Brief survey on phytochemicals to prevent COVID-19

BackgroundThe recent pandemic by COVID-19 is a global threat to human health. The disease is caused by SARS-CoV-2 and the infection rate is increased more quickly than MERS and SARS as their rapid adaptation to varied climatic conditions through rapid mutations. It becomes more severe due to the lack of proper therapeutic drugs, insufficient diagnostic tool, scarcity of appropriate drug, life supporting medical facility and mostly lack of awareness. Therefore, preventive measure is one of the important strategies to control. In this context, herbal medicinal plants received a noticeable attention to treat COVID-19 in Indian subcontinent. Here, 44 Indian traditional plants have been discussed with their novel phytochemicals that prevent the novel corona virus. The basic of SARS-CoV-2, their common way of transmission including their effect on immune and nervous system have been discussed. We have analysed their mechanism of action against COVID-19 following in-silico analysis. Their probable mechanism and therapeutic approaches behind the activity of phytochemicals to stimulate immune response as well as inhibition of viral multiplication discussed rationally. Thus, mixtures of active secondary metabolites/phytochemicals are the only choice to prevent the disease in countries where vaccination will take long time due to overcrowded population density.     

Identification of phytobioconstituents present in Simmondsia chinensis L. seeds extract by GC-MS analysis

Simmondsia chinensis L. commonly called as Jojoba and belongs to family Simmondsiaceae. It has shown positive pharmacological activities of these compounds which include antidiabetic, antirheumatic, anthelminthic, antipsoriatic, antioxidant, antiepileptic, antigonorrheal, analgesic, anti-inflammatory, and pesticidal activity of jojoba. The multifaceted action of numerous bioactives existing in the seed extract with therapeutic activity have attracted great research interest by pharmaceutical industries. n-hexane extract of Simmondsia chinensis L. (SC) Seeds was analysed by gas chromatography-mass spectroscopy for identification and characterization of phytobioconstituents and its therapeutic claim by traditional system. The major compounds discovered in SC seeds extract are cis-9-octadecen-1-ol (24.85%), 9-octadecen-1-ol, (Z)- (18.24%), Stigmast-5-en-3-ol (14.10%), Ergost-5-en-3-ol, (3-β)-ol (5.26%), (Z)-14-tricosenyl formate (5.24%), Thiositosteroldisulfide (3.64%), Silane, Dimethyl (dimethylpentyloxysilyloxy) tetradecyloxy- (3.41%), Ergost-5-ene, 3-methoxy-, (3β,24R)- (2.55%), Ergosta-5,22-dien-3-ol (2.22%), 1,19-eicosadiene (2.17%), Pentacosane (2.02%), Stigmasta-5,22-dien-3-ol (1.64%), 1,19-eicosadiene (1.57%), 9-octadecen-1-ol, (Z)- (1.46%), 9,19-cyclo-9β-lanostan-3β-ol, 24-methylene- (1.14%), (9Z)-9-octadecenyl palmitate (1.50%), Hexadecanoic acid, 9-octadecenyl ester, (Z) (1.37%), 9Z)-9-octadecenyl (9Z)-9-hexadecenoate (1.01%). The hexane extract of Simmondsia chinensis seeds comprises various polar and nonpolar phytobioconstituents. These compounds were established qualitatively via GC-MS evaluation. GC-MS reports will be promising in pharmaceutical sector in identification of variety of Phytobioconstituents in distinct plant extracts, polyherbal extract and the standardization of particular plant materials.     

