scholarly journals Universally available herbal teas based on sage and perilla elicit potent antiviral activity against SARS-CoV-2 in vitro

2020 ◽  
Author(s):  
Vu Thuy Khanh Le-Trilling ◽  
Denise Mennerich ◽  
Corinna Schuler ◽  
Yulia Flores-Martinez ◽  
Benjamin Katschinski ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Low Income ◽  
Treatment Options ◽  
Herd Immunity ◽  
Cost Effective ◽  
Efficient Treatment ◽  
Potent Antiviral Activity ◽  
Approved Drugs ◽  
Socioeconomic Crisis

AbstractThe current SARS-CoV-2/COVID-19 pandemic represents an unprecedented medical and socioeconomic crisis. Highly efficient treatment options preventing morbidity and mortality are not broadly available and approved drugs are hardly affordable in developing countries. Even after vaccine approvals, it will take several months until the vaccinated and convalescent individuals establish herd immunity. Meanwhile, non-pharmaceutical interventions and antiviral treatments are indispensable to curb the death toll of the pandemic. To identify cost-effective and ubiquitously available options, we tested common herbs consumed worldwide as herbal teas. We found that aqueous infusions prepared by boiling leaves of the Lamiaceae plants perilla and sage elicit potent antiviral activity against SARS-CoV-2 in human cells. Sustained antiviral activity was evident even when cells were treated for only half an hour, and in therapeutic as well as prophylactic regimens. Given the urgency, such inexpensive and broadly available substances might provide help during the pandemic - especially in low-income regions.

scholarly journals Pharmacologic treatment of osteoporosis – 2011

2011 ◽  
Vol 152 (33) ◽  
pp. 1320-1326 ◽  
Author(s):  
Péter Lakatos
Keyword(s):  
Bone Loss ◽  
Fracture Risk ◽  
Hormone Replacement ◽  
Treatment Options ◽  
Osteoporotic Fractures ◽  
Cost Effective ◽  
Similar Efficacy ◽  
High Fracture ◽  
Efficient Treatment ◽  
Treatment Of Osteoporosis

Osteoporosis affects approximately 9% of the population in Hungary resulting in about 100 000 osteoporotic fractures annually. Thirty-five percent of patients with hip fractures due to osteoporosis will die within 1 year. Direct costs of osteoporosis exceed 25 billion forints per year. Apparently, cost-effective reduction of bone loss and consequent fracture risk will add up to not only financial savings but improvement in quality of life, as well. A number of pharmacological modalities are available for this purpose. The mainstay of the treatment of osteoporosis is the bisphosphonate group that includes effective anti-resorptive compounds mitigating bone loss and fragility. The recently registered denosumab exhibits similar efficacy by neutralizing RANK ligand, however, marked differences can be observed between the two drug classes. Strontium has a unique mechanism of action by rebalancing bone turnover, and thus, providing an efficient treatment option for the not fast bone losers who are at high fracture risk. The purely anabolic teriparatide is available for the extremely severe osteoporotic patients and for those who do not respond to other types of therapy. Older treatment options such as hormone replacement therapy, raloxifene, tibolone or calcitonin may also have a restricted place in the management of osteoporosis. Orv. Hetil., 2011, 152, 1320–1326.

scholarly journals Artemisia annua L. extracts prevent in vitro replication of SARS-CoV-2

2021 ◽  
Author(s):  
Manoj S Nair ◽  
Yaoxing Huang ◽  
David A Fidock ◽  
Stephen J Polyak ◽  
Jessica Wagoner ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Antimalarial Drug ◽  
Artemisia Annua ◽  
Cost Effective ◽  
Hot Water ◽  
Total Flavonoids ◽  
Leaf Extracts ◽  
Artemisinin Derivatives

