Marine Bacillus haynesii chitinase: Purification, characterization and antifungal potential for sustainable chitin bioconversion.

The development of chitinase tailored for the bioconversion of chitin to chitin oligosaccharides has attracted significant attention due to its potential to alleviate environmental pollution associated with chemical conversion processes. In this present investigation, we purified extracellular chitinase derived from marine Bacillus haynesii to homogeneity and subsequently characterized it. The molecular weight of BhChi was approximately 35 kDa. BhChi displayed its peak catalytic activity at pH 6.0, with an optimal temperature of 37 °C. It exhibited stability across a pH range of 6.0-9.0. In addition, BhChi showed activation in the presence of Mn2+ with the improved activity of 105 U mL-1. Ca2+ and Fe2+ metal ions did not have any significant impact on enzyme activity. Under the optimized enzymatic conditions, there was a notable enhancement in catalytic activity on colloidal chitin with Km of 0.01 mg mL-1 and Vmax of 5.75 mmol min-1. Kcat and catalytic efficiency were measured at 1.91 s-1 and 191 mL mg-1 s-1, respectively. The product profiling of BhChi using thin layer chromatography and Mass spectrometric techniques hinted an exochitinase mode of action with chitobiose and N-Acetyl glucosamine as the products. This study represents the first report on an exochitinase from Bacillus haynesii. Furthermore, the chitinase showcased promising antifungal properties against key pathogens, Fusarium oxysporum and Penicillium chrysogenum, reinforcing its potential as a potent biocontrol agent.

Targeted discovery of unusual diterpenoids with anti-fungal activity from the root of Euphorbia lathyris.

Lathyrisone A (1), a diterpene with an undescribed tricyclic 6/6/6 fused carbon skeleton, along with spirolathyrisins B-D (3-5), three diterpenes with a rare [4.5.0] spirocyclic carbon skeleton, and one known compound (2) were isolated from the roots of Euphorbia lathyris. Their chemical structures were characterized by extensive spectroscopic analysis, X-ray crystallography, ECD and quantum chemistry calculation. A plausible biosynthetic pathway for compounds 1-5 was proposed, which suggested it is a competitive pathway for ingenol biosynthesis in the plant. The anti-fungal activities of these compounds were tested, especially, compound 2 showed stronger anti-fungal activities against Fusarium oxysporum and Alternaria alternata than the positive control fungicide thiophanate-methyl. The preliminary structure-activity relationship of compounds 1-5 was also discussed. These results not only expanded the chemical diversities of E. lathyris, but also provided a lead compound for the control of plant pathogens.

Enhanced resistance to heat and fungal infection in transgenic Trichoderma via over-expressing the HSP70 gene.

Heat stress is one of the major abiotic stresses affecting the growth, sporulation, colonization and survival of Trichoderma viride. This study aimed to gain a better insight into the underlying mechanism governing the heat stress response of T. viride Tv-1511. We analysed the transcriptomic changes of Tv-1511 under normal and heat stress conditions using RNA sequencing. We observed that Tv-1511 regulates the biosynthesis of secondary metabolites through a complex network of signalling pathways. Additionally, it significantly activates the anti-oxidant defence system, heat shock proteins and stress-response-related transcription factors in response to heat stress. TvHSP70 was identified as a key gene, and transgenic Tv-1511 overexpressing TvHSP70 (TvHSP70-OE) was generated. We conducted an integrated morphological, physiological and molecular analyses of the TvHSP70-OE and wild-type strains. We observed that TvHSP70 over-expression significantly triggered the growth, anti-oxidant capacity, anti-fungal activity and growth-promoting ability of Tv-1511. Regarding anti-oxidant capacity, TvHSP70 primarily up-regulated genes involved in enzymatic and non-enzymatic anti-oxidant systems. In terms of anti-fungal activity, TvHSP70 primarily activated genes involved in the synthesis of enediyne, anti-fungal and aminoglycoside antibiotics. This study provides a comparative analysis of the functional significance and molecular mechanisms of HSP70 in Trichoderma. These findings provide a valuable foundation for further analyses.

Design of a delivery vehicle chitosan-based self-assembling: controlled release, high hydrophobicity, and safe treatment of plant fungal diseases.

