Given the prevalence of the malignant weed Chinese Sprangletop (Leptochloa chinensis (L.) Nees) in rice fields, the development of novel herbicides against this weed has aroused wide interest. Here, we report a novel diphenyl ether-pyrimidine hybrid, DEP-5, serving as a systematic pre/postemergence herbicide candidate for broad-spectrum weed control in rice fields, specifically for L. chinensis. Notably, DEP-5 exhibits over 80% herbicidal activity against the resistant biotypes even at 37.5 g a.i./ha under greenhouse conditions and has complete control of L. chinensis at 150 g a.i./ha in the rice fields. We uncover that DEP-5 acts as a noncompetitive inhibitor of acetohydroxyacid synthase (AHAS) with an inhibition constant (Ki) of 39.4 μM. We propose that DEP-5 binds to AHAS in two hydrophobic-driven binding modes that differ from commercial AHAS inhibitors. Overall, these findings demonstrate that DEP-5 has great potential to be developed into a herbicide for L. chinensis control and inspire fresh concepts for novel AHAS-inhibiting herbicide design.
Herbicides are useful tools for managing weeds and promoting food production and sustainable agriculture. In this study, we report on the development of a novel class of lipophilic pyrimidine-biphenyl (PMB) herbicides. Firstly, three PMBs, Ia, IIa, and IIIa, were rationally designed via a scaffold hopping strategy and were determined to inhibit acetohydroxyacid synthase (AHAS). Computational simulation was carried out to investigate the molecular basis for the efficiency of PMBs against AHAS. With a rational binding mode, and the highest in vitro as well as in vivo potency, Ia was identified as a preferable hit. Furthermore, these integrated analyses guided the design of eighteen new PMBs, which were synthesized via a one-step Suzuki–Miyaura cross-coupling reaction. These new PMBs, Iba-ic, were more effective in post-emergence control of grass weeds compared with Ia. Interestingly, six of the PMBs displayed 98–100% inhibition in the control of grass weeds at 750 g ai/ha. Remarkably, Ica exhibited ≥ 80% control against grass weeds at 187.5 g ai/ha. Overall, our comprehensive and systematic investigation revealed that a structurally distinct class of lipophilic PMB herbicides, which pair excellent herbicidal activities with new interactions with AHAS, represent a noteworthy development in the pursuit of sustainable weed control solutions.
Soybean is a crucial source of oil, protein, and biofuel, necessitating efficient transformation systems for advancing research. Agrobacterium-mediated transformation is currently the primary method used in the soybean transformation industry and scientific research. However, the low efficiency and genotype dependency of this technology leave significant room for improvement. This study aimed to enhance soybean transformation efficiency by generating and validating three reporter vectors (ZsGreen, TdTomato, and Ruby) and using Agrobacterium Auxiliary Solution (AAS) containing Silwet L-77 and hormone mixtures. Our findings demonstrate that AAS significantly improves hairy root transformation rates. Specifically, this combination increased total root and cotyledon transformation efficiencies compared to the control. We also found that larger vectors like Ruby reduced transformation efficiency compared to smaller markers like GFP and RFP. Furthermore, AAS slightly reduced the co-transformation rate of two separate vectors compared to single vector transformations. Additionally, AAS enhanced soybean hypocotyl transformation rates across various varieties, consistently increasing positive root and explant efficiencies. Notably, transformation rates varied significantly between varieties, with Forrest differing from Williams 82 and Dongnong 50. This research highlights the importance of auxiliary agents and vector size in optimizing soybean transformation, providing insights for future advancements in genetic modification and biotechnology.