SARS-CoV-2 (Covid-19) globally has infected and killed millions of people. Besides remdesivir, there are no approved small molecule-based therapeutics. Here we show that extracts of the medicinal plant, Artemisia annua L., which produces the antimalarial drug artemisinin, prevents SARS-CoV-2 replication in vitro. We measured antiviral activity of dried leaf extracts of seven cultivars of A. annua sourced from four continents. Hot-water leaf extracts based on artemisinin, total flavonoids, or dry leaf mass showed antiviral activity with IC50 values of 0.1-8.7 μM, 0.01-0.14 μg, and 23.4-57.4 μg, respectively. One sample was >12 years old, but still active. While all hot water extracts were effective, concentrations of artemisinin and total flavonoids varied by nearly 100-fold in the extracts and antiviral efficacy was inversely correlated to artemisinin and total flavonoid contents. Artemisinin alone showed an estimated IC50 of about 70 μM, and antimalarial artemisinin derivatives artesunate, artemether, and dihydroartemisinin were ineffective or cytotoxic at elevated micromolar concentrations. In contrast, the antimalarial drug amodiaquine had an IC50 = 5.8 μM. The extracts had minimal effects on infection of Vero E6 or Calu-3 cells by a reporter virus pseudotyped by the SARS-CoV-2 spike protein. There was no cytotoxicity within an order of magnitude of the antiviral IC90 values. Results suggest the active component in the extracts is likely something besides artemisinin or is a combination of components acting synergistically to block post-entry viral infection. Further studies will determine in vivo efficacy to assess whether A. annua might provide a cost-effective therapeutic to treat SARS-CoV-2 infections.

scholarly journals Synthesis and Broad Antiviral Activity of Novel 2-aryl-isoindolin-1-ones towards Diverse Enterovirus A71 Clinical Isolates

Molecules ◽  
2019 ◽  
Vol 24 (5) ◽  
pp. 985 ◽  
Author(s):  
Yixuan Wang ◽  
Huiqiang Wang ◽  
Xinbei Jiang ◽  
Zhi Jiang ◽  
Tingting Guo ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Enterovirus 71 ◽  
Foot And Mouth Disease ◽  
Viral Disease ◽  
Clinical Isolates ◽  
Dependent Manner ◽  
Potent Antiviral Activity ◽  
Sar Studies ◽  
Enterovirus A71

Enterovirus 71 (EV-A71) is the main causative pathogen of childhood hand, foot and mouth disease. Effective medicine is currently unavailable for the treatment of this viral disease. Using the fragment-hopping strategy, a series of 2-aryl-isoindolin-1-one compounds were designed, synthesized and investigated for their in vitro antiviral activity towards multiple EV-A71 clinical isolates (H, BrCr, Shenzhen98, Jiangsu52) in Vero cell culture in this study. The structure–activity relationship (SAR) studies identified 2-phenyl-isoindolin-1-ones as a new potent chemotype with potent antiviral activity against EV-A71. Ten out of the 24 tested compounds showed significant antiviral activity (EC50 < 10 µM) towards four EV-A71 strains. Compounds A3 and A4 exhibited broad and potent antiviral activity with the 50% effective concentration (EC50) values in the range of 1.23–1.76 μM. Moreover, the selectivity indices of A3 and A4 were significantly higher than those of the reference compound, pirodavir. The western blotting experiment indicated that the viral VP1 was significantly decreased at both the protein and RNA level in a dose-dependent manner following treatment with compound A3. Moreover, compound A3 inhibited the viral replication by acting on the virus entry stage. In summary, this study led to the discovery of 2-aryl-isoindolin-1-ones as a promising scaffold with potent anti-EV-A71 activities, which deserves further in-depth studies.

