Green Monkey Kidney Cell Line Research Articles

Janus Dendrimers as Nanocarriers of Ibuprofen, Chlorambucil and their Anticancer Activity.

Janus Dendrimer represents a novel class of synthetic nanocarriers. Since it is possible to introduce multiple drugs and target moieties, this helps the designing of new biocompatible forms with pharmacological activities comprised of different drugs with tailor-made functionalities, such as anticancer and nonsteroidal anti-inflammatory, which could improve the anticancer activity with less toxicity. This study aimed to determine the anticancer activity of the Janus dendrimers formed by two dendrons. One dendron conjugates with chlorambucil, and the other dendron conjugates with Ibuprofen. The cytotoxicity of the drug carriers was determined by the sulforhodamine B (SRB) assay for three cell lines. PC-3 (human prostatic adenocarcinoma), HCT-15 (human colorectal adenocarcinoma), MFC-7 (human breast cancer) and the COS-7 African green monkey kidney (used as a control) cell lines were seeded into 96-well plates at a density of 5x103 cells/well and cultured for 24 h before use. All the obtained compounds were characterized by 1H and 13C NMR one and two dimensions, UVvis, FTIR, MALDI-TOF, Electrospray mass, and FAB+. Microscopic images were taken in an Inverted microscope Nikon, Diaphot 300, 10x4 in culture medium. Janus dendrimers (G1 and G2) were synthesized via an azide-alkyne click-chemistry reaction attaching on one face dendrons with ibuprofen molecules and, on the other face, attached a chlorambucil- derivative. The IC50 behavior of the conjugates of the first and second generations showed anticancer activity against PC-3, HCT-15, and MFC-7 cell lines. The second generation was more active against PC-3, HCT-15 and MFC-7 with IC50 of 3.8±0.5, 3.0±0.2 and 3.7 ± 1.1 mM, respectively. The new Janus dendrimers with anticancer chlorambucil and nonsteroidal antiinflammatory Ibuprofen can improve the anticancer activity of chlorambucil with less toxicity. Now, we are working on the synthesis of new Janus dendrimers using the most effective and fine methods. Moreover, we hope that we shall be able to obtain different generations that are more selective against cancer cells.

New thiazol-pyridazine derivatives as antimicrobial and antiviral candidates: Synthesis, and application

In this manuscript, we are motivated to investigate the reaction site-selectivity for the hydrazo thiazole derivatives (6a–c) with different types of active methylene groups such as malononitrile, and ethyl cyanoacetate. Based on their structural investigations and spectrum data, the results of these reactions have been established to be iminopyridazines (7a–c) and 6-oxopyridazine derivatives (8a–c). We tested the ability of the newly synthesized pyridazine derivatives to inhibit the microbes and COVID-19 proteins. Human coronavirus 229E (HCoV-229E) was used to investigate the antiviral efficacy of prepared compounds. Green monkey kidney (Vero-E6) cell lines were used to investigate MTT and cytopathic effect (CPE). The new 6-oxopyridazine derivatives (8a–c) revealed significant inhibitory efficacy and were capable of inhibiting the human coronavirus 229E. Moreover, the antimicrobial result showed that compounds iminopyridazine (7c) followed by iminopyridazine (7a) followed by iminopyridazine (7b) exhibited excellent antimicrobial properties toward all utilized strains, usually greater than that of common reference drugs, with MIC values ranging from 13 to 21 ppm, from 9 to 14 ppm, and from 8 to 19 ppm whereas, the remaining substances appeared to be promising effective. Structure-activity relationship (SAR) revealed that pyridazine scaffolds containing NH group, as well as substituted electron withdrawal group (Cl) in para-position for benzene ring attributed to thiazole moiety have the best activity. The current study successfully illustrated the possible application of heterocyclic derivatives with pyridazie nucleus including thiazole ring as the main compound in the development of dual antiviral (COVID-19) and antibacterial pharmaceuticals in the future.

