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Cyclic dinucleotides (CDNs) play important physiological roles in bacteria, mammals and insects as a novel class of signaling molecules. However, the application of CDNs in agricultural pest control has not been reported yet. To explore the potential bioactivity of CDNs on agricultural pests, we synthesized ten kinds of CDNs containing adenine and guanine bases with different internucleotide linkages (3′,3′; 2′,3′; 2′,2′). The target CDNs were used to determine the antifeedant and insecticidal activity against common Lepidoptera pests including S. frugiperda, M. separata, and H. armigera. The bioassay tests indicated that 3′,3′-c-di-AMP showed the highest antifeedant activity (EC50 = 0.59 mg/L) against M. separata larvae among all the tested CDNs. Regarding insecticidal activity, 2′,3′-c-di-AMP showed higher insecticidal activity against M. separata larvae with LC50 of 55.4 mg/L. RNA-seq further revealed that 3′,3′-c-di-AMP and 2′,3′-c-di-AMP exhibited a significant effect on the growth and development process of insects. More importantly, the bioactivity of 3′,3′-c-di-AMP was also closely correlated with the stimulation of insect immune inflammation. These results indicated that cyclic dinucleotides can affect the normal physiological process of insects, providing a new direction for managing pests.

In this study, three eugenol fragment-containing haptens were synthesized, and a monoclonal antibody (mAb) selective for five commonly-found eugenol compounds (EUGs, i.e., eugenol, isoeugenol, methyl eugenol, methyl isoeugenol, and acetyl isoeugenol) was obtained. Based on this mAb, a broad-spectrum indirect competitive ELISA for high-throughput detection of five EUGs was developed. The detection limits for eugenol, isoeugenol, methyl eugenol, methyl isoeugenol and acetyl isoeugenol in both tilapia and shrimp samples were 25.3/ 50.6 μg/kg, 0.075/0.15 μg/kg, 0.48/0.96 μg/kg, 0.16/0.32 μg/kg, and 18.16/36.32 μg/kg, respectively. The recoveries for five EUGs ranged from 80.4 to 114.0 % with a coefficient of variation less than 11.5 %. Moreover, homology modelling and molecular docking were conducted to elucidate the interactions mechanism of mAb-EUGs. The work provides a promising tool for high-throughput screening of EUGs in aquatic products, which can serve as a benchmark for designing haptens and developing immunoassays for other small molecules.

Abstract [Objective] Apocynum venetum L. is an important wild plant germplasm in China, which has important medicinal, ecological, and economic values. Although A . venetum is strong in salt tolerance, its wild population is gradually declining due to habitat destruction and increased soil salinization. Therefore, exploring the mechanism of salt tolerance in A . venetum is crucial for the protection and utilization of wild germplasm resources. [Methods] In the present study, a tandem mass tag (TMT)-based quantitative proteomics technology was used to conduct quantitative proteomic study of A . venetum under salt stress. Common differentially expressed proteins and core proteins were screened using Venn analysis and protein network interaction analysis methods. [Results] (1) Eleven common differentially expressed proteins were identified, which were mainly involved in protein-FAD linkage, negative regulation of transporter activity, negative regulation of ion transporter activity, negative regulation of anion transmembrane transport, negative regulation of anion channel activity, and thiazole metabolism. (2) Ribosomal proteins were the main proteins obtained by the interaction of differential protein networks at different stress times, among which the ribosomal protein L2-2 (TRINITY_DN13265_c0_g1_i1_9) was the core protein in differential proteins at 12 h and 24 h under stress. The results indicate that the ribosomal proteins play an important role in response to salt stress in A . venetum . [Conclusion] In the present study, the key proteins of A . venetum in response to salt stress were screened, and the molecular resources in response to salt stress in A . venetum were expanded, which provide theoretical bases for the discovery and utilization of natural resistant germplasms of A . venetum .

Abstract In conventional solid-phase peptide synthesis (SPPS), α-amino groups are protected with alkoxycarbonyl groups (e.g., 9-fluorenylmethoxycarbonyl [Fmoc]). However, during SPPS, inherent side reactions of the protected amino acids (e.g., α-C racemization and aspartimide formation) generate by-products that are hard to remove. Herein, we report a thiol-labile amino protecting group for SPPS, the 2,4-dinitro-6-phenyl-benzene sulfenyl (DNPBS) group, which is attached to the α-amino group via a S–N bond and can be quantitatively removed in minutes under nearly neutral conditions (1 M p-toluenethiol/pyridine). The use of DNPBS greatly suppresses the main side reactions observed during conventional SPPS. Although DNPBS SPPS is not as efficient as Fmoc SPPS, especially for synthesis of long peptides, DNPBS and Fmoc are orthogonal protecting groups; and thus DNPBS SPPS and Fmoc SPPS can be combined to synthesize peptides that are otherwise difficult to obtain.

