Search Results (44)

Bacterial leaf blight (BLB), a destructive disease of rice caused by Xanthomonas oryzae pv. oryzae (Xoo), continues to limit rice productivity worldwide. Although biologically synthesized zinc oxide nanoparticles (ZnO NPs) have been extensively investigated, knowledge regarding the antibacterial activity and biocompatibility of commercially available ZnO NPs is still limited. In this study, commercial ZnO NPs were systematically characterized and evaluated for their antibacterial mechanisms and biocompatibility in mammalian cells. FE-SEM and TEM analyses revealed irregular polyhedral, hexagonal, and short rod-like morphologies with an average particle size of ~33 nm, consistent with crystallite sizes estimated by XRD. The nanoparticles exhibited pronounced antibacterial activity against Xoo, with a minimum inhibitory concentration (MIC) of 16 µg/mL and a clear dose-dependent response. Mechanistic assays confirmed multifaceted bactericidal actions involving membrane disruption, ROS generation, Zn²⁺ release, and ultrastructural damage. Biocompatibility testing in human dermal fibroblasts showed enhanced proliferation at 8–32 µg/mL, no cytotoxicity up to 256 µg/mL, and reduced viability only at ≥512 µg/mL. These findings represent the first mechanistic evaluation of commercial ZnO NPs against Xoo, together with cytotoxicity assessment in mammalian cells, highlighting their structural distinctness and dual functionality that combine potent antibacterial activity with minimal mammalian cytotoxicity. Overall, the results underscore their potential as safe nanobiocontrol agents for sustainable rice disease management. Full article

Bacterial leaf blight (BLB), caused by Xanthomonas oryzae pv. oryzae (Xoo), poses a serious threat to rice cultivation. This study presents the green synthesis of zinc oxide nanoparticles (ZnO NPs) using an aqueous leaf extract of the medicinal plant Centella asiatica (L.) Urban and evaluates their potential as dual-function nanopesticides. The synthesized CA-ZnO NPs exhibited high crystallinity, a hexagonal to quasi-spherical morphology, and nanoscale dimensions (~22.5 nm), as confirmed by UV–Vis spectroscopy, XRD, FTIR, SEM, TEM, and SAED analyses. These nanoparticles demonstrated potent antibacterial activity against a highly virulent, field-derived Thai Xoo strain, with a minimum inhibitory concentration (MIC) of 8 µg/mL. Mechanistic investigations revealed substantial membrane disruption, intracellular nanoparticle penetration, and elevated reactive oxygen species (ROS) generation in treated cells. Cytotoxicity testing using human dermal fibroblasts (HDFs) revealed excellent biocompatibility, with no statistically significant reduction in cell viability at concentrations up to 500 µg/mL. In contrast, viability markedly declined at 1000 µg/mL. These findings underscore the selective antibacterial efficacy and minimal mammalian cytotoxicity of CA-ZnO NPs. Overall, CA-ZnO NPs offer a promising green nanopesticide platform that integrates potent antibacterial activity with biocompatibility, supporting future applications in sustainable crop protection and biomedical nanotechnology. Full article

Invasive bacteria have caused tremendous losses to global ecosystems and agricultural production, yet effective control measures remain elusive. Plant specialized metabolites are being investigated as an important source of antimicrobial active substances. And Ailanthus altissima is an abundant tree widespread throughout Northeast China. In this study, we identified 21 compounds from A. altissima leaves, including steroids, terpenes, phenolics, and coumarins. Two new steroidal compounds, ailanstigol A (1) and ailanstigol B (2), and one new coumarin (2′R,3′R)-7-(2′,3′,6′-trihydroxy-3′-methylhexyloxy)-6,8-dimethoxycoumarin (3) were isolated. Antibacterial screening revealed that compounds 1 and 2 exhibited inhibitory activity against two invasive bacteria, Xanthomonas oryzae pv. oryzae PXO 71A and PXO 86A and Pseudomonas syringae pv. maculicola ES4326. Further mechanistic screening unveiled that the steroidal compounds 1 and 2 may inhibit bacterial growth and reproduction by reducing cell viability, disrupting the cell membrane and increasing protein leakage, and inhibiting biofilm formation. In summary, our results enriched the known chemical diversity of A. altissima and provided a foundation for investigating the mechanisms by which steroidal compounds inhibit invasive bacterial growth. Full article

