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The green synthesis of Iron oxide nanoparticles (IONPs) has shown numerous advantages over conventional physical and chemical synthesis methods as these methods non-ecofriendly and uses toxic chemicals and complicated equipments. In present study, Iron oxide nanoparticles (IONPs) were created using simple, sustainable, eco-friendly and green chemistry protocol. The roots of novel medicinal plant Sageretia thea was used as a bio-template for the preparation of IONPs. Further, the synthesis of IONPs was confirmed using different analytical tools like UV-Vis, FT-IR, XRD, EDX, and SEM. The average sizes of (NPs) were found to be 16.04 nm. Further, asynthesized IONPs were evaluated for several biological potentials including antibacterial, antifungal Anti-radical potentials (DPPH) and cytotoxicity assays. Antibacterial potencies were investigated using bacterial strains (in the concentration range of 1000–31.25 µg/mL) revealing significant antibacterial potentials. ABA and SAU was reported to be least susceptible while KPN was observed to be most susceptible strain in bactericidal studies. Further, different fungal strains were used to investigate the antifungal potentials of IONPs (in the concentration range of 1000–31.25 µg/mL) and revealed strong antifungal potencies against different pathogenic strains. Furthermore, MRA, FA and ANI were most susceptible and ABA was least susceptible in fungicidal examination. Significant cytotoxicity potential was examined using brine shrimps cytotoxicity assay, thus revealing the cytotoxic potential of asynthesized IONPs. The IC50 for S. thea based IONPs was recorded as 33.85 µg/mL. Strong anti-radical potentials (DPPH) assay was performed to evaluate the ROS scavenging potential of S.T@IONPs. The highest scavenging potential was noted as 78.06%, TRP as 81.92% and TAC as 84% on maximum concentration of 200 µg/mL. In summary, our experimental results concluded, that asynthesized IONPs have strong antibacterial, antifungal, DPPH scavenging and cytotoxic potentials and can be used in different biological applications. In nutshell, our as-prepared nanoparticles have shown potential bioactivities and we recommend, different other in vitro and in vivo biological and bioactivities to further analyze the biological potentials. [ABSTRACT FROM AUTHOR]

AbstractCarvacrol is a consolidated natural antimicrobial. However, its use in food is a challenge due to characteristic odour and high volatility. Nanoencapsulation has emerged to overcome these drawbacks. Aspergillus spp. represent a concern in grapes for causing rot and producing mycotoxins. This study aimed to evaluate the effect of carvacrol (unencapsulated and loaded into Eudragit® and chia nanocapsules) on the growth of Aspergillus species. Spore germination and mycelial growth of Aspergillus spp. were evaluated using the agar dilution culture method. The stability of nanocapsules during storage was monitored monthly by evaluating the particle size distribution, polydispersity index, and zeta potential. Antifungal and antitoxigenic effectiveness of nanocapsules were assessed by counting fungal colony-forming units and determining mycotoxin levels in grapes. A dose-dependent effect of carvacrol (unencapsulated and encapsulated forms) on spore germination and mycelial growth was observed. During 180 days of storage, carvacrol into Eudragit® nanocapsules preserved their nanometric dimensions, whereas chia nanocapsules maintained this characteristic for 30 days. The antifungal effectiveness of both encapsulated forms persisted for 210 days. No mycotoxin was found, even when fungal growth was not completely suppressed. Nanoencapsulated carvacrol proved to be a new promising antifungal product to ensure quality and safety in the grape production chain. [ABSTRACT FROM AUTHOR]

Candida albicans, the most common opportunistic pathogenic fungus, is also the main pathogenic organism for oral candidiasis. This condition is particularly prevalent among the elderly, children, and individuals undergoing radiotherapy or suffering from HIV. The lack of new antifungal drugs, and drug resistance coupled with the side effects of current antifungal agents have increased the challenges of clinical antifungal therapies. Polyenes, including amphotericin B and nystatin, are clinical fungicidal drugs, however, their side effects and low solubility have limited their clinical applications. Here, we identified that moxidectin, a novel approved antiparasitic agent, could synergize with both amphotericin B and nystatin to inhibit the growth and biofilm formation of Candida albicans including 60 clinical isolates. The transcriptome and RT-PCR analysis indicated that moxidectin activated the biosynthesis pathway of ergosterol, the direct target of polyenes, further being verified by the loss of the synergistic activities with polyenes against ergosterol pathway mutants, including Δ/Δerg3, Δ/Δerg11 and Δ/Δerg3 Δ/Δerg11. Moxidectin was then confirmed to elevate the ergosterol biosynthesis levels of C. albicans and enhance the binding between cells and polyenes. In a mouse oral candidiasis model, moxidectin combined with low dosages of polyenes to significantly reduce the infection area, colonization of C. albicans and the inflammatory degree of tongue mucosa. Our study originally demonstrated that moxidectin could activate the ergosterol biosynthesis then elevate the ergosterol contents to enhance the antifungal effects of polyenes against C. albicans and its infections. Moxidectin can serve as the candidate potentiator of polyenes for further clinical practice. Key points: • Moxidectin synergized with polyenes against Candida albicans. • Moxidectin activated the ergosterol biosynthesis of Candida albicans. • Moxidectin combined with polyenes to effectively combat oral candidiasis in mice. [ABSTRACT FROM AUTHOR]

Trimethyl lock (TML) systems have become increasingly important in medicinal and bioorganic chemistry, particularly for their roles in the targeted delivery of therapeutic agents and as integral components in fluorogenic probes for cellular imaging. The simplicity and efficiency of their synthesis have established TML systems as versatile platforms for the controlled release of active molecules under particular physiological conditions. This review consolidates recent advancements in the application of TML systems, with a focus on their use in drug delivery, cellular imaging, and other areas where precise molecular release is crucial. Additionally, we discuss the synthetic strategies employed to construct TML‐based conjugates, underscoring their potential to enhance the specificity and efficacy of bioactive compounds in various biomedical applications. [ABSTRACT FROM AUTHOR]

Mortalities due to mycoses have dramatically increased with the emergence of drug‐resistant strains and growing immune‐compromised populations globally. Azole antifungals have been the first choice against fungal infections of a wide spectrum and several azole derivatives with ester function were reported for their potentially promising and favorable activity against Candida spp. In this study, we designed and synthesized a series of 1‐(aryl)−2‐(1H‐imidazol‐1‐yl/1H‐1,2,4‐triazol‐1‐yl)ethyl esters, and tested them against seven reference Candida strains using EUCAST reference microdilution method. Among the series, 6a, 6d, and 6g proved highly potent in vitro compared to fluconazole; especially against Candida albicans and Candida tropicalis with minimum inhibitor concentration (MIC) values as low as 0.125 and 0.06 mg/L, respectively, although their activities against Candida krusei and Candida glabrata remained limited. The compounds also showed minimal toxicity to murine fibroblasts according to the in vitro cytotoxicity tests. Molecular modeling predicted 6g as an orally available druglike compound according to all parameters and CYP51 inhibition as the likely mechanism for their antifungal effects. The study underpins the promise of azoles with ester functionality as a potential scaffold for small‐molecule antifungal drug design. [ABSTRACT FROM AUTHOR]

Healthcare‐associated infections (HAI) are illnesses acquired during healthcare and are often the most important adverse event during healthcare. With the aim of increasing the effectiveness of disinfection/decontamination processes in the health service with safe and not promote microbial resistance, we propose the development of portable equipment associated with type C ultraviolet light (UVC). The efficiency of the irradiance emitted by the equipment (at dosages 3.5, 5.0, and 60 mJ/cm2) was determined by the action exerted after exposure against four different bacterial (Acinetobacter baumannii, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus) and three different fungi (Candida albicans, C. parapsilosis, and Aspergillus section Fumigati). It was possible to observe that all treatments were capable of inactivating the bacterial species evaluated (p < 0.05), causing the irreversible death of these microorganisms. The most effective elimination of fungal agents was at a dose of 60 mJ/cm2 of UVC radiation, with a decrease in the fungal inoculum varying between 94% and 100% in relation to the control without exposure. Thus, our study showed that the application of the portable prototype with UVC light (254 nm) at a distance of 48 mm, allowed an average irradiance of 3.5 mW/cm2, with doses of 3.5 ≈ 60 mJ/cm2 (from 1 to 60 s of exposure), which can promote the total reduction of the bacteria evaluated and significantly reduce fungal growth. Therefore, this prototype could be used safely and effectively in the hospital environment, considerably reducing contamination and contributing to the reduction of healthcare‐associated infection risk. [ABSTRACT FROM AUTHOR]

