Evaluation of the inhibitory potential of essential oils and aromatic extracts on SARS-CoV-2 Mpro and PLpro

Author(s):  
Daniel Strub ◽  
Michał Talma ◽  
Maria Strub ◽  
Wioletta Rut ◽  
Mikołaj Żmudziński ◽  
...  

Abstract Essential oils and aromatic extracts (oleoresins, absolutes, concretes, resinoids) are often used as food flavorings and constituents of fragrance compositions. The flavor and fragrance industry observes significant growth in sales of some natural materials during the COVID-19 outbreak. Some companies worldwide are making false claims regarding their essential oils or blends to be effective (or indirectly points towards this conclusion) against coronaviruses even though the available data on the activity of plant materials against highly pathogenic human coronaviruses is very scarce. Our exploratory study aimed to develop pioneering knowledge, and provide the first experimental results on the inhibitory properties of hundreds of flavor & fragrance materials against SARS-CoV-2 main- and papain-like proteases. As essential oils are volatile products, they could provide an interesting subsidiary inhalation therapeutic strategy in the long term.

2021 ◽  
Author(s):  
Daniel Strub ◽  
Michał Talma ◽  
Maria Strub ◽  
Wioletta Rut ◽  
Mikołaj Żmudziński ◽  
...  

Abstract Essential oils and aromatic extracts (oleoresins, absolutes, concretes, resinoids) are often used as food flavorings and constituents of fragrance compositions. The flavor and fragrance industry observes significant growth in sales of some natural materials during the COVID-19 outbreak. Some companies worldwide are making false claims regarding their essential oils or blends to be effective (or indirectly points towards this conclusion) against coronaviruses even though the available data on the activity of plant materials against highly pathogenic human coronaviruses is very scarce. Our exploratory study aimed to develop pioneering knowledge and provide the first experimental results on the inhibitory properties of hundreds of flavor & fragrance materials against SARS-CoV-2 main- and papain-like proteases, and antiviral potential of the most active protease inhibitors. As essential oils are volatile products, they could provide an interesting subsidiary inhalation therapeutic strategy in the long term.


Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2692
Author(s):  
Adriana Trifan ◽  
Gokhan Zengin ◽  
Mihai Brebu ◽  
Krystyna Skalicka-Woźniak ◽  
Simon Vlad Luca

The essential oil industry of aromatic herbs and spices is currently producing a significant amount of by-products, such as the spent plant materials remaining after steam or hydrodistillation, that are simply discarded. The aim of this study was to comparatively investigate the phytochemical composition, antioxidant and multi-enzymatic inhibitory potential of the essential oils and spent plant material extractives obtained from cinnamon, cumin, clove, laurel, and black pepper. The essential oils were characterized by the presence of several phytochemical markers (cinnamaldehyde, cuminaldehyde, eugenol, eucalyptol, α-terpinene, limonene, β-caryophyllene or β-pinene). On the other hand, the LC-HRMS/MS profiling of the spent material extracts allowed the annotation of species specific and non-specific metabolites, such as organic acids, phenolic acids, flavonoids, proanthocyanidins, hydrolysable tannins, fatty acids, or piperamides. All samples exhibited very strong antioxidant effects, with the clove essential oil displaying the strongest radical scavenging (525.78 and 936.44 mg TE/g in DPPH and ABTS assays), reducing (2848.28 and 1927.98 mg TE/g in CUPRAC and FRAP), and total antioxidant capacity (68.19 mmol TE/g). With respect to the anti-acetylcholinesterase (0.73–2.95 mg GALAE/g), anti-butyrylcholinesterase (0–3.41 mg GALAE/g), anti-tyrosinase (0–76.86 mg KAE/g), anti-amylase and anti-glucosidase (both 0–1.00 mmol ACAE/g) assays, the spice samples showed a modest activity. Overall, our study reports that, not only the volatile fractions of common spices, but also their spent plant materials remaining after hydrodistillation can be regarded as rich sources of bioactive molecules with antioxidant and multi-enzymatic inhibitory effects.


2020 ◽  
Vol 17 ◽  
Author(s):  
Anisha D’Souza ◽  
Ranjita Shegokar

: In recent years, SLNs and NLCs are among the popular drug delivery systems studied for delivery of lipophilic drugs. Both systems have demonstrated several beneficial properties as an ideal drug-carrier, optimal drug-loading and good long-term stability. NLCs are getting popular due to their stability advantages and possibility to load various oil components either as an active or as a matrix. This review screens types of oils used till date in combination with solid lipid to form NLCs. These oils are broadly classified in two categories: Natural oils and Essential oils. NLCs offer range advantages in drug delivery due to the formation of imperfect matrix owing to the presence of oil. The type and percentage of oil used determines optimal drug loading and stability. Literature shows that variety of oils is used in NLCs mainly as matrix, which is from natural origin, triglycerides class. On the other hand, essential oils not only serve as a matrix but as an active. In short, oil is the key ingredient in formation of NLCs, hence needs to be selected wisely as per the performance criteria expected.


