Search Results (41)

Metallic nanoparticles have found wide applications due to their unique physical and chemical properties. Green biosynthesis using plants, microbes, and plant/microbial extracts provides an environmentally friendly approach for nanoparticle synthesis. This review discusses the mechanisms and factors governing the biosynthesis of metallic nanoparticles such as silver, gold, and zinc using various plant extracts and microorganisms, including bacteria, fungi, and algae. The phytochemicals and biomolecules responsible for reducing metal ions and stabilizing nanoparticles are discussed. Key process parameters like pH, temperature, and precursor concentration affecting particle size are highlighted. Characterization techniques for confirming the formation and properties of nanoparticles are also mentioned. Applications of biosynthesized nanoparticles in areas such as antibacterial delivery, cancer therapy, biosensors, and environmental remediation are reviewed. Challenges in scaling up production and regulating nanoparticle properties are addressed. Power Point 365 was used for creating graphics. Overall, green biosynthesis is an emerging field with opportunities for developing eco-friendly nanomanufacturing platforms using abundant natural resources. Further work on optimizing conditions, standardizing protocols, and exploring new biosources is needed to realize the full potential of this approach. Full article

Tinospora bakis (A.Rich.) Miers (Menispermaceae) has traditionally been used to alleviate headaches, rheumatism, mycetoma, and diabetes, among others. Despite its extensive use, the active components of the plant have never been investigated. In this work, a series of furanoditerpenoids (1–18) and five compounds from other classes (19–23) were isolated from T. bakis. Notably, two new compounds were discovered and named: tinobakisin (1) and tinobakiside (10). Their molecular structures were elucidated with NMR, MS, UV, IR, and ECD spectra. Additionally, known compounds (2–9 and 11–23) were corroboratively identified through spectral comparisons with previously reported data, while highlighting and addressing some inaccuracies in the prior literature. Remarkably, compounds 6, 7, 13, and 17 exhibited a superior anti-glycation effect, outperforming established agents like rutin and quercetin in a lab model of protein glycation with glucose. The overall findings suggest that furanoditerpenoids play a crucial role in the antidiabetic properties of T. bakis. This research marks the first comprehensive phytochemical investigation of T. bakis, opening the door for further investigation into furanoditerpenoids and their biological mechanisms. Full article

Background: Dermatitis is skin disorder that is complicated by recurrent infections of skin by bacteria, viruses, and fungi. Spilanthol is an active constituent of Spilanthes acmella, which possess strong anti-bacterial properties. The purpose of this study was to develop a herbal emulgel for the treatment of dermal bacterial infections, as microscopic organisms have created solid resistance against anti-microbials. Methods: Emulgels were prepared and characterized for parameters such as physical examination, rheological studies, spreading coefficient, bio-adhesive strength measurement, extrudability study, antibacterial activity, FTIR analysis, in vitro drug dissolution, and ex vivo permeation studies. Result: With a statistically significant p-value = 0.024, 100% antibacterial activity was observed by F4 against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli (mean ± S.D) (25.33 ± 0.28, 27.33 ± 0.5, and 27 ± 0.5). However, maximum antibacterial effect 100% formulations produced zones of inhibitions against E. colip-value = 0.001. The mean zone of inhibition produced by F4 was greatest among all at 26.44 ± 0.37 mm (mean ± S.D). The F4 formulation produced a maximum percentage dissolution, permeation, and flux of 86.35 ± 0.576, 55.29 ± 0.127%, and 0.5532 ug/cm²/min, respectively. Conclusions: The present study therefore, suggests the use of S. acmella extract and olive oil containing emulgel for treating bacterial skin infections. Full article

There exists a considerable amount of evidence regarding short-term outcomes of shoulder arthroscopy in athletes; however, mid- to long-term data are limited. Therefore, the purpose of this review is to evaluate studies assessing mid- to long-term outcomes and rates of return to sport in athletes undergoing primary shoulder arthroscopy. A search for the systematic review was performed in PubMed, Scopus, and Embase on 14 March 2023. Study parameters, as well as their respective outcomes, were described in detail and compiled into diagrams. Five studies were included, which contained data on a total of 307 shoulders in patients with mean ages ranging from 20.3 to 26.9 years and mean follow-up times ranging from 6.3 to 14 years. The arthroscopic Bankart repair was the primary surgical intervention performed in all five studies. The overall rate of return to sport was 84% (range, 70–100%) across the studies. The rate of return to sport at pre-injury level was 65.2% (range, 40–82.6%) across four studies. The overall rate of recurrent instability was 17.3%, with redislocation specifically occurring in 13.7% of patients across all studies. The overall rate of revision surgery was 11.1%. Athletes who underwent primary shoulder arthroscopy demonstrated favorable outcomes and a high rate of RTS at a minimum follow-up of 5 years. However, rates of recurrent instability, redislocation, and revision surgery occurred at less than favorable numbers, which emphasizes the importance of proper patient selection when considering candidates for arthroscopic versus open repairs. Full article

