Pectin-coated hollow organosilicon construction of a dual pH and pectinase stimulation-responsive prochloraz delivery system for the control of rice sheath blight.

Degradable mesoporous organosilicon nanoparticles coated with chitosan-Cu2+ complexes with dual stimulus-response for efficient prochloraz delivery.

Rice sheath blight is a globally important rice disease. Unfortunately, this critical disease has not been effectively controlled, and the intensive and continuous use of the same fungicide might increase the risk of resistance development in the pathogen. To discover new active agents against rice sheath blight, in this study, three series of β-carboline urea, benzoylurea and benzoylthiourea derivatives were designed, synthesized and evaluated for in vitro and in vivo fungicidal activity against Rhizoctonia solani. All these compounds (EC50 : 0.131-1.227 mmol L-1 ) exhibited better fungicidal activity than harmine itself (EC50 : 2.453 mmol L-1 ). Significantly, compound 17c (EC50 : 0.131 mmol L-1 ) displayed the best efficacy in vitro and superior fungicidal activity compared with validamycin A (EC50 : 0.397 mmol L-1 ). Moreover, the in vivo bioassay also indicated that compound 17c could be effective for the control of rice sheath blight. Based on the bioassay result and quantitative structure-activity relationship (QSAR) information, structure modification in β-carboline warrants further investigation and its benzoylurea derivative 17c, which showed the best fungicidal activities, could emerge as a potential fungicide against rice sheath blight. © 2018 Society of Chemical Industry.

Rice sheath blight is a serious disease caused by Rhizoctonia solani that reduces rice yield. Currently, there is a lack of efficient and environmentally friendly control methods. In this study, we found that Bacillus velezensis (B. velezensis) Y6 could significantly inhibit the growth of mycelium in Rhizoctonia solani, and its control efficiency against rice sheath blight was 58.67% (p < 0.01) in a pot experiment. Lipopeptides play an important role in the control of rice sheath blight by B. velezensis Y6, among which iturin and fengycin are essential, and iturin W, a novel lipopeptide in B. velezensis, plays a major role in lipopeptide antagonism to Rhizoctonia solani. In the field, we also found that inoculation with B. velezensis Y6 can increase rice yield (dry weight) by 11.75%. Furthermore, the transcriptome profiling results of the rice roots revealed that there were a total of 1227 differential genes (DEGs) regulated when treated with Y6, of which 468 genes were up-regulated and 971 genes were down-regulated in rice roots compared with the control. Among them, the DEGs were mainly distributed in biological processes (BP) and were mainly enriched in response to stimulus (GO:0050896), response to stress (GO:0006950), and response to abiotic stimulus (GO:0009628). According to the KEGG pathway analysis, there were 338 DEGs classified into 87 KEGG functional pathway categories. Compared with the control, a large number of enriched genes were distributed in phenylpropanoid biosynthesis (map00940), glutathione metabolism (map00480), glycolysis/gluconeogenesis (map00010), and amino sugar and nucleotide sugar metabolism (map00520). In summary, this investigation provides a new perspective for studying the molecular mechanism of B. velezensis in controlling rice sheath blight.