Drug repurposing platform for deciphering the druggable SARS-CoV-2 interactome

The coronavirus disease 2019 (COVID-19) pandemic has heavily challenged the global healthcare system. Despite the vaccination programs, the new virus variants are circulating. Further research is required for understanding of the biology of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection and for discovery of therapeutic agents against the virus. Here, we took advantage of drug repurposing to identify if existing drugs could inhibit SARS-CoV-2 infection. We established an open high throughput platform for in vitro screening of drugs against SARS-CoV-2 infection. We screened ∼1000 drugs for their ability to inhibit SARS-CoV-2–induced cell death in the African green monkey kidney cell line (Vero-E6), analyzed how the hit compounds affect the viral N (nucleocapsid) protein expression in human cell lines using high-content microscopic imaging and analysis, determined the hit drug targets in silico, and assessed their ability to cause phospholipidosis, which can interfere with the viral replication. Duvelisib was found by in silico interaction assay as a potential drug targeting virus–host protein interactions. The predicted interaction between PARP1 and S protein, affected by Duvelisib, was further validated by immunoprecipitation. Our results represent a rapidly applicable platform for drug repurposing and evaluation of the new emerging viruses’ responses to the drugs. Further in silico studies help us to discover the druggable host pathways involved in the infectious cycle of SARS-CoV-2.

Characterization and bioactivity of copaiba essential oil carried in a self-nanoemulsifying drug delivery system

Copaiba essential oil (CEO) is the volatile part of copaiba balsam, which has been topically used for various inflammatory conditions. However, there are some concerns about the CEO safety for oral use. The lipophilic character of CEO also limits its application in the pharmaceutical field. This study prepared a self-nanoemulsifying drug delivery system (SNEDDS) containing CEO and evaluated its toxic effects against a primary culture from pig liver (PLP2) and Green monkey kidney cell line (Vero). The inhibition of oxide nitric production was also evaluated on RAW 264.7 macrophage cell line to access the anti-inflammatory effect. The CEO was extracted by hydrodistillation and β-caryophyllene accounted for 51.8% of the oil. The formulation (FSNEDDS) consisting of CEO, Cremophor and ethyl linoleate was characterized in relation to morphology, stability, rheology, simulated digestion and bioaccessibility in vitro. FSNEDDS displayed Newtonian flow behavior with viscosity depending only on temperature and, in an aqueous medium, it formed small spherical particles (<100 nm size diameter). The FSNEDDS showed higher oxidative stability than the non-formulated CEO. In the simulated digestion, FSNEDDS formed nanoemulsifying droplets in gastric phase and tiny micelles in intestinal phase, and a bioaccessibility of 63%. The FSNEDDS showed a superior anti-inflammatory activity (+11%) than non-formulated CEO and this beneficial concentration was achieved with a non-toxic concentration for none of the cell lines tested. In conclusion, FSNEDDS improves the physicochemical stability, bioaccessibility and bioactivity of CEO, and it could be a phytotherapic option for per oral administration to treat inflammatory diseases.