Fluorine is characterized by high electronegativity and small atomic size, which provide this molecule with the unique property of augmenting the potency, selectivity, metabolic stability, and pharmacokinetics of drugs. Fluorine (F) substitution has been extensively explored in drug research as a means of improving biological activity and enhancing chemical or metabolic stability. Selective F substitution onto a therapeutic or diagnostic drug candidate can enhance several pharmacokinetic and physicochemical properties such as metabolic stability and membrane permeation. The increased binding ability of fluorinated drug target proteins has also been reported in some cases. An emerging line of research on F substitution has been addressed by using ¹⁸F as a radiolabel tracer atom in the extremely sensitive methodology of positron emission tomography (PET) imaging. This review aims to report on the fluorinated drugs approved by the US Food and Drug Administration (FDA) from 2016 to 2022. It cites selected examples from a variety of therapeutic and diagnostic drugs. FDA-approved drugs in this period have a variety of heterocyclic cores, including pyrrole, pyrazole, imidazole, triazole, pyridine, pyridone, pyridazine, pyrazine, pyrimidine, triazine, purine, indole, benzimidazole, isoquinoline, and quinoline appended with either F-18 or F-19. Some fluorinated oligonucleotides were also authorized by the FDA between 2019 and 2022. Full article

Ferrocenyl-based compounds have many applications in diverse scientific disciplines, including in polymer chemistry as redox dynamic polymers and dendrimers, in materials science as bioreceptors, and in pharmacology, biochemistry, electrochemistry, and nonlinear optics. Considering the horizon of ferrocene chemistry, we attempted to condense the neoteric advancements in the synthesis and applications of ferrocene derivatives reported in the literature from 2016 to date. This paper presents data on the progression of the synthesis of diverse classes of organic compounds having ferrocene scaffolds and recent developments in applications of ferrocene-based organometallic compounds, with a special focus on their biological, medicinal, bio-sensing, chemosensing, asymmetric catalysis, material, and industrial applications. Full article

Honey intake is advantageous to human health due to its antioxidant, anticancer, anti-inflammatory, and antimicrobial properties, all of which are attributed to the rich bioactive compound contents. Moreover, hepatoprotective, wound healing, and gastrointestinal protective properties have been documented. Honey’s nutritional value is significantly affected by its chemical composition, which varies depending on botanical and geographical origin. In particular, after Manuka honey, Sidr honey from the Ziziphus species is the most popular. The chemical compositions, physicochemical properties, bioactive compounds, and sensory characteristics of two Sidr honey samples from Egypt and Saudi Arabia were investigated in the current study. Moisture content, electrical conductivity (EC), pH, free acidity (FA), total acidity, lactone hydroxymethylfurfural (HMF) content, and diastase (α-amylase) activity were measured. By using high-performance liquid chromatography (HPLC), mass spectrometry (LC-MS/MS), nuclear magnetic resonance (¹HNMR), and solid-phase micro-extraction (SPME) coupled with gas chromatography (GC-MS) analyses, the sugar profile, non-volatile, and volatile compounds were also identified. The physicochemical analysis revealed the following results for Sidr honey from Saudi Arabia and Egypt, respectively: a moisture content of 18.03 ± 0.05% and 19.03 ± 0.06%, EC values of 1.18 ± 0.05 and 1.16 ± 0.01 mS/cm, pH values of 4.87 ± 0.08 and 5.10 ± 0.01, FA of 37.50 ± 0.05 and 36.50 ± 0.05 meq/kg, total acidity of 41.06 ± 0.05 and 37.50 ± 0.05 meq/kg, lactone of 3.49 ± 0.005 and 1 ± 0.0 meq/kg, HMF of 20.92 ± 0.02 and 11.33 ± 0.01 mg/kg, and diastase of 59.97 ± 0.05 and 8.64 ± 0.06g/100 g. Honey from Saudi Arabia and Egypt displayed 22.51 ± 0.05 and 26.62 ± 0.16 % glucose, 40.33 ± 0.06 and 35.28 ± 0.01% fructose, 8.94 ± 0.17, and 8.87 ± 0.01% sucrose, and 8.22 ± 0.006 and 8.13 ± 0.01% maltose, respectively. According to the International Honey Commission (IHC) and GCC Standardization Organization (GSO) regulations, the levels of glucose, fructose, sucrose, and maltose were near the standard levels. Flavonoids, sugars, vitamins, and nitrogen contents were additionally measured using LC-MS/MS, whereas GC-MS was employed to identify aldehydes, ketones, phenols, acids, esters, anthraquinone, hydrocarbons, and nitrogenous compounds. The results of a study on the effect of honey’s geographic origin on its broad quality are summarized. As a result, knowing its optimal chemical and physical characteristics served as the criterion and indicator of the honey’s quality. Full article