BACKGROUND: Traditional pesticides are poorly water-soluble and suffer from low bioavailability. N-succinyl chitosan (NSCS) is a water-soluble chitosan derivative, has been recently used to encapsulate hydrophobic drugs to improve their bioavailability. However, it remains challenging to synthesize pesticides of a wide variety of water-soluble drugs and to scale up the production in a continuous manner. RESULTS: A synthetic method for preparing water-soluble nanopesticides with a polymer carrier was applied. The bioactive molecule BTL-11 was loaded into hollow NSCS to promote drug delivery, improve solubility and anti-fungal activity. The synthesized nanopesticides had well controlled sizes of 606 nm and the encapsulation rate was 80%. The release kinetics, drug toxicity and drug activity were further evaluated. The inhibitory activity of nanopesticides against Rhizoctonia solani (R. solani) was tested in vivo and in vitro. In vivo against R. solani trials revealed that BTL-11 has excellent control efficiency for cultivated rice leaf and sheath was 79.6 and 76.5%, respectively. By contrast, for BTL-11@NSCS NPs, the anti-fungal ability was strongly released and afforded significant control efficiencies of 85.9 and 81.1%. Those effects were significantly better than that of the agricultural fungicide azoxystrobin (51.5 and 66.5%). The proposed mechanism was validated by successfully predicting the synthesis outcomes. CONCLUSIONS: This study demonstrates that NSCS is a promising biocompatible carrier, which can enhance the efficacy of pesticides, synergistically improve plant disease resistance, protect crop growth, and can be used for the delivery of more insoluble pesticides.

Plant root associated chitinases: structures and functions.

Chitinases degrade chitin, a linear homopolymer of ß-1,4-linked N-acetyl-D-glucosamine (GlcNAc) residues found in the cell walls of fungi and the exoskeletons of arthropods. They are secreted by the roots into the rhizosphere, a complex and dynamic environment where intense nutrient exchange occurs between plants and microbes. Here we modeled, expressed, purified, and characterized Zea mays and Oryza sativa root chitinases, and the chitinase of a symbiotic bacterium, Chitinophaga oryzae 1303 for their activities with chitin, di-, tri-, and tetra-saccharides and Aspergillus niger, with the goal of determining their role(s) in the rhizosphere and better understanding the molecular mechanisms underlying plant-microbe interactions. We show that Zea mays basic endochitinase (ZmChi19A) and Oryza sativa chitinase (OsChi19A) are from the GH19 chitinase family. The Chitinophaga oryzae 1303 chitinase (CspCh18A) belongs to the GH18 family. The three enzymes have similar apparent K M values of (20-40 µM) for the substrate 4-MU-GlcNAc3. They vary in their pH and temperature optima with OsChi19A activity optimal between pH 5-7 and 30-40°C while ZmChi19A and CspCh18A activities were optimal at pH 7-9 and 50-60°C. Modeling and site-directed mutation of ZmChi19A identified the catalytic cleft and the active residues E147 and E169 strategically positioned at ~8.6Å from each other in the folded protein. Cleavage of 4-MU-GlcNAc3 was unaffected by the absence of the CBD but diminished in the absence of the flexible C-terminal domain. However, unlike for the soluble substrate, the CBD and the newly identified flexible C-terminal domain were vital for inhibiting Aspergillus niger growth. The results are consistent with the involvement of the plant chitinases in defense against pathogens like fungi that have chitin exoskeletons. In summary, we have characterized the functional features and structural domains necessary for the activity of two plant root chitinases that are believed to be involved in plant defense and a bacterial chitinase that, along with the plant chitinases, may participate in nutrient recycling in the rhizosphere.

Semisynthesis, anti-oomycete and anti-fungal activities of ursolic acid ester derivatives.

Using ursolic acid (UA) as the lead compound, thirteen UA ester derivatives (3 and 7a-l) were synthesized by modifying their C-3 and C-28 positions, respectively, and their structures were well characterized by 1H NMR, 13C NMR, HRMS and melting points. Furthermore, we evaluated the anti-oomycete and anti-fungal activities of these compounds against Phytophthora capsici and Fusarium graminearum in vitro. The results showed that compound 7h exhibited prominent anti-oomycete and anti-fungal activities, and the median effective concentration (EC50) values of 7h against P. capsici and F. graminearum were 70.49 and 113.21 mg/L, respectively. This study suggested that the anti-oomycete and anti-fungal activities of esters synthesized by introducing acyloxy group at C-3 position of UA was more conspicuous than that of esters synthesized by introducing benzyloxy group at C-28 position. This result will pave the way for further modification of UA to develop potential new fungicides.

