Sambucus ebulus (Elderberry) Fruits Modulate Inflammation and Complement System Activity in Humans.

Sambucus ebulus (SE) fruits are used for immune stimulation and amelioration of gastrointestinal inflammatory conditions. Currently, there is no scientific evidence of their effects on various aspects of the immune response mechanisms in humans. The purpose of this study was to evaluate the immunomodulatory potential of SE fruit infusion intake in healthy humans. Anthocyanin content was determined with UPLC-ESI-MS/MS. Fifty-three volunteers enrolled in a 4-week SE infusion intake intervention. Blood count, serum total protein, Interleukin 1 beta (IL-1ß), Interleukin 6 (IL-6), Tumor Necrosis Factor Alpha (TNFα), High-sensitivity C-reactive protein (hs-CRP), C3, and C4 levels were measured on automatic analyzers, and Interleukin 8 (IL-8) was measured manually with an ELISA kit. Cyanidin-3-O-galactoside (48.15 mg/g DW), followed by cyaniding-3-sambubioside (43.41 ± 1.07 mg/g DW), were the most abundant anthocyanins in SE samples. A significant decrease in total protein (2.82%), IL-6 (20.15%), TNFα (5.38%), IL-8 (5.50%), C3 (4.16%), and C4 (14.29%) was established in the whole group. Total protein, IL-8, TNFα, and C4 decreased in women (3.11%, 4.76%, 5.09%, and 11.11%), and IL-6 decreased (40.61%) in men. Hb (1.20%) and hematocrit (1.55%) levels decreased in the whole group and in the women group (1.61% and 2.20%). SE fruits exert immune-modulatory activity as revealed by decreased pro-inflammatory status and complement activity markers in healthy volunteers after a 4-week intervention.

Corozo (Bactris guineensis) fruit extract has antiviral activity in vitro against SARS-CoV-2

Background: Given the current COVID-19 pandemic, numerous drug development studies are being carried out for the treatment and control of this disease. This study aimed to evaluate the in vitro antiviral potential of Corozo fruit extract (Bactris guineensis) against SARS-CoV-2.Methods: Corozo extract (CE) was prepared from the pulp of mature Corozo fruits. The total content of phenols, flavonoids, and anthocyanins in the extracts was determined using the Folin-Ciocalteu, aluminum chloride, and pH differential methods, respectively. The cytotoxicity on Vero E6 cells was evaluated by MTT assay. Antiviral activity was evaluated by pre-post-treatment using a Colombian isolate of SARS-CoV-2. Viral titer was quantified by plaque assay.Results: Anthocyanin concentration of CE was 144.95 +/- 10.3 mg cyanidin-3-glucoside/L. The cytotoxicity of CE on Vero E6 was lower to 20 % at 15.6 g/L. Corozo extract inhibited SARS-CoV-2 at 15.6, 7.8, 3.9 and 1.9 g/L with inhibition percentages of 88.2%, 84%, 59.6% and 56.3%, respectively.Conclusion: This is the first report on the in vitro antiviral effect of Corozo fruit extract against SARS-CoV-2. Since this is a natural product, proven safe for consumption, in the future and with further studies, it could be considered an important functional food that can be useful in preventing strategies to fight against COVID-19.

Geographic Variability of Berry Phytochemicals with Antioxidant and Antimicrobial Properties.

The aim of this study was to determine the variability of several chemical compounds and the antioxidant and antimicrobial activities of eight types of berries harvested from two different geographical regions in the same year. The analyses were performed on bilberry, black currant, gooseberry, red currant, raspberry, sea buckthorn, strawberry and sour cherry, which were handpicked during the summer of 2019, in the same periods when they are typically harvested for consumer purposes. Total anthocyanins content (TAC), total flavonoids content (TFC), total polyphenolic compounds (TPC), determination of the Ferric-Reducing Antioxidant Power (FRAP), determination of the DPPH free radical scavenging assay (RSA), determination of nine phenolic compounds by HPLC-UV assay and antimicrobial activity were determined for undiluted hydroalcoholic extracts of all the studied berries. The results showed that the berries from Romania were richer in antioxidant compounds than the berries from Russia. The TPC content varied between 4.13-22.2 mg GAE/g d.w., TFC between 3.33-8.87 mg QE/g d.w. and TAC between 0.13-3.94 mg/g d.w. The highest variability was determined for TPC. Regarding the antioxidant activity assessed by FRAP assay, values were between 6.02-57.23 µmols TE/g d.w. and values for the RSA method between 18.44-83.81%. From the eight types of berries analyzed, bilberries and raspberries had the highest antioxidant activity considering both regions and both determination methods. Not only the type, but also the environmental and cultivation conditions in which the berries grow, can lead to variations in their chemical composition. The extracted polyphenolic compounds from the studied berries showed antibacterial properties on pathogens, such as Escherichia coli, Bacillus subtilis and Staphyloccocus aureus. The inhibitory action on Salmonella typhi and fungi Candida albicans and Aspegillus niger was absent to very low. The antimicrobial activity of the hydroalcoholic extracts was dependent on the provenance of the berries, too.