Inversion tillage with straw amendment is widely applied in northeastern China, and it can substantially increase the storage of carbon and improve multiple subsoil functions. Soil microorganisms are believed to be the key to this process, but research into their role in subsoil amelioration is limited. Therefore, a field experiment was conducted in 2018 in a region in northeastern China with Hapli-Udic Cambisol using four treatments: conventional tillage (CT, tillage to a depth of 15 cm with no straw incorporation), straw incorporation with conventional tillage (SCT, tillage to a depth of 15 cm), inversion tillage (IT, tillage to a depth of 35 cm) and straw incorporation with inversion tillage (SIT, tillage to a depth of 35 cm). The soils were managed by inversion to a depth of 15 or 35 cm every year after harvest. The results indicated that SIT improved soil multi-nutrient cycling variables and increased the availability of key nutrients such as soil organic carbon, total nitrogen, available nitrogen, available phosphorus and available potassium in both the topsoil and subsoil. In contrast to CT and SCT, SIT created a looser microbial network structure but with highly centralized clusters by reducing the topological properties of average connectivity and node number, and by increasing the average path length and the modularity. A Random Forest analysis found that the average path length and the clustering coefficient were the main determinants of soil multi-nutrient cycling. These findings suggested that SIT can be an effective option for improving soil multi-nutrient cycling and the structure of microbial networks, and they provide crucial information about the microbial strategies that drive the decomposition of straw in Hapli-Udic Cambisol.

Spirotryprostatin alkaloids, a class of alkaloids with a unique spirocyclic indoledionepiperazine structure, were first extracted from the fermentation broth of Aspergillus fumigatus and have garnered significant attention in the fields of biology and pharmacology. The investigation into the pharmacological potential of this class of alkaloids has unveiled promising applications in drug discovery and development. Notably, certain spirotryprostatin alkaloids have demonstrated remarkable anti-cancer activity, positioning them as potential candidates for anti-tumor drug development. In recent years, organic synthetic chemists have dedicated efforts to devise efficient and viable strategies for the total synthesis of spirotryprostatin alkaloids, aiming to meet the demands within the pharmaceutical domain. The construction of the spiro-C atom within the spirotryprostatin scaffold and the chirality control at the spiro atomic center emerge as pivotal aspects in the synthesis of these compounds. This review categorically delineates the synthesis of spirotryprostatin alkaloids based on the formation mechanism of the spiro-C atom.

Breast cancer, characterized by its molecular intricacy, has witnessed a surge in targeted therapeutics owing to the rise of small-molecule drugs. These entities, derived from cutting-edge synthetic routes, often encompassing multistage reactions and chiral synthesis, target a spectrum of oncogenic pathways. Their mechanisms of action range from modulating hormone receptor signaling and inhibiting kinase activity, to impeding DNA damage repair mechanisms. Clinical applications of these drugs have resulted in enhanced patient survival rates, reduction in disease recurrence, and improved overall therapeutic indices. Notably, certain molecules have showcased efficacy in drug-resistant breast cancer phenotypes, highlighting their potential in addressing treatment challenges. The evolution and approval of small-molecule drugs have ushered in a new era for breast cancer therapeutics. Their tailored synthetic pathways and defined mechanisms of action have augmented the precision and efficacy of treatment regimens, paving the way for improved patient outcomes in the face of this pervasive malignancy. The present review embarks on a detailed exploration of small-molecule drugs that have secured regulatory approval for breast cancer treatment, emphasizing their clinical applications, synthetic pathways, and distinct mechanisms of action.

Moso bamboo is one of the economically most important plants in China. Moso bamboo is a monocarpic perennial that exhibits poor and slow germination. Thus, the flowering often causes destruction of moso bamboo forestry. However, how control of flowering and seed germination are regulated in moso bamboo is largely unclear. In this study, we identified 5 members (PhFT1-5) of the phosphatidyl ethanolamine-binding proteins (PEBP) family from moso bamboo genome that regulate flowering, flower architecture and germination, and characterized the function of these PEBP family genes further in Arabidopsis. Phylogenetic analysis revealed that 3 (PhFT1, PhFT2 and PhFT3), 1 (PhFT4) and 1 (PhFT5) members belong to the TFL1-like clade, FT-like clade, and MFT-like clade, respectively. These PEBP family genes possess all structure necessary for PEBP gene function. The ectopic overexpression of PhFT4 and PhFT5 promotes flowering time in Arabidopsis, and that of PhFT1, PhFT2 and PhFT3 suppresses it. In addition, the overexpression of PhFT5 promotes seed germination rate. Interestingly, the overexpression of PhFT1 suppressed seed germination rate in Arabidopsis. The expression of PhFT1 and PhFT5 is significantly higher in seed than in tissues including leaf and shoot apical meristem, implying their function in seed germination. Taken together, our results suggested that the PEBP family genes play important roles as regulators of flowering and seed germination in moso bamboo and thereby are necessary for the sustainability of moso bamboo forest.

