ABSTRACT
Objective: To predict the target of Seabuckthorn polysaccharides in the prevention and treatment of cervical cancer, and to explore its multi-target and multi-pathway mechanism. Methods: Using the Swisstarget database, a total of 61 potential targets of polysaccharide active components were obtained. Cervical cancer related targets were obtained from the GeneCards database. The correlation score was greater than 5 targets for 2727; 15 intersection targets of active ingredients and disease were obtained by Venn diagram. Cytoscape3.6.0 software was used to construct the Polysaccharide composition-Target-Disease Network and Protein-Protein Interaction Networks (PPI). Cytoscape3.6.0 software was used for visualization and network topology analysis to obtain core targets. Kyoto encyclopedia of Genes and Genomes (KEGG) and Gene Ontology (GO) were analyzed using Metascape database. SailVina and PyMOL software were used for molecular docking to verify binding strength. Results: A total of 15 core targets were obtained for cervical cancer. These targets are significantly enriched in HIF-1 signaling pathway, Galactose metabolism, EGFR tyrosine kinase inhibitor resistance, growth factor receptor binding, carbohydrate binding, protein homodimerization activity and other GO and KEGG entries; Molecular docking showed that ADA and GLB1 were well bound to Glucose, D-Mannose, and Galactose. Conclusion: The effect of seabuckthorn polysaccharides on the prevention and treatment of cervical cancer is characterized by multi-component, multi-target and multi-pathway, which provides scientific basis for further research on the activity of seabuckthorn polysaccharides.
ABSTRACT
In order to investigate the fermentation process of Artemisia polysaccharides, this paper showcases an investigation into the effects of fermentation time, fermentation temperature, strain inoculum, Artemisia annua addition, and shaker speed on the polysaccharides production of Artemisia annua. The yield of Artemisia polysaccharides content was determined based on the optimization of single-factor test, and then a response surface test was conducted with temperature, inoculum, and time as response variables and the yield of Artemisia polysaccharides as response values. The fermentation process was then optimized and the antioxidant activity of Artemisia polysaccharides was monitored using DPPH, ABTS+, OH, and total reducing power. The optimum fermentation process was determined by the test to be 5% inoculum of Aspergillus niger, temperature 36°C, time 2 d, shaker speed 180 r/min, and 4% addition of Artemisia annua, and the extraction of Artemisia polysaccharides was up to 17.04% by this condition of fermentation. The polysaccharides from Artemisia annua fermented by Aspergillus Niger had scavenging effects on DPPH, ABTS, and OH free radicals.
ABSTRACT
OBJECTIVE: To predict the target of the active ingredient of lotus leaf for lowering fat and losing weight. Explore its multicomponent, multitarget, multipath mechanism. METHODS: Screen the main active ingredients of lotus leaves through the TCMSP database, and use the TCMSP database to predict the potential targets of the active ingredients. Obtain obesity-related targets from the human genome annotation (GeneCards) database. Use Venn software to take the intersection of the two to obtain the effect target of the lotus leaf lipid-lowering and weight-reducing effects. Use Cytoscape 3.6.0 software to construct an effective ingredient-target network. Use the STRING database to construct an intersection target protein interaction (PPI) network, visualize it with Cytoscape 3.6.0 software, and perform network topology analysis to obtain the core target. Use the DAVID database to perform gene ontology (GO) and metabolic pathway (KEGG) enrichment analysis for the above targets. Use AutoDockTools software for molecular docking to verify the binding strength. RESULTS: A total of 15 main active ingredients such as quercetin, isorhamnetin, sitosterol, and kaempferol were obtained, which can act on 135 targets related to obesity. These targets are significantly enriched in multiple GO and KEGG entries such as hypoxia response, positive regulation of gene expression, response to toxic substances, aging, and positive regulation of RNA polymerase II promoter transcription. Molecular docking shows that flavonoids such as quercetin have better binding to the target protein Akt1. CONCLUSION: The lipid-lowering and weight-reducing effects of lotus leaf embody the characteristics of multicomponent, multitarget, and multipathway of traditional Chinese medicine, which provides a certain scientific basis for the screening and in-depth study of the effective ingredients of lotus leaf.
ABSTRACT
BACKGROUND: Paclitaxel, a natural diterpenoid compound, has anti-tumor effect by acting on tubulin, whereas coumarin, another kind of natural product, has anti-tumor effect, along with some other effects, such as anti-bacterial-., Moreover, it also possesses fluorescence. OBJECTIVE: Multi targeting is an effective strategy in drug design to combat tumor. Therefore, a combination of paclitaxel with other active molecular drugs for exploring the novel lead with multi-functions is in demand. MATERIALS AND METHODS: To synthsize paclitaxel-coumarin conjugate via click chemistry and to investigate anticancer activity by MTT assay and the scratch test. RESULTS AND DISCUSSION: The results of MTT assay showed that compared tothe paclitaxel, the anti-tumor activity of the conjugate was significantly improved. The results of flow cytometry showed that the conjugate had a stronger ability to induce apoptosis. The scratch test results showed that the conjugate had better anti- metastasis ability than paclitaxel. CONCLUSION: These findings indicated that paclitaxel and coumarin had a synergistic effect, which paved the way for the development of paclitaxel through fluorescence.