Solanaceae Family Phytochemicals as Inhibitors of 3C-Like Protease of SARS-CoV-2: An In Silico Analysis.

COVID-19, caused by the coronavirus SARS-CoV-2, emerged in late December 2019 in Wuhan, China. As of 8 April 2022, the virus has caused a global pandemic, resulting in 494,587,638 infections leading to 6,170,283 deaths around the world. Although several vaccines have received emergency authorization from USA and UK drug authorities and two more in Russia and China, it is too early to comment on the prolonged effectiveness of the vaccines, their availability, and affordability for the developing countries of the world, and the daunting task to vaccinate 7 billion people of the world with two doses of the vaccine with additional booster doses. As a result, it is still worthwhile to search for drugs and several promising leads have been found, mainly through in silico studies. In this study, we have examined the binding energies of several alkaloids and anthocyanin derivatives from the Solanaceae family, a family which contains common consumable vegetables and fruit items such as eggplant, pepper, and tomatoes. Our study demonstrates that Solanaceae family alkaloids such as incanumine and solaradixine, as well as anthocyanins and anthocyanidins, have very high predicted binding energies for the 3C-like protease of SARS-CoV-2 (also known as Mpro). Since Mpro is vital for SARS-CoV-2 replication, the compounds merit potential for further antiviral research towards the objective of obtaining affordable drugs.

Cyanidin-3-O-glucoside and Peonidin-3-O-glucoside-Rich Fraction of Black Rice Germ and Bran Suppresses Inflammatory Responses from SARS-CoV-2 Spike Glycoprotein S1-Induction In Vitro in A549 Lung Cells and THP-1 Macrophages via Inhibition of the NLRP3 Inflammasome Pathway.

Black rice is a functional food that is high in anthocyanin content, primarily C3G and P3G. It possesses nutraceutical properties that exhibit a range of beneficial effects on human health. Currently, the spike glycoprotein S1 subunit of SARS-CoV-2 (SP) has been reported for its contribution to pathological inflammatory responses in targeting lung tissue and innate immune cells during COVID-19 infection and in the long-COVID phenomenon. Our objectives focused on the health benefits of the C3G and P3G-rich fraction of black rice germ and bran (BR extract) on the inhibition of inflammatory responses induced by SP, as well as the inhibition of NF-kB activation and the NLRP3 inflammasome pathway in an in vitro model. In this study, BR extract was identified for its active anthocyanins, C3G and P3G, using the HPLC technique. A549-lung cells and differentiated THP-1 macrophages were treated with BR extract, C3G, or P3G prior to exposure to 100 ng/mL of SP. Their anti-inflammatory properties were then determined. BR extract at concentrations of 12.5-100 µg/mL exhibited anti-inflammation activity for both A549 and THP-1 cells through the significant suppression of NLRP3, IL-1ß, and IL-18 inflammatory gene expressions and IL-6, IL-1ß, and IL-18 cytokine secretions in a dose-dependent manner (p < 0.05). It was determined that both cell lines, C3G and P3G (at 1.25-10 µg/mL), were compatibly responsible for the significant inhibition of SP-induced inflammatory responses for both gene and protein levels (p < 0.05). With regard to the anti-inflammation mechanism, BR extract, C3G, and P3G could attenuate SP-induced inflammation via counteraction with NF-kB activation and downregulation of the inflammasome-dependent inflammatory pathway proteins (NLRP3, ASC, and capase-1). Overall, the protective effects of anthocyanins obtained from black rice germ and bran can be employed in potentially preventive strategies that use pigmented rice against the long-term sequelae of COVID-19 infection.

Nutraceutical potential of Amazonian oilseeds in modulating the immune system against COVID-19 - A narrative review.