Potent antiviral activity of Solanum rantonnetii and the isolated compounds against hepatitis C virus in vitro

2014 ◽  
Vol 11 ◽  
pp. 185-191 ◽  
Author(s):  
Khaled Rashed ◽  
Marie-Emmanuelle Sahuc ◽  
Gaspard Deloison ◽  
Noémie Calland ◽  
Priscille Brodin ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Antiviral Activity ◽  
Potent Antiviral Activity

scholarly journals In Vitro Assessment of the Antiviral Activity of Ketotifen, Indomethacin and Naproxen, Alone and in Combination, against SARS-CoV-2

Viruses ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 558
Author(s):  
Pantea Kiani ◽  
Andrew Scholey ◽  
Thomas A. Dahl ◽  
Lauren McMann ◽  
Jacqueline M. Iversen ◽  
...  
Keyword(s):  
Infectious Disease ◽  
Severe Acute Respiratory Syndrome ◽  
Antiviral Activity ◽  
Synergistic Effect ◽  
Treatment Options ◽  
Drug Combinations ◽  
Cytotoxic Effects ◽  
Viral Yield ◽  
In Vitro Assessment

The 2019 coronavirus infectious disease (COVID-19) is caused by infection with the new severe acute respiratory syndrome coronavirus (SARS-CoV-2). Currently, the treatment options for COVID-19 are limited. The purpose of the experiments presented here was to investigate the effectiveness of ketotifen, naproxen and indomethacin, alone or in combination, in reducing SARS-CoV-2 replication. In addition, the cytotoxicity of the drugs was evaluated. The findings showed that the combination of ketotifen with indomethacin (SJP-002C) or naproxen both reduce viral yield. Compared to ketotifen alone (60% inhibition at EC50), an increase in percentage inhibition of SARS-CoV-2 to 79%, 83% and 93% was found when co-administered with 25, 50 and 100 μM indomethacin, respectively. Compared to ketotifen alone, an increase in percentage inhibition of SARS-CoV-2 to 68%, 68% and 92% was found when co-administered with 25, 50 and 100 μM naproxen, respectively. For both drug combinations the observations suggest an additive or synergistic effect, compared to administering the drugs alone. No cytotoxic effects were observed for the administered dosages of ketotifen, naproxen, and indomethacin. Further research is warranted to investigate the efficacy of the combination of ketotifen with indomethacin (SJP-002C) or naproxen in the treatment of SARS-CoV-2 infection in humans.

scholarly journals Broad anti-coronaviral activity of FDA approved drugs against SARS-CoV-2 in vitro and SARS-CoV in vivo

2020 ◽  
Author(s):  
Stuart Weston ◽  
Christopher M. Coleman ◽  
Rob Haupt ◽  
James Logue ◽  
Krystal Matthews ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Rapid Development ◽  
Drug Repurposing ◽  
Ic50 Values ◽  
Human Use ◽  
Approved Drugs ◽  
Fda Approved Drugs

AbstractSARS-CoV-2 emerged in China at the end of 2019 and has rapidly become a pandemic with roughly 2.7 million recorded COVID-19 cases and greater than 189,000 recorded deaths by April 23rd, 2020 (www.WHO.org). There are no FDA approved antivirals or vaccines for any coronavirus, including SARS-CoV-2. Current treatments for COVID-19 are limited to supportive therapies and off-label use of FDA approved drugs. Rapid development and human testing of potential antivirals is greatly needed. A quick way to test compounds with potential antiviral activity is through drug repurposing. Numerous drugs are already approved for human use and subsequently there is a good understanding of their safety profiles and potential side effects, making them easier to fast-track to clinical studies in COVID-19 patients. Here, we present data on the antiviral activity of 20 FDA approved drugs against SARS-CoV-2 that also inhibit SARS-CoV and MERS-CoV. We found that 17 of these inhibit SARS-CoV-2 at a range of IC50 values at non-cytotoxic concentrations. We directly follow up with seven of these to demonstrate all are capable of inhibiting infectious SARS-CoV-2 production. Moreover, we have evaluated two of these, chloroquine and chlorpromazine, in vivo using a mouse-adapted SARS-CoV model and found both drugs protect mice from clinical disease.

scholarly journals Therapeutic efficacy of an oral nucleoside analog of remdesivir against SARS-CoV-2 pathogenesis in mice.