Strigolactones (SLs) are a new class of phytohormones that not only act as signalling molecules with external rhizospheric fungus and stimulate the seed germination of root parasite weeds, but also regulate many aspects of plant development, such as regulating root and shoot architecture. These intriguing properties, which in turn, make SLs great potency for applications in agriculture. In this review, we highlight the recent advancements in applying SLs and their agonists or antagonists for agricultural applications, including controlling root parasite weeds, improving plant nutrient availability, and regulating abiotic stress responses. Although many SL agonists or antagonists have been synthesized since the first isolation of SL, strigol, in 1966, there is still no commercial application of this class of molecule. We also present an overview of the possible challenges for the practical application of SL agonists or antagonists.

Strigolactone agonists could potentially help control noxious weeds by promoting suicidal germination. Here the authors describe a series of small molecule agonists that stimulate germination via the Striga ShHTL7 receptor and show that stereochemistry and hydrolysis-independent signalling mediate potency.

In the context of global food crisis, applying the phytohormone-brassinosteroids (BRs) in combination with the fungicide-pyraclostrobin (Pyr) was beneficial for plant quality and productivity in several field trials. However, in addition to the benefits of disease control due to the innate fungicidal activity of Pyr, it remains to be understood whether the coapplication of BL+ Pyr exerts additional growth-promoting effects. For this purpose, the effects of BL treatment, Pyr treatment, and BL+ Pyr treatment in Arabidopsis thaliana were compared. The results showed that the yield increased at a rate of 25.6% in the BL+Pyr group and 9.7% in the BL group, but no significant change was observed in the Pyr group. Furthermore, the BL+Pyr treatment increased the fresh weight of both the leaves and the inflorescences. In contrast, the Pyr and BL treatments only increased the fresh weight of leaves and inflorescences, respectively. Additionally, the BL + Pyr treatment increased the Pn, Gs, Tr, Vc, max, Jmax, VTPU, ETR, Fv’/Fm’, ΦPSII, Rd, AYE and Rubisco enzyme activity by 26%, 38%, 40%, 16%, 19%, 15%, 9%, 10%, 17%, 179%, 18% and 32%, respectively. While, these paraments did not change significantly by the BL or Pyr treatments. Treatment with BL + Pyr and Pyr, rather than BL, improved the chlorophyll a and chlorophyll b contents by upregulating genes related to chlorophyll biosynthesis and downregulating genes related to chlorophyll degradation. Additionally, according to transcriptomic and metabolomic analysis, the BL+ Pyr treatment outperformed the individual BL or Pyr treatments in activating the transcription of genes involved in photosynthesis and increasing sugar accumulation. Our results first validated that the combined usage of BL and Pyr exerted striking synergistic effects on enhancing plant biomass and yield by increasing photosynthetic efficiency. These results might provide new understanding for the agricultural effects by the co-application of BL and Pyr, and it might stimulate the efforts to develop new environment-friendly replacement for Pyr to minimize the ecotoxicology of Pyr.

Abstract Conquering the mutational drug resistance is a great challenge in anti-HIV drug development and therapy. Quantitatively predicting the mutational drug resistance in molecular level and elucidating the three dimensional structure-resistance relationships for anti-HIV drug targets will help to improve the understanding of the drug resistance mechanism and aid the design of resistance evading inhibitors. Here the MB-QSAR (Mutation-dependent Biomacromolecular Quantitative Structure Activity Relationship) method was employed to predict the molecular drug resistance of HIV-1 protease mutants towards six drugs, and to depict the structure resistance relationships in HIV-1 protease mutants. MB-QSAR models were constructed based on a published data set of K i values for HIV-1 protease mutants against drugs. Reliable MB-QSAR models were achieved and these models display both well internal and external prediction abilities. Interpreting the MB-QSAR models supplied structural information related to the drug resistance as well as the guidance for the design of resistance evading drugs. This work showed that MB-QSAR method can be employed to predict the resistance of HIV-1 protease caused by polymorphic mutations, which offer a fast and accurate method for the prediction of other drug target within the context of 3D structures.