Three new diterpenoids isolated from Euphorbia nematocypha Hand.-Mazz and their anti-fungal activity.

Three new diterpenoids, named nematocynine A-C (1-3), together with twelve known compounds (4-15) were isolated from the aerial part of Euphorbia nematocypha Hand.-Mazz (Hereinafter referred to E. nematocypha). Their structures were elucidated by detailed spectroscopic analysis and comparison with literature data. In addition, all the compounds were tested for their anti-candida albicans activities used alone or in combination with fluconazole against sensitive strain and resistant strain in vitro. Wherein only compound 11 shows weak activity against candida albicans resistant strain (MIC50 = 128.15 µg/mL) when used alone. Compounds 1, 4, 7, 8, 9, 10, 12, 13 and 15 in combination with fluconazole showed potent anti-fungal activities (MIC50 = 15 ± 5 µg/mL, FICI = 0.05 ± 0.04) against the Candida albicans resistant strain SC5314-FR. The synergistic effects were weaker against the Candida albicans resistant strain SC5314-FR when the compounds 2, 3, 5 and 14 were combined with fluconazole (FICI = 0.16 ± 0.06).

Biogenic synthesis of dopamine/carboxymethyl cellulose/TiO2 nanoparticles using Psidium guajava leaf extract with enhanced antimicrobial and anticancer activities.

The green synthesis of metal oxide nanoparticles (NPs) has garnered considerable attention from researchers due to its utilization of eco-friendly solvents during synthesis and cost-effective approaches. This study focuses on the synthesis of titanium oxide (TiO2) and dopamine (DA) carboxymethyl cellulose (CMC)-doped TiO2 (DA/CMC/TiO2) NP using Psidium guajava leaf extract, while also investigating the structural, optical, and morphological and biocidal potential of the prepared NPs. Significantly larger zones of inhibition were observed for DA/CMC/TiO2 NPs compared to TiO2 against various pathogens. Moreover, the MTT assay was carried out to evaluate the anticancer activity of the prepared samples against MG-63 cells, and the results revealed that DA/CMC/TiO2 NPs exhibited significantly higher level of anticancer activity compared to TiO2. The experimental results demonstrated that DA/CMC/TiO2 NPs exhibited enhanced anticancer activity in a dose-dependent manner when compared to TiO2 NPs.

Electrospun Fibers of Biocompatible and Biodegradable Polyesters, Poly(Ethylene Oxide) and Beeswax with Anti-Bacterial and Anti-Fungal Activities.

Fibrous materials composed of core-sheath fibers from poly(ethylene oxide) (PEO), beeswax (BW) and 5-nitro-8-hydroxyquinoline (NQ) were prepared via the self-organization of PEO and BW during the single-spinneret electrospinning of a homogeneous blend solution of the partners. Additionally, the application of the same approach enabled the preparation of fibrous materials composed of core-double sheath fibers from PEO, poly(L-lactide) (PLA) and NQ or 5-chloro-7-iodo-8-hydroxyquinoline (CQ), as well as from PEO, poly(ε-caprolactone) (PCL) and NQ. The consecutive selective extraction of BW and of the polyester with hexane and tetrahydrofuran, respectively, evidenced that core-double sheath fibers from PEO/polyester/BW/drug consisted of a PEO core, a polyester inner sheath and a BW outer sheath. In order to evaluate the possibility of the application of fibrous materials from PEO/BW/NQ, PEO/PLA/BW/NQ, PEO/PCL/BW/NQ and PEO/PLA/BW/CQ for plant protection, microbiological studies were performed using both phytopathogenic microorganisms (Pseudomonas corrugata, Fusarium graminearum and Fusarium avenaceum) and beneficial microorganisms (Pseudomonas chlororaphis, Bacillus amyloliquefaciens and Trichoderma asperellum). It was found that the fibrous materials had anti-bacterial and anti-fungal activity against both phytopathogenic and beneficial microorganisms. This is the first report on the activity of fibrous materials loaded with 8-hydroxyquinoline derivatives not only against phytopathogenic but also against beneficial microorganisms that are of importance in agriculture.

Stone fruit phenolic and triterpenoid compounds modulate gene expression of Monilinia spp. in culture media.