Gene therapy has emerged as a powerful tool to treat various diseases, such as cardiovascular diseases, neurological diseases, ocular diseases and cancer diseases. In 2018, the FDA approved Patisiran (the siRNA therapeutic) for treating amyloidosis. Compared with traditional drugs, gene therapy can directly correct the disease-related genes at the genetic level, which guarantees a sustained effect. However, nucleic acids are unstable in circulation and have short half-lives. They cannot pass through biological membranes due to their high molecular weight and massive negative charges. To facilitate the delivery of nucleic acids, it is crucial to develop a suitable delivery strategy. The rapid development of delivery systems has brought light to the gene delivery field, which can overcome multiple extracellular and intracellular barriers that prevent the efficient delivery of nucleic acids. Moreover, the emergence of stimuli-responsive delivery systems has made it possible to control the release of nucleic acids in an intelligent manner and to precisely guide the therapeutic nucleic acids to the target site. Considering the unique properties of stimuli-responsive delivery systems, various stimuli-responsive nanocarriers have been developed. For example, taking advantage of the physiological variations of a tumor (pH, redox and enzymes), various biostimuli- or endogenous stimuli-responsive delivery systems have been fabricated to control the gene delivery processes in an intelligent manner. In addition, other external stimuli, such as light, magnetic fields and ultrasound, have also been employed to construct stimuli-responsive nanocarriers. Nevertheless, most stimuli-responsive delivery systems are in the preclinical stage, and some critical issues remain to be solved for advancing the clinical translation of these nanocarriers, such as the unsatisfactory transfection efficiency, safety issues, complexity of manufacturing and off-target effects. The purpose of this review is to elaborate the principles of stimuli-responsive nanocarriers and to emphasize the most influential advances of stimuli-responsive gene delivery systems. Current challenges of their clinical translation and corresponding solutions will also be highlighted, which will accelerate the translation of stimuli-responsive nanocarriers and advance the development of gene therapy.

Thifluzamide is a SDHI (succinate dehydrogenase inhibitor) fungicide, which interferes with succinate ubiquinone reductase in the mitochondrial electron transport chain of fungi. Presently, jinggangmycin is the major fungicide extensively used for the control of rice sheath blight caused by Rhizoctonia solani and resistance to jinggangmycin was first reported to occur in China. A total of 128 isolates of R. solani from Anhui Province of China were characterised for the baseline sensitivity to thifluzamide. The isolates were very sensitive to thifluzamide and the baseline sensitivity curve was unimodal with an average EC50 value of 0.058 ± 0.012 µg mL−1. However, EC50 values of boscalid (another SDHI fungicide) for inhibition of mycelial growth of 22 arbitrarily selected R. solani isolates ranged from 1.89 to 2.68 µg mL−1. Thifluzamide applied at 110 µg mL−1 exhibited excellent protective and curative activity against rice sheath blight and provided 81.1–91.0% protective or curative control efficacy. In field trials in 2010 and 2011, control efficacies of thifluzamide at 82 g.a.i ha−1 15 and 30 days after second application were 84.2% and 86.7%, respectively, suggesting excellent activity against sheath blight. There was a statistically significant difference in the efficacy between thifluzamide and boscalid or jinggangmycin. These results suggested that thifluzamide should be a good alternative fungicide to jinggangmycin for the control of rice sheath blight.

Sheath blight caused by Rhizoctonia solani Kühn is a major disease of rice that greatly reduces yield and grain quality and jinggangmycin is the most widely used fungicide to control this disease in China. Bacillus subtilis NJ-18 has broad antimicrobial activity to many phytopathogenic bacteria and fungi; it is especially effective against Rhizoctonia solani. Laboratory, greenhouse and field tests were conducted to determine the effect of combining the biological control agent Bacillus subtilis NJ-18 with the fungicide jinggangmycin for control of rice sheath blight. Growth of NJ-18 in vitro was not affected by jinggangmycin. In a greenhouse experiment, disease control was greater with a mixture of NJ-18 and jinggangmycin than with either alone; a mixture of NJ-18 at 10(8) cfu mL(-1) and jinggangmycin at 50 or 100 mg L(-1) reduced lesion length by 35% and 20%, respectively, and the combinations showed a synergistic action. In three field trials, disease control was significantly greater with a mixture of NJ-18 at 10(8) cfu mL(-1) and jinggangmycin at 75 or 150 g a.i. ha(-1) than with either component alone. The results of the study indicate that, when Bacillus subtilis NJ-18 strain was combined with jinggangmycin, there was an increased suppression of rice sheath blight, and thus could provide an alternative disease control option.