Fungal infections present a significant health risk, particularly in immunocompromised individuals. Berberine, a natural isoquinoline alkaloid, has demonstrated broad-spectrum antimicrobial activity, though its antifungal potential and underlying mechanisms against both yeast-like and filamentous fungi are not fully understood. This study investigates the antifungal efficacy of berberine against Candida albicans, Cryptococcus neoformans, Trichophyton rubrum, and Trichophyton mentagrophytes in vitro, as well as its therapeutic potential in a murine model of cryptococcal infection. Berberine showed strong antifungal activity, with MIC values ranging from 64 to 128 µg/mL. SEM and TEM analyses revealed that berberine induced notable disruptions to the cell wall and membrane in C. neoformans. No signs of cell necrosis or apoptosis were observed in fungal cells treated with 2 × MIC berberine, and it did not increase intracellular ROS levels or affect mitochondrial membrane potential. Molecular docking and binding affinity assays demonstrated a strong interaction between berberine and the fungal enzyme CYP51, with a dissociation constant (KD) of less than 1 × 10−12 M, suggesting potent inhibition of ergosterol biosynthesis. In vivo studies further showed that berberine promoted healing in guinea pigs infected with T. mentagrophytes, and in a murine cryptococcal infection model, it prolonged survival and reduced lung inflammation, showing comparable efficacy to fluconazole. These findings indicate that berberine exerts broad-spectrum antifungal effects through membrane disruption and CYP51 inhibition, highlighting its potential as a promising therapeutic option for fungal infections. [ABSTRACT FROM AUTHOR]

We studied the allelopathic effects of aqueous extracts of two weed species viz., Ageratum conyzoides L. and Parthenium hysterophorus L. on seed germination and early seedling growth of bell pepper plants infected by Phytophthora capsici. The parameters studied were: Percent disease index (PDI), seed germination, seedling fresh weight and seedling height of bell pepper. The inhibition (%) of different aqueous extracts of both donor weed plants ranged from 74.82 % to 91.16 %. Of all 4-aqueous extracts, ethanolic extract of leaves showed the best antifungal effects. The GC-MS analysis revealed that these extracts had anti-fungal properties due to the presence of distinct groups of active compounds, suggesting their applied role in disease management. These allelochemicals can be potential tool to manage important plant diseases and replace synthetic fungicides for crop disease management. [ABSTRACT FROM AUTHOR]

Summary: A 3‐year‐old Quarter Horse gelding originating from Texas presented for fever and inappetence. An encapsulated, mixed echogenic cranial mediastinal mass visible ultrasonographically in the left and right fourth intercostal space that displaced the heart caudally was identified. Histological evaluation of needle biopsies obtained under general anaesthesia revealed a severe pyogranulomatous inflammatory process associated with intralesional round, 15–25 μm in diameter, thick double‐contoured cell wall fungal structures. Sequencing of products obtained from DNA extracted from the paraffin‐embedded biopsy sample and a panfungal PCR assay targeting the large ribosomal unit region had a 99.1% identity to either Coccidioides immitis or C. posadessii. Bronchoscopy revealed purulent exudate in the right primary bronchus. Cytological evaluation of bronchial alveolar lavage fluid (BALF) contained 96% moderately degenerative neutrophils and 4% macrophages. Fungal structures were not appreciated in the BALF. However, the mediastinitis could have resulted from inhalation and dissemination of arthroconidia through lymphatics or directly from the lung parenchyma. Quantitative immunodiffusion of serum for the presence of coccidioidal IgG antibodies yielded a titre of 1:256 suggestive of disseminated coccidioidomycosis. After oral fluconazole for 24 months, the horse's general health and athletic performance had returned to normal and the mediastinal mass was not appreciated sonographically. [ABSTRACT FROM AUTHOR]

This study represents a sustainable and environmentally friendly approach to synthesizing silver nanoparticles employing the seed extract of Phaseolus vulgaris. Spectrophotometric analysis at a wavelength 433 nm revealed distinct and well-defined peaks in the optical spectrum of the silver nanoparticles. The crystal structure of the synthesized silver nanoparticles was investigated through X-ray diffraction, which demonstrated four prominent diffraction peaks. Noteworthy peaks were observed in the Fourier-transformation infrared spectroscopy results, specifically at the wavenumbers 3350 cm−1, 2926 cm−1, 1740 cm−1, 1369 cm−1, 1214 cm−1 and 1051 cm−1, further confirming the charcteristics of silver nanoparticles. High-resolution transmission electron microscopy revealed an array of shapes such as round, rectangular, diamond, and cylindrical, with an average diameter of approximately 24.8 nm. Subsequent energy dispersive X-rays analysis provided insights into the elemental composition of the silver nanoparticles, confirming their silver nature. The silver nanoparticles synthesized from P. vulgaris demonstrated notable antioxidant potential, as evidenced by their remarkable reactive oxygen species (ROS) quenching ability against 2,2-diphenyl-1-picrylhydrazyl (90%), hydrogen peroxide (60%), and superoxide dismutase (13%). Expanding the scope of investigation, P. Vulgaris silver nanoparticles exhibited robust inhibition against various fungal strains, including Alternaria alternate and Fusarium oxysporum, as well as bacterial strains like Listeria monocytogenes, Pseudomonas aeruginosa, Salmonella enterica and Staphylococcus aureus. Furthermore, in cytotoxicity evaluations using HeLa cell lines, the synthesized nanoparticles exhibited promising anti-proliferative properties with an IC50 value of 146.16 ± 1.70 μM/mL, indicative of their ability to impede cell proliferation. In conclusion, the environmentally friendly synthesis of silver nanoparticles using Phaseolus vulgaris seed extract showcases their multifaceted potential, ranging from antioxidant properties and antimicrobial efficacy to anti-proliferative effects, highlighting their promise as a sustainable and versatile material for various biological applications while aligning with eco-conscious principles. [ABSTRACT FROM AUTHOR]

Featured Application: Salicylaldehyde and 4-isopropyl-3-methylphenol can be used as potential antifungal and anti-mycotoxigenic agents for crops/foods to be processed. Crops such as tree nuts, corn and peanut are highly susceptible to infestation by the aspergilli Aspergillus flavus or Aspergillus parasiticus and subsequent aflatoxin (AF) contamination, a serious threat to public food safety. Conventional control of the aspergilli has been through the application of fungicides; however, certain fungicides at sub-optimal doses have been correlated with increased production of mycotoxins including AF. Natural products (NP) have been a potential source of antifungal agents. In this study, we performed risk assessment testing, for which thirteen NP/derivatives (generally recognized as safe) were examined at sub-inhibitory concentrations to determine the enhancement of AF production in aspergilli. We found that benzaldehyde derivatives or thymol (THY) enhanced AF production in aspergilli, while 4-isopropyl-3-methylphenol (4I3M), a synthetic analog of the NP THY and carvacrol, or salicylaldehyde (SLD) exerted a potent antifungal or mycotoxin-inhibitory effect. In seed testing (corn, pistachio kernels), SLD effectively prevented fungal growth as a fumigant, while 4I3M completely inhibited AF production at ≥1.0 mM. Therefore, we concluded that NP/derivatives that do not have any significant environmental impact can be a potent source of antifungal or anti-mycotoxigenic agents, either in their nascent form or as leads for more effective derivatives; however, NP should be applied at optimum concentrations to prevent the abnormal enhancement of mycotoxin production by fungi. [ABSTRACT FROM AUTHOR]

The cashew industry produces extremely toxic effluent that seriously endangers life. Furthermore, cashew nut shell liquid (CNSL) a by-product, from the cashew industry is underutilized resulting in its presence in effluent. This liquid is extremely toxic and poses a threat to the environment if discharged without removal. Therefore, this comprehensive review delves into the intricacies of cashew nut processing, with a particular focus on the production of CNSL, its chemical profiling, and the imperative need for thorough characterization to ascertain its chemical composition. The manuscript underscores the potential of CNSL as a promising solution in the agricultural sector due to its skyrocketing potential as an insecticidal, fungicidal, antioxidant, anticorrosive, and termite resistant, and its ability to be blended with biodiesel as it improves lubrication properties in comparison with traditional diesel and helps extend the lifespan of engines, further necessitating minimal maintenance. It explores the necessity for chemical modifications in CNSL, presenting recent insights and advancements, particularly in the realm of phyto-nano-emulsions of CNSL with increased bioavailability. Additionally, it highlights the burgeoning role of artificial intelligence and machine learning models in predicting CNSL emissions, yield, crop health, and cashew kernel quality checks, offering a holistic decision support system for supply chain optimization. By succinctly mapping out the roadmap for CNSL production, chemical enhancements, and its application as an antifungal agent, the manuscript advocates for the integration of AI and ML to enhance agricultural outcomes and boost farmers' profits.Article Highlights: Chemical profiling and characterization details of Cashew nut shell liquid- an underutilized cashew industry by-product which is rich in chemical constituents. Recent insights on the exceptional multifaceted potential of Cashew Nut Shell Liquid (CNSL) to achieve sustainability in the agricultural sector. An Update on how the integration of AI and machine learning in CNSL production and applications can enhance decision support systems-ultimately increasing farmers’ profits. [ABSTRACT FROM AUTHOR]

