Search Results (131)

The fungus Alternaria alternata, which causes tobacco brown spot disease, poses a serious threat to the tobacco industry. Beneficial microorganisms and their secondary metabolites have emerged as a promising green strategy for disease management. This study recovered 16 endophytic bacterial strains from Mentha haplocalyx Briq., a therapeutic herb. The study revealed that strain B5, with an inhibition rate of 82.76%, exhibited the highest antifungal activity against A. alternata. This strain exhibited broad-spectrum antifungal activity, with inhibition rates ranging from 66.34% to 87.23%. Phylogenetic analysis of 16S rDNA and gyrA gene sequences identified it as Bacillus velezensis (GenBank: PV168970 and PV173738). Further characterization revealed that strain B5 can secrete cell wall-degrading enzymes, produce IAA, and synthesize siderophores. The growth of mycelium in A. alternata was greatly reduced by both the ethyl acetate extract and the filtered liquid from the sterile fermentation, resulting in marked morphological abnormalities. Multiple antifungal active substances were identified through liquid LC-MS analysis. Greenhouse experiments demonstrated that the B5 fermentation broth effectively suppressed the occurrence of tobacco brown spot disease, achieving a relative control efficacy of 60.66%, comparable to that of 10% difenoconazole water dispersible granule (WDG). Additionally, strain B5 enhances plant disease resistance by activating the activities of key defense enzymes. B. velezensis B5 serves as a safe alternative to chemical fungicides and is highly effective at controlling tobacco brown spot disease. Full article

In response to the urgent need for innovative fungicides to ensure food security and safety, a series of twenty-three novel trifluoromethylpyridine compounds were designed and synthesized using a scaffold hopping strategy derived from dehydrozingerone. This approach involved converting the α, β-unsaturated ketone moiety into a pyridine ring. Bioassay results indicated that the majority of these compounds exhibited promising in vitro antifungal activity, particularly against Rhizoctonia solani and Colletotrichum musae. Notably, compound 17 showed the highest efficacy and broad-spectrum activity, with median effective concentrations (EC₅₀) ranging from 2.88 to 9.09 μg/mL. Phenoxytrifluoromethylpyridine derivatives, including compound 17, exhibited superior antifungal activity compared to benzyloxytrifluoromethylpyridine derivatives. In vivo tests revealed that both compounds 17 and 23 exhibited moderate control effects against C. musae. The degradation half-lives of compounds 17 and 23 in bananas were determined to be 176.9 h and 94.8 h, respectively, indicating the stability of their structures in the environment. Molecular docking studies indicated that compound 23 interacts with succinate dehydrogenase, offering valuable insights for the structural optimization of compound 23. Full article

Plant fungal diseases remain a major threat to global agricultural production, necessitating eco-friendly and sustainable strategies. Conventional chemical fungicides often lead to the development of resistant pathogen strains and cause environmental contamination. Therefore, the development of biocontrol agents is particularly important. In this study, we identified Burkholderia stagnalis YJ-2 from the rhizosphere soil of Woodsia ilvensis as a promising biocontrol strain using 16S rRNA and whole-genome sequencing. This strain demonstrated broad-spectrum antifungal activity against plant fungal pathogens, with its bioactive extracts maintaining high stability across a temperature range of 25–100 °C and pH range of 2–12. We used in vitro assays to further show that the metabolites of B. stagnalis YJ-2 disrupted the hyphal morphology of Valsa mali, resulting in swelling, reduced branching, and increased pigmentation. Fluorescence labeling confirmed that B. stagnalis YJ-2 stably colonized the roots and stems of tomato and wheat plants. Furthermore, various formulations of microbial agents based on B. stagnalis YJ-2 were evaluated for their efficacy against plant pathogens. The seed-coating formulation notably protected tomato seedlings from Alternaria solani infection without affecting germination (p > 0.1), while the wettable powder exhibited significant control effects on early blight in tomatoes, with the preventive treatment showing better efficacy than the therapeutic treatment. Additionally, the B. stagnalis YJ-2 bone glue agent showed a substantial inhibitory effect on apple tree canker. Whole-genome analysis of B. stagnalis YJ-2 revealed a 7,705,355 bp genome (67.68% GC content) with 6858 coding genes and 20 secondary metabolite clusters, including three clusters (YJ-2_GM002015-YJ-2_GM002048, YJ-2_GM0020090-YJ-2_GM002133, and YJ-2_GM06534-YJ-2_GM006569) that are related to the antifungal activity of YJ-2 and are homologous to the biosynthetic gene clusters of known secondary metabolites, such as icosalide, ornibactin, and sinapigladioside. We further knocked out core biosynthetic genes of two secondary metabolic gene clusters and found that only the YJ-2_GM006534-YJ-2_GM006569 gene cluster had a corresponding function in two potential antifungal gene clusters. In contrast to the wild-type strain YJ-2, only deletion of the YJ-2_GM006563 gene reduced the antifungal activity of B. stagnalis YJ-2 by 8.79%. These findings highlight the biocontrol potential of B. stagnalis YJ-2, supporting a theoretical foundation for its development as a biocontrol agent against plant fungal diseases and thereby promoting sustainable agricultural disease management. Full article

