidence of adverse reactions did not differ between the flavonoids and the control group. CONCLUSION: Results from this systematic review and meta-analysis suggested that flavonoids were efficacious and safe in treating viral ARTIs including the common cold, influenza, COVID-19, acute non-streptococcal tonsillopharyngitis, acute rhinosinusitis, acute bronchitis, bronchial pneumonia, and upper respiratory tract infections. However, uncertainty remains because there were few RCTs per type of ARTI and many of the RCTs were small and of low quality with a substantial risk of bias. Given the limitations, we suggest that the conclusions need to be confirmed on a larger scale with more detailed instructions in future studies.Systematic Review Registration: inplasy.com/inplasy-2021-8-0107/, identifier: INPLASY20218010.


Тема - темы
COVID-19 , Respiratory Tract Infections , COVID-19/drug therapy , Flavonoids/therapeutic use , Humans , Randomized Controlled Trials as Topic , Respiratory Tract Infections/drug therapy , SARS-CoV-2
9.
J Mol Model ; 28(4): 82, 2022 Mar 05.
Статья в английский | MEDLINE | ID: covidwho-1729317

Реферат

Novel SARS coronavirus or SARS-CoV-2 is a novel coronavirus that was identified and spread from Wuhan in 2019. On January 30th, the World Health Organization declared the coronavirus outbreak as a Global Public Health Emergency. Although Remdesivir and Molnupiravir are FDA-approved drugs for COVID-19, finding new efficient and low-cost antiviral drugs against COVID-19 for applying in more countries can still be helpful. One of the potential sources for finding new and low-cost drugs is the herbal compounds in addition to repurposing FDA-approved drugs. So, in this study, we focused on finding effective drug candidates against COVID-19 based on the computational approaches. As ACE2 serves as a critical receptor for cell entry of this virus. Inhibiting the binding site of SARS-CoV-2 on human ACE2 provides a promising therapeutic approach for developing drugs against SARS-CoV-2. Herein, we applied a bioinformatics approach to identify possible potential inhibitors of SARS-CoV-2. A library of FDA-approved compounds and five natural compounds was screened using Smina docking. Top-docking compounds are then applied in Molecular Dynamics (MD) simulation to assess the stability of ACE2-inhibitor complexes. Results indicate that Luteolin and Chrysin represent high conformation stability with ACE2 during 120 ns of Molecular Dynamics simulation. The binding free energies of Luteolin and Chrysin were calculated by the Molecular Mechanics/Poisson-Boltzmann Surface Area method (MM/PBSA) which confirmed the relative binding free energy of these drugs to ACE2 in favor of the effective binding. So, Luteolin and Chrysin could sufficiently interact with ACE2 and block the Spike binding pocket of ACE2 and can be a potential inhibitor against the binding of SARS-CoV-2 to ACE2 receptor which is an early stage of infection. Luteolin and Chrysin could be suggestive as beneficial compounds for preventing or reducing SARS-CoV-2 transmission and infection which need experimental work to prove.


Тема - темы
Angiotensin-Converting Enzyme 2/metabolism , COVID-19/prevention & control , Flavonoids/pharmacology , Luteolin/pharmacology , SARS-CoV-2/metabolism , Spike Glycoprotein, Coronavirus/metabolism , Angiotensin-Converting Enzyme 2/antagonists & inhibitors , Antiviral Agents/pharmacology , Antiviral Agents/therapeutic use , Binding Sites , COVID-19/metabolism , COVID-19/transmission , Drug Repositioning , Flavonoids/therapeutic use , Humans , Luteolin/therapeutic use , Molecular Dynamics Simulation , Protein Binding
10.
Molecules ; 27(5)2022 Mar 01.
Статья в английский | MEDLINE | ID: covidwho-1715569

Реферат

COVID-19 is an endothelial disease. All the major comorbidities that increase the risk for severe SARS-CoV-2 infection and severe COVID-19 including old age, obesity, diabetes, hypertension, respiratory disease, compromised immune system, coronary artery disease or heart failure are associated with dysfunctional endothelium. Genetics and environmental factors (epigenetics) are major risk factors for endothelial dysfunction. Individuals with metabolic syndrome are at increased risk for severe SARS-CoV-2 infection and poor COVID-19 outcomes and higher risk of mortality. Old age is a non-modifiable risk factor. All other risk factors are modifiable. This review also identifies dietary risk factors for endothelial dysfunction. Potential dietary preventions that address endothelial dysfunction and its sequelae may have an important role in preventing SARS-CoV-2 infection severity and are key factors for future research to address. This review presents some dietary bioactives with demonstrated efficacy against dysfunctional endothelial cells. This review also covers dietary bioactives with efficacy against SARS-CoV-2 infection. Dietary bioactive compounds that prevent endothelial dysfunction and its sequelae, especially in the gastrointestinal tract, will result in more effective prevention of SARS-CoV-2 variant infection severity and are key factors for future food research to address.