Potent chemical-free approaches are much needed to control multi-drug resistant pathogens such as biofilm-forming Staphylococcus aureus and rice blast fungus Magnaporthe oryzae. Environmentally safe agricultural practices and wound healing scaffolds based on hydrogels have a limitation arising from formulations containing environmentally toxic cross-linkers or photo-initiators. We have developed non-toxic starch hydrogels with uniformly dispersed silver nanoparticles (AgNP) having wide-spectrum antimicrobial activity for biomedical or agricultural applications. AgNPs were synthesized with Emblica officinalis extract, surface functionalized with the nutraceutical chemical groups in the extract as revealed by Fourier transform infrared spectroscopy. Scanning electron microscopy images show uniform dispersion of AgNP (5 ± 2 nm size) in the hydrogel matrix. AgNP-starch hydrogels are observed to have an excellent antifungal activity to M. oryzae with complete growth inhibition for 10 days compared to the control-starch hydrogel without AgNP and agar gel, even in the presence of the favourable growth medium of yeast extract + glucose. Antibacterial activity was also observed for gram-negative bacteria Escherichia coli and gram-positive bacteria S. aureus using diffusion assay with antibiotic mixture, with four-fold enhancement in zone of inhibition area in case of AgNP-starch hydrogels compared to control starch hydrogels, showing good release efficiency. Sustained release of botanical extracts showed promising bacterial growth inhibition. AgNP hydrogel surface-inhibition of bacterial growth for B. subtilis and E. coli persisted for 8–10 h and S. aureus until 6 h. Starch hydrogels have a high storage modulus G′ = ~ 17 kPa, and AgNP-starch hydrogels have a softer matrix with G′ = 3.6 kPa. Both are stable for a wide range of strain frequencies in the linear viscoelastic regime, revealing the potential for a strong, stable printable scaffold for wound healing. In the dried state, the AgNP-starch films show higher yield point and elongation at break compared to nascent cross-linked starch films under uniaxial tensile forces. Although AgNP-starch hydrogels show a nanoporous morphology enabling controlled drug release, there is negligible AgNP release from the hydrogel matrix. [ABSTRACT FROM AUTHOR]

AbstractPurposeMethodsResultsConclusionFungal keratitis (FK) is a difficult condition to treat, particularly in underdeveloped nations. The study aimed to compare the in vitro activity of chlorhexidine (CHX) and seven antifungal agents against a collection of fungi recovered from FK patients.Seventy-three fungi were collected from patients with FK included in study. The antifungal agents tested were fluconazole, voriconazole, posaconazole, miconazole, natamycin, amphotericin B, and caspofungin. The concentration range for CHX was 1–1024 μg/mL. Assessments of antifungal susceptibility were conducted using the EUCAST broth microdilution reference method.The findings demonstrated the beneficial in vitro inhibition of filamentous and yeast fungi by CHX. CHX demonstrated efficacy against Fusarium spp., Aspergillus spp., Candida spp., S. apiospermum and dematiceous fungi at concentrations of 4–64, 32–64, 4–32, 8, and 4–16 µg/mL respectively. The median MICs and MIC distributions of CHX showed no significant differences among the evaluated spp. (p > 0.05). The most effective antifungal drug was posaconazole, which was followed by voriconazole, caspofungin, and amphotericin B.In situations where access to a range of antifungal medications and microbiological facilities is limited, CHX should be further investigated as a potential treatment for FK. It might be able to treat the condition as an inexpensive topical treatment. [ABSTRACT FROM AUTHOR]

Ultrasonic-assisted synthesis of ZnO/TiO₂ and Fe₃O₄/TiO₂ bi-oxide nanocomposites at low frequencies (60 kHz) with their characterizations and antibacterial/antifungal applications are investigated in this study. Using nanotechnology as the next-generation solution, this research explored the potential of metal oxide nanoparticles as effective antibacterial agents. Nanomaterials were synthesized via a novel and facile method (sono-synthesis) and characterized using various techniques (XRD, SEM, FTIR, zeta potential analysis, Raman spectroscopy, and XPS), revealing nanoscale sizes of 25 nm for ZnO/TiO₂ and 31 nm for Fe₃O₄/TiO₂. Structural analysis demonstrated the distinct crystalline phases of the synthesized nanomaterials: TiO₂ with anatase structure (25 %), hexagonal wurtzite structure for ZnO, and Fe₃O₄ with inverse spinel structure, formed in nano-dimensions (19–31 nm) with a near-spherical shape. Antibacterial and antifungal assays highlighted the efficacy of both bi-nanocomposites against gram-positive (Staphylococcus aureus) and gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria, along with their potent activity against Candida albicans and non-albicans Candida. Moreover, principal component analysis (PCA) was used to identify potential relationships between the physicochemical properties (zeta potential, size, conductivity, and concentration) of all nanomaterials tested and their zone of inhibition (ZOI) against all bacterial species tested. Overall, this study emphasizes the novelty of employing a simple and efficient sono-synthetic route to synthesize ZnO/TiO₂ and Fe₃O₄/TiO₂ bi-nanocomposites and investigate their significant antibacterial and antifungal activities. Additionally, it identifies the potential relationships between the physicochemical properties of the nanomaterials tested and their antimicrobial activity. This approach provides a robust framework for future applications of bi-nanocomposites in combating microbial infections. • Effectively synthesized Fe₃O₄, ZnO, Fe₃O₄/TiO₂, and ZnO–TiO₂ bi-nanocomposites using an ultrasonic process via one-pot synthesis, while also uncovering their inherent antimicrobial potential. • The sono-synthesized nanomaterials were characterized and confirmed by various spectroscopic and microscopic techniques. • XRD confirmed the successful synthesis of bi-nanocomposites and showed the average crystallite size of Fe₃O₄/TiO₂ as 15.79 nm and ZnO/TiO₂ as 10.35 nm. • Particularly, Fe₃O₄/TiO₂ and Fe₃O₄ showed significant antimicrobial activity against both Gram-negative and Gram-positive bacteria. • Both Fe₃O₄/TiO₂ and ZnO/TiO₂ bi-nanocomposites exhibited remarkable antibacterial activity against E. coli and antifungal activity against non-albicans Candida, suggesting their effectiveness in combating fungal pathogens. [ABSTRACT FROM AUTHOR]

In the present study, fluconazole (FLU) showed the highest solubility in clove oil and was selected as the oil phase for the FLU-loaded nanoemulsion (FLU-NE). Among the studied cosurfactants, Labrafac was better than ethanol at providing globules with acceptable sizes and a lower polydispersity index (PDI) when Tween 80 was the surfactant. This optimized FLU-NE was thermodynamically stable. Furthermore, FLU-NE stored at 40 ± 2 °C and 75 ± 5% relative humidity for 6 months demonstrated good stability. The FLU-NE was converted to a FLU-loaded nanoemulsion gel (FLU-NEG) using 2% w/v sodium carboxymethyl cellulose. The FLU-NEG was acceptable in terms of visual appearance and spreadability. Rheological studies revealed pseudoplastic behavior for FLU-NEG. The viscosity of FLU-NEG decreased when the applied rpm was increased. FLU-NEG showed greater drug release than that from a FLU-GEL formulation. Furthermore, the FLU release from FLU-NEG followed the Higuchi model. The results from the in vitro antifungal evaluation of FLU-NEG on Candida albicans ATCC 76615 strain confirmed the increase in the antifungal activity of FLU by clove oil. Significant differences were observed in the zones of inhibition produced by FLU-NEG compared to those produced by the blank nanoemulsion gel (B-NEG), fluconazole suspension (FLU-SUS), and nystatin samples. Thus, the increase in the antifungal activity of FLU using clove oil as the oil phase in its nanoemulsion formulation was quite evident from our results. Therefore, the developed FLU-NEG could be considered a potential candidate for further preclinical and clinical studies. [ABSTRACT FROM AUTHOR]