Effervescent fast-disintegrating bacterial formulation for biological control of rice sheath blight

Rice sheath blight, caused by Rhizoctonia solani pathogen, poses a significant threat to global food security. To address this challenge, we designed and synthesized diphenyl ether hydrazone derivatives (3aa-3bb) as potential succinate dehydrogenase inhibitors. Most of these derivatives achieved 100% inhibition against R. solani at 50 μg/mL concentration. Notably, compound 3az exhibited an exceptional efficacy of 95% control rate with an EC50 of 0.28 μg/mL, which significantly outperformed boscalid at a concentration of 200 μg/mL, without affecting the rice growth and development. Furthermore, after treatment with 3az, the growth morphology and intracellular changes of R. solani mycelia were consistent with those observed with boscalid. Additionally, the IC50 values of compounds 3ay and 3az were 1.55 and 1.11 μM, respectively, which were better than the IC50 value of boscalid (1.85 μM). The finding by molecular docking studies revealed that compound 3az interacts with novel binding sites, offering an opportunity for the development of innovative SDH inhibitors for the efficient control of rice sheath blight disease.

Epiphytic microorganisms on the phyllosphere of traditional and high-yielding rice varieties were isolated from different agroecological zones of Sri Lanka and screened for theirin vitro andin vivo antagonism againstRhizoctonia solani Kuhn AG-1 1A, the sheath blight pathogen of rice. Among a total of 196 bacterial and 91 fungal isolates, 12 bacterial and two fungal isolates which showed more than 50% growth inhibition ofR. solani were tested for theirin vivo antagonism. Among the 14 antagonists tested, six bacterial and one fungal isolate substantially reduced the incidence of sheath blight (by more than 82%) and severity (by more than 92%) of the rice varieties BG94-1 and IR8 grown in a pot experiment under open field conditions. Using five antagonists that showed the bestin vitro antagonism, a pot experiment was conducted to determine whether the presence of indigenous microflora on the rice sheath had any effect on the effectiveness of antagonism. Three isolates (B4, GbB5 and HMWB4) controlled sheath blight incidence and severity equally well in the presence and absence of indigenous microflora. Two isolates (BG352B1 and BG300B1) were more effective when they were introduced into the rice sheath without indigenous microflora. Among the effective antagonists determined by the pot experiment, isolates B4, B16, BG94-1B5, GbB5, HMWB4 and BG379-F2 were tested under field conditions for two consecutive growing seasons. Under field conditions, severity of rice sheath blight was significantly reduced by the application of all the tested antagonists as a spray on rice sheath at a concentration of 108 cfu ml−1, starting 3 days after the development of symptoms and continuing for three applications at 10-day intervals. Antagonistic performances were consistent in the two seasons under field conditions andB. megatarium A (isolate B16) andAspergillus niger (isolate BG379-F2) performed as the most effective antagonists in both seasons. When disease severity was quantified as percentage sheath area covered by the disease lesions, the respective reductions in disease severity were greater than 50% and 61% byB. megaterium A (isolate B16) andAspergillus niger (isolate BG379-F2), respectively, in both seasons.

Rice sheath blight, caused by Rhizoctonia solani, is a globally important rice disease and the increasing resistance of this pathogen highlights the need for new active compounds against rice sheath blight. In this study, natural β-carboline alkaloids were optimized to obtain a series of 1,2,4,9-tetrahydro-3-thia-9-aza-fluorene derivatives and evaluated for their fungicidal activity and mode of action against R. solani. Of these compounds, 18 exhibited significant in vitro fungicidal activity against R. solani, with an EC50 value of 2.35 μg/mL, and was more active than validamycin A. In vivo bioassay also demonstrated that 18 displayed superior protective and curative activities as compared to validamycin A. Mechanistically, 18 not only induced the loss of mitochondrial membrane potential and accumulation of reactive oxygen species, but also interfered with DNA synthesis. Therefore, compound 18 displayed pronounced in vitro and in vivo fungicidal activity against R. solani and could be used as a potential candidate for the control of rice sheath blight.