Background/Objective: Amphibian skin is a valuable source of host defense peptides (HDPs). This study aimed to identify HDPs with novel amino acid sequences from the skin of Rana tagoi yakushimensis and analyze their functions. Methods: cDNAs encoding HDP precursors were cloned and sequenced using RT-PCR and 3′-RACE. The novel HDPs were synthesized to evaluate their antimicrobial activity, antioxidant activity, and cytotoxicity. Antimicrobial activity was evaluated by way of broth microdilution and endotoxin- and β-glucan-binding capacity using an enzyme-linked endotoxin binding assay (ELEBA) and a modified ELEBA, respectively. Results: Nine cDNAs encoding precursors for various HDP families, including temporin, ranatuerin-2, brevinin-1, amurin-9, and a novel yakushimin peptide, were identified. Brevinin-1TYa exhibited antibacterial activity against Staphylococcus aureus, and brevinin-1TYa and amurin-9TYa induced morphological changes in Escherichia coli and S. aureus. Yakushimin-TYa, amurin-9TYa, and brevinin-1TYa showed concentration-dependent antibacterial effects against the plant pathogens Xanthomonas oryzae pv. oryzae and Clavibacter michiganensis subsp. michiganensis. Amurin-9TYa demonstrated strong binding affinity to lipopolysaccharide, lipoteichoic acid, and β-glucan, exhibited antioxidant activity, and lacked cytotoxicity, making it a promising therapeutic candidate. Moreover, brevinin-1TYa showed strong cytotoxicity, whereas yakushimin-TYa exhibited weak cytotoxicity. Conclusions: These findings highlight the potential of these peptides, particularly amurin-9TYa, for future applications as antimicrobial and therapeutic agents. Full article

Bacterial virulence plays an important role in infection. Antibacterial virulence factors are effective for preventing crop bacterial diseases. Resin acid copper salt as an effective inhibitor exhibited excellent anti-Xanthomonas oryzae pv. oryzae (Xoo) activity with an EC₅₀ of 50.0 μg mL⁻¹. Resin acid copper salt (RACS) can reduce extracellular polysaccharides’ (EPS’s) biosynthesis by down-regulating gumB relative expression. RACS can also effectively inhibit the bio-mass of Xoo biofilm. It can reduce the activity of Xoo extracellular amylase at a concentration of 100 μg mL⁻¹. Meanwhile, the results of virtual computing suggested that RACS is an enzyme inhibitor. RACS displayed good curative activity with a control effect of 38.5%. Furthermore, the result of the phytotoxicity assessment revealed that RACS exhibited slight toxicity compared with the control at a concentration of 200 μg mL⁻¹. The curative effect was increased to 45.0% using an additional antimicrobial agent like orange peel essential oil. RACS markedly inhibited bacterial pathogenicity at a concentration of 100 μg mL⁻¹ in vivo. Full article

SYAUP-491 is a novel alkyl sulfonamide. In this study, in vivo and in vitro tests were performed along with a proteomic analysis to determine the effects and underlying mechanisms of the antibacterial activity of SYAUP-491 against the causative agent of bacterial leaf blight in rice. The antibacterial test results suggested that SYAUP-491 exhibited significant activities against Xanthomonas oryzae pv. oryzae (Xoo) in vitro and in vivo. The minimal EC₅₀ values reached 6.96 μg/mL and the curative activity reached 74.1%. Detailed studies demonstrated that SYAUP-491 altered membrane permeability and caused morphological changes. Based on proteomics results, SYAUP-491 might inhibit bacterial protein synthesis. SYAUP-491 may disrupt and alter cell membrane permeability and could further act on ribosomes in the bacterial body. Given the above results, SYAUP-491 could serve as a new lead compound in the research of antibacterial control of plant pathogenic bacterial disease. Full article