Phenolic and triterpenoid compounds are essential components in stone fruit skin and flesh tissues. They are thought to possess general antimicrobial activity. However, regarding brown rot disease, investigations were only confined to a limited number of phenolics, especially chlorogenic acid. The activity of triterpenoids against Monilinia spp., as an essential part of the peach cuticular wax, has not been studied before. In this work, the anti-fungal effect of some phenolics, triterpenoids, and fruit surface compound (FSC) extracts of peach fruit at two developmental stages were investigated on Monilinia fructicola and Monilinia laxa characteristics during in vitro growth. A new procedure for assaying anti-fungal activity of triterpenoids, which are notoriously difficult to assess in vitro because of their hydrophobicity, has been developed. Measurements of colony diameter, sporulation, and germination of second-generation conidia were recorded. Furthermore, the expression of twelve genes of M. fructicola associated with germination and/or appressorium formation and virulence-related genes was studied relative to the presence of the compounds. The study revealed that certain phenolics and triterpenoids showed modest anti-fungal activity while dramatically modulating gene expression in mycelium of M. fructicola on culture medium. MfRGAE1 gene was overexpressed by chlorogenic and ferulic acids and MfCUT1 by betulinic acid, at 4- and 7- days of mycelium incubation. The stage II FSC extract, corresponding to the period when the fruit is resistant to Monilinia spp., considerably up-regulated the MfLAE1 gene. These findings effectively contribute to the knowledge of biochemical compounds effects on fungi on in vitro conditions.

Synthesis, Anti-Oomycete and Anti-fungal Activities of Novel Cinchona Alkaloid Derivatives Containing Sulfonate Moiety.

Using cinchona alkaloid as the lead compound, twenty-four cinchona alkaloid sulfonate derivatives (1 a-l, 2 a-c, 3 a-c, 4 a-c, and 5 a-c) were designed and prepared by modifying their C9 position, and structurally confirmed by 1 H-NMR, 13 C-NMR, HR-MS and melting points. Moreover, the stereochemical configurations of compounds 1 f and 1 l were unambiguously confirmed by single-crystal X-ray diffraction. Furthermore, we determined the anti-oomycete and anti-fungal activities of these target compounds against Phytophthora capsici and Fusarium graminearum in vitro. The results showed that two compounds 4 b and 4 c exhibited prominent anti-oomycete activity, and the median effective concentration (EC50 ) values of 4 b and 4 c against P. capsici were 22.55 and 16.32 mg/L, respectively. This study suggested that when the C9 position of cinchona alkaloid sulfonate derivatives is in the S configuration and the 6'-position methoxy group is not present, the anti-oomycete activity is superior. In addition, five compounds 1 e, 1 f, 1 k, 3 c and 4 c displayed significant anti-fungal activity, with EC50 values of 43.64, 45.07, 80.18, 48.58 and 41.88 mg/L against F. graminearum, respectively. This result indicates that only when a specific substituent is introduced into the structural framework of the target compound, the corresponding compound exhibits significant inhibitory activity against fungi.

Silver nanoparticles green synthesized with leaf extract of disease-resistant amaranthus genotypes effectively suppress leaf blight (Rhizoctonia solani Kühn) disease in a susceptible red amaranthus cultivar.

Silver nanoparticles (AgNPs) were green synthesized using leaf extract of the leaf blight disease (Rhizoctonia solani) susceptible red amaranthus (Amaranthus tricolor L.) and the disease-resistant green (A. dubius) and the wild amaranthus (A. viridis) genotypes, physically characterized, and assessed for their anti-fungal effects against R. solani. The green synthesized nanostructures showed an absorption maximum typical of silver nanoparticles in spectroscopy, and face-centered cubic structures in X-ray diffraction. Field Emission Scanning Electron Microscopic analysis and High-Resolution Transmission Electron Microscopy revealed the size range to be 35-45 nm for all the samples. In vitro mycelial growth inhibition of the pathogen occurred with 500 and 750 ppm concentrations of the nanoparticles in a poisoned-food assay. Further, detached leaves of red amaranthus variety were sprayed with the nanoparticles, and then challenged with the pathogen. There was significant difference in lesion development on leaves sprayed with Ad-AgNPs and Av-AgNPs compared to those treated with At-AgNPs. In the in vivo assay, challenging with the pathogen after spraying the foliage of the leaf blight susceptible red amaranthus variety with Ad-AgNPs at 750 ppm concentration recorded the lowest disease index (7.40) followed by that received Av-AgNPs spray at the same concentration (17.69), five days after inoculation. At-AgNPs treated plants had a disease index of 49.38. Our findings suggest that application of AgNPs green synthesized with leaf extract of disease-resistant genotypes of amaranthus effectively suppressed leaf blight disease incidence in a susceptible amaranthus genotype. To our knowledge, this is the first report on the improved plant pathogen-suppressive activity of any metal nanoparticle when biogenically synthesized using extracts from a disease-resistant plant genotype.

