Objective:To synthesize substituted pyridine propynyl carbamates and to test their antimicrobial activities. Methods: Eight novel compounds were designed and synthesized. Antimicrobial tests in vitro were carried out with 8 common mildews (Aspergullus niger, Aspergillus flavus, Aspergillus versicolor, Trichoderma viride, Paecilomium varioti Bainier, Chaetomium globsum, Penicillium citrinum, Cladochytrium clodospoium) and 5 bacteria (Escherichia coli, Pseudomonas fluorescens, Bacillus fluorescens, Bacillus megatherium). Results: All compounds synthesized showed antimicrobial activity, especially the compound 1f, whose activity was more potent than that of compound 3-iodo-2-propynyl-butyl-carbamate (IPBC). Conclusion: Compound 1f is worth further studying and exploration.

The Chinese traditional medicine database intelligent inquiry and subject selecting system manages 4 databases of information on disease, herbs, their pharmacological effects and compound prescription intelligently and relatively. When a key word is input into the system, the associated information of herbs, their compound prescription, action and effects can be displayed immediately. The compound prescription can be quantitatively estimated as monarch, minister, assistant and guide in order. Following all associated data that are collected, the effective density of herbs can be arranged from a line. The design of the system has the characteristics of pertinence, flexibility, exoteric, convenience, friendship, multi-function, which can help investigator to select subject of traditional medicine scientifically. Moreover, it can be updated and extended when required. The system can promote information and modernization of researches on Chinese traditional medicine.

Objective:To investigate the mechanism of Coptidis rhizoma in the treatment of gastritis based on network pharmacology. Methods:The main components and targets of Coptidis rhizoma were screened by TCMSP and TCMID database. GeneCards were used to select the target genes related to gastritis from the human gene database, and the target genes related to gastritis were screened by Genemap in the OMIM database. We used R language VennDiagram package to crosse the gene targets of drugs and diseases, and screen the target of the main components of Coptidis rhizoma in the treatment of gastritis, and to use Cytoscape software to map the gene regulatory network of galangal in the treatment of gastritis, and to use the String database to construct the gene-protein of Coptidis rhizoma. The interaction visualization network map for protein- protein interaction (PPI) were screened out the core genes, and the Bioconductor in the R language was used to analyze the GO and KEGG pathways for the selected gene targets. Results:Fourteen main active compounds of Coptidis rhizoma were screened, and 71 gene targets may be involved in the treatment of gastritis. The results of GO and KEGG pathway analysis indicated that berberine mainly involves cytokine receptor binding, regulation of cytokine activity, and biological processes such as binding to heme, by regulating AGE-RAGE, IL-17, TNF, NF-kappa B and HIF-1. The signaling pathway acts to treat gastritis. Conclusions:This study constructed the role of berberine in the treatment of gastritis with multi-active component, multi-gene, multi-target pathway through network pharmacology. It comprehensively predicted the gene target and signaling pathway of Coptidis rhizoma in the treatment of gastritis, in order to further study the treatment of berberine. The mechanism of action of gastritis provides a reference basis.

Pyroptosis, a form of cell death associated with inflammation, is known to be involved in diabetic nephropathy (DN), and discoid domain receptor 1 (DDR1), an inflammatory regulatory protein, is reported to be associated with diabetes.However, the mechanism underlying DDR1 regulation and pyroptosis in DN remains unknown. We aimed to investigate the effect of DDR1 on renal tubular epithelial cell pyroptosis and the mechanism underlying DN. In this study, we used high glucose (HG)-treated HK-2 cells and rats with a single intraperitoneal injection of streptozotocin as DN models. Subsequently, the expression of pyroptosis-related proteins (cleaved caspase-1, GSDMD-N, Interleukin-1β [IL-1β], and interleukin-18 [IL-18]), DDR1, phosphorylated NF-κB (p-NF-κB), and NLR family pyrin domain-containing 3 (NLRP3) inflammasomes were determined through Western blotting. IL-1β and IL-18 levels were determined using ELISA. The rate of pyroptosis was assessed by propidium iodide (PI) staining. The results revealed upregulated expression of pyroptosisrelated proteins and increased concentration of IL-1β and IL-18, accompanied by DDR1, p-NF-κB, and NLRP3 upregulation in DN rat kidney tissues and HG-treated HK-2 cells. Moreover, DDR1 knockdown in the background of HG treatment resulted in inhibited expression of pyroptosis-related proteins and attenuation of IL-1β and IL-18 production and PI-positive cell frequency via the NF-κB/NLRP3 pathway in HK-2 cells. However, NLRP3 overexpression reversed the effect of DDR1 knockdown on pyroptosis. In conclusion, we demonstrated that DDR1 may be associated with pyroptosis, and DDR1 knockdown inhibited HG-induced renal tubular epithelial cell pyroptosis. The NF-κB/NLRP3 pathway is probably involved in the underlying mechanism of these findings.