The regulatory role of zinc in bone formation extends to the activation of proteins associated with bone homeostasis. Furthermore, copper is well known for its antibacterial properties. This dual function underscores the significance of zinc and copper in maintaining a balance of bone structure and function. In light of the aforementioned, zinc sulphide/copper oxide nanocomposites were created in this instance using a straightforward coprecipitation technique. Copper oxide was used as a nanocomposite to improve the structural, morphological, and biological performance of zinc sulphide nanoparticles. The X-ray diffraction pattern confirmed a transformation in the crystal structure from cubic to rhombohedral, along with increase in intensity. Fourier transforms infrared analysis indicated the presence of functional groups. Scanning electron microscopy images demonstrated a morphological shift from non-uniform to distinct spherical nanoparticles, impacting the enhancement of material properties. The pathogenic activity of the zinc sulphide/copper oxide nanocomposites was tested against nine bacterial strains. In antimicrobial testing, zinc sulphide/copper oxide nanocomposites showed promising results, particularly against Klebsiella pneumoniae (zone of inhibition: 14 mm at 100 µg/mL compared to 7 mm by standard) and Escherichia coli (zone of inhibition: 11 mm at 100 µg/mL compared to 10 mm by standard) after 24 h with zone of inhibition matching or exceeding that of the standard (chloramphenicol). Zinc sulphide nanoparticles and zinc sulphide/copper oxide nanocomposites were evaluated for their antifungal activity against fungal stains from Trichophyton rubrum, Aspergillus niger, and Aspergillus flavus. After a 24-h period, it was discovered that zinc sulphide/copper oxide nanocomposites were effective against Aspergillus flavus (zone of inhibition: 19.4 mm at 100 µg/mL compared to 6.3 mm by standard) at all concentrations (25–100 mg/mL), with zones of inhibition identical to or greater than those of the standard (fluconazole). Certainly, based on these results, zinc sulphide/copper oxide nanocomposites could be promising materials for drug delivery. Clinical trial registration: Not applicable. [ABSTRACT FROM AUTHOR]

An appealing strategy for finding novel bioactive molecules in Nature consists in exploring underrepresented and -studied microorganisms. Here, we investigated the antimicrobial and tumoral anti-proliferative bioactivities of twenty-three marine and estuarine bacteria of the fascinating phylum Planctomycetota. This was achieved through extraction of compounds produced by the Planctomycetota cultured in oligotrophic medium followed by an antimicrobial screening against ten relevant human pathogens including Gram-positive and Gram-negative bacteria, and fungi. Cytotoxic effects of the extracts were also evaluated against five tumoral cell lines. Moderate to potent activities were obtained against Enterococcus faecalis, methicillin-sensitive and methicillin-resistant Staphylococcus aureus and vancomycin-sensitive and vancomycin-resistant Enterococcus faecium. Anti-fungal effects were observed against Trichophyton rubrum, Candida albicans and Aspergillus fumigatus. The highest cytotoxic effects were observed against human breast, pancreas and melanoma tumoral cell lines. Novipirellula caenicola and Rhodopirellula spp. strains displayed the widest spectrum of bioactivities while Rubinisphaera margarita ICM_H10T affected all Gram-positive bacteria tested. LC-HRMS analysis of the extracts did not reveal the presence of any known bioactive natural product, suggesting that the observed activities are most likely caused by novel molecules, that need identification. In summary, we expanded the scope of planctomycetal species investigated for bioactivities and demonstrated that various strains are promising sources of novel bioactive compounds, which reenforces the potential biotechnological prospects offered by Planctomycetota. [ABSTRACT FROM AUTHOR]

Piperazine, a nitrogen‐containing heterocyclic compound, has potential in medical chemistry due to its versatile structure and ease of modification. Therefore, researchers have designed novel piperazine derivatives with various biological activities, including antiviral, antibacterial, and antifungal properties. In this study, a new series of 2‐(4‐((5‐bromo‐2‐methoxyphenyl)sulfonyl) piperazine‐1‐yl) acetamide derivatives (7a‐l) were synthesized and their structures were identified using 1H‐NMR, 13C‐NMR, and HRMS spectroscopic methods. The in vitro antimicrobial activity of these compounds was tested against four bacterial strains and two fungi strains. Some of the sulfonyl piperazine derivatives (7d, 7e, 7f, 7j, 7k, and 7l) exhibited relatively good antimicrobial and antifungal activities compared to standard drugs. Further analysis using computational docking confirmed strong binding interactions, aligning with our results. Our compounds exhibited improved potency compared to existing standard treatments. [ABSTRACT FROM AUTHOR]

The current study aims to explore the efficacy of antifungal photodynamic therapy (PDT) on C. albicans biofilms by combining photosensitizers, bisdemethoxycurcumin (BDMC), and melatonin (MLT) or acetyl-melatonin (AcO-MLT). Additionally, the relationship between different types of reactive oxygen species and PDT's antifungal efficacy was investigated. BDMC, MLT and AcO-MLT were applied, alone and in combination, to 48-hour C. albicans biofilm cultures (n = 6/group). Blue and red LED light (250 mW/cm2 with 37.5 J/cm2 for single or 75 J/cm2 for dual photosensitizer groups) were used to irradiate BDMC groups and MLT/AcO-MLT groups, respectively. For combination groups, blue LEDs and subsequently red LEDs were used. Drop plate assays were performed at 0, 1 and 6 h post-treatment. Colony forming units (CFUs) were then counted after 48 h. Hydroxyl radicals and singlet oxygen were measured using fluorescence spectroscopy and electron spin resonance (ESR) spectroscopy. Additionally, cell cytotoxicity was tested on human oral keratinocytes. Significant CFU reductions were observed with combinations 20 µM BDMC + 20 µM AcO-MLT and 60 µM BDMC + 20 µM MLT at 0 and 1 h post-treatment, respectively. Singlet oxygen production increased with the addition of MLT/AcO-MLT and had moderate-substantial correlations with inhibition at all times. Hydroxyl radical production was not significantly different from the control. Additionally, BDMC exhibited subtle cytotoxicity on human oral keratinocytes. PDT using BDMC + MLT or AcO-MLT, with blue and red LED light, effectively inhibits C. albicans biofilm through singlet oxygen generation. Melatonin acts as a photosensitizer in PDT to inhibit fungal infection. [ABSTRACT FROM AUTHOR]

Pulmonary coccidioidomycosis is a relatively common fungal disorder in dogs that have lived in or traveled to endemic regions and fluconazole is a common antifungal treatment. Liver enzymopathy can occur with fluconazole administration, but the frequency of occurrence nor potentially associative factors have been explored in dogs with pulmonary coccidioidomycosis. Therefore, our objectives were to describe the occurrence and magnitude of liver enzyme activity (LEA) elevation in dogs with pulmonary coccidioidomycosis during treatment with per os fluconazole and identify variables associated with liver enzymopathy. This was a retrospective observational study that analyzed serum biochemical data obtained from a separate prospective study that included 32 client-owned dogs with newly diagnosed pulmonary coccidioidomycosis from October 2020 to February 2021. Per os fluconazole administration (median dosage: 16.2 mg/kg/day) was initiated after diagnosis and dogs were evaluated once every 3 months thereafter until remission or for a maximum of 12 months. Recorded biochemical parameters at each visit (including baseline) included alanine transaminase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (GGT). Magnitude of increased LEA was based on the fold increase above the upper limit of the reference interval and defined as mild (<5×), moderate (5-10×) or severe (>10×). Forty-seven percent (15/32) of dogs were documented to have elevations in one or more LEAs after initiation of fluconazole administration during the study period. Thirty-four percent and 25% of dogs had elevated ALP and ALT activities, respectively, at some point during treatment. Elevations in AST and GGT activities were rare. The magnitude of LEA elevation was mild in all cases. Logistic regression models did not identify associations between age, weight, sex, neutered status, prednisone administration, fluconazole dose or duration of treatment with the occurrence of liver enzymopathy. Approximately half of dogs with pulmonary coccidioidomycosis are expected to develop mild increases in activities of ALP and/or ALT with rare involvement of AST or GGT at some point during treatment with fluconazole up to 12 months. [ABSTRACT FROM AUTHOR]