Dual action of epigallocatechin-3-gallate in virus-induced cell Injury

BackgroundViral infections cause damage and long-term injury to infected human tissues, demanding therapy with antiviral and wound healing medications. Consequently, safe phytochemical molecules that may control viral infections with an ability to provide wound healing to viral-induced tissue injuries, either topically or systemically, are advantageous. Herein, we hypothesized that epigallocatechin-3-gallate (EGCG), the most abundant polyphenol in green tea, might be effective as a wound healing, antiviral, and antifibrotic therapy. ResultsThe antiviral activities of EGCG against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and Herpes simplex virus type 2 (HSV-2) as well as its wound healing activities against different monolayer tissue (continuous and primary) systems were investigated. Consider its possible wound-healing advantages as well. To determine the safe concentrations of EGCG in green monkey kidney (Vero) and Vero-E6 cell lines, MTT assay was performed and showed high CC50 values of 405.1 and 322.9 μM, respectively. The antiviral activities of EGCG against SARS-CoV-2 and HSV-2, measured as half-maximal concentration 50 (IC50) concentrations, were 36.28 and 59.88 μM, respectively. These results confirm that the EGCG has remarkable viral inhibitory activities and could successfully suppress the replication of SARS-CoV-2 and HSV-2 in vitro with acceptable selectivity indices (SI) of 11.16 and 5.39, respectively. In parallel, the EGCG exhibits significant and dose/time-dependent anti-migration effects in human breast cancer cells (MCF-7), its resistant variation (MCF-7adr), and human skin fibroblast (HSF) indicating their potential to heal injuries in different internal and topical mammalian systems. ConclusionsThe EGCG has proven to be an efficient antiviral against SARS-CoV-2 and HSV-2, as well as a wound-healing phytochemical. We assume that EGCG may be a promising option for slowing the course of acute cellular damage induced by systemic (Coronavirus Disease 2019 (COVID-19)) or topical (HSV-2) viral infections.

Toxicity assessment of bioplastics on brine shrimp (Artemia franciscana) and cell lines

Polylactic acid (PLA) and polybutylene succinate (PBS), are categorized as biodegradable bioplastics that have progressively being utilized as food packaging replacing the obtrusive petroleum plastic. This study aims to evaluate the toxicity of bioplastics and petroleum-based plastic polyethylene (PE) on Artemia franciscana and animal cell lines. Each plastic sample was assessed in its powdered form, and the size distribution of PE, PLA, and PBS microplastic particles was observed by optical microscopy. Additionally, the toxicity of hatching percentage and mortality rate was investigated. The results demonstrated that the percentage of hatching and the mortality rate post treatment with PLA and PBS particles for 24 and 48 h did not significantly alter in comparison to those treated with PE particles. However, the percentage of Artemia hatching reduced post treatment with plastic particles in comparison to the control, as well as the mortality rate increased with a high concentration of plastic particles. The morphology of Artemia after ingesting microplastic particles was obtained using phase contrast inverted microscopy. The accumulation of plastic in the Artemia gut was observed succeeding its exposure to PE, PLA, and PBS particles. In addition, the cytotoxicity of plastics on human keratinocyte (HaCaT), normal human dermal fibroblast (NHDF), and African green monkey kidney (Vero) cell lines were determined by MTT assay. The result exhibited that increasing concentrations of microplastic particles had substantially less toxic to practically nontoxic effect on the cells. The biomolecule profile by synchrotron-IR technique displayed that plastics potentially have more alteration effect in epithelial kidney cells (Vero) than fibroblasts (NHDF) and keratinocytes (HaCaT). Our results demonstrate that PE, PLA, and PBS had toxicity on Artemia following ingestion, in accordance with the concentration and duration tests. Moreover, microplastic particles were nontoxic or harmless to animal cell lines and altered some intracellular biomolecule profiles. These discoveries are essential not only for environmental health risk assessment but also in order to establish recommendations toward safer utilization of bioplastics-based materials for a robust lifestyle.

Design, synthesis and biological evaluation of novel 3-hydroxypyridin-4(1H)-ones based hybrids as Pseudomonas aeruginosa biofilm inhibitors