Background and objectives: The inappropriate use of antibiotics in hospitals can potentially lead to the development and spread of antibiotic resistance, increased mortality, and high economic burden. The objective of the study was to assess current patterns of antibiotic use in leading hospitals of Pakistan. Moreover, the information collected can support in policy-making and hospital interventions aiming to improve antibiotic prescription and use. Methodology and materials: A point prevalence survey was carried out with data abstracted principally from patient medical records from 14 tertiary care hospitals. Data were collected through the standardized online tool KOBO application for smart phones and laptops. For data analysis, SPSS Software was used. The association of risk factors with antimicrobial use was calculated using inferential statistics. Results: Among the surveyed patients, the prevalence of antibiotic use was 75% on average in the selected hospitals. The most common classes of antibiotics prescribed were third-generation cephalosporin (38.5%). Furthermore, 59% of the patients were prescribed one while 32% of the patients were prescribed two antibiotics. Whereas the most common indication for antibiotic use was surgical prophylaxis (33%). There is no antimicrobial guideline or policy for 61.9% of antimicrobials in the respected hospitals. Conclusions: It was observed in the survey that there is an urgent need to review the excessive use of empiric antimicrobials and surgical prophylaxis. Programs should be initiated to address this issue, which includes developing antibiotic guidelines and formularies especially for empiric use as well as implementing antimicrobial stewardship activities. Full article

Applications of a quadrotor with payload, particularly for chemical spraying, have increased in recent times. The variation in payload mass over time causes a change in the moments of inertia (MOI). Moreover, large tilt angles are required for fast reference tracking and external disturbance rejection. These variations in plant parameters (i.e., mass and inertia) and large tilt angles can degrade the control scheme’s performance and stability. This article proposes a linear matrix inequalities (LMIs)-based linear parameter varying (LPV) control scheme for a quadrotor subject to time-varying mass, time-varying inertia, mass flow rate, and large tilt angles. The control strategy is designed by solving LMIs derived from quadratic ${\mathcal{H}}_{\infty }$ performance and D-stability. The robust stability and quadratic ${\mathcal{H}}_{\infty }$ performance are assessed by LMIs. The efficacy of the proposed methodology is established using numerical simulations, and its performance is compared to the linear time-invariant (LTI) ${\mathcal{H}}_{\infty }$ design with pole placement constraints. The results obtained show that the LPV control scheme gives better tracking performance in the presence of time-varying parameters, noise, and external disturbances without actuator saturation. In comparison to the LTI design technique, the proposed LPV scheme improves the rise time ($t_r$), settling time ($t_s$), and mean squared error (MSE) by up to $14\%$, $15\%$, and $30\%$, respectively. Moreover, smooth transitions are observed in the tilt angles and control signals with the LPV scheme, contrary to the LTI controller, which exhibits significant oscillations. Full article

