Natural products and herbal medicine have been widely used in drug discovery for treating infectious diseases. Recent outbreak of COVID-19 requires various therapeutic strategies. Here, we used ...YSK-A, a mixture of three herbal components Boswellia serrata, Commiphora myrrha, and propolis, to evaluate potential antiviral activity against SARS-CoV-2. We showed that YSK-A inhibited SARS-CoV-2 propagation with an IC
values of 12.5 µg/ml and 15.42 µg/ml in Vero E6 and Calu-3 cells, respectively. Using transcriptome analysis, we further demonstrated that YSK-A modulated various host gene expressions in Calu-3 cells. Among these, we selected 9 antiviral- or immune-related host genes for further study. By siRNA-mediated knockdown experiment, we verified that MUC5AC, LIF, CEACAM1, and GDF15 host genes were involved in antiviral activity of YSK-A. Therefore, silencing of these genes nullified YSK-A-mediated inhibition of SARS-CoV-2 propagation. These data indicate that YSK-A displays an anti-SARS-CoV-2 activity by targeting multiple antiviral genes. Although the exact antiviral mechanism of each constituent has not been verified yet, our data indicate that YSK-A has an immunomodulatory effect on SARS-CoV-2 and thus it may represent a novel natural product-derived therapeutic agent for treating COVID-19.
Mice exhibiting deficits in social behavior may provide valuable models for autistic-like behavioral problems. We tested social interactions in male mice from three inbred strains: C57BL/6J (B6), ...BALB/cJ (C) and DBA/2J (D2). All three strains showed gradual habituation of the number of social interactions with an ovariectomized female over four subsequent 2
min sessions, returning to initial levels when presented with another stimulus mouse. Next, we studied males with a knockout mutation in the
Fmr1 gene on a B6 background. KO animals showed strongly reduced levels of social interaction, which were about similar as those of habituated controls. This social behavior deficit suggests that
Fmr1 KO mice could possibly be used as models for autistic behaviors.
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of coronavirus disease 2019 (COVID-19). SARS-CoV-2 propagation is mediated by the protein interaction between viral ...proteins and host cells. Tyrosine kinase has been implicated in viral replication, and hence, it has become a target for developing antiviral drugs. We have previously reported that receptor tyrosine kinase inhibitor blocks the replication of hepatitis C virus (HCV). In the present study, we investigated two receptor tyrosine kinase-specific inhibitors, amuvatinib and imatinib, for their potential antiviral efficacies against SARS-CoV-2. Treatment with either amuvatinib or imatinib displays an effective inhibitory activity against SARS-CoV-2 propagation without an obvious cytopathic effect in Vero E6 cells. Notably, amuvatinib exerts a stronger antiviral activity than imatinib against SARS-CoV-2 infection. Amuvatinib blocks SARS-CoV-2 infection with a 50% effective concentration (EC
) value ranging from ~0.36 to 0.45 μM in Vero E6 cells. We further demonstrate that amuvatinib inhibits SARS-CoV-2 propagation in human lung Calu-3 cells. Using pseudoparticle infection assay, we verify that amuvatinib blocks SARS-CoV-2 at the entry step of the viral life cycle. More specifically, amuvatinib inhibits SARS-CoV-2 infection at the binding-attachment step. Moreover, amuvatinib exhibits highly efficient antiviral activity against emerging SARS-CoV-2 variants. Importantly, we demonstrate that amuvatinib inhibits SARS-CoV-2 infection by blocking ACE2 cleavage. Taken together, our data suggest that amuvatinib may provide a potential therapeutic agent for the treatment of COVID-19.
Tyrosine kinase has been implicated in viral replication and has become an antiviral drug target. Here, we chose two well-known receptor tyrosine kinase inhibitors, amuvatinib and imatinib, and evaluated their drug potencies against SARS-CoV-2. Surprisingly, amuvatinib displays a stronger antiviral activity than imatinib against SARS-CoV-2. Amuvatinib blocks SARS-CoV-2 infection by inhibiting ACE2 cleavage and the subsequent soluble ACE2 receptor. All these data suggest that amuvatinib may be a potential therapeutic agent in SARS-CoV-2 prevention for those experiencing vaccine breakthroughs.