To effectively control the infection of plant pathogens, we designed and synthesized a series of phenylthiazole derivatives containing a 1,3,4-thiadiazole thione moiety and screened for their antibacterial potencies against Ralstonia solanacearum, Xanthomonas oryzae pv. oryzae, as well as their antifungal potencies against Sclerotinia sclerotiorum, Rhizoctonia solani, Magnaporthe oryzae and Colletotrichum gloeosporioides. The chemical structures of the target compounds were characterized by ¹H NMR, ¹³C NMR and HRMS. The bioassay results revealed that all the tested compounds exhibited moderate-to-excellent antibacterial and antifungal activities against six plant pathogens. Especially, compound 5k possessed the most remarkable antibacterial activity against R. solanacearum (EC₅₀ = 2.23 μg/mL), which was significantly superior to that of compound E1 (EC₅₀ = 69.87 μg/mL) and the commercial agent Thiodiazole copper (EC₅₀ = 52.01 μg/mL). Meanwhile, compound 5b displayed the most excellent antifungal activity against S. sclerotiorum (EC₅₀ = 0.51 μg/mL), which was equivalent to that of the commercial fungicide Carbendazim (EC₅₀ = 0.57 μg/mL). The preliminary structure-activity relationship (SAR) results suggested that introducing an electron-withdrawing group at the meta-position and ortho-position of the benzene ring could endow the final structure with remarkable antibacterial and antifungal activity, respectively. The current results indicated that these compounds were capable of serving as promising lead compounds. Full article

Equisetin was isolated from endophytic fungus Fusarium sp. JDJR1 via bioassay-guided isolation, and it was evaluated as an anti-microbial and herbicidal agent. Bioactivity assessments revealed that equisetin exhibited a broad spectrum of fungicidal and anti-bacterial activity against various plant pathogens. The EC₅₀ values against Botrytis cinerea, Fusarium graminearum, Sclerotinia sclerotiorum, and Rhizoctonia solani ranged from 10.7 to 21.0 μg/mL. Notably, equisetin demonstrated activity against Xanthomonas oryzae pv. oryzicola, Xanthomonas oryzae pv. oryzae and Pseudomonas solanacearum with an MIC range of 4–16 μg/mL, surpassing the efficacy of the positive control: streptomycin sulfate. Equisetin, at a concentration of 100 μg/mL, could completely inhibit the spore germination of F. graminearum. In in vivo protection experiments, the protective efficacy of equisetin against B. cinerea on tomato fruits at 200 μg/mL reached 72.9%. Furthermore, in herbicidal activity tests that use the Petri dish bioassay method, equisetin had a good inhibitory effect on the root growth of weeds. At a concentration of 100 μg/mL, the inhibition rates for Echinochloa crusgalli and Eclipta prostrata root were 98.8 and 94.4%, respectively. Full article

To explore more efficient and less toxic antibacterial and antifungal pesticides, we utilized 2,6-difluorobenzamide as a starting material and ultimately synthesized 23 novel benzoylurea derivatives containing a pyrimidine moiety. Their structures were characterized and confirmed by ¹H NMR, ¹³C NMR, ¹⁹F NMR, and HRMS. The bioassay results demonstrated that some of the title compounds exhibited moderate to good in vitro antifungal activities against Botrytis cinerea in cucumber, Botrytis cinerea in tobacco, Botrytis cinerea in blueberry, Phomopsis sp., and Rhizoctonia solani. Notably, compounds 4j and 4l displayed EC₅₀ values of 6.72 and 5.21 μg/mL against Rhizoctonia solani, respectively, which were comparable to that of hymexazol (6.11 μg/mL). Meanwhile, at 200 and 100 concentrations, the target compounds 4a–4w exhibited lower in vitro antibacterial activities against Xanthomonas oryzae pv. oryzicola and Xanthomonas citri subsp. citri, respectively, compared to those of thiodiazole copper. Furthermore, the molecular docking simulation demonstrated that compound 4l formed hydrogen bonds with SER-17 and SER-39 of succinate dehydrogenase (SDH), providing a possible explanation for the mechanism of action between the target compounds and SDH. This study represents the first report on the antifungal and antibacterial activities of novel benzoylurea derivatives containing a pyrimidine moiety. Full article