Soybean ( Glycine max L.), a crucial crop that provides essential nutrition, is experiencing increasing demand to meet protein and oil requirements. However, the menace of soybean cyst nematode (SCN) disease, caused by Heterodera glycines , poses a substantial threat globally, resulting in significant annual economic losses. While cultivating resistant varieties is an eco-friendly approach to control SCN, the excessive use of a single variety triggers ongoing evolution of SCN races, jeopardizing the soybean industry's stability. Leveraging advanced technologies, research on soybean SCN resistance mechanisms has progressed significantly across genetics, transcriptomics, and protein functions. This review consolidates insights into major resistance loci ( rhg1 and Rhg4 ), elucidating their connections with vesicle transport and plant hormone signaling pathways. It also discusses the role of key functional proteins in soybean resistance and addresses potential research issues. This study explores superior soybean resistance genes, laying a foundation for creating new SCN-resistant germplasms, thereby ensuring the sustainable growth of the global soybean industry.
为解决传统加热法合成异喹啉-离子液体存在的问题,开发了一种超声辅助合成异喹啉-离子液体的方法.通过异喹啉季铵化过程的对比研究,证明了该方法具有环保性强、产率高、反应时间短等优点.将其扩展至阴离子交换反应,发现超声辐射法有效促进了异喹啉溴化物与简单阴离子[N(CF3SO2)2]?和[PF6]?,以及与复杂阴离子2,4-二氯苯氧乙酸的阴离子交换反应.对所得到的异喹啉-离子液体进行了结构表征以及热行为和溶解度的研究和讨论.结果表明,所得液体具有良好的热稳定性,为快速、高效建立绿色多功能化离子液体库奠定了基础.
Pathogenic bacteria seriously endanger human health. Metal-organic framework (MOF)-enzyme composites are novel antibacterial materials for effective bacterial inactivation. In this study, we develop a MOF-based nanozyme hybrid for synergistic bacterial eradication, which integrates features of bacterial capture, magnetic assembly, lysozyme hydrolysis, and light-triggered thermal generation and carvacrol release. Core-shell nanoparticles (Fe3O4@PVP@NH2-MIL-88B(Fe), FPM; PVP = polyvinylpyrrolidone) are synthesized by loading PVP-modified Fe3O4 to NH2-MIL-88B(Fe), and then covalently immobilizing lysozyme onto the FPM surface through enzymatic reaction by microbial transglutaminase. The lysozyme-covered FPM is further employed as a host matrix for loading antibacterial carvacrol to synthesize Fe3O4@PVP@MIL-88B(Fe)-NH-lysozyme/carvacrol (FPMLC) nanozyme hybrid. This FPMLC can capture bacteria by electrostatic attraction and the FPMLC-bacteria composite is then assembled by an extra magnet. The lysozyme layer can degrade peptidoglycan of the bacterial cell wall, and the released carvacrol can disrupt the bacterial cell membrane under near-infrared (NIR) irradiation. Systematic antibacterial results demonstrate that the developed FPMLC nanozyme hybrid at a low dose of 100 mu g/mL completely inactivates (100%) both Escherichia coli and Staphylococcus aureus at cell density of 106 CFU/mL. This FPMLC exhibits high-efficiency antibacterial efficacy but no significant cytotoxicity in vitro, and therefore provides promising antibacterial applications in biomedical, environmental, and food fields.
The synthesis of highly diverse libraries has become of paramount importance for obtaining novel leads for drug and agrochemical discovery. Herein, the step-economical diversity-oriented synthesis of a library of various pyrimidine-N-heterocycle hybrids was developed, in which a 4,6-dimethoxypyrimidine core was incorporated into nine kinds of N-heterocycles. A total of 34 structurally diverse compounds were synthesized via a two-step process from very simple and commercially available starting materials. Further, in vivo biological screening of this library identified 11 active compounds that exhibited good post-emergence herbicidal activity against D. sanguinalis at 750 g ai per ha. More importantly, pyrimidine-tetrahydrocarbazole hybrid 5q showed good to excellent herbicidal activity against five test weeds at the same dosage. Pyrimidine-tetrahydrocarbazole hybrids represent a novel class of herbicidal agents that may become promising lead compounds in the herbicidal discovery process.
An efficient solvent-controlled regioselective reaction has been developed. The reaction represents a novel protocol for the divergent one-pot synthesis of pyrimidine and dihydrodibenzo[b,f][1,4]oxazepine derivatives.