Background/Objectives: Difenoconazole (DFC) is a broad-spectrum fungicide. However, its application is limited due to poor aqueous solubility. Drugs with low solubility can be better absorbed using nanostructured lipid carriers (NLCs). Hence, the application of DFC in an NLC delivery system is proposed. Methods: Difenoconazole-loaded nanostructured lipid carriers (DFC-NLCs) with different solid–liquid lipid ratios were prepared by solvent diffusion method. Key physicochemical parameters, including particle diameter, surface charge (zeta potential), drug encapsulation efficiency, and morphological characteristics, were systematically characterized. Using Rhizoctonia solani (R. solani) as the model strain, inhibitory efficiency of DFC-NLC dispersion was compared with that of commercial dosage forms, such as 25% DFC emulsifiable concentrate (DFC-EC) and 40% DFC suspension concentrate (DFC-SC). Additionally, uptakes of DFC-NLC dispersions in R. solani were further observed by fluorescence probe technology. The safety profiles of DFC-NLCs and commercial dosage forms were evaluated using zebrafish as the model organism. Acute toxicity studies were conducted to determine the maximum non-lethal concentration (MNLC) and 10% lethal concentration (LC₁₀). Developmental toxicity studies were performed to observe toxic phenotypes. Results: DFC-NLC dispersions were in the nanometer range (≈200 nm) with high zeta potential, spherical in shape with encapsulation efficiency 69.1 ± 1.8%~95.0 ± 2.6%, and drug loading 7.1 ± 0.3%~9.7 ± 0.6% determined by high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Compared with commercial dosage forms, the antifungal effect of the DFC-NLC on R. solani was significantly improved in in vitro antibacterial experiments (p < 0.05). The 50% effective concentration (EC₅₀) values were 0.107 mg·L⁻¹ (DFC-NLC), 0.211 mg·L⁻¹ (DFC-EC), and 0.321 mg·L⁻¹ (DFC-SC), respectively. The uptakes of FITC-labeled DFC-NLC demonstrated that an NLC was appropriate to deliver DFC into pathogen to enhance the target effect. In safety assessment studies, DFC-NLCs exhibited a superior safety profile compared with commercial formulations (p < 0.05). Conclusions: This study investigates the feasibility of NLCs as delivery systems for poorly water-soluble fungicides, demonstrating their ability to enhance antifungal efficacy and reduce environmental risks. Full article

Alkaloids are nitrogen-containing compounds naturally occurring in plants, microorganisms, and marine organisms. Potent biological activities have been reported to date, ranging from neuroprotective to antioxidant and anticancer effects. Alkaloids have recently gained attention as potential antifungal agents for crop protection due to their broad spectrum of activity, eco-friendly nature, and ability to overcome some of the issues associated with synthetic fungicides, such as resistance development and environmental contamination. Several efforts have been made to obtain natural and nature-derived alkaloids endowed with significant activity against numerous pathogenic fungal strains. In this review, we collect synthetic strategies developed over the past decade to produce alkaloid fungicides for crop protection. Special emphasis is given to recent advancements in obtaining pure natural compounds and more potent analogs endowed with tailored and optimized properties. Full article