2021 ◽  
Author(s):  
Alexandra Schafer ◽  
David R Martinez ◽  
John J Won ◽  
Fernanado R Moreira ◽  
Ariane J Brown ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Therapeutic Efficacy ◽  
Treatment Options ◽  
Pharmacokinetic Profile ◽  
Nucleoside Analog ◽  
Lung Pathology ◽  
Orally Bioavailable ◽  
Therapeutic Monoclonal Antibodies

The COVID-19 pandemic remains uncontrolled despite the rapid rollout of safe and effective SARS-CoV-2 vaccines, underscoring the need to develop highly effective antivirals. In the setting of waning immunity from infection and vaccination, breakthrough infections are becoming increasingly common and treatment options remain limited. Additionally, the emergence of SARS-CoV-2 variants of concern with their potential to escape therapeutic monoclonal antibodies emphasizes the need to develop second-generation oral antivirals targeting highly conserved viral proteins that can be rapidly deployed to outpatients. Here, we demonstrate the in vitro antiviral activity and in vivo therapeutic efficacy of GS-621763, an orally bioavailable prodrug of GS-441524, the parental nucleoside of remdesivir, which targets the highly conserved RNA-dependent RNA polymerase. GS-621763 exhibited significant antiviral activity in lung cell lines and two different human primary lung cell culture systems. The dose-proportional pharmacokinetic profile observed after oral administration of GS-621763 translated to dose-dependent antiviral activity in mice infected with SARS-CoV-2. Therapeutic GS-621763 significantly reduced viral load, lung pathology, and improved pulmonary function in COVID-19 mouse model. A direct comparison of GS-621763 with molnupiravir, an oral nucleoside analog antiviral currently in human clinical trial, proved both drugs to be similarly efficacious. These data demonstrate that therapy with oral prodrugs of remdesivir can significantly improve outcomes in SARS-CoV-2 infected mice. Thus, GS-621763 should be explored as a potential treatment for COVID-19 in humans.

Drug repositioning: A Unique Approach to Refurbish Drug Discovery

2021 ◽  
Vol 18 ◽  
Author(s):  
Mayura A Kale ◽  
Prashant B Shamkuwar ◽  
Vishnukant K Mourya ◽  
Aishwarya B Deshpande ◽  
Priyanka A Shelke
Keyword(s):  
Drug Discovery ◽  
Drug Repositioning ◽  
Cost Effective ◽  
Positive Outcomes ◽  
Computational Tools ◽  
Therapeutic Implications ◽  
Novel Drugs ◽  
Unique Approach ◽  
Approved Drugs

: Since a decade, it has been observed that there is remarkable decrease in the quantum of novel clinically approved drugsin spite of modernization in research and development process. We have highlighted repositioning of drugs as a methodology that has found new therapeutic implications for clinically approved drugs but with different indications. This can be considered as an upbringing strategy to deliver timely and cost-effective solutions which still needexplorationtoget over the shortage of number of novel drugs reaching market. This review focuses on activity-based drug repositioning approach, which is used to explore new uses of known drugs that are already approved for specific indications and are now being used for other indications on the basis ofthe fact that single drug interacts with multiple targets. It also includes current research trends related to drug repositioning which depends on strong knowledge of medicinal chemistry and involves elucidation of mechanisms of action and validation of novel targets. The review highlights theimportance totheusage of computational tools and databases of various forms for drug repositioning purposes which have enhanced the ability to pose reasonable and testable hypotheses. The critical nature of this aspect is obvious in cases where data gathered from in vitro or animal models do not confirm in subsequent clinical trials. Hence, considering positive outcomes of drug repositioning, it can be surmised that this approach can serve as promising one that can develop into a robust drug discovery strategy.

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