Objective: To investigate the inhibition of rutaecarpine, a main component in Evodiae Fructus, on the hepatic metabolism of five Coptis alkaloids, and to provide the basis for further study of compatibility mechanism between Coptidis Rhizoma and Evodiae Fructus. Methods: Using rat liver microsome incubation method, the inhibition of rutaecarpine on hepatic metabolism of five Coptis alkaloids in vitro was investigated. Results: Rutaecarpine could inhibit the in vitro hepatic metabolisms of coptisine, epiberberine, berberine, palmatine, and jatrorrhizine. The half inhibitory concentration (IC50) was all greater than 50 μmol/L which showed rutaecarpine had a weak inhibition on Coptis alkaloids. The differences of inhibition constant (Ki) were statistically significant (P < 0.05). The order of inhibited extent was as follows: berberine > jatrorrhizine > palmatine > epiberberine > coptisine. Conclusion: The results could provide the basis to learn the major role on the links that Evodiae Fructus acted on Coptis alkaloids and reveal the compatibility mechanism between Coptidis Rhizoma and Evodiae Fructus.

Abstract: Objective　To analyze the distribution and drug resistance evolution characteristics of pathogenic bacteria of bloodstream infection in nine tertiary hospitals in Yunnan Province from 2017 to 2021, so as to provide reliable basis for rational selection of antibiotics in clinic. Methods Using the drug sensitive paper method or instrument method, the bacteria identification and drug sensitivity test were carried out in nine tertiary hospitals in different regions according to the unified technical scheme. The results were judged according to the Clinical and Laboratory Standards Institute (CLSI) breakpoint standard in 2021, and use WHONET5.6 for data statistical analysis. Results A total of 12 003 strains of pathogenic bacteria were isolated from bloodstream infection samples in the past five years, including 7 442 strains of Gram-negative bacteria (62.0%) and 4562 strains of Gram-positive bacteria (38.0%), with an increasing trend in the number of isolated strains; of these, 163 strains (1.4%) were isolated from outpatients and 11 840 strains (98.6%) were isolated from inpatients. The top three gram-negative bacteria were Escherichia coli, Klebsiella pneumoniae and Acinetobacter baumannii, of which 309 strains (4.2%) were carbapenem-resistant Klebsiella pneumoniae (CR-KPN), 29 strains (0.4%) carbapenem-resistant Escherichia coli and 19 strains (0.3%) carbapenem-resistant Enterobacter cloacae, and the number of CR-KPN was on the rise year by year. The top three Gram-positive bacteria were coagulase-negative staphylococci, Staphylococcus aureus and Enterococcus faecium, of which methicillin-resistant Staphylococcus aureus (MRSA) was detected for 213 strains, accounting for 27.7%, and decreased from 40.0% in 2017 to 23.4% in 2021, showing a downward trend year by year. No vancomycin-resistant staphylococci and enterococci were found. Conclusions The detection and composition of bloodstream infection pathogenic bacteria in multicenter have not changed much in the past five years, but each hospital has its own characteristics. The number of carbapenem resistant Enterobacteriaceae increased year by year, which should be paid more attention.

Tibetan Herbal medicine has its own complete theory based on five sources doctrine. And the theories of "Liuwei", "Baxing" and "Shiqi Gongxiao" formed the basic core components of the property theory of Tibetan medicine. However, books and literature of Tibetan medicine have never been systematically expounded and discussed about it specially which thus will limit the further development of Tibetan medicine theory. In this thesis, we firstly introduced three basic core components of the property theory-the "Liu Wei", "Baxing", and "Shiqi Gongxiao" and their interactions as well. At the same time, the links and similarities between the theory of Tibetan medicine and Chinese medicine theory were compared. The job of the thesis done above is to lay the foundation for further systematic reveal and development of Tibetan medicine theory.
Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Medicine, East Asian Traditional ; Phytotherapy ; Plants, Medicinal ; chemistry

OBJECTIVETo study effects of Yishen Kangxian Compound (YKC) and benazepril containing serums on HK-2 cells (human renal proximal tubule epithelial cells) in the process of renal tubular epithelial cells to mesenchymal myofibroblasts transdifferentiation (TEMT) by gene chip.