Bulaşıcı hastalıklar yıllardan beri dünya çapında ölümlerin önde gelen nedenlerinden biridir. Özellikle çoklu ilaç direncine sahip Metisiline Dirençli Staphylococcus aureus (MRSA) suşları, dünya çapında halk sağlığını tehdit eden en önemli unsurların başında gelir. Basidiomycetes grubu mantarlar umut verici bir antibakteriyel bileşik kaynağı olarak bilinmektedirler. Bu çalışmada Ramaria aurea (Schaeff.) Quél.'nın metanol ve etanol ekstraktlarının patojen standart mikroorganizmalara karşı antimikrobiyal ve klinik örneklerden izole edilen MRSA suşlarına karşı anti-MRSA aktivitesinin belirlenmesi amaçlanmıştır. Antimikrobiyal aktiviteyi belirlemek için sıvı mikrodilüsyon metodu kullanılmıştır. Kullanılan suşlara ekstraktların 12.5-0.006 mg/ml arasındaki konsantrasyonları uygulanmıştır. Metanol ve etanol ekstraktlarının, standart bakteri suşlarına karşı 0.19-6.25 mg/ml aralığındaki dozlarda antibakteriyal aktiviteye sahip olduğu tespit edilirken, her iki ekstraktın da en etkili olduğu suşun 0.19 mg/ml dozla Bacillus cereus suşu olduğu görülmüştür. Ayrıca metanol ve etanol ekstraklarının her ikisinin de antifungal bir etkisi belirlenememiştir. Metanol ekstraktının çalışılan tüm MRSA suşlarına karşı 0.04-6.25 mg/ml aralığındaki dozlarda anti-MRSA aktivitesi gösterdiği belirlenirken, etanol ekstraktının bu suşların tamamına karşı 0.19-3.12 mg/ml aralığındaki dozlarda anti-MRSA aktivitesine sahip olduğu tespit edilmiştir. Sonuç olarak çalışılan Ramaria aurea ekstraklarının antibakteriyal ve anti-MRSA etkiye sahip olduğu belirlenmiş olup bu türün antimikrobiyal ajanların doğal bir kaynağı olabileceği ve farmakoloji endüstrisinde kullanılabileceği söylenebilir. Infectious diseases have been one of the leading causes of death worldwide for years. Especially multidrug-resistant Methicillin-Resistant Staphylococcus aureus (MRSA) strains are among the most important threats to public health worldwide. Basidiomycetes group fungi are known as a promising source of antibacterial compounds. This study aimed to determine the antimicrobial activity of methanol and ethanol extracts of Ramaria aurea (Schaeff.) Quél. against pathogenic standard microorganisms and anti-MRSA activity against MRSA strains isolated from clinical samples. Broth microdilution method was used to determine the antimicrobial activity. Concentrations between 12.5-0.006 mg/ml of the extracts were applied to the strains used. While methanol and ethanol extracts were found to have antibacterial activity against standard bacterial strains at doses ranging from 0.19 to 6.25 mg/ml, the most effective strain of both extracts was Bacillus cereus at a dose of 0.19 mg/ml. In addition, no antifungal effect was determined for both methanol and ethanol extracts. While methanol extract was found to have anti-MRSA activity against all studied MRSA strains at doses ranging from 0.04 to 6.25 mg/ml, ethanol extract was found to have anti-MRSA activity against all these strains at doses ranging from 0.19 to 3.12 mg/ml. As a result, it was determined that the studied Ramaria aurea extracts had antibacterial and anti-MRSA activity, and it can be said that this species may be a natural source of antimicrobial agents and may be used in the pharmaceutical industry. [ABSTRACT FROM AUTHOR]

Limited antifungal treatment options and drug resistance require innovative approaches to effectively combat fungal infections. Combination therapy is a promising strategy that addresses these pressing issues by concurrently targeting multiple cellular sites. The drug targets usually selected for combination therapy are from different cellular pathways with the goals of increasing treatment options and reducing development of resistance. However, some circumstances can prevent the implementation of combination therapy in clinical practice. These could include the increased risk of adverse effects, drug interactions, and even the promotion of drug resistance. Furthermore, robust clinical evidence supporting the superiority of combination therapy over monotherapy is limited and underscores the need for further research. Despite these challenges, synergies detected with different antifungal classes, such as the azoles and echinocandins, suggest that treatment strategies can be optimized by better understanding the underlying mechanisms. This review provides an overview of multi-targeting combination strategies with a primary focus on Candidozyma auris infections. [ABSTRACT FROM AUTHOR]

Developing bio-based and biodegradable materials has become important to meet current market demands, government regulations, and environmental concerns. The packaging industry, particularly for food and beverages, is known to be the world's largest consumer of plastics. Therefore, the demand for sustainable alternatives in this area is needed to meet the industry's requirements. This review presents the most commonly used bio-based and biodegradable packaging materials, bio-polyesters, and polysaccharide-based polymers. At the same time, a major problem in food packaging is presented: fungal growth and, consequently, food spoilage. Different types of antifungal compounds, both natural and synthetic, are explained in terms of structure and mechanism of action. The main uses of these antifungal compounds and their degree of effectiveness are detailed. State-of-the-art studies have shown a clear trend of increasing studies on incorporating antifungals in biodegradable materials since 2000. The bibliometric networks showed studies on active packaging, biodegradable polymers, films, antimicrobial and antifungal activities, essential oils, starch and polysaccharides, nanocomposites, and nanoparticles. The combination of the development of bio-based and biodegradable materials with the ability to control fungal growth promotes both sustainability and the innovative enhancement of the packaging sector. [ABSTRACT FROM AUTHOR]

The growing emergence of multi-drug resistant microbial strains has kept the scientific world searching for novel bioactive compounds with specific chemical characteristics. Accordingly, researchers have started exploring the understudied metabolites from endophytes as a new source of bioactive compounds. In this context, the current study was designed to evaluate the bioactive properties of endophytic fungi from the Mokrzański forest in Wrocław, Poland that have not yet been fully researched. Forty-three endophytic fungi were isolated from twelve distinct plants. Following their cultivation, fungal extracts were separately prepared from biomass and cell-free filtrates, and their antibacterial, antifungal (against human and plant pathogens), and antioxidant properties were examined. Five promising fungi after screening were identified to possess all of these activities. These strains and their respective plant hosts were Trichoderma harzianum BUK-T (Fagus sylvatica), Aspergillus ochraceus ROB-L1 (Robinia pseudoacacia), Chaetomium cochliodes KLON-L1, Fusarium tricinctum KLON-L2 (Acer platanoides), and Penicillium chrysogenum SOS-B2 (Pinus sylvestris). Moreover, gamma irradiation at several doses (Gy) was separately applied to the fungal cultures to study their effects on the recorded activities. Finally, compounds after preparative thin-layer chromatography fractionation of the five fungal strains were identified by GC-MS. These findings suggest that the isolated endophytic fungi could serve as novel sources of bioactive metabolites with antibacterial, antifungal, and antioxidant properties, potentially paving the way for future research and the development of new bioactive compounds. [ABSTRACT FROM AUTHOR]

Active, fully biobased film-forming dispersions (FFDs) with highly promising results for sliced soft bread preservation were successfully elaborated from carboxymethyl cellulose (CMC) and chitosan (CH) using a simple method based on pH adjustments. They consisted of the association of polysaccharides and oleic acid (OL) added with cinnamon (CEO) or ginger (GEO) essential oils. The chemical compositions of the commercial essential oils were first determined via GC/MS, with less than 3% of compounds unidentified. The films obtained from FFDs were characterized by SEM, FTIR and DSC, indicating specific microstructures and some interactions between essential oils and the polymer matrix. CEO-based films exhibited higher antioxidant properties and a lower minimal inhibitory concentration in terms of antifungal properties. From experiments on sliced soft bread, the ginger-based films could increase the shelf life up to 20 days longer than that of the control. Even more promising, cinnamon-based films led to complete fungal inhibition in bread slices that was maintained beyond 60 days. Enumeration of the yeasts and molds for the FFD-coated breads revealed complete inhibition even after 15 days of storage with the FFDs containing the highest concentration of CEO. [ABSTRACT FROM AUTHOR]