Approaches for Mitigating Microbial Biofilm-Related Drug Resistance: A Focus on Micro- and Nanotechnologies

Biofilms play an essential role in chronic and healthcare-associated infections and are more resistant to antimicrobials compared to their planktonic counterparts due to their (1) physiological state, (2) cell density, (3) quorum sensing abilities, (4) presence of extracellular matrix, (5) upregulation of drug efflux pumps, (6) point mutation and overexpression of resistance genes, and (7) presence of persister cells. The genes involved and their implications in antimicrobial resistance are well defined for bacterial biofilms but are understudied in fungal biofilms. Potential therapeutics for biofilm mitigation that have been reported include (1) antimicrobial photodynamic therapy, (2) antimicrobial lock therapy, (3) antimicrobial peptides, (4) electrical methods, and (5) antimicrobial coatings. These approaches exhibit promising characteristics for addressing the impending crisis of antimicrobial resistance (AMR). Recently, advances in the micro- and nanotechnology field have propelled the development of novel biomaterials and approaches to combat biofilms either independently, in combination or as antimicrobial delivery systems. In this review, we will summarize the general principles of clinically important microbial biofilm formation with a focus on fungal biofilms. We will delve into the details of some novel micro- and nanotechnology approaches that have been developed to combat biofilms and the possibility of utilizing them in a clinical setting.     

Novel Semi-Synthetic Cu (II)–Cardamonin Complex Exerts Potent Anticancer Activity against Triple-Negative Breast and Pancreatic Cancer Cells via Inhibition of the Akt Signaling Pathway

Cardamonin is a polyphenolic natural product that has been shown to possess cytotoxic activity against a variety of cancer cell lines. We previously reported the semi-synthesis of a novel Cu (II)–cardamonin complex (19) that demonstrated potent antitumour activity. In this study, we further investigated the bioactivity of 19 against MDA-MB-468 and PANC-1 cancer cells in an attempt to discover an effective treatment for triple-negative breast cancer (TNBC) and pancreatic cancer, respectively. Results revealed that 19 abolished the formation of MDA-MB-468 and PANC-1 colonies, exerted growth-inhibitory activity, and inhibited cancer cell migration. Further mechanistic studies showed that 19 induced DNA damage resulting in gap 2 (G2)/mitosis (M) phase arrest and microtubule network disruption. Moreover, 19 generated reactive oxygen species (ROS) that may contribute to induction of apoptosis, corroborated by activation of caspase-3/7, PARP cleavage, and downregulation of Mcl-1. Complex 19 also decreased the expression levels of p-Akt and p-4EBP1, which indicates that the compound exerts its activity, at least in part, via inhibition of Akt signalling. Furthermore, 19 decreased the expression of c-Myc in PANC-1 cells only, which suggests that it may exert its bioactivity via multiple mechanisms of action. These results demonstrate the potential of 19 as a therapeutic agent for TNBC and pancreatic cancer.     

Methoxy-Substituted Tyramine Derivatives Synthesis,Computational Studies and Tyrosinase Inhibitory Kinetics

Targeting tyrosinase for melanogenesis disorders is an established strategy. Hydroxyl-substituted benzoic and cinnamic acid scaffolds were incorporated into new chemotypes that displayed in vitro inhibitory effects against mushroom and human tyrosinase for the purpose of identifying anti-melanogenic ingredients. The most active compound 2-((4-methoxyphenethyl)amino)-2-oxoethyl (E)-3-(2,4-dihydroxyphenyl) acrylate (Ph9), inhibited mushroom tyrosinase with an IC₅₀ of 0.059 nM, while 2-((4-methoxyphenethyl)amino)-2-oxoethyl cinnamate (Ph6) had an IC₅₀ of 2.1 nM compared to the positive control, kojic acid IC₅₀ 16700 nM. Results of human tyrosinase inhibitory activity in A375 human melanoma cells showed that compound (Ph9) and Ph6 exhibited 94.6% and 92.2% inhibitory activity respectively while the positive control kojic acid showed 72.9% inhibition. Enzyme kinetics reflected a mixed type of inhibition for inhibitor Ph9 (K_i 0.093 nM) and non-competitive inhibition for Ph6 (K_i 2.3 nM) revealed from Lineweaver–Burk plots. In silico docking studies with mushroom tyrosinase (PDB ID:2Y9X) predicted possible binding modes in the catalytic site for these active compounds. Ph9 displayed no PAINS (pan-assay interference compounds) alerts. Our results showed that compound Ph9 is a potential candidate for further development of tyrosinase inhibitors.     