Тема - темы
Endothelium/drug effects , Flavonoids/pharmacology , Functional Food/analysis , SARS-CoV-2/drug effects , COVID-19/drug therapy , COVID-19/pathology , COVID-19/virology , Endothelium/metabolism , Flavonoids/metabolism , Flavonoids/therapeutic use , Humans , Polysaccharides/pharmacology , Polysaccharides/therapeutic use , Risk Factors , SARS-CoV-2/isolation & purification , Stilbenes/pharmacology , Stilbenes/therapeutic use , Terpenes/pharmacology , Terpenes/therapeutic use
11.
Med Sci Monit ; 27: e935379, 2021 Dec 30.
Статья в английский | MEDLINE | ID: covidwho-1593238

Реферат

BACKGROUND This retrospective study aimed to investigate outcomes and hospitalization rates in patients with a confirmed diagnosis of early COVID-19 treated at home with prescribed and non-prescribed treatments. MATERIAL AND METHODS The medical records of a cohort of 158 Italian patients with early COVID-19 treated at home were analyzed. Treatments consisted of indomethacin, low-dose aspirin, omeprazole, and a flavonoid-based food supplement, plus azithromycin, low-molecular-weight heparin, and betamethasone as needed. The association of treatment timeliness and of clinical variables with the duration of symptoms and with the risk of hospitalization was evaluated by logistic regression. RESULTS Patients were divided into 2 groups: group 1 (n=85) was treated at the earliest possible time (<72 h from onset of symptoms), and group 2 (n=73) was treated >72 h after the onset of symptoms. Clinical severity at the beginning of treatment was similar in the 2 groups. In group 1, symptom duration was shorter than in group 2 (median 6.0 days vs 13.0 days, P<0.001) and no hospitalizations occurred, compared with 19.18% hospitalizations in group 2. One patient in group 1 developed chest X-ray alterations and 2 patients experienced an increase in D-dimer levels, compared with 30 and 22 patients, respectively, in group 2. The main factor determining the duration of symptoms and the risk of hospitalization was the delay in starting therapy (P<0.001). CONCLUSIONS This real-world study of patients in the community showed that early diagnosis and early supportive patient management reduced the severity of COVID-19 and reduced the rate of hospitalization.


Тема - темы
COVID-19/diagnosis , COVID-19/drug therapy , Hospitalization/statistics & numerical data , Time-to-Treatment/statistics & numerical data , Aged , Aged, 80 and over , Aspirin/therapeutic use , Betamethasone/therapeutic use , Cohort Studies , Dietary Supplements , Early Diagnosis , Female , Flavonoids/therapeutic use , Follow-Up Studies , Heparin, Low-Molecular-Weight/therapeutic use , Humans , Indomethacin/therapeutic use , Italy , Male , Middle Aged , Omeprazole/therapeutic use , Patient Acuity , Retrospective Studies , Risk Assessment , SARS-CoV-2 , Time , Treatment Outcome
12.
Int J Mol Sci ; 22(23)2021 Nov 23.
Статья в английский | MEDLINE | ID: covidwho-1538409

Реферат

Several coronaviruses (CoVs) have been associated with serious health hazards in recent decades, resulting in the deaths of thousands around the globe. The recent coronavirus pandemic has emphasized the importance of discovering novel and effective antiviral medicines as quickly as possible to prevent more loss of human lives. Positive-sense RNA viruses with group spikes protruding from their surfaces and an abnormally large RNA genome enclose CoVs. CoVs have already been related to a range of respiratory infectious diseases possibly fatal to humans, such as MERS, SARS, and the current COVID-19 outbreak. As a result, effective prevention, treatment, and medications against human coronavirus (HCoV) is urgently needed. In recent years, many natural substances have been discovered with a variety of biological significance, including antiviral properties. Throughout this work, we reviewed a wide range of natural substances that interrupt the life cycles for MERS and SARS, as well as their potential application in the treatment of COVID-19.