Since the outbreak of COVID-19 disease, medical and scientific communities are facing a challenge to contain its spread, develop effective treatments, and reduce its sequelae. Together with the therapeutical treatments, the use of dietary bioactive compounds represents a promising and cost-effective strategy to modulate immunological responses. Amazonian oilseeds are great sources of bioactive compounds, thus representing not only a dietary source of nutrients but also of substances with great interest for human health. This narrative review compiled the available evidence regarding the biochemical properties of some Amazonian oilseeds, especially Brazil nut, Açaí berry, Bacaba, Peach palm, Sapucaya and Tucuma fruits, on human health and its immune system. These effects were discussed from an etiological and pathophysiological perspective, emphasizing their potential role as a co-adjuvant strategy against COVID-19. Besides this, the cost associated with these strategies hinders their applicability in many nations, especially low-income countries and communities living in social insecurity.

In-Silico Evaluation of 10 Structurally Different Glucosinolates on the Key Enzyme of SARS-CoV-2

The novel coronavirus (2019-nCoV) triggered a worldwide rise in the prevalence of the coronavirus outbreak (COVID-19) and surfaced as a universal wellbeing matter. Analogous with SARS-CoV and MERS-CoV, the main 3-chymotrypsin-alike cysteine protease (3CL(Pro)) virus enzyme that manages the replications of 2019-nCoV and regulates its existence span, possibly will be considered like a medication break through focus. In this study, the binding potential of 10 glucosinolates (Glu) having a variety of structures was studied with the catalytic dyad remains of 2019-nCoV-3CL(Pro ) by molecular cutting developing. The outcomes have shown that Glu containing sinigrin (SN) have been shown to be realistically bound to the 2019-nCoV-3CL(Pro) receptor and catalytic dyad binding sites (Cys145 and His41). Our simulation results have shown that sinigrin have a potential activity against 2019-nCoV and could be further used for drug production and optimization in the battle against COVID-19. In details, SN-SARS-CoV-2-3CL(Pro)-facilityacted without exhibit whichever observable variations, with reference to the constancy of Glu-enzyme complexes by means of average RMSD of 1.5 +/- 0.02 angstrom. Meanwhile, the ordinary behavior of a SN-SARS-CoV-2-3CL(Pro) complex continued as compact and steady during (50 ns) MD simulations. Current investigation has revealed that Glu with a specific structure could be successful against COVID-19 as natural components.

Molecular binding studies of anthocyanins with multiple antiviral activities against SARS-CoV-2.

Background: The search for ideal drugs with absolute antiviral activity against SARS-CoV-2 is still in place, and attention has been recently drawn to natural products. Several molecular targets have been identified as points of therapeutic intervention. The targets used in this study include SARS-CoV-2 helicase, spike protein, RNA-dependent RNA polymerase, main protease, and human ACE-2. An integrative computer-aided approach, which includes molecular docking, pharmacophore modeling, and pharmacokinetic profiling, was employed to identify anthocyanins with robust multiple antiviral activities against these SARS-CoV-2 targets. Result: Four anthocyanins (Delphinidin 3-O-glucosyl-glucoside, Cyanidin 3-O-glucosyl-rutinoside, Cyanidin 3-(p-coumaroyl)-diglucoside-5-glucoside), and Nasunin) with robust multiple inhibitory interactions were identified from a library of 118 anthocyanins using computer-aided techniques. These compounds exhibited very good binding affinity to the protein targets and moderate pharmacokinetic profiles. However, Cyanidin 3-O-glucosyl-rutinoside is reported to be the most suitable drug candidate with multiple antiviral effects against SARS-CoV-2 due to its good binding affinity to all five protein targets engaged in the study. Conclusions: The anthocyanins reported in this study exhibit robust binding affinities and strong inhibitory molecular interactions with the target proteins and could be well exploited as potential drug candidates with potent multiple antiviral effects against COVID-19.

Special Issue: Natural products for healthy living, Khulna 2020. (Special Issue: Natural products for healthy living, Khulna 2020.)

This special issue contains 8 papers presenting recent advances in research on the use of natural products to have a healthy life. Some of these papers investigate the efficacy of phytochemicals in improving endothelial function;molecular combination networks in medicinal plants;potential health benefits of anthocyanins in oxidative stress-related disorders;efficacy of natural products alternatives in the induction of male infertility and/or proceeding of spermicidal action;and promising flavonoids with anti-COVID-19 potential.

Pigmented Potatoes: A Potential Panacea for Food and Nutrition Security and Health?

Although there are over 4000 potato cultivars in the world, only a few have been commercialized due to their marketability and shelf-life. Most noncommercialized cultivars are pigmented and found in remote regions of the world. White-fleshed potatoes are well known for their energy-enhancing complex carbohydrates; however, pigmented cultivars are potentially high in health-promoting polyphenolic compounds. Therefore, we reveal the comprehensive compositions of pigmented cultivars and associated potential health benefits, including their potential role in ameliorating hunger, food, and nutrition insecurity, and their prospects. The underutilization of such resources is a direct threat to plant-biodiversity and local traditions and cultures.