Naphthylimides play a pivotal role as aromatic heterocyclic compounds, serving as the foundational structures for numerous pharmacologically significant drugs. These drugs encompass antibacterial, antifungal, anticancer, antimalarial, antiviral, anti-inflammatory, antithrombotic, and antiprotozoal agents. The planar and heteroaromatic characteristics of naphthylimides grant them a strong ability to intercalate into DNA. This intercalation property renders naphthylimide derivatives highly valuable for various biological activities. The advantageous pharmacological activity and ease of synthesis associated with naphthylimides and their derivatives provide significant benefits in the design and development of new compounds within this class. Currently, only a few such molecules are undergoing preclinical and clinical evaluations. In this paper, we have compiled the literature on naphthylimides reported by researchers from 2006 to 2024. Our focus lies on exploring the pharmacological activities of their analogues from a drug development and discovery perspective, while examining their structure–activity relationship and mechanisms of action. [ABSTRACT FROM AUTHOR]

Objective: In the current situation, human beings face challenges in the design and fabrication of new pyridine-based multifunctional hybrids for various applications. Pyridine-based scaffolds sparked tremendous scientific interest in discovering new active components in medicinal areas. Methods: Here we report the synthesis of pyridine-clubbed hydrazide with substituted aldehyde building blocks via a green chemistry approach. In this work, we demonstrate the synthesis of a small library of compounds via enaminone to Schiff base formation by using microwave techniques. Moreover, the final moieties' drug-likeness profile and toxic effects were assessed by in silico ADMET prediction analysis. Results and Discussion: Synthesized compounds were characterized by MS, FT-IR, 1H, 13C NMR, and other analytical techniques. Furthermore, synthesized compounds (IVa–IVj) were screened against Gram-positive, Gram-negative, and fungal stains for their antimicrobial assay using the broth dilution method and Ciprofloxacin, and nystatin were used as standards. Conclusions: The result shows that at a concentration of 25 µg/mL, the compounds with substitutions in thio, indole, and pyridine (IVc), (IVd), and (IVh) had excellent antibacterial activity and compounds with substituted chloro and methoxy (IVb) and (IVi) exhibited excellent antifungal activity at a concentration of 100 µg/mL. [ABSTRACT FROM AUTHOR]

Objective: The most comprehensive collection of imine was synthesized via a simple, efficient, economical, and rapid method via Schiff base formation. Methods: ((E)-1,5-dimethyl-2-phenyl-4-(((2-phenylimidazo[1,2-a]pyridine-3-yl)methylene)amino)-1,2-dihydro-3H-pyrazol-3-one and their derivatives are synthesized using 4-aminoantipyrine and some substituted 2-phenylimidazo[1,2-a]pyridine-3-carbaldehyde derivatives (SB01) to (SB10). Results and Discussion: The newly synthesized molecules were confirmed using various analytical techniques MS, FT-IR, 1H, and 13C NMR spectrometric analyses. Newly synthesized imidazo[1,2-a]pyridine compounds undergo their biological evaluation with Gram-positive and Gram-negative bacteria as well as antifungal. Conclusions: (SB10), (SB07), (SB05), and (SB01) molecules show good, moderate, and excellent results against tested drugs. [ABSTRACT FROM AUTHOR]

Coumarins are the natural products which are characterized as 1,2-benzopyrones. The discovery of coumarins is done with enlarged chemical space through many synthetic course of action. They are found in many plants such as cinnamon, tonka beans, and sweet clover. Cassia cinnamon has the highest amount of coumarin whereas Ceylon cinnamon has the lowest. Many biological activities and applications of coumarins are attributed to their capacity to engage in non-covalent interactions with numerous enzymes and receptors found in living organisms. Some of the pharmacological properties are anticancer, anticoagulant, antifungal, antiviral, antitubercular, antioxidant, anti-inflammatory, antidiabetic, antibacteria, antihypertensive, antihyperglycemic, anticonvulsant, antiparasitic, antineurodegenerative, etc. A review has been carried out based on various pharmacological activities containing Coumarin derivatives to rationalize the activities based on the structural variations. Coumarin derivatives have been attracting increasing interest for their usefulness and excellent contribution in the prevention, curing, and treatment of the diseases, growth modulation, cell growth and regulation of immune response. [ABSTRACT FROM AUTHOR]

The use of cow urine (CU) in treating a variety of illness can be traced back to ancient ages. It has been referred as an important and integral component of Cowpathy – an age-old practice in Indian sub-continent since the Vedic period (1500 BC – 600 BC). The CU contains several important compounds that are essential in maintaining a balance between the well-being of human and the nature. It is composed of about 95 % water and other useful ingredients such as urea, hormones, lyase enzyme, and salts containing Fe, Ca, P, Mn, S, N, and K. In addition, it also contains lactose, cytokine, and amino acid which are the fundamental building blocks of protein. Researchers have developed various processes for the green synthesis of CU concentrate and evaluated its usefulness in treating various diseases owing to its antibacterial and antifungal properties. Further, CU has also shown promising immunity boosting and anti-oxidant characteristics. Even though human civilization has benefited from the use of CU in treating various types illness but the modern scientific understanding of the cause-effect relationships was partly developed in the last few decades. There exists a huge knowledge gap and a comprehensive study on exploring the science and application of CU hasn't been reported. This paper reviews the historical perspective, compositional analysis, processing, applications, knowledge gap, and future research required in the field of therapeutic usage of CU. [ABSTRACT FROM AUTHOR]

Repeated epidemics caused by bacterial and fungal diseases pose a threat to global crop yields and food security, therefore, updating the structure of existing microbicides and improving the pesticide bioavailability are challenging tasks, perhaps planning to develop versatile supramolecular antimicrobial materials. Here, a low‐cost multifunctional supramolecular complex, named FT6@β‐CD, is constructed by host‐guest encapsulation of a thienyl‐engineered ingredient (FT6) into β‐cyclodextrin. This integrated architecture can significantly reduce the bounce and splash behaviors of droplets, improve the wetting performance, and eventually acquire excellent foliar deposition and targeted delivery. Whereafter, FT6@β‐CD can inhibit the transcription of type III secretion system (T3SS)‐associated genes, hypersensitive reaction, and final pathogenicity from a destructive pathogen Xanthomonas oryzae pv. oryzae (Xoo). Importantly, at a lower dosage of 200 µg mL−1, FT6@β‐CD presented excellent in vivo control effects (protection 48.1%, curative 50.1%) against Xoo, remarkably better than the commercial bactericidal formulation thiodiazole‐copper. Additionally, other supramolecular antifungal materials (FT24/FT25@HP‐β‐CD/β‐CD/Me‐β‐CD) constructed in this study can effectively treat Botryosphaeria dothidea and Botrytis cinerea with higher control efficiencies of 86.8% and 90.1% at 200 µg mL−1, respectively. This study provides a bright guidance for developing low‐cost, green, and eco‐friendly supramolecular microbicides for controlling agricultural diseases. [ABSTRACT FROM AUTHOR]

A diminutive chemical library of acyl thiotriazinoindole (ATTI) based bioactive scaffolds was synthesized, instigated by taking the economical starting material Isatin, through a series of five steps. Isatin was first nitrated followed by the attachment of pentyl moiety via nucleophilic substitution reaction. The obtained compound was reacted with thiosemicarbazide to obtain thiosemicarbazone derivative, which was eventually cyclized using basic conditions in water as solvent. Finally, the reported series was obtained through reaction of nitrated thiotriazinoindole moiety with differently substituted phenacyl bromides. The synthesized compounds were characterized using NMR spectroscopy and elemental analysis. Finally, the synthesized motifs were scrutinized for their potential to impede urease, α-glucosidase, DPPH, and α-amylase. Compound 5 h with para cyano group manifested the most pivotal biological activity among all, displaying IC50 values of 29.7 ± 0.8, 20.5 ± 0.5 and 36.8 ± 3.9 µM against urease, α-glucosidase, and DPPH assay, respectively. Simultaneously, for α-amylase compound 5 g possessing a p-CH3 at phenyl ring unfolded as most active, with calculated IC50 values 90.3 ± 1.1 µM. The scaffolds were additionally gauged for their antifungal and antibacterial activity. Among the tested strains, 5d having bromo as substituent exhibited the most potent antibacterial activity, while it also demonstrated the highest potency against Aspergillus fumigatus. Other derivatives 5b, 5e, 5i, and 5j also exhibited dual inhibition against both antibacterial and antifungal strains. The interaction pattern of derivatives clearly displayed their SAR, and their docking scores were correlated with their IC50 values. In molecular docking studies, the importance of interactions like hydrogen bonding was further asserted. The electronic factors of various substituents engendered variety of interactions between the ligands and targets implying their importance in the structures of the synthesized heterocyclic scaffolds. To conclude, the synthesized compounds had satisfactory biological activity against various important targets. Further studies are therefore encouraged by attachment of different substitutions in the structure at various positions to enhance the activity of these compounds. Exploring Acyl Thiotriazinoindole based Pharmacophores: Design, Synthesis, and SAR studies with Molecular Docking and Biological Activity Profiling against Urease, α-amylase, α-glucosidase, Antimicrobial, and Antioxidant Targets An updated synthetic pathway to furnish acyl thiotriazinoindole based scaffolds was developed starting from Isatin and the novel compounds were assessed for various biological applications. [ABSTRACT FROM AUTHOR]