Тема - темы
Antiviral Agents/therapeutic use , COVID-19/prevention & control , COVID-19/therapy , Alkaloids/chemistry , Alkaloids/therapeutic use , Antiviral Agents/chemistry , COVID-19/epidemiology , Disease Outbreaks , Flavonoids/chemistry , Flavonoids/therapeutic use , Humans , Mutation , Pandemics , SARS-CoV-2/genetics , Terpenes/chemistry , Terpenes/therapeutic use
13.
Int J Mol Sci ; 22(22)2021 Nov 09.
Статья в английский | MEDLINE | ID: covidwho-1512384

Реферат

Coronaviruses cause diseases in humans and livestock. The SARS-CoV-2 is infecting millions of human beings, with high morbidity and mortality worldwide. The main protease (Mpro) of coronavirus plays a pivotal role in viral replication and transcription, which, in theory, is an attractive drug target for antiviral drug development. It has been extensively discussed whether Xanthohumol is able to help COVID-19 patients. Here, we report that Xanthohumol, a small molecule in clinical trials from hops (Humulus lupulus), was a potent pan-inhibitor for various coronaviruses by targeting Mpro, for example, betacoronavirus SARS-CoV-2 (IC50 value of 1.53 µM), and alphacoronavirus PEDV (IC50 value of 7.51 µM). Xanthohumol inhibited Mpro activities in the enzymatical assays, while pretreatment with Xanthohumol restricted the SARS-CoV-2 and PEDV replication in Vero-E6 cells. Therefore, Xanthohumol is a potent pan-inhibitor of coronaviruses and an excellent lead compound for further drug development.


Тема - темы
3C Viral Proteases/antagonists & inhibitors , Flavonoids/chemistry , Propiophenones/chemistry , Protease Inhibitors/chemistry , SARS-CoV-2/enzymology , 3C Viral Proteases/chemistry , 3C Viral Proteases/metabolism , Alphacoronavirus/enzymology , Alphacoronavirus/physiology , Amino Acid Sequence , Animals , Binding Sites , Biological Products/chemistry , Biological Products/metabolism , Biological Products/pharmacology , Biological Products/therapeutic use , COVID-19/drug therapy , COVID-19/virology , Catalytic Domain , Chlorocebus aethiops , Coronavirus/enzymology , Coronavirus/physiology , Flavonoids/metabolism , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Molecular Docking Simulation , Propiophenones/metabolism , Propiophenones/pharmacology , Propiophenones/therapeutic use , Protease Inhibitors/metabolism , Protease Inhibitors/pharmacology , Protease Inhibitors/therapeutic use , SARS-CoV-2/isolation & purification , Sequence Alignment , Vero Cells , Virus Replication/drug effects
14.
Int J Mol Sci ; 22(20)2021 Oct 14.
Статья в английский | MEDLINE | ID: covidwho-1470888

Реферат

The ongoing COVID-19 pandemic, caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) became a globally leading public health concern over the past two years. Despite the development and administration of multiple vaccines, the mutation of newer strains and challenges to universal immunity has shifted the focus to the lack of efficacious drugs for therapeutic intervention for the disease. As with SARS-CoV, MERS-CoV, and other non-respiratory viruses, flavonoids present themselves as a promising therapeutic intervention given their success in silico, in vitro, in vivo, and more recently, in clinical studies. This review focuses on data from in vitro studies analyzing the effects of flavonoids on various key SARS-CoV-2 targets and presents an analysis of the structure-activity relationships for the same. From 27 primary papers, over 69 flavonoids were investigated for their activities against various SARS-CoV-2 targets, ranging from the promising 3C-like protease (3CLpro) to the less explored nucleocapsid (N) protein; the most promising were quercetin and myricetin derivatives, baicalein, baicalin, EGCG, and tannic acid. We further review promising in silico studies featuring activities of flavonoids against SARS-CoV-2 and list ongoing clinical studies involving the therapeutic potential of flavonoid-rich extracts in combination with synthetic drugs or other polyphenols and suggest prospects for the future of flavonoids against SARS-CoV-2.