METHODSYKC and benazepril containing serums were prepared. Their inhibitory effects on HK-2 cells in the transforming growth factor-beta1 (TGF-beta1)-induced TEMT process were observed. HK-2 cells were randomly divided into four groups, i.e., the blank control group, the model group, the benazepril group, and the YKC group. The gross RNAs were extracted and purified by taking advantage of the HumanHT-12 v4 of IlluminaBeadChip. Differentially expressed genes were obtained after they were reversely transcribed to cDNA, incorporating biotin labeling probe, hybridized with GeneChip, picture signals of fluorescence in gene array scanned and compared with differential genes by computer analysis.

RESULTSDifferentially expressed genes were successfully identified by gene chip. Compared with the model group, there were 227 differentially expressed genes in the benazepril group, including 118 up-regulated genes and 109 downregulated genes. Compared with the model group, there were 97 differentially expressed genes in the YKC group, including 69 up-regulated genes and 28 down-regulated genes. The Gene Ontology (GO) analysis indicated that YKC was more actively involved in the regulatory process than benazepril in terms of cell damage, apoptosis, growth, NF-KB, protein kinase, neuron, and blood vessel growth.

CONCLUSIONSYKC and benazepril could inhibit the TEMT process of HK-2 cells. But YKC also had taken part in cell damage, apoptosis, growth,and more pathways of early stage TEMT.

Cell Line ; Cell Transdifferentiation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Epithelial Cells ; cytology ; drug effects ; Genomics ; Humans ; Kidney Tubules, Proximal ; cytology ; pathology

OBJECTIVETo evaluate the changes of plasma levels of the excitatory amino acid neurotransmitter aspartic acid (Asp), inhibitory neurotransmitter glycine (Gly) and asparagine (Asn) in patients with major depressive disorder (MDD).

METHODSPlasma samples were collected from 15 MDD patients (9 males and 6 females, aged 32-64 y) and 14 healthy subjects (7 males and 7 females, aged 30-65 y); and also collected from 7 MDD patients (5 males and 2 females) 2 months after antidepressant treatment. The plasma levels of amino acids were determined by high performance liquid chromatography with fluorescence detection method.

RESULTSPlasma Asp and Gly levels were significantly lower in MDD patients than those in controls (P<0.04). There were positive correlations between plasma levels of Gly and Asp, and between Gly and Asn (P<0.005) in the control group; while in MDD patients, a significant positive correlation was found only between plasma levels of Gly and of Asp (P<0.001). MDD patients did not show significant changes in plasma Asp, Asn and Gly levels after antidepressant treatment compared to those before treatment.

CONCLUSIONThe reduced plasma Asp and Gly levels may serve as a clinical biomarker for MDD.

Adult ; Aged ; Antidepressive Agents ; therapeutic use ; Asparagine ; blood ; Aspartic Acid ; blood ; Depressive Disorder, Major ; blood ; drug therapy ; Female ; Glycine ; blood ; Humans ; Male ; Middle Aged

OBJECTIVE[corrected] To study the cyclic peptides from Psammosilene tunicoides.

METHODThe constituents were separated and purified with chromatographic methods, identified by NMR, MS, UV and IR.

RESULTThree cyclic dipeptides: cyclo(-Pro-Val-) (1), cyclo(-Pro-Ala-) (2) and cyclo(-Pro-Pro-) (3), were isolated and identified.

CONCLUSIONCompound 1 and 2 are new natural products, compound 3 was isolated for the first time from Psammosilene tunicoides.