Pseudomonas aeruginosa (P. aeruginosa) is a gram-negative pathogenic bacterium, often causative drug-resistance related human infections, given its great capacity to form bioflm. It uses three major quorum sensing (QS) systems, las, rhl, and pqs, to regulate the expression of genes related to virulence and biofilm formation. Consequently, strategies for inhibiting QS have garnered considerable attention as antimicrobial therapies. In this study, we designed and synthesized several 3-hydroxypyridin-4(1H)-one hybrids and assessed their potential as the inhibitors of P. aeruginosa biofilm formation. The most active compound identified was 12h; it exhibited satisfactory biofilm inhibitory activity (IC50: 10.59 ± 1.17 μM). Mechanistic studies revealed that 12h significantly inhibited the fluorescence of the PAO1-lasB-gfp and PAO1-pqsA-gfp fluorescent reporter strains and the production of Las-regulated (elastase) and Pqs-regulated (pyocyanin) virulence factors. These findings indicate that 12h inhibited biofilm formation by suppressing the expression of lasB and pqsA, thereby inactivating the las and pqs pathways. Furthermore, 12h improved the antibiotic susceptibility of P. aeruginosa and reduced the acute virulence of this bacterium in the African green monkey kidney cell line Vero. In conclusion, 3-hydroxypyridin-4(1H)-one hybrids, such as 12h, represent a promising class of antibacterial agents against P. aeruginosa.

Design, synthesis of Janus dendrons conjugated with ketoprofen and prednisone for human chronic myelogenous therapy

Herein we present the synthesis of ketoprofen dendrons of first and second generation, with oxobutanoic acid chain lengths, a β-d-galactose derivative, an alkyne terminal group and the other dendrons with prednisone-triethylene glycol with an azide terminal group. Finally, the Janus dendrons were obtained by a coupling azide-alkyne “click” reaction. The cytotoxicity in vitro of the dendrons was evaluated against six different cancer cell lines and only showed activity against human chronic myelogenous leukemia (K-562) cells, the African green monkey kidney (COS-7) cell line was used as reference. The IC50 of the dendrons of first and second generation against K-562 was from 51.29 ± 0.1 μM, 47.17 ± 0.7 μM and 37.15 ± 0.6 μM respectively. However, the Janus dendron of first and second generation showed IC50 (13.43 ± 0.5 μM and 7.02 ± 0.2 μM) respectively. The most interesting result was obtained with the Janus dendrimer of second generation, which was found to be the best inhibitor of this series against the K-562 cell line.

Fabrication, Characterization, and Biocompatibility Study of Gelatin-Blended Fibroin Scaffold

This research investigates the biocompatibility of gelatin-blended fibroin scaffold fabricated by freeze-dry process. The morphology showed interconnected spongy spheres and polygons shapes with a pore size of 14.144 ± 11.31 and 19.4822 ± 18.71 micrometers, respectively. The formula ratio of fibroin: gelatin of 8:2 contained more random coil, while the formula ratio of fibroin: gelatin of 7:3 exhibited more β-sheet structure. The result revealed that gelatin influences fibroin conformational transition from random coil to beta, which might result from better hydrophobic characteristics. The surface of the formula ratio of fibroin: gelatin at 8:2 and 7:3 was 125.88 ± 9.85 and 130.07 ± 3.72 degrees, indicating the formula ratio of fibroin: gelatin at 7:3 had more hydrophobicity than the formula ratio of fibroin: gelatin at 8:2. The biocompatibility of scaffolds was determined for both formulas of human keratinocyte (HaCaT) and African green monkey kidney (Vero) cell lines by MTT assay. The formula ratio of fibroin: gelatin at 8:2 with various concentrations of 62.50, 125, 250, 500, and 1,000 µg/mL had cell viability percentages of 96.31, 101.74, 97.81, 104.15, and 103.22%, respectively. The formula ratio of fibroin: gelatin at 7:3 with various concentrations of 62.50, 125, 250, 500, and 1,000 µg/mL had cell viability percentages of 106.38, 104.28, 108.54, 97.42, and 97.65%, respectively. The growth of cell lines showed better performance with the hydrophilic characteristics of the scaffold, and it did not make it toxic to the HaCaT and Vero cell lines. These results demonstrated the possibility of gelatin-blended scaffold as a supporting material for skin tissue engineering, especially for wound healing.

Antiviral effects and tissue exposure of tetrandrine against SARS-CoV-2 infection and COVID-19.