Тема - темы
Antiviral Agents/therapeutic use , COVID-19/drug therapy , Flavonoids/therapeutic use , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , COVID-19/virology , Coronavirus 3C Proteases/antagonists & inhibitors , Coronavirus 3C Proteases/metabolism , Coronavirus Nucleocapsid Proteins/antagonists & inhibitors , Coronavirus Nucleocapsid Proteins/metabolism , Flavonoids/chemistry , Flavonoids/pharmacology , Humans , Middle East Respiratory Syndrome Coronavirus/drug effects , Middle East Respiratory Syndrome Coronavirus/physiology , Phosphoproteins/antagonists & inhibitors , Phosphoproteins/metabolism , Rhinovirus/drug effects , Rhinovirus/physiology , SARS-CoV-2/isolation & purification , SARS-CoV-2/metabolism , Virus Internalization/drug effects
15.
Clin Microbiol Infect ; 27(10): 1494-1501, 2021 Oct.
Статья в английский | MEDLINE | ID: covidwho-1454090

Реферат

OBJECTIVES: To determine if commercially available mouthwash with ß-cyclodextrin and citrox (bioflavonoids) (CDCM) could decrease the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) salivary viral load. METHODS: In this randomized controlled trial, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) PCR-positive patients aged 18-85 years with asymptomatic to mild coronavirus disease 2019 (COVID-19) symptoms for <8 days were recruited. A total of 176 eligible patients were randomly assigned (1:1) to CDCM or placebo. Three rinses daily were performed for 7 days. Saliva sampling was performed on day 1 at 09.00 (T1), 13.00 (T2) and 18.00 (T3). On the following 6 days, one sample was taken at 15.00. Quantitative RT-PCR was used to detect SARS-CoV-2. RESULTS: The intention-to-treat analysis demonstrated that, over the course of 1 day, CDCM was significantly more effective than placebo 4 hours after the first dose (p 0.036), with a median percentage (log10 copies/mL) decrease T1-T2 of -12.58% (IQR -29.55% to -0.16%). The second dose maintained the low median value for the CDCM (3.08 log10 copies/mL; IQR 0-4.19), compared with placebo (3.31 log10 copies/mL; IQR 1.18-4.75). At day 7, there was still a greater median percentage (log10 copies/mL) decrease in salivary viral load over time in the CDCM group (-58.62%; IQR -100% to -34.36%) compared with the placebo group (-50.62%; IQR -100% to -27.66%). These results were confirmed by the per-protocol analysis. CONCLUSIONS: This trial supports the relevance of using CDCM on day 1 (4 hours after the initial dose) to reduce the SARS-CoV-2 viral load in saliva. For long-term effect (7 days), CDMC appears to provide a modest benefit compared with placebo in reducing viral load in saliva.


Тема - темы
Antiviral Agents/therapeutic use , COVID-19/prevention & control , Mouthwashes/therapeutic use , SARS-CoV-2/drug effects , Adolescent , Adult , Aged , Antiviral Agents/chemistry , Asymptomatic Infections , COVID-19/transmission , Double-Blind Method , Female , Flavonoids/analysis , Flavonoids/therapeutic use , Humans , Intention to Treat Analysis , Male , Middle Aged , Mouthwashes/chemistry , SARS-CoV-2/isolation & purification , Saliva/virology , Viral Load/drug effects , Young Adult , beta-Cyclodextrins/analysis , beta-Cyclodextrins/therapeutic use
17.
Trop Biomed ; 38(3): 360-365, 2021 Sep 01.
Статья в английский | MEDLINE | ID: covidwho-1404405

Реферат

COVID-19, caused by the SARS-CoV-2 virus, can lead to massive inflammation in the gastrointestinal tract causing severe clinical symptoms. SARS-CoV-2 infects lungs after binding its spike proteins with alveolar angiotensin-converting enzyme 2 (ACE2), and it also triggers inflammation in the gastrointestinal tract. SARS-CoV-2 invades the gastrointestinal tract by interacting with Toll-like receptor-4 (TLR4) that induces the expression of ACE2. The influx of ACE2 facilitates cellular binding of more SARS-CoV-2 and causes massive gastrointestinal inflammation leading to diarrhea. Diarrhea prior to COVID-19 infection or COVID-19-induced diarrhea reportedly ends up in a poor prognosis for the patient. Flavonoids are part of traditional remedies for gastrointestinal disorders. Preclinical studies show that flavonoids can prevent infectious diarrhea. Recent studies show flavonoids can inhibit the multiplication of SARS-CoV-2. In combination with vitamin D, flavonoids possibly activate nuclear factor erythroid-derived-2-related factor 2 that downregulates ACE2 expression in cells. We suggest that flavonoids have the potential to prevent SARS-CoV-2 induced diarrhea.