The tropylium ion is a non-benzenoid aromatic species that works as a catalyst. This chemical entity brings about a large number of organic transformations, such as hydroboration reactions, ring contraction, the trapping of enolates, oxidative functionalization, metathesis, insertion, acetalization, and trans-acetalization reactions. The tropylium ion also functions as a coupling reagent in synthetic reactions. This cation’s versatility can be seen in its role in the synthesis of macrocyclic compounds and cage structures. Bearing a charge, the tropylium ion is more prone to nucleophilic/electrophilic reactions than neutral benzenoid equivalents. This ability enables it to assist in a variety of chemical reactions. The primary purpose of using tropylium ions in organic reactions is to replace transition metals in catalysis chemistry. It outperforms transition-metal catalysts in terms of its yield, moderate conditions, non-toxic byproducts, functional group tolerance, selectivity, and ease of handling. Furthermore, the tropylium ion is simple to synthesize in the laboratory. The current review incorporates the literature reported from 1950 to 2021; however, the last two decades have witnessed a phenomenal upsurge in the utilization of the tropylium ion in the facilitation of organic conversions. The importance of the tropylium ion as an environmentally safe catalyst in synthesis and a comprehensive summary of some important reactions catalyzed via tropylium cations are described. Full article

Bis-acyl-thiourea derivatives, namely N,N’-(((4-nitro-1,2-phenylene)bis(azanediyl)) bis(carbonothioyl))bis(2,4-dichlorobenzamide) (UP-1), N,N’-(((4-nitro-1,2-phenylene) bis(azanediyl))bis(carbonothioyl))diheptanamide (UP-2), and N,N’-(((4-nitro-1,2-phenylene)bis(azanediyl))bis(carbonothioyl))dibutannamide (UP-3), were synthesized in two steps. The structural characterization of the derivatives was carried out by FTIR, ¹H-NMR, and ¹³C-NMR, and then their DNA binding, anti-urease, and anticancer activities were explored. Both theoretical and experimental results, as obtained by density functional theory, molecular docking, UV-visible spectroscopy, fluorescence (Flu-)spectroscopy, cyclic voltammetry (CV), and viscometry, pointed towards compounds’ interactions with DNA. However, the values of binding constant (K_b), binding site size (n), and negative Gibbs free energy change (ΔG) (as evaluated by docking, UV-vis, Flu-, and CV) indicated that all the derivatives exhibited binding interactions with the DNA in the order UP-3 > UP-2 > UP-1. The experimental findings from spectral and electrochemical analysis complemented each other and supported the theoretical analysis. The lower diffusion coefficient (D_o) values, as obtained from CV responses of each compound after DNA addition at various scan rates, further confirmed the formation of a bulky compound–DNA complex that caused slow diffusion. The mixed binding mode of interaction as seen in docking was further verified by changes in DNA viscosity with varying compound concentrations. All compounds showed strong anti-urease activity, whereas UP-1 was found to have comparatively better inhibitory efficiency, with an IC₅₀ value of 1.55 ± 0.0288 µM. The dose-dependent cytotoxicity of the synthesized derivatives against glioblastoma MG-U87 cells (a human brain cancer cell line) followed by HEK-293 cells (a normal human embryonic kidney cell line) indicated that UP-1 and UP-3 have greater cytotoxicity against both cancerous and healthy cell lines at 400 µM. However, dose-dependent responses of UP-2 showed cytotoxicity against cancerous cells, while it showed no cytotoxicity on the healthy cell line at a low concentration range of 40–120 µM. Full article

A series of hydrazine-1-carbothioamides derivatives (3a–3j) were synthesized and analyzed for inhibitory potential towards bovine carbonic anhydrase II (b-CA II) and 15-lipoxygenase (15-LOX). Interestingly, four derivatives, 3b, 3d, 3g, and 3j, were found to be selective inhibitors of CA II, while other derivatives exhibited CA II and 15-LOX inhibition. In silico studies of the most potent inhibitors of both b-CA II and 15-LOX were carried out to find the possible binding mode of compounds in their active site. Furthermore, MD simulation results confirmed that these ligands are stably bound to the two targets, while the binding energy further confirmed the inhibitory effects of the 3h compound. As these compounds may have a role in particular diseases, the reported compounds are of great relevance for future applications in the field of medicinal chemistry. Full article