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Onychomycosis is a prevalent fungal infection of the nails, which causes thickening, discoloration, and detachment of the nail bed. The condition is mainly caused by various fungal species, including dermatophytes, yeasts and molds. Treatment of onychomycosis is complex, with antifungal drugs playing a key role. This research aimed to evaluate the effectiveness of various antifungal treatments, both topical and systemic, in managing onychomycosis. This research used a descriptive qualitative approach, using secondary data through documentation analysis. Data were triangulated to increase reliability and validity. The findings showed that the effectiveness of antifungal treatment varied depending on the type of drug, duration of treatment, and patient compliance. Systemic antifungals, such as terbinafine and itraconazole, showed higher cure rates compared to topical treatments such as ciclopirox and amorolfine. However, all treatments had high relapse rates, underscoring the need for continuous monitoring and customized therapy. The implications of this research demonstrate the importance of personalized treatment plans and the development of strategies to prevent relapse, which remains a significant challenge in the management of onychomycosis. [ABSTRACT FROM AUTHOR]

Cordyceps militaris, a medicinal fungus, has gained considerable attention owing to its potential health benefits, notably the production of bioactive compounds such as cordycepin. Cordycepin possesses significant antifungal, antibacterial, and antiviral properties. The present study focused on optimizing the fermentation conditions for C. militaris to boost the production of mycelia and cordycepin, alongside investigating its antifungal properties using in silico and in vitro approaches. The optimal conditions, yielding the highest cordycepin and mycelial biomass, were a temperature of 20°C and a pH range of 4–6, with glucose and sucrose as carbon sources and yeast extract and casein hydrolysate as nitrogen sources. Under these conditions, cordycepin production peaked at low pH (600–1000 mg/L) and with carbon and maltose (400–500 mg/L). The low temperature favored cordycepin production (400 mg/L), whereas casein hydrolysate as a nitrogen source boosted cordycepin yield (600 mg/L). The docking analysis indicated that cordycepin had the highest binding affinity for the tubulin beta chain 2 (−10.4 kcal/mol) compared to the fungicide tebuconazole (−7.9 kcal/mol for both targets). The in silico results were corroborated by in vitro studies, where the mycelial extract of C. militaris inhibited approximately 75% of fungal growth at a concentration of 6000 ppm. These findings suggest that optimizing fermentation conditions significantly enhances cordycepin production, and cordycepin shows antifungal solid activity, making it a promising agent for biocontrol in agriculture. [ABSTRACT FROM AUTHOR]

This study aimed to improve the thermal stability of 42 kDa chitinase from T. asperellum SH16 produced in N. benthamiana through site-directed mutagenesis for application in post-harvest fruit and vegetable preservation. In this work, thermostable mutants were predicted using bioinformatics tools, gene expression was analyzed by SDS-PAGE and Western blot, chitinase activity was determined spectrophotometrically, and the antifungal activity of chitinase was evaluated through inhibition of mycelial growth. The results showed that six selected mutants were successfully expressed in N. benthamiana and had in vitro antifungal activity against Colletotrichum siamense AD1.2. Among them, mutant I168L has a higher optimal temperature, thermal stability, and enzymatic activity than native chitinase and other mutants. Further analysis showed that, after 6 h of treatment at 40 °C, the relative activity of I168L remained about 50%, but that of native chitinase was only more than 15%. Besides, the I168L mutant could maintain a relative activity of about 78% and 50% after 30 min at 60ºC and 70ºC, while the native chitinase had only 38% and 12%, respectively. The Km and Vmax of the I168L mutant were both lower than those of native chitinase: 6.99 mg/mL and 254 units/mg vs. 11.24 mg/mL and 512 units/mg, respectively. Mutant I168L showed the ability to prevent and treat chili anthracnose disease caused by C. siamense CH26.1, which was many times stronger than the native chitinase at 35ºC. This finding suggests that the thermostable chitinase, I168L, has potential for applications in post-harvest fruit and vegetable preservation.Key message: This study screened insilico a mutant chitinase named I168L, derived from Trichoderma asperellum. The I168L exhibited significantly greater thermostability and Collectotrichum antifungal activity than the native chitinase. [ABSTRACT FROM AUTHOR]

Green synthesis of nanomaterials harnesses naturally occurring materials, including plant extracts, to offer environmentally friendly alternatives to conventional biomedicine, agriculture, and other field applications. This study explores the green route to Fe2O3 and cerium-doped Fe2O3 (Ce-doped Fe2O3) nanoparticles synthesized for the first time using the leaf extract of Platycladus orientalis. The synthesized nanoparticles were characterized for their structural, morphological, chemical, and optical properties. The hematite phase of Fe2O3 nanoparticles with spherical morphology was obtained. The introduction of Ce as a dopant into Fe2O3 increased the lattice strain of Ce-doped Fe2O3 nanoparticles (0.51%) compared to pristine Fe2O3 (0.46%) even though the size of both nanomaterials was similar. Compared to pristine Fe2O3 nanoparticles, Ce-doped Fe2O3 nanoparticles also demonstrated enhanced antimicrobial and antifungal activities against Escherichia coli, Enterococcus faecalis, Listeria monocytogenes, Penicillium chrysogenum, Aspergillus niger, and Mucor mucedo. The green-synthesized Ce-doped Fe2O3 nanoparticles possess potential for application in biomedical and environmental fields based on their relevance to human health and food safety, diversity in microbial characteristics, and potential for resistance to conventional treatments. [ABSTRACT FROM AUTHOR]

Purpose: To evaluate the efficacy and safety of oral ibrexafungerp (HS-10366) versus placebo in Chinese patients with vulvovaginal candidiasis (VVC). Methods: A double-blind, placebo-controlled, randomized, multicenter phase III study was conducted in symptomatic VVC patients. Patients received (2:1) twice-daily oral ibrexafungerp 300 mg or matching placebo for 1 day. The primary endpoint was clinical cure (vulvovaginal signs and symptoms [VSS] score = 0) at test-of-cure (TOC) on day 11 ± 3. The secondary endpoints included mycological eradication, overall response, and clinical improvement (VSS score ≤ 1) at TOC, and vulvovaginal symptom resolution at follow-up on day 25 ± 4. Results: In total, 360 patients were included in the modified intention-to-treat set (defined as positive Candida cultured and receiving at least one study drug; 239 for ibrexafungerp, 121 for placebo). Compared with placebo, patients receiving ibrexafungerp had a significantly higher proportion of clinical cure (51.0% vs. 25.6%), mycological eradication (55.6% vs. 18.2%), overall response (33.9%, vs. 8.3%) at TOC and complete symptom resolution (74.5% vs. 39.7%, all P < 0.001) at follow-up. Subgroup analysis of clinical cure indicated that patients with C. albicans could benefit from ibrexafungerp over placebo. A similar benefit trend was also observed in those with non-albicans Candida by post-hoc analysis. Further analyses revealed similar efficacy of ibrexafungerp between patients with fluconazole non-susceptible C. albicans and fluconazole susceptible C. albicans regarding clinical cure and mycological eradication. Ibrexafungerp was generally well tolerated. Adverse events were primarily gastrointestinal and were mainly mild in severity. Conclusions: As a first-in-class antifungal agent, ibrexafungerp demonstrated promising efficacy and favorable safety for VVC treatment in Chinese patients. Chinadrugtrials.org.cn registry number: CTR20220918. [ABSTRACT FROM AUTHOR]