Тема - темы
COVID-19/complications , Diarrhea/prevention & control , Flavonoids/therapeutic use , SARS-CoV-2 , Angiotensin-Converting Enzyme 2/physiology , Diarrhea/etiology , Humans
18.
Biomed Pharmacother ; 140: 111596, 2021 Aug.
Статья в английский | MEDLINE | ID: covidwho-1385083

Реферат

Flavonoids are natural phytochemicals known for their antiviral activity. The flavonoids acts at different stages of viral infection, such as viral entrance, replication and translation of proteins. Viruses cause various diseases such as SARS, Hepatitis, AIDS, Flu, Herpes, etc. These, and many more viral diseases, are prevalent in the world, and some (i.e. SARS-CoV-2) are causing global chaos. Despite much struggle, effective treatments for these viral diseases are not available. The flavonoid class of phytochemicals has a vast number of medicinally active compounds, many of which are studied for their potential antiviral activity against different DNA and RNA viruses. Here, we reviewed many flavonoids that showed antiviral activities in different testing environments such as in vitro, in vivo (mice model) and in silico. Some flavonoids had stronger inhibitory activities, showed no toxicity & the cell proliferation at the tested doses are not affected. Some of the flavonoids used in the in vivo studies also protected the tested mice prophylactically from lethal doses of virus, and effectively prevented viral infection. The glycosides of some of the flavonoids increased the solubility of some flavonoids, and therefore showed increased antiviral activity as compared to the non-glycoside form of that flavonoid. These phytochemicals are active against different disease-causing viruses, and inhibited the viruses by targeting the viral infections at multiple stages. Some of the flavonoids showed more potent antiviral activity than the market available drugs used to treat viral infections.


Тема - темы
Antiviral Agents/pharmacology , Antiviral Agents/therapeutic use , Flavonoids/pharmacology , Flavonoids/therapeutic use , Virus Diseases/drug therapy , Viruses/drug effects , Animals , Cell Proliferation/drug effects , Glycosides/metabolism , Humans , Virus Diseases/metabolism
19.
Int J Mol Sci ; 22(16)2021 Aug 20.
Статья в английский | MEDLINE | ID: covidwho-1374421

Реферат

Polyphenols, such as flavonoids and phenolic acids, are a group of specialized metabolites in plants that largely aid in plant defense by deterring biotic stressors and alleviating abiotic stress. Polyphenols offer a wide range of medical applications, acting as preventative and active treatments for diseases such as cancers and diabetes. Recently, researchers have proposed that polyphenols may contribute to certain applications aimed at tackling challenges related to the COVID-19 pandemic. Understanding the beneficial impacts of phytochemicals, such as polyphenols, could potentially help prepare society for future pandemics. Thus far, most reviews have focused on polyphenols in cancer prevention and treatment. This review aims to provide a comprehensive discussion on the critical roles that polyphenols play in both plant chemical defense and human health based on the most recent studies while highlighting prospective avenues for future research, as well as the implications for phytochemical-based applications in both agricultural and medical fields.


Тема - темы
Plants/metabolism , Polyphenols/pharmacology , Polyphenols/therapeutic use , Animals , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents/pharmacology , Antiviral Agents/pharmacology , Biological Availability , COVID-19/drug therapy , COVID-19/prevention & control , Flavonoids/pharmacology , Flavonoids/therapeutic use , Humans , Hydroxybenzoates/pharmacology , Hypoglycemic Agents/pharmacology , Neoplasms/drug therapy , Phytochemicals , Plants/chemistry , Polyphenols/metabolism , Prospective Studies , SARS-CoV-2/drug effects
20.
Biomolecules ; 11(8)2021 08 23.
Статья в английский | MEDLINE | ID: covidwho-1367768

Реферат

In 2019, COVID-19 emerged as a severe respiratory disease that is caused by the novel coronavirus, Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). The disease has been associated with high mortality rate, especially in patients with comorbidities such as diabetes, cardiovascular and kidney diseases. This could be attributed to dysregulated immune responses and severe systemic inflammation in COVID-19 patients. The use of effective antiviral drugs against SARS-CoV-2 and modulation of the immune responses could be a potential therapeutic strategy for COVID-19. Studies have shown that natural phenolic compounds have several pharmacological properties, including anticoronavirus and immunomodulatory activities. Therefore, this review discusses the dual action of these natural products from the perspective of applicability at COVID-19.


Тема - темы
Antiviral Agents/therapeutic use , COVID-19/drug therapy , Flavonoids/therapeutic use , Immunologic Factors/therapeutic use , Phytochemicals/therapeutic use , Protease Inhibitors/therapeutic use , Animals , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Coronavirus/drug effects , Flavonoids/chemistry , Flavonoids/pharmacology , Humans , Immunologic Factors/chemistry , Immunologic Factors/pharmacology , Phytochemicals/chemistry , Phytochemicals/pharmacology , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology
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