Triazoles are important fragments in the development of fungicidal compounds. Fungi have gradually developed drug resistance against traditional fungicides due to long-term overuse. Therefore, there is an urgent need to discover new candidate compounds. A series of 1,2,4-triazole derivatives containing amino acid fragments were designed and synthesized based on mefentrifluconazole. All the target compounds were characterized by ¹H-NMR, ¹³C-NMR, and HRMS techniques. Their antifungal activities against five kinds of phytopathogenic fungi were evaluated in vitro. The results revealed that most compounds had broad-spectrum fungicidal activities at 50 μg/mL and four compounds exhibited better antifungal activity than the control drug mefentrifluconazole. Interestingly, the synthesized compounds 8d and 8k exhibited exceptional antifungal activity against Physalospora piricola, with EC₅₀ values of 10.808 µg/mL and 10.126 µg/mL, respectively. Molecular docking studies demonstrate that the 1,2,4-triazole derivatives 8d and 8k, which incorporate amino acid groups, exhibit strong binding affinity to 14α-demethylase (CYP51). These findings highlight the potential of these compounds as effective antifungal agents. Full article

Pine needle blight of Pinus massoniana caused by pathogens of the Pestalotiopsis genus is a destructive disease worldwide, especially in young forests. Chemical fungicides accelerate the formation of resistant strains among plant pathogenic fungi, which makes microbial biocontrol particularly important. In this study, we identified Neopestalotiopsis camelliae-oleiferae as a new pathogen of pine needle blight in P. massoniana via pathogen isolation, inoculation, pathogenicity assays, morphology observations, and multilocus phylogenetic analyses of the ITS, TEF1, and TUB2 regions. PSM-6, an endophytic bacterium, was subsequently isolated from pine needles and was shown to have excellent antagonistic activity against N. camelliae-oleiferae in vitro. Based on the morphology, physiology, and molecular analysis, we identified this strain as P. silvicola. The extracellular secondary metabolites of PSM-6 were further proven to cause the shrinkage and collapse of pathogen hyphae. The decreased disease index and mortality indicated that pretreatment with PSM-6 may effectively protect pine seedlings from pathogen infection. In addition, PSM-6 exhibited broad-spectrum antifungal activity in several phytopathogenic fungi, including Fusarium graminearum, Botrytis cinerea, and Verticillium dahliae. These findings establish PSM-6 as a promising biocontrol agent, offering an environmentally friendly alternative to chemical fungicides for managing pine needle blight and other fungal diseases. Full article

Difenoconazole, as a systemic triazole fungicide, is a broad-spectrum, highly effective agent that has been widely used for controlling fungal diseases in 46 different crops (or crop categories), including rice, wheat, and corn. Due to the improper use of difenoconazole, concerns about its environmental residues and toxicity to non-target organisms have drawn significant attention from researchers. In response to this issue, this study aimed to isolate microbial strains capable of degrading difenoconazole from the environment. A novel difenoconazole-degrading strain, Acinetobacter sp. A-1, was screened and identified, demonstrating the ability to degrade 62.43% of 50 mg/L difenoconazole within seven days. Further optimization of the degradation conditions was conducted using single-factor experiments and response surface methodology experiments. The results showed that the optimal degradation conditions for strain A-1 were a difenoconazole concentration of 55.71 mg/L, a pH of 6.94, and an inoculation volume of 1.97%, achieving a degradation rate of 79.30%. Finally, strain A-1 was immobilized using sodium alginate, and its stability and bioremediation efficiency were evaluated. The results indicated that the immobilized strain A-1 exhibited high stability and significantly reduced the half-life of difenoconazole in the water–sediment contamination system. In the sterilized water–sediment system, the degradation rate of difenoconazole by the immobilized strain A-1 reached 65.26%. Overall, this study suggests that Acinetobacter sp. A-1 is a promising candidate for difenoconazole degradation, and immobilization technology can effectively enhance its removal efficiency in water–sediment systems. Full article