On model for Darcy–Forchheimer 3D nanofluid flow subject to heat flux boundary condition

Journal of Thermal Analysis and Calorimetry - This paper provides a theoretical study of 3D nanofluid flow with zero nanoparticles mass and constant heat fluxes conditions. An incompressible...     

Analysis of a “3-(Naphthalen-1-ylimino)indolin-2-one” Compound and Its Antimicrobial Assessment Using Lipid-Based Self-Nanoemulsifying Formulations

In recent years, indole derivatives have acquired conspicuous significance due to their wide spectrum of biological activities—antibacterial, antiviral, and anticonvulsant. This compound is derived from naturally grown plants. Therefore, synthesis of a novel “3-(Naphthalen-1-ylimino)indolin-2-one” compound (2) and its analysis using UPLC systems along with antimicrobial assessment was the aim of the current study. Isatin was used as a parent drug for synthesizing compound (2). Liquid Chromatographic analysis was performed using a C18 BEH column (1.7 μm 2.1 × 50 mm) by UPLC systems. Degradation studies were carried out to see whether acid, base, thermal, and oxidizing agents had any impact on the synthesized molecule in stress conditions (100 °C). A lipid-based self-nanoemulsifying formulation was developed and selectivity, specificity, recovery, accuracy, and precision were measured as part of the UPLC system’s validation process. Antimicrobial studies were conducted using gram-positive and gram-negative bacteria. The standard samples were run with a concentration range of 5.0–100.0 μg/mL using the isocratic mobile phase comprising of methanol/water (70/30 %v/v) at 234 nm; good linearity (R² = 0.9998) was found. The lower limits of detection (LOD) and quantitation (LOQ) of the method were found to be 0.81 μg/mL and 2.5 μg/mL, respectively. The coefficients of variation were found to be less than 2%. The antimicrobial study suggests that compound (2) has a substantial growth effect against gram-negative bacteria. It was successfully synthesized and applied to measure the concentrations in lipid-based dosage form, along with potent antimicrobial activities.     

Quinoline Functionalized Schiff Base Silver (I) Complexes: Interactions with Biomolecules and In Vitro Cytotoxicity,Antioxidant and Antimicrobial Activities

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO₃, AgClO₄ and AgCF₃SO₃. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)₂]NO₃ Q1, [Ag(L1)₂]ClO₄ Q6, [Ag(L2)₂]ClO₄ Q7, [Ag(L2)₂]CF₃SO₃ Q12 and [Ag(L4)₂]CF₃SO₃ Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC₅₀ between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)₂]ClO₄ Q7 with a benzothiazole moiety and [Ag(L4)₂]ClO₄ Q9 with a methyl substituent had excellent cytotoxicity against HELA cells.     

Robust projective lag synchronization in drive-response dynamical networks via adaptive control

This paper investigates the problem of projective lag synchronization behavior in drive-response dynamical networks (DRDNs) with identical and non-identical nodes. An adaptive control method is designed to achieve projective lag synchronization with fully unknown parameters and unknown bounded disturbances. These parameters were estimated by adaptive laws obtained by Lyapunov stability theory. Furthermore, sufficient conditions for synchronization are derived analytically using the Lyapunov stability theory and adaptive control. In addition, the unknown bounded disturbances are also overcome by the proposed control. Finally, analytical results show that the states of the dynamical network with non-delayed coupling can be asymptotically synchronized onto a desired scaling factor under the designed controller. Simulation results show the effectiveness of the proposed method.     

Production of textile filaments from carboxymethylated cellulosic pulps

Cellulose - Textile filaments were fabricated from a solution obtained from carboxymethylated cellulose dissolved in aqueous NaOH solution, by wet spinning in an acid coagulation bath. Spinning is...