Rice bacterial leaf blight is a destructive bacterial disease caused by Xanthomonas oryzae pv. oryzae (Xoo) that seriously threatens crop yields and their associated economic benefits. In this study, a series of improved dissolubility 7-aliphatic amine tryptanthrin derivatives was designed and synthesized, and their potency in antibacterial applications was investigated. Notably, compound 6e exhibited excellent activity against Xoo, with an EC₅₀ value of 2.55 μg/mL, compared with the positive control bismerthiazol (EC₅₀ = 35.0 μg/mL) and thiodiazole copper (EC₅₀ = 79.4 μg/mL). In vivo assays demonstrated that 6e exhibited a significant protective effect on rice leaves. After exposure, the morphology of the bacteria was partially atrophied by SEM. Furthermore, 6e increased the accumulation of intracellular reactive oxygen species, causing cell apoptosis and the formation of bacterial biofilms. All the results indicated that 6e could be a potential agrochemical bactericide for controlling phytopathogenic bacteria. Full article

An N-heterocyclic carbene (NHC)-catalyzed atroposelective annulation reaction is disclosed for quick and efficient access to thiazine derivatives. A series of axially chiral thiazine derivatives bearing various substituents and substitution patterns were produced in moderate to high yields with moderate to excellent optical purities. Preliminary studies revealed that some of our products exhibit promising antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) that causes rice bacterial blight. Full article

Isolation for antibacterial compounds from natural plants is a promising approach to develop new pesticides. In this study, two compounds were obtained from the Chinese endemic plant Piper austrosinense using bioassay-guided fractionation. Based on analyses of ¹H-NMR, ¹³C-NMR, and mass spectral data, the isolated compounds were identified as 4-allylbenzene-1,2-diol and (S)-4-allyl-5-(1-(3,4-dihydroxyphenyl)allyl)benzene-1,2-diol. 4-Allylbenzene-1,2-diol was shown to have strong antibacterial activity against four plant pathogens, including Xanthomonas oryzae pathovar oryzae (Xoo), X. axonopodis pv. citri (Xac), X. oryzae pv. oryzicola (Xoc) and X. campestris pv. mangiferaeindicae (Xcm). Further bioassay results exhibited that 4-allylbenzene-1,2-diol had a broad antibacterial spectrum, including Xoo, Xac, Xoc, Xcm, X. fragariae (Xf), X. campestris pv. campestris (Xcc), Pectobacterium carotovorum subspecies brasiliense (Pcb) and P. carotovorum subsp. carotovorum (Pcc), with minimum inhibitory concentration (MIC) values ranging from 333.75 to 1335 μmol/L. The pot experiment showed that 4-allylbenzene-1,2-diol exerted an excellent protective effect against Xoo, with a controlled efficacy reaching 72.73% at 4 MIC, which was superior to the positive control kasugamycin (53.03%) at 4 MIC. Further results demonstrated that the 4-allylbenzene-1,2-diol damaged the integrity of the cell membrane and increased cell membrane permeability. In addition, 4-allylbenzene-1,2-diol also prevented the pathogenicity-related biofilm formation in Xoo, thus limiting the movement of Xoo and reducing the production of extracellular polysaccharides (EPS) in Xoo. These findings suggest the value of 4-allylbenzene-1,2-diol and P. austrosinense could be as promising resources for developing novel antibacterial agents. Full article