New Guaiane-Type Sesquiterpenoids Biscogniauxiaols A-G with Anti-Fungal and Anti-Inflammatory Activities from the Endophytic Fungus Biscogniauxia Petrensis.

Seven undescribed guaiane-type sesquiterpenoids named biscogniauxiaols A-G (1-7) were isolated from the endophytic fungus Biscogniauxia petrensis on Dendrobium orchids. Their structures were determined by extensive spectroscopic analyses, electronic circular dichroism (EC) and specific rotation (SR) calculations. Compound 1 represented a new family of guaiane-type sesquiterpenoids featuring an unprecedented [5/6/6/7] tetracyclic system. A plausible biosynthetic pathway for compounds 1-7 was proposed. The anti-fungal, anti-inflammatory and multidrug resistance reversal activities of the isolates were evaluated. Compounds 1, 2 and 7 exhibited potent inhibitory activities against Candida albicans with MIC values ranging from 1.60 to 6.30 µM, and suppressed nitric oxide (NO) production with IC50 ranging from 4.60 to 20.00 µM. Additionally, all compounds (100 µg/mL) enhanced the cytotoxicity of cisplatin in cisplatin-resistant non-small cell lung cancer cells (A549/DDP). This study opened up a new source for obtaining bioactive guaiane-type sesquiterpenoids and compounds 1, 2, and 7 were promising for further optimization as multifunctional inhibitors for anti-fungal (C. albicans) and anti-inflammatory purposes.

Discovery of Barakacin and Its Derivatives as Novel Antiviral and Fungicidal Agents.

Pesticides are essential for the development of agriculture. It is urgent to develop green, safe and efficient pesticides. Bisindole alkaloids have unique and concise structures and broad biological activities, which make them an important leading skeleton in the creation of new pesticides. In this work, we synthesized bisindole alkaloid barakacin in a simple seven-step process, and simultaneously designed and synthesized a series of its derivatives. Biological activity research indicated that most of these compounds displayed good antiviral activities against tobacco mosaic virus (TMV). Among them, compound 14b exerted a superior inhibitory effect in comparison to commercially available antiviral agent ribavirin, and could be expected to become a novel antiviral candidate. Molecular biology experiments and molecular docking research found that the potential target of compound 14b was TMV coat protein (CP). These compounds also showed broad-spectrum anti-fungal activities against seven kinds of plant fungi.

In silico study of novel marine alkaloid jolynamine and other marine compounds via molecular docking, MM-GBSA binding energy prediction, ADMET evaluation, and molecular dynamics simulation.

In this research article bacterial (Escherichia coli and Pseudomonas aeruginosa) and fungal (Aspergillus niger and Candida albicans) enzymes are used for molecular docking of novel marine alkaloid jolynamine (10) and six marine natural compounds. Till date, no computational studies have been reported. In addition, MM/GBSA analysis is conducted for estimation of binding free energies. Furthermore, ADMET physicochemical properties were explored to understand the drug likeness property of compounds. In silico results showed that jolynamine (10) has more negative predicted binding energy among natural products. The ADMET profile of all compounds accepted the Lipinski rule and jolynamine also showed negative MM/GBSA binding free energy. Moreover, MD simulation was subjected to check structure stability. The outcomes of MD simulation of jolynamine (10) showed structure stability over 50 ns simulation. This study will hopefully facilitate the finding of other natural products and expedite the drug discovery process to screen drug like chemical compounds.

Effect of H2O2 @CuONPs in the UV Light-Induced Removal of Organic Pollutant Congo Red Dye: Investigation into Mechanism with Additional Biomedical Study.

