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Natural products have long been a crucial source of, or provided inspiration for new agrochemical discovery. Naturally occurring 18β-glycyrrhetinic acid shows broad-spectrum bioactivities and is a potential skeleton for novel drug discovery. To extend the utility of 18β-glycyrrhetinic acid for agricultural uses, a series of novel 18β-glycyrrhetinic acid amide derivatives were prepared and evaluated for their antibacterial potency. Notably, compound 5k showed good antibacterial activity in vitro against Xanthomonas oryzae pv. oryzae (Xoo, EC50=3.64 mg L–1), and excellent protective activity (54.68%) against Xoo in vivo. Compound 5k induced excessive production and accumulation of reactive oxygen species in the tested pathogens, resulting in damaging the bacterial cell envelope. More interestingly, compound 5k could increase the activities of plant defense enzymes including catalase, superoxide dismutase, peroxidase, and phenylalanine ammonia lyase. Taken together, these enjoyable results suggested that designed compounds derived from 18β-glycyrrhetinic acid showed potential for controlling intractable plant bacterial diseases by disturbing the balance of the phytopathogen’s redox system and activating the plant defense system.

Studies in the past few years have shown that simple salts, such as pyridinium salts and imidazole salts, have excellent antibacterial activity. However, their application in drugs and agrichemicals development has been limited due to their high toxicity. In this study, we found that synthesized target compounds with pyridinium salt unit A1 and B6 displayed excellent anti-Xac (Xanthomonas. axonopodis pv. citri) and Xoo (Xanthomonas oryzae pv. oryzae) activity, with EC50 values of 7.67 μg/mL and 1.37 μg/mL, respectively. On searching for a toxicity reduction strategy, an ion exchange method was adopted to obtain a new type of various organic acid-decorated pyridinium salt derivatives containing with glycyrrhetinic acid framework, and their structure was characterized by FTIR and 1H NMR. Furthermore, bioassays and toxicity tests were used to show that these organic acid-exchanged compounds not only exhibited lower toxicity to plants but also had excellent antibacterial activity towards virulent phytopathogenic bacteria, especially compound D3, which provided an EC50 of 1.60 μg/mL toward Xoo. Subsequently, the pot experiments determined that compound D3 exhibited suitable protective and curative activities for the management of rice bacterial leaf blight at 200 μg/mL, with control efficacies of 54.09% and 38.50%, respectively. In addition, studies evaluating potential antibacterial mechanisms suggested that apoptosis was responsible for the antibacterial behavior of the target compounds. Overall, this study proved that the ion exchange method was a feasible strategy to reduce the toxicity of pyridinium salts and was promising for use in the development of novel antimicrobial agents.

Mammalian centromeres are generally composed of dispersed repeats and the satellites such as α-satellites in human and major/minor satellites in mouse. Transcription of centromeres by RNA polymerase II is evolutionary conserved and critical for kinetochore assembly. In addition, it has been found that the transcribed satellite RNAs can bind DNA repair proteins such as MRE11 and PRKDC, and excessively expressed satellite RNAs could induce genome instability and facilitate tumorigenesis. During the maturation of female oocyte, centromeres are critical for accurate segregation of homologous chromosomes and sister chromatids. However, the dynamics of oocyte centromere transcription and whether it associated with DNA repair proteins are unknown. In this study, we found the transcription of centromeres is active in growing oocytes but it is silenced when oocytes are fully grown. DNA repair proteins like Mlh1, Mre11 and Prkdc are found associated with the minor satellites and this association can be interfered by RNA polymerase II inhibitor α-amanitin. When the growing oocyte is in vitro matured, Mlh1/Mre11/Prkdc foci would release from centromeres to the ooplasm. If the oocytes are treated with Mre11 inhibitor Mirin, the meiosis resumption of growing oocytes with Mre11 foci can be suppressed. These data revealed the dynamic of centromeric transcription in oocytes and its potential association with DNA repair proteins, which provide clues about how oocytes maintain centromere stability and assemble kinetochores.

Abstract: Zinc tin oxide (ZnSnO3) materials, native and doped with Ti nanocomposites, were prepared by coprecipitation. In particular, we focus on the effect of Ti dopant on the ethanol sensing behavior of the ZnSnO3-based sensor. Results show that adding Ti ions evidently enhanced gas response of ZnSnO3. A gas adsorption model based on first principles was proposed to address the gas sensing mechanism. This study may open up an avenue for exploring other ABO3-type sensing materials. [Copyright &y& Elsevier]

Objective: To investigate the hydrolytic degradation of the kinetic characteristics of Potassium Dehydroandrographolidi Succinas (DAS-K) in aqueous solution., Methods: The HPLC method was used to determine the degradation kinetic parameters of DAS-K aqueous solution at different initial concentration, different pH, different ionic strength. various temperatures and in different buffer solutions., Results: DAS-K hydrolytic degradation followed first-order kinetics as measured by HPLC. From pH 8, the hydrolytic degradation rate of DAS-K markedly increased with pH. DAS-K was unstable in alkaline pH solution. The species of buffer solutions seem to have different impact on the catalytic process. The ionic strength did not have significant effect on the stability of the drug. According to the Arrhenius plot, the dependence of the decomposition on temperature was a determining factor, the activation energy was estimated to be 95.68 KJ/mol in phosphate buffer solution at pH 8 and temperature from 60 to 90 degrees C., Conclusion: It was found that the hydrolytic degradation of DAS-K complied with first-order kinetics. The rate of hydrolytic degradation of DAS-K depended on the pH of solution, the buffer concentration, the buffer species and the temperature. Especially, pH value was an important factor in determining the rate of the hydrolytic degradation of the drug.