ABSTRACT
Coptidis Rhizoma-Evodia Fructus is a classic herb pair in traditional Chinese medicine prescriptions, the famous prescription is called Zuojinwan, which comes from Danxi Xinfa, is composed of Coptidis Rhizoma-Evodia Fructus (6∶1). In this formula, Coptidis Rhizoma has the effect of clearing heat and drying diuresis, purging fire to remove toxin and clearing heart. Evodia Fructus has the effects of expelling cold and alleviating pain, checking upward adverse flow of Qi tostop vomiting, and assisting yang to stop diarrhea. Coptidis Rhizoma has the properties of bitter and cold, and Evodia Fructus has the properties of pungent and calidus. Pungent drugs have divergent effects, and bitter drugs have sedimentation effect, when used in combination, they can clear the liver and purge fire, calm the adverse-rising energy and stop vomiting. On the basis of Zuojinwan, Coptidis Rhizoma-Evodia Fructus medicine has derived different compatibility ratios. Different ratios are different in terms of efficacy, usage, clinical application. Although with the application of modern analytical instruments and the development of molecular pharmacology theory, the chemical constituents and Pharmacological effects of Coptidis Rhizoma and Evodia Fructus have been fully studied, as to the principle of compatibility, and the study of pharmacological effects and chemical constituents after the compatibility of the two drugs in different proportions, there is still no comprehensive system summary. This article makes a systematic and comprehensive explanation of Coptidis Rhizoma-Evodia Fructus from the aspects of famous literature, chemical composition, pharmacological effects and clinical applicationthrough querying literature and ancient books. In order to make this herb pair more standardized, and provide reference materials for further research and development for this herb pair.
ABSTRACT
Objective: To clarify the characteristics of drug pair of Coptidis Rhizoma-Euodiae Fructus on multi-components, multi-targets and multi-pathways based on the network pharmacology, and provide a theoretical reference for further study on the pharmacodynamic basis and mechanism of Coptidis Rhizoma-Euodiae Fructus against cancer and cardio-cerebrovascular diseases. Methods: Through the Traditional Chinese Medicine Systems Pharmacology (TCMSP) database, the parameters of oral bioavailability (OB ≥ 30%) and drug-likeness (DL ≥ 0.18) combined with the biological function, contents, research hotspot and other factors were used to screen out the active ingredients of the medicine pair of Coptidis Rhizoma - Euodiae Fructus. DrugBank and TCMSP databases were used to predict and analyze the targets, and Uniprot database was used to sort out all relevant genes affecting the targets. Combining the KEGG database for GO analysis and pathway analysis, "ingredients-targets-related diseases" network was constructed using Cytoscape software. Results: A total of 41 compounds and 212 potential target genes, as well as 44 signaling pathways were obtained after screening from Coptidis Rhizoma-Euodiae Fructus, and there were 44 major signaling pathways involved in 30 pathways related to cancer, seven pathways which were related to cardio-cerebrovascular diseases, seven pathways which were related to cancer and cardio-cerebrovascular diseases. Conclusion: The active ingredients of Coptidis Rhizoma-Euodiae Fructus can up-regulate the expression of cancer apoptosis genes through multi-components, multi-targets and multi-pathways, down-regulate the expression of cell cycle and apoptosis-related genes, and produce anti-cancer effect; Protecting vascular cells by inhibiting vascular calcification, and to achieve the effect of treating cardio-cerebrovascular diseases by inhibiting apoptosis and proliferation.
ABSTRACT
Viriditoxin is a fungal secondary metabolite of the fungus Paecilomyces variotii derived from the inner tissues of the giant jellyfish Nemopilema nomurai. Viriditoxin exhibits antibacterial activity against Streptococcus iniae and Streptococcus parauberis, which are major pathogens of aqua cultured fish. Viriditoxin induced abnormal cell morphologies in the fish pathogens S. iniae and S. parauberis, presumably by inhibiting FtsZ polymerization as was previously observed in Escherichia coli. Synthetic analogues of viriditoxin, designed based on docking simulation results to FtsZ of Staphylococcus aureus, were prepared and compared with viriditoxin for antibacterial activity. Reconstitution of free hydroxyl or carboxyl groups of the methoxyl or methyl ester groups of viriditoxin led to significant reduction of antibacterial activity, implying that the natural molecule is optimized for antibacterial activity to deter bacteria potentially harmful to Paecilomyces.
Subject(s)
Anti-Bacterial Agents/pharmacology , Scyphozoa/microbiology , Streptococcus/drug effects , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/metabolism , Bacterial Proteins/antagonists & inhibitors , Bacterial Proteins/metabolism , Binding Sites , Cytoskeletal Proteins/antagonists & inhibitors , Cytoskeletal Proteins/metabolism , Gram-Negative Bacteria/drug effects , Microbial Sensitivity Tests , Molecular Docking Simulation , Naphthols/chemistry , Naphthols/metabolism , Naphthols/pharmacology , Oxytetracycline/pharmacology , Paecilomyces/metabolism , Protein Structure, Tertiary , Staphylococcus aureus/metabolismABSTRACT
<p><b>OBJECTIVE</b>To observe the clinical efficacy and adverse reactions of Paroxetine combined with electro-acupuncture (EA) in treating depression.</p><p><b>METHODS</b>Forty-two patients with depression were randomly assigned to the observation group (22 patients) treated with EA combined with Paroxetine, and the control group (20 patients) treated with Paroxetine alone, and the therapeutic course for both groups was 6 weeks. The therapeutic efficacy and adverse reactions were evaluated with scores by Hamilton depression scale (HAMD) and treatment emergent symptoms scale (TESS), respectively.</p><p><b>RESULTS</b>HAMD scores determined at the end of the 1st, 2nd, 4th, and 6th week of the treatment course were significantly lower in the observation group than those in the control group (P<0.05). The significant improvement rate evaluated at the end of the 6-week treatment was remarkably higher in the observation group than that in the control group (72.7% vs 40.0%). No significant difference of TESS scores was found between the two groups.</p><p><b>CONCLUSION</b>EA combined with Paroxetine has better clinical efficacy than that of Paroxetine alone, with milder adverse reaction and quicker initiation of effect.</p>