Hazardous dyes in industrial wastewater are an internationally recognized issue for community health. Nanoparticles synthesized through green protocols are a fascinating research field with numerous applications. The current study mainly aimed to investigate the degradation of Congo red (CR) dye under UV light in the presence of H2O2 and the photocatalytic activity of copper oxide nanoparticles (CuONPs). For CuONP formation, Citrus maxima extract contains a high number of phytochemical constituents. The size of CuONPs ranges between 25 and 90 nm. The photocatalytic activity of CuONPs with the addition of H2O2 was observed and analyzed under UV light to eliminate CR dye. The UV light caused the decomposition of H2O2, which produced ·OH radicals. The results revealed a significant increment in dye degradation during the presence of H2O2. The effect of concentration on the degradation of the CR dye was also studied. The degradation pathway of organic pollutants was reputable from the hydroxy radical medicated degradation of CR. Advanced Oxidation Treatment depends on the in situ production of reactive ·OH species and is presented as the most effective procedure for decontamination. The biological activity of CuONPs was evaluated against Escherichia coli Bacillus subtillis, Staphylococcus aureus, Shigella flexenari, Acinetobacter Klebsiella pneumonia, Salmonella typhi and Micrococcus luteus. The newly synthesised nanomaterials showed strong inhibition activity against Escherichia coli (45%), Bacillus subtilis (42%) and Acinetobacter species (25%). The activity of CuONPs was also investigated against different fungus species such as: Aspergillus flavus, A. niger, Candida glabrata, T. longifusus, M. Canis, C. glabrata and showed a good inhibition zone against Candida glabrata 75%, Aspergillus flavus 68%, T. longifusus 60%. The materials showed good activity against C. glaberata, A. flavus and T. longifusus. Furthermore, CuONPs were tested for antioxidant properties using 2, 2 diphenyl-1-picrylhydrazyl) (DPPH).

Enhanced piroctone olamine retention from shampoo for superior anti-dandruff efficacy.

BACKGROUND: Dandruff is a pervasive chronic condition which negatively impacts quality of life. Effective treatment requires efficient delivery of scalp benefit agents that control commensal scalp Malassezia levels. Delivery of benefit agents from shampoos requires balancing many technical parameters to achieve the desired outcome without sacrificing secondary parameters, such as cosmetic attributes. AIM: To develop formulation technologies that increase the shampoo delivery efficiency of the scalp benefit agent piroctone olamine (PO). Increased delivery should result in increased anti-dandruff efficacy. METHODS: Micellar Stability and Association parameters were quantified via dynamic surface tension and nuclear magnetic resonance (NMR) diffusion parameters, respectively. PO delivery has been assessed in vivo both on the scalp surface and follicular infindibula using extraction procedures and analytical analysis. Clinical anti-dandruff efficacy was assessed for an advanced delivery technology prototype in comparison to standard delivery technology. RESULTS: Shampoo prototypes have been developed that increase the delivery efficiency of PO. Both surfactant and polymer coacervate-based approaches have been developed. Decreased micellar stability results in weaker association between PO and micelles, resulting in more efficient PO retention on the scalp surface and delivery to the infundibula. Increased charge density of cationic polymers optimizes coacervation enabling improved PO delivery as well. Increased PO delivery has been shown clinically to result in higher anti-dandruff efficacy as measured by both visible flakes and underlying biomarkers. CONCLUSION: Increased efficiency PO delivery shampoos have been developed by optimization of both surfactant and coacervate parameters. The increased deposition efficiency results in significantly more products with significantly greater anti-dandruff efficacy.

CONTEXTE: Les pellicules sont une maladie chronique omniprésente qui a un impact négatif sur la qualité de vie. Un traitement efficace nécessite une administration efficace d'agents bénéfiques pour le cuir chevelu qui contrôlent les niveaux commensaux de Malassezia. L'administration d'agents bénéfiques à partir de shampooings nécessite d'équilibrer de nombreux paramètres techniques pour obtenir le résultat souhaité sans sacrifier des paramètres secondaires tels que les attributs cosmétiques. BUT: Développer des technologies de formulation qui augmentent l'efficacité d'administration du shampooing de l'agent bénéfique pour le cuir chevelu piroctone olamine (PO). Une livraison accrue devrait entraîner une efficacité antipelliculaire accrue. MÉTHODES: La stabilité micellaire et les paramètres d'association ont été quantifiés via les paramètres de tension superficielle dynamique et de diffusion RMN, respectivement. L'administration de PO a été évaluée in vivo à la fois sur la surface du cuir chevelu et sur l'indibula folliculaire à l'aide de procédures d'extraction et d'analyses analytiques. L'efficacité antipelliculaire clinique a été évaluée pour un prototype de technologie d'administration avancée par rapport à la technologie d'administration standard. RÉSULTATS: Des prototypes de shampooing ont été développés pour augmenter l'efficacité de livraison des PO. Des approches à base de tensioactifs et de coacervats polymères ont été développées. Une diminution de la stabilité micellaire entraîne une association plus faible entre le PO et les micelles, ce qui entraîne une rétention plus efficace du PO sur la surface du cuir chevelu et une livraison à l'infundibula. L'augmentation de la densité de charge des polymères cationiques optimise la coacervation, permettant également une meilleure administration de PO. Il a été démontré cliniquement que l'augmentation de l'administration de PO entraîne une efficacité antipelliculaire plus élevée, mesurée à la fois par les squames visibles et les biomarqueurs sous-jacents. CONCLUSION: Des shampooings à libération de PO à efficacité accrue ont été développés en optimisant à la fois les paramètres du tensioactif et du coacervat. L'efficacité de dépôt accrue se traduit par beaucoup plus de produits avec une efficacité antipelliculaire nettement supérieure.