Molecular docking of anthocyanins and ternatin in Clitoria ternatea as coronavirus disease oral manifestation therapy.

Herbal active compound with immunoregulator ability is considered a potential therapy for COVID-19 oral manifestation by downregulating pro-inflammatory cytokine storm. Meanwhile, anthocyanin and ternatin are the active compounds in Clitoria ternatea, which may act as a potential immunoregulator for COVID-19 therapy. The intention of this investigation was to investigate anthocyanin and ternatin as active compounds in C. ternatea that may be able to increase anti-inflammatory cytokine and inhibit pro-inflammatory cytokine and key proteins of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). This study implemented bioinformatic approach to analyze anthocyanin and ternatin as active compounds in C. ternatea with anti- and pro-inflammatory cytokines and antiviral examination history through blind molecular docking study (in silico). Moreover, anthocyanins and ternatin were obtained from PubChem database by minimizing ligand structure in PyRx software to increase the flexibility. RCSB database was employed for preparing the protein samples consisting of interleukin (IL)-6, SARS-CoV-2-ACE2 glycoprotein complex, tumor necrosis factor-α receptor (TNF-αR), matrix metalloproteinase-9 (MMP-9), IL-6, IL-10, and human beta defensin-2 (HBD-2). In addition, The PyMol sofware was used to sterilize the protein samples to obtain the molecular docking optimization. This investigation found that, in the molecular docking simulation, the anthocyanin and ternatin showed producing the negative binding affinity to the ACE2 domain which interacted with RBD glycoprotein SARS-CoV-2. Anthocyanin and ternatin were then predicted to be able to influence any inhibitory activity of TNF-αR, MMP-9, and IL-6; increase IL-10; and increase HBD2 binding affinity values negatively. It can be predicted through molecular docking that anthocyanin and ternatin as the active compounds in C. ternatea contribute as a potential agent for COVID-19 oral manifestation therapy.

Properties of Ethnomedicinal Plants and Their Bioactive Compounds: Possible Use for COVID-19 Prevention and Treatment.

BACKGROUND: The coronavirus disease 2019 (COVID-19) pandemic has changed the global scenario. To date, there are no treatment or preventive options. The discovery of a new drug will take time. In addition, the new drug will have side effects, and the virus will gradually become resistant to it. Therefore, it is important to search for a drug with a natural origin. OBJECTIVE: In this review, we analyzed and summarized various ethnomedicinal plants and their bioactive compounds as a source of antiviral agents for COVID-19 prevention and treatment. METHODS: From the literature, we selected different natural compounds that can act as potential targets at low cost with broad-spectrum antiviral activity. RESULTS: Of the 200 Chinese herbal extracts tested for their possible role against SARS-CoV, Lycoris radiata, Artemisia annua, Pyrrosia lingua, and Lindera aggregate showed anti-SARS-CoV effects with the median effective concentration = 2.4-88.2 µg/mL. CONCLUSION: Ethnomedicinal herbs can be used as an alternative source of novel, promising antiviral agents that might directly or indirectly inhibit the COVID-19 progression.

Polyacylated anthocyanins constructively network with catalytic dyad residues of 3CLpro of 2019-nCoV than monomeric anthocyanins: A structural-relationship activity study with 10 anthocyanins using in-silico approaches.

Coronavirus epidemic 2019 (COVID-19), caused by novel coronavirus (2019-nCoV), is newly increasing worldwide and elevating global health concerns. Similar to SARS-CoV and MERS-CoV, the viral key 3-chymotrypsin-like cysteine protease enzyme (3CLPro), which controls 2019-nCoV duplications and manages its life cycle, could be pointed as a drug discovery target. Herein, we theoretically studied the binding ability of 10 structurally different anthocyanins with the catalytic dyad residues of 3CLpro of 2019-nCoV using molecular docking modelling. The results revealed that the polyacylated anthocyanins, including phacelianin, gentiodelphin, cyanodelphin, and tecophilin, were found to authentically bind with the receptor binding site and catalytic dyad (Cys145 and His41) of 2019-nCoV-3CLpro. Our analyses revealed that the top four hits might serve as potential anti-2019-nCoV leading molecules for further optimization and drug development process to combat COVID-19. This study unleashed that anthocyanins with specific structure could be used as effective anti-COVID-19 natural components.