Difenoconazole, a broad-spectrum systemic fungicide, can effectively prevent and control plant diseases such as rice blast, leaf spot, and black spot caused by Colletotrichum godetiae, Alternaria alternata, and Neopestalotiopsis rosae. However, its residual accumulation in the environment may pose potential toxicity risks to non-target organisms. In this study, a highly efficient DIF-degrading microbial consortium TA01 was enriched from long-term pesticide-contaminated soil by a laboratory-based adaptive evolution strategy. The microbial consortium TA01 was able to degrade 83.87% of 50 mg/L of DIF within 3 days. In addition, three intermediate metabolites were identified using HPLC–MS/MS, and the results indicated that the degradation of DIF by microbial consortium TA01 may involve catalytic reactions such as hydrolysis, dehalogenation, and hydroxylation. High-throughput sequencing results showed that Pantoea, Serratia, Ochrobactrum, and Bacillus were the dominant microbial members involved in the degradation process. Finally, bioremediation capacity experiments showed that inoculation with microbial consortium TA01 was able to accelerate the degradation of DIF in the water–sediment system. The findings of this study not only enrich the microbial resources available for DIF degradation but also offer new potential strategies for in situ remediation of DIF contamination. Full article

To discover novel fungicides with good inhibitory effects on plant fungal diseases, twenty-five 3-indolyl-3-hydroxy oxindole derivatives (3a–3y) were synthesized. These newly derivatives were characterized by NMR and HRMS. Their antifungal activities against five plant pathogenic fungi were assessed in vitro. Most of the compounds exhibited moderate to excellent antifungal activities against the five pathogenic fungi. Notably, compounds 3t, 3u, 3v, and 3w displayed remarkable and broad-spectrum antifungal activities comparable to or superior to those of the fungicides carvacrol (CA) and phenazine-1-carboxylic acid (PCA). Among them, compound 3u displayed the most excellent antifungal activity against Rhizoctonia solani Kühn (R. solani), with an EC₅₀ of 3.44 mg/L, which was superior to CA (7.38 mg/L) and PCA (11.62 mg/L). Preliminary structure–activity relationship (SAR) results indicated that the introduction of I, Cl, or Br substituents at position 5 of the 3-hydroxy-2-oxindole and indole rings is crucial for compounds to exhibit good antifungal activity. The in vivo antifungal activity assay showed that compound 3u has good curative effects against R. solani. The current results suggest that these compounds are capable of serving as promising lead compounds. Full article

A series of novel triazone derivatives containing aldehyde hydrazone or ketone hydrazone moieties were designed, synthesized and their biological activities were investigated against Aphis craccivora, Culex pipiens pallens, Helicoverpa armigera, Ostrinia nubilalis, Mythimna separata and 14 Kinds of fungi. Most of the aldehyde hydrazone exhibited excellent insecticidal activities against A. craccivora. In particular, the aphicidal activities of compounds 3t (35%) and 3w (30%) were equivalent to pymetrozine (30%) at 5 mg/kg. The aphicidal activities of derivatives 3p, 3u, 3y, 5g, 5i, 5l, 5q and 5u against C. pipiens pallens were higher than that of pymetrozine. Compound 3u (100%) exhibited good larvicidal activities against C. pipiens pallens at 0.25 mg/kg. Most derivatives exhibited broad-spectrum fungicidal activities against 14 kinds of plant fungi at 50 mg/kg. Thirty-nine compounds exhibited a more than 50% inhibition rate against Physalospora piricola. Compounds 3h, 3t and 3w were expected to be the leading structure for the development of new triazone insecticides agents. Full article

The highly selective and sensitive determination of pesticide residues in food is critical for human health protection. Herein, the specific selectivity of molecularly imprinted polymers (MIPs) was proposed to construct an electrochemical sensor for the detection of carbendazim (CBD), one of the famous broad-spectrum fungicides, by combining with the synergistic effect of bioelectrocatalysis and nanocomposites. Gold nanoparticle-reduced graphene oxide (AuNP-rGO) composites were electrodeposited on a polished glassy carbon electrode (GCE). Then the MIP films were electropolymerized on the surface of the nanolayer using CBD as the template molecule and o-phenylenediamine (OPD) as the monomer. The detection sensitivity of CBD on the heterogeneous structure films was greatly amplified by AuNP-rGO composites and the bioelectrochemical oxidation of glucose, which was catalyzed by glucose oxidase (GOD) with the help of mediator in the underlying solution. The developed sensor showed high selectivity, good reproducibility, and excellent stability towards CBD with the linear range from 2.0 × 10⁻⁹ to 7.0 × 10⁻⁵ M, and the limit of detection (LOD) of 0.68 nM (S/N = 3). The expected system would provide a new idea for the development of simple and sensitive molecularly imprinted electrochemical sensors (MIESs). Full article