Tetrandrine (TET) has been used to treat silicosis in China for decades. The aim of this study was to facilitate rational repurposing of TET against SARS-CoV-2 infection. In this study, we confirmed that TET exhibited antiviral potency against SARS-CoV-2 in the African green monkey kidney (Vero E6), human hepatocarcinoma (Huh7), and human lung adenocarcinoma epithelial (Calu-3) cell lines. TET functioned during the early-entry stage of SARS-CoV-2 and impeded intracellular trafficking of the virus from early endosomes to endolysosomes. An in vivo study that used adenovirus (AdV) 5-human angiotensin-converting enzyme 2 (hACE2)-transduced mice showed that although TET did not reduce pulmonary viral load, it significantly alleviated pathological damage in SARS-CoV-2-infected murine lungs. The systemic preclinical pharmacokinetics were investigated based on in vivo and in vitro models, and the route-dependent biodistribution of TET was explored. TET had a large volume of distribution, which contributed to its high tissue accumulation. Inhaled administration helped TET target the lung and reduced its exposure to other tissues, which mitigated its off-target toxicity. Based on the available human pharmacokinetic data, it appeared feasible to achieve an unbound TET 90% maximal effective concentration (EC90) in human lungs. This study provides insights into the route-dependent pulmonary biodistribution of TET associated with its efficacy.

Structural diversity-guided optimization of carbazole derivatives as potential cytotoxic agents.

Carbazole alkaloids, as an important class of natural products, have been widely reported to have extensive biological activities. Based on our previous three-component reaction to construct carbazole scaffolds, we introduced a methylene group to provide a rotatable bond, and designed series of carbazole derivatives with structural diversity including carbazole amide, carbazole hydrazide and carbazole hydrazone. All synthesized carbazole derivatives were evaluated for their in vitro cytotoxic activity against 7901 (gastric adenocarcinoma), A875 (human melanoma) and MARC145 (African green monkey kidney) cell lines. The preliminary results indicated that compound 14a exhibited high inhibitory activities on 7901 and A875 cancer cells with the lowest IC50 of 11.8 ± 1.26 and 9.77 ± 8.32μM, respectively, which might be the new lead compound for discovery of novel carbazole-type anticancer agents.

Characterization of the camel pox virus strain used in producing camel pox virus vaccine

Background: The camel pox virus is a widespread infectious viral disease of camels. It is necessary to conduct research on new strains for the development of vaccines. Aim: The research aims to characterize a novel strain isolated from the camel pox virus used to produce a camel pox virus vaccine. Methods: The objects of the study were the “M-0001” strain isolated from a sample of animals infected with the camel pox virus during the epidemic. The cultural and reproductive properties of the virus isolate were studied using primary cell lines from primary trypsinized lamb kidney and testicular cell cultures (LK and LT). Other samples included kidney cell lines from transplanted sheep) as well as a kidney cell line from transplanted cattle, Vero (transplanted green monkey kidney cell line), and calf trachea. The strain was PCR-tested and sequenced for characterization purposes. Results: The PCR results show that the study sample is species specific and corresponds to the camel pox virus by the size of the cumulative amplifications, which is 241 bp. Given the maximum percentage of a sequence match analyzed by the BLAST algorithm based on the international database and the results of phylogenetic analysis, the M0001 sample was determined to belong to the Camel pox virus (gene bank inventory number KP768318.1). Conclusion: The sample “M0001” is located on the same branch with a representative from CMLV (Camel pox virus). Among the cell cultures tested, the LK and LT cell lines were the most sensitive to the isolated CMLV isolate. Reproducing the virus in these cell cultures remains stable even after 15 consecutive passes. The cytopathic effect of the virus was less pronounced and low in transplanted cell lines, and the cytopathic effect was no longer apparent in the third passage. A genome alignment of the virus has identified potentially conserved sites, and analysis of loci in different virus types revealed one maximally conserved locus. An epizootic strain of the camelina virus “M-0001” candidate to produce vaccines for the camels was obtained. An experimental vaccine sample based on an isolated and charred camellia virus will be created in the future.