Rice sheath blight is one of the most important rice diseases in the world and the succinate dehydrogenase inhibitor fungicide flutolanil has potential for its control. In this study, a total of 112 Rhizoctonia solani isolates from Jiangsu province in China were characterized for their baseline sensitivity to flutolanil. The baseline sensitivity curve was unimodal with an average EC50 value of 0.0736 ± 0.0331 μg mL−1 for inhibition of mycelial growth. Flutolanil exhibited excellent acropetal movement in rice, and better protective and curative activity than validamycin against rice sheath blight. In field trials in 2011 and 2012, flutolanil used at a concentration of 150 g a.i. ha−1 provided control efficacy ranging from 63.7 to 88.9 %, and its control efficacy could reach 83.9 % ~ 96.5 % at a concentration of 300 g a.i. ha−1. These results suggested that flutolanil will be a good alternative fungicide to validamycin for control of rice sheath blight.

Evaluation of crude toxin and metabolite produced by Helminthosporium gramineum Rabenh for the control of rice sheath blight in paddy fields

Fluxapyroxad,3-(difluoromethyl)-1-methyl-N-(3’,4’,5’-trifluorobiphenyl-2-yl) pyrazole-4-carboxamide (C18H12F5N3O, Fig. 1), is a SDHI fungicide, which is a new active ingredient that interferes with succinate ubiquinone reductase in the electron transport chain of fungi. Between 2008 and 2010, a total of 128 isolates of Rhizoctonia solani from Anhui Province of China were characterized for the baseline sensitivity to fluxapyroxad. The isolates collected between 2008 and 2010 all showed similar sensitivity to fluxapyroxad. Baseline sensitivity was distributed as unimodal curves with an average EC50 value of 0.054 ± 0.014 μg ml−1. However, EC50 values of boscalid for inhibition of mycelial growth of R. solani isolates ranged from 1.89 to 2.68 μg/ml and the average (±SE) EC50 value was 2.212 ± 0.228 μg/ml, indicating that the R. solani isolates were less sensitive to boscalid than that of fluxapyroxad. Fluxapyroxad exhibited excellent protective and curative activity against rice sheath blight and provided 82.6–94.2 % protective or curative control efficacy. In field trials, control efficacy of fluxapyroxad at 100 g a.i/ha 15 days and 30 day after second application was 83.4–88.0 %, suggesting excellent activity against sheath blight. Control efficacy of boscalid at a dosage of 600 g a.i/ha 15 days and 30 day after second application was about 51.7–57.0 %. There was a significant difference in the efficacy between fluxapyroxad and boscalid or jinggangmycin. These results suggested that fluxapyroxad is a good alternative fungicide to jinggangmycin for the control of rice sheath blight.

Isolation, identification, and biocontrol mechanisms of endophytic Burkholderia vietnamiensis C12 from Ficus tikoua Bur against Rhizoctonia solani

A pathogenicity assay for in planta screening of biological control agents (BCAs) towards sheath blight in rice was developed, and used to evaluate a panel of Rhizoctonia solani Kuhn hyphae-associated bacteria for their ability to control sheath blight under screenhouse conditions. The best performing BCA, Burkholderia sp. strain A-7.3, was selected for field trials. Disease incidence and disease severity were significantly reduced leading to a significant grain yield increase of 7%. Furthermore, R. solani sclerotia formation and sclerotia viability were significantly reduced, thus lowering the reservoir for primary infections in the next crop cycle. The paper presents a reliable pathogenicity assay that can be used to test BCA performance under different scenarios e.g. plant variety and soil conditions, and help predict translation of results obtained under screenhouse conditions to field performance. Furthermore, it supports the hypothesis that hyphae-associated bacteria are a promising source of niche-specific BCAs towards fungal pathogens.