African swine fever virus (ASFV), an extremely contagious virus with high mortality rates, causes severe hemorrhagic viral disease in both domestic and wild pigs. Fortunately, ASFV cannot be ...transmitted from pigs to humans. However, ongoing ASFV outbreaks could have severe economic consequences for global food security. Although ASFV was discovered several years ago, no vaccines or treatments are commercially available yet; therefore, the identification of new anti-ASFV drugs is urgently warranted. Using molecular docking and machine learning, we have previously identified pentagastrin, cangrelor, and fostamatinib as potential antiviral drugs against ASFV. Here, using machine learning combined with docking simulations, we identified natural products with a high affinity for
Asfv
PolX proteins. We selected five natural products (NPs) that are located close in chemical space to the six known natural flavonoids that possess anti-ASFV activity. Polygalic acid markedly reduced
Asfv
PolX polymerase activity in a dose-dependent manner. We propose an efficient protocol for identifying NPs as potential antiviral drugs by identifying chemical spaces containing high-affinity binders against ASFV in NP databases.
In this study, the essential oils from lemon (Citrus aurantifolia) peels were extracted using hydrodistillation and microwave-assisted hydrodistillation and their volatile compositions were compared ...via gas chromatography-mass spectrometry (GC-MS) analysis. Microwave-assisted hydrodistillation (MHD) achieved the oil yield of 2.48% at microwave power of 470W and extraction time of 60 min. The yield obtained using conventional hydrodistillation (HD) was 2.2% at 90 min at 120 °C. GC-MS analysis revealed a total of 17 and 8 components existing in the oil samples produced by MHD and HD methods respectively. The main components shared by both samples were limonene, α-pinene, β-pinene, β-cymene, ocimene, and sabinene. Overall, these results suggest that MHD could produce lemon (Citrus aurantifolia) peels essential oil at a higher yield within a shortened period of time as compared to the traditional HD, thus it could be used as an alternative for HD to reduce costs of the extraction process.
The mandarin (Citrus reticulata Blanco) essential oil is well-known for bactericidal, antioxidant and anti-cancer properties. Thus, an effective extraction method is required to obtain high oil yield ...with an abundant content of bioactive compounds. In the present study, the chemical profiles of essential oils extracted from the peels of Mandarin) via hydrodistillation (HD), microwave-assisted hydrodistillation (MAHD) and microwave extraction (ME) were reported in this study. Extraction techniques were carried out at their optimal conditions and the results were compared with each other. Gas chromatography-mass spectrometry (GC-MS) was employed to perform compositional determination. A total of 5 components was determined, accounting for almost 100% of total oil content. The extraction efficiencies were 3.6%, 6.8%, and 5.5% respectively obtained from HD, MAHD and ME. The results showed that MAHD seemed to result in higher yield and essential oil with identical chemical composition and quality in comparison with those of other methods, suggesting that MAHD was a potential alternative method to HD to reduce the time and cost of the extraction process.
The essential oils (EOs) from peels of Citrus grandis (L.) Osbeck was investigated for their antimicrobial activities against food-related microorganisms by hydrodistillation method (HD), and ...microwave-assisted extraction (MAHD). The total yield of the volatile fractions obtained through HD and MAHD was 4.4 mL/g and 4.75 mL/g, respectively. The gas chromatography-mass spectrometry (GC-MS) analyses of the oils revealed the presence of different compounds in Citrus grandis EOs obtained from MAHD and HD methods, including α-pinene, sabinene, β-myrcene, α-phellandrene and d-limonene. The essential oils obtained from the two extraction methods were found to inhibit six bacteria strains including Bacillus cereus, Bacillus subtilis, Pseudomonas aeruginosa, E. coli, Clostridium perfringens and Salmonella typhi. The results of antibacterial properties of Citrus grandis (L.) Osbeck EOs against six bacterial strains showed that essential oil extracted from the HD method were more bacteriostatic than the oil extracted from MAHD method. With this result, the essential oil obtained by the HD method was more active than that of the MADH method against the bacteria.
The essential oils (EOs) was extracted from Persian lime (Citrus latifolia) peels collected in Hau Giang province, Vietnam. Volatile compositions of EOs obtained by three extraction methods of ...hydrodistillation (HD), steam distillation (SD) and microwave extraction (ME) were analyzed and compared. The volatile compounds in EOs were analyzed based on gas chromatography-mass spectrometry (GC-MS). An amount of 3 ml/g, 2.3 ml/g and 4 ml/g of EOs was obtained from HD, SD and ME with twenty-one compounds were identified, accounting for 99% -100% of the total oil content. Limonene, β-pinene, α-pinene, γ-Terpinene, α-citral, β-citral and Sabinene are the major compound in essential oil. However, there were qualitative and quantitative differences between oil samples obtained by the three extraction methods. The difference is probably due to the influence of different environmental factors and specific characteristics of each extraction method. The results of this study will provide information on the content and chemical composition of Lemon peels. C. latifolia and serve as a stepping stone for further research into the applications of the compound to cosmetic, food and pharmaceutical products.
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