One-pot two-component synthesis of halogenated xanthone, 3-o substituted xanthone, and prenylated xanthone derivatives as aromatase inhibitors

This study describes the synthesis, characterization, and biological activities of halogenated xanthone, 3-O substituted xanthone, and prenylated xanthone derivatives. The molecular structures of these compounds were identified using 1H NMR, 13C NMR, 2D NMR, FTIR and DIMS. All synthesized compounds were evaluated against two cancer cell lines: breast adenocarcinoma MCF-7 and MDA-MB-231 by application of the MTT assay. With this approach, xanthones 9 and 13 were identified as putative aromatase activating agents through the inhibition of interactions with MCF-7 and MDA-MB-231. The selected compounds, 9 and 13, were further examined for toxicity against the African Green Monkey Kidney cell (VERO) and Non-tumorigenic Lung Epithelial cell lines (BEAS-2B). In addition, in-silico docking studies were conducted to estimate the binding poses and residues implicated in probable MCF-7 and MDA-MB-231 interactions.

A potential role for SARS-CoV-2 small viral RNAs in targeting host microRNAs and modulating gene expression

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes coronavirus disease (COVID-19) in humans, with symptoms ranging from mild to severe, including fatality. The molecular mechanisms surrounding the effects of viral infection on the host RNA machinery remain poorly characterized. We used a comparative transcriptomics approach to investigate the effects of SARS-CoV-2 infection on the host mRNA and sRNA expression machinery in a human lung epithelial cell line (Calu-3) and an African green monkey kidney cell line (Vero-E6). Upon infection, we observed global changes in host gene expression and differential expression of dozens of host miRNAs, many with known links to viral infection and immune response. Additionally, we discovered an expanded landscape of more than a hundred SARS-CoV-2-derived small viral RNAs (svRNAs) predicted to interact with differentially expressed host mRNAs and miRNAs. svRNAs are derived from distinct regions of the viral genome and sequence signatures suggest they are produced by a non-canonical biogenesis pathway. 52 of the 67 svRNAs identified in Calu-3 cells are predicted to interact with differentially expressed miRNAs, with many svRNAs having multiple targets. Accordingly, we speculate that these svRNAs may play a role in SARS-CoV-2 propagation by modulating post-transcriptional gene regulation, and that methods for antagonizing them may have therapeutic value.

Characterisation, structural investigations and biological activity of substituted salicylidene-based compounds

Seven salicylidene base compounds (1 – 7), p-NO2-SalH-R, (R = halogen, hydroxyl, or nitro group on either the para (p-) or ortho (o-) position); were prepared by condensing 2-hydroxy-5-nitrobenzaldehyde with p-hydroxyaniline (1), p-nitroaniline (2), p-fluoroaniline (3), p-chloroaniline (4), p-bromoaniline (5) o-fluoroaniline (6) and o-hydroxyaniline (7), to form the respective ligands (1 – 7). The compounds were fully characterised via 1H and 13C NMR, IR, UV/Vis, and elemental analysis. Luminescence studies were performed and single crystals, suitable for X-ray diffraction, were obtained for four of the compounds. The compounds were assayed for cytotoxicity against human breast adenocarcinoma (MCF-7), human cervical cancer (HeLa), human lung adenocarcinoma (A549), liver hepatocellular carcinoma (HepG2), human colorectal adenocarcinoma (Caco-2) and African green monkey kidney (Vero) cell lines and for antibacterial activity against 3 nosocomial pathogenic bacteria (E. coli, E. faecalis, and S. aureus) to correlate between structural variations and bioactivity. Compound 2 showed anticancer activity against MCF-7 and HepG2 cell lines with LC50 values of 48.78 µM and 59.26 µM, respectively. Compound 7 exhibited anticancer activity against HeLa and A549 cell lines with LC50 values of 50.27 µM and 37.88 µM, respectively. Compounds 4 and 5 demonstrated anticancer activity against the MCF-7 cell line with LC50 values of 48.04 µM and 56.58 µM, respectively. The compounds showed no antibacterial activity against the three tested nosocomial pathogenic bacterial strains.