Candida albicans (C. albicans) adhering to denture-based resins (DBRs) is a known cause of denture stomatitis. A new approach to prevent denture stomatitis is to include antimicrobial substances within DBRs. Here, we examined the mechanical performance and antifungal properties of DBRs containing benzyldimethyldodecyl ammonium chloride (C12BDMA-Cl) as an antimicrobial compound. C12BDMA-Cl is a quaternary ammonium compound, and its antifungal properties have never been investigated when combined with dental acrylic resin. Therefore, we modified a commercially available heat-polymerized acrylic DBR to contain 3 and 5 wt.% of C12BDMA-Cl. Unmodified DBR was used as a control group. Specimens were prepared using the conventional heat processing method. The specimen's flexural strength, elastic modulus, microhardness, and surface roughness were evaluated. C. albicans biofilm was grown on the specimens and assessed via colony-forming units (CFUs) and scanning electron microscopy (SEM). In silico molecular docking was applied to predict the potential C12BDMA-Cl inhibition activity as an antifungal drug. The 3% C12BDMA-Cl DBR demonstrated antifungal activities without a deterioration effect on the mechanical performance. SEM images indicated fewer colonies in DBR containing C12BDMA-Cl, which can be a potential approach to managing denture stomatitis. In conclusion, C12BDMA-Cl is a promising antifungal agent for preventing and treating denture stomatitis. [ABSTRACT FROM AUTHOR]

Titanium and its alloys are commonly used in dentistry for implants due to their strength, lightweight nature, durability, corrosion resistance, and biocompatibility. These implants can osseointegrate after surface treatments such as SLA, plasma-spray, and nanotubes, providing a stable foundation for prostheses. However, Candida albicans, an opportunistic fungal pathogen, can threaten the success of titanium dental implants, causing oral infections in vulnerable individuals. A dual novel silane blend of 3-acryloxypropyltrimethoxysilane (ACPS) and bis-1,2-(triethoxysilyl)ethane (BTSE) has been shown to improve the shear bond strength in resin cement bonds with titanium and ceramics. This study evaluated the effects of Candida albicans colonization on blended silane-coated SLA-Ti surfaces compared to non-coated SLA-Ti (positive control) and flat titanium (negative control). Candida albicans biofilms were cultured on all surfaces, and it was found that silane-coated SLA-Ti had significantly lower CFU counts than non-coated SLA-Ti. However, no significant differences were observed in the RT-PCR results. In conclusion, a combination of 1.0 vol% ACPS and 0.3 vol% BTSE shows promise as a silane coupling agent with potential antifungal properties for inhibiting Candida albicans proliferation. [ABSTRACT FROM AUTHOR]

Nanocomposites based on inorganic/graphene nanoparticles have gained remarkable interest as a novel class of hybrid materials. Scientific community attention towards these substances has been increasing, because of their peculiar characteristics in combining anticipated features of building constructs for specified applications. Graphene oxide (GO) and metal nanoparticles (MNPs) are using separately in different applications due to their specific limitations. Researchers continue to explore ways to overcome these challenges and create functional nanomaterials for various fields by combining unique advantages of GO and MNPs. Here, we used a facile one-step method for the synthesis of reduced graphene oxide–palladium composite (RGO/Pd). Environmental-friendly biofabricated palladium nanoparticles adhered to Polyscias scutellaria (PS) leaf extract mediated RGO/Pd have been presented in the current investigation. The biofabricated nanohybrid (RGO/Pd) was analysed utilizing several microscopic and spectroscopic techniques. Further, we have also examined the catalytic function for the reduction of 2-nitroaniline (2-NA) in detail. Primarily, we observed that the synthesized nanocomposite can catalyse simultaneous reduction of 2-NA. Furthermore, an added advantage of the as prepared RGO/Pd nanocomposite is its antimicrobial and antifungal ability. Further, we exhibited that the mesenchymal stem cells of adult goat were viable in the presence of RGO/Pd of 0.1 mg/mL concentration and their properties of stem cells were retained. The outcomes displayed that the nanocomposites exhibited outstanding functioning in the killing of dangerous microbial and fungal pathogens. All these results strengthen the RGO/Pd composite applicability in future for potential therapy in bone tissue engineering applications. [ABSTRACT FROM AUTHOR]

The aim of the study was to evaluate the antifungal activity of different drugs and preparations. The current findings demonstrated that the drugs and medicinal plant extracts that were examined for antifungal properties against various species. These species demonstrated antifungal activity almost on par with the commercial fungicide used as a positive control, even at low dosages. For further of the bioactive substances causing the noted antifungal activity, more research is required. Natural fungicides generated from plants could provide new active molecules, especially those with antifungal properties. The high percentage of active extracts in the species under investigation, which were chosen based on known ethnobotanical data, supports the applicability of this method for choosing plant species when looking for a certain activity. [ABSTRACT FROM AUTHOR]

The study's objective was to assess the antifungal efficacy of various medications and formulations. Medicinal plant extracts and medications that were tested for antifungal qualities against different species were shown to have antifungal capabilities. Even at modest dosages, these species showed antifungal activity that was nearly identical to that of the commercial fungicide used as a positive control. More research is needed to determine which bioactive compounds are responsible for the observed antifungal action. Plant-based natural fungicides may yield novel active compounds, particularly those with antifungal qualities. The relevance of this strategy for selecting plant species when seeking a certain activity is supported by the high percentage of active extracts in the species under inquiry, which were selected based on established ethnobotanical data. [ABSTRACT FROM AUTHOR]

A lot of people use emulsion gels because they are easier to use than creams and ointments and because they release drugs faster and more thoroughly. The study's goals were to develop and clarify an antifungal emulgel that can be put on the skin. In the Miconazole Emulgel method, the gelling agent, carbopol 934 is used with great accuracy. For the water phase, Tween 20 is an emulsifier. Propylene glycol is a co-surfactant. Methyl and propyl paraben are preservatives. And liquid paraffin is the oil in the oil phase mixture. Triethanolamine is used to bring the pH of the emulgel to between 6 and 6.4. Miconazole, which is like cholesterol for fungi, stops fungi from growing by decreasing ergosterol production, which makes membranes more mobile. There were no signs of phase separation in the improved F6 formulation. The improved mix had better drug content, spreadability, extrudability and viscosity. A 14-17 mm zone of blockage showed that the antifungal worked against Candida albicans and the drug released in vitro was 97.45%. All of the items had a pH level between 6 and 6.4, which means they were safe for the skin. The results show that the topical Miconazole Emulgel with Carbopol 934 is very smooth, easy to apply and calming. [ABSTRACT FROM AUTHOR]

Traditional herbal medicines have been used for millennia and they are currently experiencing a surge in popularity among both medical experts and those who are looking for therapy. One can find a wide variety of phytopharmaceuticals that are derived from plants in them. The most recent clinical trial demonstrated that the methanolic extract of Samadera indica was risk-free and would not cause any harm to any individual. Due to the fact that they have favorable physical qualities, the components that were created were suitable for use on the skin. When it came to eliminating bacteria and fungi in the laboratory, the gel that was produced from the methanolic extract of Samadera indica proved to be far more successful than the product that is commonly accessible. Further evidence that the substance was both chemically and physically stable was provided by the fact that the formulae that were developed demonstrated short-term stability. [ABSTRACT FROM AUTHOR]

Ngari is a non-salted fermented fish of Manipur and was made by the indigenous people of Manipur North east India. Traditional Knowledge (TK) possessed by different communities is often closely linked to their way of life. The present study tried to document the control of microbial contaminants isolated from Ngari (A fermented fish product) by natural plants products. Two fungi were isolated from the "Ngari" stored at room temperature (150C-200C) for 45 day. Antimicrobial activity of plant extract was done by agar well diffusion method. Of 8 plants extracts, cinnamon ethanolic extract showed antifungal activity with zone of inhibition 55mm and 15mm against green coloured and black coloured fungal isolates, respectively. Mango ethanolic extract showed antifungal activity against black coloured fungal isolate with zone of inhibition 10mm. Mulberry, neen, guava, curry and stem of ginger and termaric extracts did not show any activity against the both fungal isolates. Antibiotic susceptibility pattern of microbial isolates was done by agar disc diffusion method. Ketaconazole showed the best activity against the both fungal i.e (green and black) with zone of inhibition (18mm) followed by Clotrimazole (CC) (12 and 20mm) and Itraconazole (IT) (12 and 17mm), respectively. Nystatin (NS) showed the activity only against the black fungal 13mm. Both fungal isolates were resistant to Amphotericin and Fluconazole. The Cinnamon ethanolic extract exhibited the MIC of 10% w/v against both fungal isolates. The photochemical analysis of cinnamon ethanolic extract was done and showed the presence of alkaloid, tannins and phenols and absence of flavonoid and saponins. It may be suggested from the findings that cinnamon ethanolic extract can be used as a potential source of natural antimicrobial compound to be used as food preservative. Further research is needed for the to identify fungal isolates from Ngari and also to isolate, purify and identify the active antifungal from the cinnamon ethanolic extract. [ABSTRACT FROM AUTHOR]