Viruses ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1457
Author(s):  
Dewald Schoeman ◽  
Burtram C. Fielding

Over the past 18 years, three highly pathogenic human (h) coronaviruses (CoVs) have caused severe outbreaks, the most recent causative agent, SARS-CoV-2, being the first to cause a pandemic. Although much progress has been made since the COVID-19 pandemic started, much about SARS-CoV-2 and its disease, COVID-19, is still poorly understood. The highly pathogenic hCoVs differ in some respects, but also share some similarities in clinical presentation, the risk factors associated with severe disease, and the characteristic immunopathology associated with the progression to severe disease. This review aims to highlight these overlapping aspects of the highly pathogenic hCoVs—SARS-CoV, MERS-CoV, and SARS-CoV-2—briefly discussing the importance of an appropriately regulated immune response; how the immune response to these highly pathogenic hCoVs might be dysregulated through interferon (IFN) inhibition, antibody-dependent enhancement (ADE), and long non-coding RNA (lncRNA); and how these could link to the ensuing cytokine storm. The treatment approaches to highly pathogenic hCoV infections are discussed and it is suggested that a greater focus be placed on T-cell vaccines that elicit a cell-mediated immune response, using rapamycin as a potential agent to improve vaccine responses in the elderly and obese, and the potential of stapled peptides as antiviral agents.


Infection ◽  
2021 ◽  
Author(s):  
Ali Hamady ◽  
JinJu Lee ◽  
Zuzanna A. Loboda

Abstract Objectives The coronavirus disease 2019 (COVID-19), caused by the novel betacoronavirus severe acute respiratory syndrome 2 (SARS-CoV-2), was declared a pandemic in March 2020. Due to the continuing surge in incidence and mortality globally, determining whether protective, long-term immunity develops after initial infection or vaccination has become critical. Methods/Results In this narrative review, we evaluate the latest understanding of antibody-mediated immunity to SARS-CoV-2 and to other coronaviruses (SARS-CoV, Middle East respiratory syndrome coronavirus and the four endemic human coronaviruses) in order to predict the consequences of antibody waning on long-term immunity against SARS-CoV-2. We summarise their antibody dynamics, including the potential effects of cross-reactivity and antibody waning on vaccination and other public health strategies. At present, based on our comparison with other coronaviruses we estimate that natural antibody-mediated protection for SARS-CoV-2 is likely to last for 1–2 years and therefore, if vaccine-induced antibodies follow a similar course, booster doses may be required. However, other factors such as memory B- and T-cells and new viral strains will also affect the duration of both natural and vaccine-mediated immunity. Conclusion Overall, antibody titres required for protection are yet to be established and inaccuracies of serological methods may be affecting this. We expect that with standardisation of serological testing and studies with longer follow-up, the implications of antibody waning will become clearer.


2020 ◽  
Vol 22 (Supplement_3) ◽  
pp. iii414-iii414
Author(s):  
Muh-Lii Liang ◽  
Tsung-Han Hsieh ◽  
Tai-Tong Wong

Abstract BACKGROUND Glial-lineage tumors constitute a heterogeneous group of neoplasms, comprising gliomas, oligodendrogliomas, and ependymomas, which account for 40%–50% of all pediatric central nervous system tumors. Advances in modern neuro-oncological therapeutics are aimed at improving neoadjuvant chemotherapy and deferring radiotherapy because radiation exposure may cause long-term side effects on the developing brain in young children. Despite aggressive treatment, more than half the high-grade gliomas (pHGGs) and one-third of ependymomas exhibit recurrence within 2 years of initial treatment. METHODS By using integrated bioinformatics and through experimental validation, we found that at least one gene among CCND1, CDK4, and CDK6 was overexpressed in pHGGs and ependymomas. RESULTS The use of abemaciclib, a highly selective CDK4/6 inhibitor, effectively inhibited cell proliferation and reduced the expression of cell cycle–related and DNA repair–related gene expression, which was determined through RNA-seq analysis. The efficiency of abemaciclib was validated in vitro in pHGGs and ependymoma cells and in vivo by using subcutaneously implanted ependymoma cells from patient-derived xenograft (PDX) in mouse models. Abemaciclib demonstrated the suppression of RB phosphorylation, downstream target genes of E2F, G2M checkpoint, and DNA repair, resulting in tumor suppression. CONCLUSION Abemaciclib showed encouraging results in preclinical pediatric glial-lineage tumors models and represented a potential therapeutic strategy for treating challenging tumors in children.


2004 ◽  
Vol 59 (9-10) ◽  
pp. 641-648 ◽  
Author(s):  
Marek Mardarowicz ◽  
Dorota Wianowska ◽  
Andrzej L. Dawidowicz ◽  
Ryszard Sawicki

Abstract Terpenes emitted by conifer trees are generally determined by analysing plant extracts or essential oils, prepared from foliage and cones using steam distillation. The application of these procedures limits experiments to cut plant materials. Recently headspace techniques have been adopted to examine terpene emission by living plants. This paper deals with the application of solid-phase micro-extraction (SPME) for the analysis of terpenes emitted by conifers foliage of Engelmann spruce (Picea engelmannii), including its seedlings. The compositions of SPME extracts obtained for destroyed and non-destroyed old and juvenile spruce needles were compared with the compositions of essential oils and pressurised liquid extraction (PLE) extracts corresponding to the same plant materials. No substantial differences have been found in the qualitative terpene composition estimated by analysing essential oil and PLE and SPME extracts from non-destroyed old and juvenile foliage. The disintegration of spruce needles results in the formation of a significant amount of myrcene in the case of the old conifer foliage and non-terpenoic compounds in the case of juvenile conifer foliage. This phenomenon can be attributed to enzymatic reactions occurring in the destroyed plant cells.


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