ObjectiveMalnutrition is a common complication of Chronic Kidney Disease (CKD), and it is the risk factor of CKD prognosis. This study aim to evaluate the nutritional status of inpatients with CKD by using the Subjective Global Assessment (SGA), and to analyze the related factors of malnutrition; and to provide effective reference for early detection of malnutrition status in patients with CKD and timely nutrition intervention.MethodsA total of 426 patients (238 male patients, 188 female patients) aged 62.62 ± 14.61 and 61.14 ± 14.82, respectively admitted to the Nephrology Department of Wannan Medical College from February 2020 to December 2020 were selected and included in to this study by convenience sampling. 426 patients with CKD were evaluated by SGA. Human body weight, hemoglobin (Hb), total protein (TP), albumin (ALB), pre-albumin (PA), qualitative analysis of urinary protein and other laboratory indexes were collected and measured. The correlation between malnutrition and age, education, gender, diet, CKD stage and other factors was analyzed by spearman correlation analysis.ResultsThe incidence of malnutrition was 85.7% among 426 patients with CKD. Gender, age, education level, CKD stage, diabetes mellitus, weight loss and reduced food intake were related to SGA nutritional assessment (P < 0.05). The expression levels of ALB, PA and Hb in the malnutrition group were significantly lower than those in the normal group (P < 0.05). The degree of malnutrition in CKD patients was significant negatively correlated with the expression levels of ALB (r = −0.188), PA (r = −0.262) and Hb (r = −0.176) (P < 0.05). The multivariate Logistic regression analysis model showed that female (OR = 2.155), ≥60 years old (OR = 7.671), weight loss (OR = 10.691), reduced food intake (OR = 28.953), moderate and severe serum ALB expression (OR = 3.391 and 8.326) were risk factors for malnutrition in patients with CKD (P < 0.05). Malnutrition was correlated with the results of qualitative examination of urinary protein (r = 0.268, P < 0.05).ConclusionGender, age, weight loss, reduced food intake, serum ALB expression were independently associated with malnutrition in patients with chronic kidney disease, Hence, the medical staff should take timely and effective nutrition intervention for the patients with malnutrition, delay the renal function damage of patients with CKD and improve the quality of life of patients. Inpatients with CKD, especially women, should increase their dietary intake, maintain normal weight and improve their nutritional status.

Herein, a copper(I)‐catalyzed asymmetric 1,4‐hydroarsination of β‐substituted α,β‐unsaturated esters is achieved in moderate to excellent yields with high to excellent enantioselectivity, based on the proposed nucleophilic [Cu]−AsPh2 species. As for α‐substituted α,β‐unsaturated esters, a 1,4‐hydroarsination/enantioselective protonation event occurs smoothly in satisfying results. Furthermore, β‐substituted α,β‐unsaturated ketone, α,β‐unsaturated amide, and α,β‐unsaturated phosphine sulfide are well applied in the present catalytic system. Finally, some control experiments show that HAsPh2 is activated through coordination with the copper(I) catalyst and HAsPh2 exhibits inferior soft Lewis basicity to HPPh2 in the presence of a copper(I)‐bisphosphine complex. [ABSTRACT FROM AUTHOR]

Problems found in the record-filing inspection of the domestic ordinary cosmetics firstly in Shandong province from 2022 to 2023 was summarized. The problems found are classified and analyzed according to the filing material items, with a focus on the summarizing the common problems and proposing the corresponding suggestions. This paper intends to provide a guidance for the cosmetic filing personnel to submit filing materials in a standardized manner, as well as provide a reference for the cosmetic technical review departments and regulatory authorities. [ABSTRACT FROM AUTHOR]

Pressure-preserved coring is an effective means to develop deep resources. However, due to the complexity of existing pressure-preserved technology, the average success rate of pressure-preserved coring is low. In response, a novel in situ magnetically controlled self-sealing pressure-preserved coring technology for deep reserves has been proposed and validated. This innovative technology distinguishes itself from conventional methods by employing noncontact forces to replace traditional pretensioning mechanisms, thereby enhancing the mechanical design of pressure-preserved coring equipment and significantly boosting the fault tolerance of the technology. Here, we report on the design, theoretical calculations, experimental validation, and industrial testing of this technology. Through theoretical and simulation calculations, the self-sealing composite magnetic field of the pressure controller was optimized. The initial pre-tensioning force of the optimal magnetic field was 13.05 N. The reliability of the magnetically controlled self-sealing pressure-preserved coring technology was verified using a self-developed self-sealing pressure performance testing platform, confirming the accuracy of the composite magnetic field calculation theory. Subsequently, a magnetically controlled self-triggering pressure-preserved coring device was designed. Field pressure-preserved coring was then conducted, preliminarily verifying the technology's effective self-sealing performance in industrial applications. Furthermore, the technology was analyzed and verified to be adaptable to complex reservoir environments with pressures up to 30 MPa, temperatures up to 80 ℃, and pH values ranging from 1 to 14. These research results provide technical support for multidirectional pressure-preserved coring, thus paving a new technical route for deep energy exploration through coring. [ABSTRACT FROM AUTHOR]