Design, synthesis, and herbicidal activity of indole-3-carboxylic acid derivatives as potential transport inhibitor response 1 antagonists.

Auxins as an important class of phytohormones play essential roles in plant life cycle; therefore, developing compounds with auxin-like properties for plant growth regulation and weed control applications is of great significance. Herein, we reported the design, synthesis, and herbicidal activity evaluation of a series of novel indole-3-carboxylic acid derivatives as auxin receptor protein TIR1 antagonists. Petri dish herbicidal activity assay demonstrated that most of the as-synthesized target compounds exhibited good-to-excellent inhibition effects (60-97% inhibitory rates) on roots and shoots of both dicotyledonous rape (B. napus) and monocotyledonous barnyard grass (E. crus-galli). The inhibition rates of compounds 10d and 10h reached up to 96% and 95% for the root of rape (B. napus) at 100 mg/L, and they also maintained 92% and 93% inhibition rates even if at 10 mg/L, respectively. Molecular docking revealed that the interactions between these synthesized target compounds and TIR1 protein include tight π-π stacking, hydrogen bond, and hydrophobic interactions. This work expands the range of auxin chemistry for the development of new auxin mimic herbicides.

[Effect of Gegen Qinlian Decoction on gut microbiota of irritable bowel syndrome with diarrhea rats].

This study aims to explore the effect of Gegen Qinlian Decoction on gut microbiota of irritable bowel syndrome with diarrhea(IBS-D) rats. A total of 36 male SD rats were randomly classified into the control group, model group, rifaximin group(150 mg·kg~(-1)), and high-dose(8.125 g·kg~(-1)), medium-dose(4.062 5 g·kg~(-1)) and low-dose(2.031 3 g·kg~(-1)) Gegen Qinlian Decoction groups with the random number table method, 6 in each group. After modeling, rats were treated for 8 days. The general state, bristol stool chart(BSC) score, and the minimum volume threshold for abdominal withdrawal reflex were recorded. Pathological changes of colon tissues were observed based on hematoxylin and eosin(HE) staining, and gut microbiota was analyzed based on 16 S rRNA sequencing. Compared with the model group, rifaximin group and high-dose and medium-dose Gegen Qinlian Decoction groups showed low BSC score(P<0.01) and high minimum volume threshold for abdominal lifting(P<0.05). HE staining showed that Gegen Qinlian Decoction could relieve intestinal inflammation. 16 S rRNA sequencing suggested obvious variation of gut microbiota in IBS-D rats. Gegen Qinlian Decoction significantly raised the richness index and diversity index of gut microbiota, regulated the number of the flora, and improved alpha diversity and beta diversity. Species composition of gut microbiota and LEfSe analysis showed that Gegen Qinlian Decoction could significantly increase the ratio of Bacteroidota to Firmicutes, elevate the abundance of probiotics such as Clostridia and Lachnospirales, and reduce the abundance of conditional pathogens such as Bacteroidales, and Prevotellaceae. PICRUSt2 analysis indicated that Gegen Qinlian Decoction was mainly related to multiple metabolic pathways such as carbohydrate metabolism and amino acid metabolism. In summary, Gegen Qinlian Decoction can significantly reduce visceral hypersensitivity of IBS-D rats, alleviate intestinal inflammation, and relieve clinical symptoms such as diarrhea. The mechanism is the likelihood that it regulates the composition and structure of gut microbiota and improves its metabolic pathway as well.

Automatic Masseter Thickness Measurement and Ideal Point Localization for Botulinum Toxin Injection.

Botulinum toxin injection is a highly efficacious treatment for masseter muscle hypertrophy, while manual injection point localization based on experience can be non-quantitative, subjective and therefore suboptimal and even side-effect risky. To address this important while challenging task, in this paper we present a methodology of automatic ideal point localization for botulinum toxin injection based on automatic segmentation, measurement and quantitative analysis. Specifically, we first present a novel three-dimensional (3D) fully convolutional neural network for fully automatic mandible and masseter regions of interest (RoI) localization and segmentation from head computed tomography (CT) images. Given the segmentation results, the ideal injection points on the face are located using ray casting based automatic thickness measurement. We conducted experiments on an internal dataset consisting of head CT images acquired from 53 patients to evaluate the segmentation performance and localization reliability. The results demonstrate that the segmentation framework outperforms the state-of-the-art method by a significant margin, and the localization system provides intuitive, interactive user interface and reliable injection point decisions.

[The coastal areas of Yantai human and swine hepatitis E virus genotyping analysis].

OBJECTIVE: Survey of the coastal city of Yantai, from human and swine hepatitis E virus (HEV) genotype correlation. METHOD: Application of reverse transcription nested polymerase chain reaction (RT-nPCR) method for local acute sporadic hepatitis E patients,normal population of HEV-IgM positive and local pig farm pigs were HEV RNA detection. And HEV RNA positive samples for cloning sequencing and sequence analysis. RESULTS: In 16 patients with acute sporadic hepatitis E in 7 cases of RNA positive stool specimens of HEV; 51 IgM positive sera of normal people in specimens with 1 HEV RNA positive; 34 pig bile specimens with 1 HEV RNA positive. Sequence analysis revealed the region HEV strains and swine strains in the ORF2 region of nucleotide sequence homology is 87%-98.1%. 7 strains of hepatitis E virus genotype in patients and 1 strains of swine hepatitis E virus genotypes are type IV, gene sequence homology between the 87%-98.1%; there were 6 patients and porcine gene sequence homology in 93.9%-98.1% between,for type a subtype; 1 patients and porcine gene sequence homology in 87%, for the type D subtype. Normal population of 1 cases of hepatitis E virus genotype for I type D subtype. Human and porcine HEV ORF2 gene fragment and HEV part I-IV representative strains were compared, and the nucleotide sequence homology were 82.5%-100%, 81.7%-92.9%, 81.4%-93.9%, 84.9%-100%. CONCLUSION: The area population prevalence of HEV in the presence of 2 genotype 3 subtype genes, mainly to IV A, in pigs with popular HEV gene with a high homology; HEV type I in the crowd disperses in the presence of.

[Isolation and sequence analysis on virus of HFMD with encephalitis in Yantal city].

OBJECTIVE: To learn about the pathogen spectrum and genetic characterization of HFMD with encephalitis in Yantai city. METHODS: Stool samples and cerebrospinal fluids (CSF) collected from HFMD with encephalitis cases in Yantai. Virus were isolated from stool samples and identified by fluorescence reverse transcription-polymerase chain reaction. The VPl region was amplified and sequenced from positive specimens. Genetic characterization was identified by sequence analysis. RESULTS: Getting 3 virus strains from 10 stool specimens and all of them belong to EV71. The nucleotide and amino acid homogeneity with the representative isolates of C4a were 98%-99% and 98.90%-99.45% respectively. CONCLUSION: The pathogen of HFMD with encephalitis in Yantai city were mainly EV71 wich belong to subgenogroup C4 cluster C4a.