The kingdom of Saudi Arabia (SA) ranks fifth in Asia in terms of area. It features broad biodiversity, including interesting flora, and was the historical origin of Islam. It is endowed with a large variety of plants, including many herbs, shrubs, and trees. Many of these plants have a long history of use in traditional medicine. The aim of this review is to evaluate the present knowledge on the plants growing in SA regarding their pharmacological and biological activities and the identification of their bioactive compounds to determine which plants could be of interest for further studies. A systematic summary of the plants’ history, distribution, various pharmacological activities, bioactive compounds, and clinical trials are presented in this paper to facilitate future exploration of their therapeutic potential. The literature was obtained from several scientific search engines, including Sci-Finder, PubMed, Web of Science, Google Scholar, Scopus, MDPI, Wiley publications, and Springer Link. Plant names and their synonyms were validated by ‘The Plant List’ on 1 October 2021. SA is home to approximately 2247 plant species, including native and introduced plants that belong to 142 families and 837 genera. It shares the flora of three continents, with many unique features due to its extreme climate and geographical and geological conditions. As plants remain the leading supplier of new therapeutic agents to treat various ailments, Saudi Arabian plants may play a significant role in the fight against cancer, inflammation, and antibiotic-resistant bacteria. To date, 102 active compounds have been identified in plants from different sites in SA. Plants from the western and southwestern regions have been evaluated for various biological activities, including antioxidant, anti-cancer, antimicrobial, antimalarial, anti-inflammatory, anti-glycation, and cytotoxic activities. The aerial parts of the plants, especially the leaves, have yielded most of the bioactive compounds. Most bioactivity tests involve in vitro assessments for the inhibition of the growth of tumour cell lines, and several compounds with in vitro antitumour activity have been reported. More in-depth studies to evaluate the mode of action of the compounds are necessary to pave the way for clinical trials. Ecological and taxonomical studies are needed to evaluate the flora of SA, and a plan for the conservation of wild plants should be implemented, including the management of the protection of endemic plants. Full article

Carbonic anhydrases (CA), having Zn²⁺ metal atoms, are responsible for the catalysis of CO₂ and water to bicarbonate and protons. Any abnormality in the functioning of these enzymes may lead to morbidities such as glaucoma and different types of cancers including brain, renal and pancreatic carcinomas. To cope with the lack of presence of a promising therapeutic agent against these cancers, searching for an efficient and suitable carbonic anhydrase inhibitor is crucial. In the current study, ten novel 3-ethylaniline hybrid imino-thiazolidinones were synthesized and characterized by FTIR, NMR (¹H, ¹³C), and mass spectrometry. Synthesis was carried out by diethyl but-2-ynedioate cyclization and different acyl thiourea substitutions of 3-ethyl amine. The CA (II) enzyme inhibition profile for all synthesized derivatives was determined. It was observed that compound 6e demonstrated highest inhibition of CA-II with an IC₅₀ value of 1.545 ± 0.016 µM. In order to explore the pharmacophoric properties and develop structure activity relationship, in silico screening was performed. In silico investigations included density functional theory (DFT) studies, pharmacophore-guided model development, molecular docking, molecular dynamic (MD) simulations, and prediction of drug likeness scores. DFT investigations provided insight into the electronic characteristics of compounds, while molecular docking determined the binding orientation of derivatives within the CA-II active site. Compounds 6a, 6e, and 6g had a reactive profile and generated stable protein-ligand interactions with respective docking scores of −6.12, −6.99, and −6.76 kcal/mol. MD simulations were used to evaluate the stability of the top-ranked complex. In addition, pharmacophore-guided modeling demonstrated that compound 6e produced the best pharmacophore model (HHAAARR) compared to standard brinzolamide. In vitro and in silico investigations anticipated that compound 6e would be an inhibitor of carbonic anhydrase II with high efficacy. Compound 6e may serve as a potential lead for future synthesis that can be investigated at the molecular level, and additional in vivo studies are strongly encouraged. Full article

The honey bee is an important economic insect due to its role in pollinating many agricultural plants. Unfortunately, bees are susceptible to many pathogens, including pests, parasites, bacteria, and viruses, most of which exert a destructive impact on thousands of colonies. The occurrence of resistance to the therapeutic substances used against these organisms is rising, and the residue from these chemicals may accumulate in honey bee products, subsequently affecting the human health. There is current advice to avoid the use of antibiotics, antifungals, antivirals, and other drugs in bees, and therefore, it is necessary to develop alternative strategies for the treatment of bee diseases. In this context, the impact of nosema diseases (nosemosis) on bee health and the negative insults of existing drugs are discussed. Moreover, attempts to combat nosema through the use of alternative compounds, including essential oils, plant extracts, and microbes in vitro and in vivo, are documented. Full article