Two new sesquiterpene derivatives, dendocarbin B and bisaborosaol C with antifungal activity from the endophytic fungus Nigrospora chinensis GGY-3.

Two novel sesquiterpene derivatives, dendocarbin B (1), bisaborosaol C (2), and nine known compounds (3-11), were isolated from Nigrospora chinensis GGY-3 derived from Ilex cornuta. The structures of new compounds were elucidated using HR-ESI-MS, 1 D and 2 D NMR spectra, X-ray diffraction analysis as well as ECD calculation and comparison. Compound 1 showed moderate antifungal activities against Rhizoctonia solani and Botrytis cinerea. Compounds 5 and 6 exhibited significant inhibitory activity against Phytophthora capsici, Magnaporthe oryzae and R. solani with EC50 values ranging from 13.91 to 29.49 µg/mL. Compounds 10 and 11 displayed moderate antibacterial effects on Bacillus subtilis and Xanthomonas oryzae pv. oryzae (Xoo), with MIC values of 16-64 µg/mL. Particularly, 11 presented strong antibacterial activity against Staphylococcus aureus with an MIC value of 4 µg/mL (2 µg/mL for streptomycin sulfate). In addition, compound 11 also possessed DPPH radical scavenging capability with an IC50 value of 14.80 µg/mL.

Terrien, a metabolite made by Aspergillus terreus, has activity against Cryptococcus neoformans.

Antimicrobial compounds, including antibiotics, have been a cornerstone of modern medicine being able to both treat infections and prevent infections in at-risk people, including those who are immune-compromised and those undergoing routine surgical procedures. Their intense use, including in people, animals, and plants, has led to an increase in the incidence of resistant bacteria and fungi, resulting in a desperate need for novel antimicrobial compounds with new mechanisms of action. Many antimicrobial compounds in current use originate from microbial sources, such as penicillin from the fungus Penicillium chrysogenum (renamed by some as P. rubens). Through a collaboration with Aotearoa New Zealand Crown Research Institute Manaaki Whenua-Landcare Research we have access to a collection of thousands of fungal cultures known as the International Collection of Microorganisms from Plants (ICMP). The ICMP contains both known and novel species which have not been extensively tested for their antimicrobial activity. Initial screening of ICMP isolates for activity against Escherichia coli and Staphylococcus aureus directed our interest towards ICMP 477, an isolate of the soil-inhabiting fungus, Aspergillus terreus. In our investigation of the secondary metabolites of A. terreus, through extraction, fractionation, and purification, we isolated nine known natural products. We evaluated the biological activity of selected compounds against various bacteria and fungi and discovered that terrein (1) has potent activity against the important human pathogen Cryptococcus neoformans.

Antifungal compounds of Chinese prickly ash against drug-resistant Candida albicans.

The leaf of Chinese prickly ash, a unique spice having typical pungent sensation, is a popular food in Southwest China with antipruritic, insecticidal and fungicidal functions, but its bioactive constituents of fungistatic capacity remain unknown. In present investigation, twenty-nine compounds were isolated from leaf of Chinese prickly ash, and their antifungal bioactivity against drug-resistant Candida albicans were evaluated in vitro and in vivo. As a result, three compounds 3, 10, 29 showed antifungal bioactivity by damage of the fungal biofilm, and they might recover sensitive of drug resistant C. albicans to Fluconazole. Then Chinese prickly ash leaf was proved to be a functional food against fungus for the first time in experiment.