Adaptation of the sheep pox virus (Poxviridae: &lt;i&gt;Capripoxvirus: Sheeppox virus&lt;/i&gt;) to African green monkey kidney cell line and evaluation of its immunobiological properties

Outbreaks of infectious diseases seriously hinder the preservation and increase of the number of small ruminants. Such infections include sheep pox virus (SPPV). According to the OIE data of 2021, SPP outbreaks were registered in countries such as Turkey, Israel, China, Maldives, Mongolia, Thailand, Russia, Algeria, Kenya, and in 2019 in Mangistau and Atyrau regions. In Kazakhstan annually conducts routine immunization of sheep at risk with a live attenuated vaccine produced by RIBSP. The object of the study was the vaccine strain of NISHI and the virulent strain A of the sheep pox virus. The virus was propagated in Vero cells. To determine the harmlessness and immunogenicity, sheep of the Kazakh fine-wool breed aged from 6 to 12 months were used. Virological, serological and immunobiological methods were used in the study. The results of the adaptation of the NISHI strain of SPPV to the Vero cell line are presented. Five passages in Vero cells resulted to the adaptation of the NISHI strain with the manifestation of a cytopathogenic effect specific to SPPV with a titer of 6.50 lg TCD50/ml. Following immunization, the formation of immunity was observed in animals on day 7 with an average protective titer 1.8 log2, which increased by day 21 to 4.33 log2. It has been established that the NISHI strain of SPPV retains its virological and immunobiological properties during reproduction in a Vero cell line.

In Vitro Assessment of Anti-inflammatory Effect of Apigenin on Renal Cell Inflammation

Objective: This study aimed to evaluate in vitro effect of apigenin on anti – and pro-inflammatory cytokines including interleukin-6 (IL-6), IL-10, tumor necrosis factor-alpha (TNF-α), and transforming growth factor-beta (TGF-β) levels in an in vitro model of renal cell inflammation induced with lipopolysaccharide (LPS).&#x0D; &#x0D; Methods: For the in vitro renal cell inflammation model, the African green monkey kidney cell line (Vero) was used. Four groups as NC (without any treatment), LPS (Vero cells treated with 10 μg/mL of LPS for 4 hours), API (Vero cells treated with 5 μg/mL of apigenin for 12 hours), and LPS+API (Vero cells treated with 5 μg/mL of apigenin for 12 hours + 10 μg/mL of LPS for 4 hours) was formed. The non-cytotoxic dose of apigenin in Vero cells was evaluated by a cell count test. IL-6, IL-10, TNF-α, and TGF-β concentrations in the cell culture medium were measured by enzyme-linked immunosorbent assay kits. All analyses were performed in four repetitions.&#x0D; &#x0D; Results: IL-6, IL-10, TNF-α, and TGF-β concentrations of the LPS group increased compared to NC, API, and LPS+API groups (p

Design, Synthesis, Antiviral Evaluation, and Molecular Dynamics Simulation Studies of New Spirocyclic Thiopyrimidinones as Anti HCoV-229E.