The development of innovative and effective strategies to combat fungal pathogens is critical to sustainable crop protection. Fungicides have been used for over two centuries, with traditional copper- and sulfur-based formulations still in use due to their broad-spectrum, multisite mode of action, which minimizes the risk of pathogen resistance. In contrast, modern systemic fungicides, though potent, often target a single site of action, leading to the accelerated emergence of resistant fungal strains. This study explores synergistic interactions between chitosan (CS) and selected fungicides, focusing on their antifungal activity against Fusarium graminearum. Among the fungicides tested, azoxystrobin (Amistar) exhibited the highest 44.88 synergy score when combined with CS (30 kDa, degree of deacetylation ≥ 90), resulting in significantly improved antifungal efficacy. Furthermore, the combination of CS and Amistar with double-stranded RNA (dsRNA) targeting selected ABC transporter genes further amplified antifungal activity by silencing genes critical for fungal tolerance to treatment. This dual synergy highlights the potential of RNA interference (RNAi) as both a functional tool to investigate fungal physiology and an effective antifungal strategy. These findings reveal a promising and environmentally friendly approach to mitigate resistance while improving fungal control. Furthermore, the remarkable synergy between azoxystrobin and CS presents a novel mechanism with significant potential for sustainable agricultural applications, which warrants further investigation to elucidate its molecular basis. Full article

Porcine blood, a significant byproduct of the pork industry, represents a potential source of antimicrobial peptides (AMPs). AMPs offer a promising alternative to chemical antimicrobials, which can be used as natural preservatives in the food industry. AMPs can exhibit both antibacterial and/or antifungal properties, thus improving food safety and addressing the growing concern of antibiotic and antifungal resistance. The objective of this study was to evaluate the antimicrobial activity of potential AMPs previously identified from porcine cruor hydrolysates. To this end, a total of sixteen peptides were chemically synthesized and their antimicrobial activities (antibacterial, anti-mold, and anti-yeast) were evaluated using microtitration and agar well diffusion methods against a wide range of microorganisms. Five new peptide sequences demonstrated antifungal activity, with Pep5 (FQKVVAGVANALAHKYH), an alpha-helix peptide, exhibiting the most promising results. Pep5 demonstrated efficacy against nine of the eleven fungal isolates, exhibiting low minimum inhibitory concentrations (MICs) and a fungicidal effect against key spoilage fungi (Rhodotorula mucilaginosa, Debaryomyces hansenii, Candida guilliermondii, Paecilomyces spp., Eurotium rubrum, Mucor racemosus, Aspergillus versicolor, Penicillium commune, and P. chrysogenum). These findings illustrate the potential of porcine blood hydrolysates as a source of AMPs, particularly antifungal peptides, which are less known and less studied than the antibacterial ones. Among the tested sequences, Pep5 exhibited the most promising characteristics, including broad-spectrum activity, low MICs, and a fungicidal effect. It is, therefore, a promising candidate for further research and for potential applications in the porcine industry and beyond. Full article

Phytophthora-induced crop diseases, commonly known as “plant plagues”, pose a significant threat to global food security. In this study, strain ASG80 was isolated from sisal roots and demonstrated a broad-spectrum antagonistic activity against several Phytophthora species and fungal pathogens. Strain ASG80 was identified as Streptomyces luteireticuli via phylogenetic analysis, digital DNA–DNA hybridization (dDDH), and average nucleotide identity (ANI). Whole-genome sequencing identified 40 biosynthetic gene clusters (BGCs) related to secondary metabolite production, including antimicrobial compounds. Strain ASG80 extract exhibited broad-spectrum inhibitory activity against Phytophthora nicotianae, P. vignae, P. cinnamomi, and P. sojae. Pot experiments showed that strain ASG80 extract significantly reduced sisal zebra disease incidence, with an efficacy comparable to the fungicide metalaxyl. These findings suggest that strain ASG80 is a promising biocontrol agent with substantial potential for managing Phytophthora-related diseases in agriculture. Full article