Plant bacterial diseases are an intractable problem due to the fact that phytopathogens have acquired strong resistances for traditional pesticides, resulting in restricting the quality and yield of agricultural products around the world. To develop new agrochemical alternatives, we prepared a novel series of sulfanilamide derivatives containing piperidine fragments and assessed their antibacterial potency. The bioassay results revealed that most molecules displayed excellent in vitro antibacterial potency towards Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac). In particular, molecule C₄ exhibited outstanding inhibitory activity toward Xoo with EC₅₀ value of 2.02 µg mL⁻¹, which was significantly better than those of the commercial agents bismerthiazol (EC₅₀ = 42.38 µg mL⁻¹) and thiodiazole copper (EC₅₀ = 64.50 µg mL⁻¹). A series of biochemical assays confirmed that compound C₄ interacted with dihydropteroate synthase, and irreversibly damaged the cell membrane. In vivo assays showed that the molecule C₄ presented acceptable curative and protection activities of 34.78% and 39.83%, respectively, at 200 µg mL⁻¹, which were greater than those of thiodiazole and bismerthiazol. This study highlights the valuable insights for the excavation and development of new bactericides that can concurrently target dihydropteroate synthase and bacterial cell membranes. Full article

Imidazole alkaloids, a common class of five-membered aromatic heterocyclic compounds, exist widely in plants, animals and marine organisms. Because of imidazole’s extensive and excellent biological and pharmacological activities, it has always been a topic of major interest for researchers and has been widely used as an active moiety in search of bioactive molecules. To find more efficient antibacterial compounds, a series of novel imidazole-fragment-decorated 2-(pyrazol-4-yl)-1,3,4-oxadiazoles were designed and synthesized based on our previous works via the active substructure splicing principle, and their bioactivities were systematically evaluated both in vitro and in vivo. The bioassays showed that some of the target compounds displayed excellent in vitro antibacterial activity toward three virulent phytopathogenic bacteria, including Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas axonopodis pv. citri (Xac) and Pseudomonas syringae pv. actinidiae (Psa), affording the lowest EC₅₀ values of 7.40 (7c), 5.44 (9a) and 12.85 (9a) μg/mL, respectively. Meanwhile, compound 7c possessed good in vivo protective and curative activities to manage rice bacterial leaf blight at 200 μg/mL, with control efficacies of 47.34% and 41.18%, respectively. Furthermore, compound 9a showed commendable in vivo protective and curative activities to manage kiwifruit bacterial canker at 200 μg/mL, with control efficacies of 46.05% and 32.89%, respectively, which were much better than those of the commercial bactericide TC (31.58% and 17.11%, respectively). In addition, the antibacterial mechanism suggested that these new types of title compounds could negatively impact the cell membranes of phytopathogenic bacteria cells and cause the leakage of the intracellular component, thereby leading to the killing of bacteria. All these findings confirm that novel 2-(pyrazol-4-yl)-1,3,4-oxadiazoles containing an imidazole fragment are promising lead compounds for discovering new bactericidal agents. Full article

Pesticides play an important role in crop disease and pest control. However, their irrational use leads to the emergence of drug resistance. Therefore, it is necessary to search for new pesticide-lead compounds with new structures. We designed and synthesized 33 novel pyrimidine derivatives containing sulfonate groups and evaluated their antibacterial and insecticidal activities. Results: Most of the synthesized compounds showed good antibacterial activity against Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac), Pseudomonas syringae pv. actinidiae (Psa) and Ralstonia solanacearum (Rs), and certain insecticidal activity. A₅, A₃₁ and A₃₃ showed strong antibacterial activity against Xoo, with EC₅₀ values of 4.24, 6.77 and 9.35 μg/mL, respectively. Compounds A₁, A₃, A₅ and A₃₃ showed remarkable activity against Xac (EC₅₀ was 79.02, 82.28, 70.80 and 44.11 μg/mL, respectively). In addition, A₅ could significantly improve the defense enzyme (superoxide dismutase, peroxidase, phenylalanine ammonia-lyase and catalase) activity of plants against pathogens and thus improve the disease resistance of plants. Moreover, a few compounds also showed good insecticidal activity against Plutella xylostella and Myzus persicae. The results of this study provide insight into the development of new broad-spectrum pesticides. Full article