The current pandemic threat presented by viral pathogens like SARS-CoV-2 (COVID-19) suggests that virus emergence and dissemination are not geographically confined. As a result, the quest for antiviral agents has become critical to control this pandemic. In the current study, we provide a novel family of spirocyclic thiopyrimidinone derivatives whose cytotoxicity and antiviral efficacy were investigated against human coronavirus 229E (HCoV-229E) as a model for the Coronaviridae family. We utilized MTT and cytopathic effect (CPE) inhibitory tests on green monkey kidney (vero-E6) cell lines. The new molecules showed varied degrees of antiviral activity against the vero-E6 cell lines with minimal cytotoxicity. With a high level of a selective index (SI=14.8), compound 9 showed outstanding inhibitory ability and could effectively suppress the human coronavirus 229E. Molecular dynamics simulation (MD) studies were performed to measure the interaction and stability of the protein-ligand complex in motion. The MD results for the most active compound 9 explored remarkable interactions with the binding pockets of the main protease (Mpro) of SARS-CoV-2 enzyme confirming the results gained from in vitro experiments. ADMET properties were also predicted for all the tested compounds. All these results demonstrated that the novel spirocyclic thiopyrimidinone derivatives would have the potential to be safe, low-cost chemical compounds that might be used as a novel therapeutic option for Coronaviridae viruses like COVID-19.

Anti-Inflammatory, Anti-Diabetic, Anti-Oxidant and Cytotoxicity Assays of South African Herbal Teas and Bush Tea Blends.

South Africa is home to a variety of herbal teas, such as bush tea (Athrixia phylicoides DC.), honeybush tea (Cyclopia intermedia E. Mey and C. subternata Vogel), special tea (Monsonia burkeana Planch. ex Harv.), and rooibos tea (Aspalathus linearis (Burm.f.) R. Dahlgren) that are known to possess anti-oxidant, anti-inflammatory and anti-diabetic properties. The objective of this study was to determine the in vitro anti-oxidant activity of selected tea blends using 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays, as well as to assess their anti-inflammatory properties using the 15-lipoxygenase inhibitory assay. Furthermore, the study measured glucose utilisation in C2C12 myotubes. Lastly, 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay was used to test the safety of the tea extracts on Vero cells (African green monkey kidney cell line). Special tea and its blend with bush tea exhibited potent anti-oxidant and anti-inflammatory activity. The blending of bush tea with special tea at different ratios resulted in increased anti-oxidant activity. Although special tea had a level of cell toxicity, its toxicity was lowered during blending. All of the tea samples showed anti-diabetic effects, although with less potency as compared to insulin. The current investigation supports the use of blended herbal teas, and the positive anti-inflammatory effect of special tea warrants further research.

Eco-Friendly Green Biosynthesis of Silver Nanoparticles (Or-AgNPs) Using Orange Peel (&lt;i&gt;Citrus sinensis&lt;/i&gt;) Waste and Evaluation of their Antibacterial and Cytotoxic Activities

Greener Nanotechnology research depends on the utilization of the reductive potency of a common byproduct of food and fruit processing industry which represent a cheap and reliable source of green reducing agents to be used in bio-nanosynthesis. One potential approach is based on silver bio-synthesis (AgNPs) using biological waste products. Recently, the production of bio-nanoparticles especially AgNPs has received enormous importance due to its good and potential physicochemical characteristics and the possibility of applications .The present work aimed to synthesis silver nanoparticles (AgNPs) using biological orange waste peels products (Citrus Sinensis) to evaluate its characterization, antimicrobial activity and cytotoxicity. The green synthesized silver nanoparticles were characterized by UV-visible spectroscopy and Scanning electron microscopy (SEM). Disk diffusion method was used for the study of antimicrobial activity of the bio-synthesized silver nanoparticles against the different bacterial and fungal strains. Characterization performed by Scanning Electron Microscope and UV visible spectrophotometer where showed the formation of spherical, and few agglomerated AgNPs forms as measured by UV–visible spectrophotometer in the range of 350-550 nm. Antimicrobial activities where showed positive activity against most of the tested human pathogenic bacteria and fungi with varying degrees and the cytotoxicity which performed against African Green Monkey Kidney cell lines (Vero) where CC50 for AgNO3 and AgNPs were ( 76.5±6.27 μl/100μl ) and (9.87±0.90μl/100μl) respectively.