Caryophyllaceae ; chemistry ; Dipeptides ; chemistry ; isolation & purification ; Molecular Structure ; Peptides, Cyclic ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry

Epiberberine, one of the most important isoquinoline alkaloid in Coptidis Rhizoma, possesses extensive pharmacological activities. In this paper, the liquid chromatography-tandem mass spectrometry (LC-MS/MS) was used to study phase I and phase II metabolites. A Thermo HPLC system (including Surveyor AS, Surveyor LC Pump, Surveyor PDA. USA) was used. The cocktail probe drugs method was imposed to determine the content change of metoprolol, dapsone, phenacetin, chlorzoxazone and tolbutamide simultaneously for evaluating the activity of CYP2D6, CYP3A4, CYP1A2, CYP2E1 and CYP2C9 under different concentrations of epiberberine in rat liver microsomes. The result showed that epiberberine may have phase I and phase II metabolism in the rat liver and two metabolites in phase I and three metabolites in phase II are identified in the temperature incubation system of in vitro liver microsomes. Epiberberine showed significant inhibition on CYP2D6 with IC50 value of 35.22 μmol L(-1), but had no obvious inhibiting effect on the activities of CYP3A4, CYP1A2, CYP2E1 and CYP2C9. The results indicated that epiberberine may be caused drug interactions based on CYP2D6 enzyme. This study aims to provide a reliable experimental basis for its further research and development of epiberberine.
Animals ; Berberine ; analogs & derivatives ; chemistry ; metabolism ; Chromatography, High Pressure Liquid ; Cytochrome P-450 CYP2D6 ; metabolism ; Cytochrome P-450 CYP2D6 Inhibitors ; chemistry ; metabolism ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Male ; Microsomes, Liver ; drug effects ; enzymology ; metabolism ; Molecular Structure ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry

To figure out the stability and intestinal bacteria metabolites of rats in vitro of astragaloside IV ( AST), this research was done to explore the stability of AST in the artificial gastric juice. artificial intestinal juice and rat liver homogenate and the metabolism in rat intestinal in vitro. HPLC was used to calculate the remaining rate of AST in biological samples by measuring the content of AST, while metabolites were determined by combining the methods of TLC, HPLC and LC-MS/MS. It turned out that AST was difficult to metabolize in the artificial gastric juice, artificial intestinal juice and rat liver. Also, the metabolic pathway of AST was stepped by deglycosylation. Firstly, AST was converted to its secondary etabolites (6-O-β-D-glucopyranosyl- cycloastragenol, CMG) by removal of xylose moiety at C-3, then transformed into cycloastragenol (CAG) after hydrolytic removal of the glucose moiety at C-6. All the results suggested that the metabolism of AST in vivo occurs mainly in the intestinal by hydrolysis of glycosyl. In conclusion, hydrolysis of intestinal flora is the main reason that AST metabolizes.
Animals ; Bacteria ; metabolism ; Chromatography, High Pressure Liquid ; Drug Stability ; Intestines ; microbiology ; Liver ; metabolism ; Rats ; Rats, Sprague-Dawley ; Saponins ; chemistry ; metabolism ; Tandem Mass Spectrometry ; Triterpenes ; chemistry ; metabolism

OBJECTIVETo evaluate the endourethral surgery for the complicated urethra stenosis and urethratresia.

METHODSThe endourethral surgery, such as internal urethrotomy transurethral scar electrosectomy or transurethral scar plasmakinetic bipolar electrocautery (PKR) or transurethral laser cicatrectomy, were carried out in 46 cases suffering from the complicated urethra stenosis and urethratresia.

RESULTSThe curative rate in this series being achieved by once and twice or three times'operation were 80.43% (39/46) and 13.04% (6/46) respectively. Three cases of treatment failure were caused by long-segment stricture and urethratresia or severe malposition of the urethral proximal and distal to a narrow-caliber area or post-operation infection. Thirty-nine cases have been followed up for 6 to 84 months. Satisfactory voiding has been achieved in all patients.

CONCLUSIONEndoscopic surgery was believed to be a safe and efficient therapeutic choice for the complicated urethra stenosis and urethratresia. The success of the treatment depends on understanding the length of the stricture before operation, resecting completely the scar tissue with electric or PKR or laser technique during the process, preventing infection and managing appropriately the urethral catheterization after operation.

Adolescent ; Adult ; Aged ; Endoscopy ; Follow-Up Studies ; Humans ; Laser Therapy ; Male ; Middle Aged ; Retrospective Studies ; Urethra ; abnormalities ; surgery ; Urethral Obstruction ; surgery ; Urethral Stricture ; surgery ; Urogenital Surgical Procedures ; methods

OBJECTIVETo assess the feasibility of gray-scale contrast-enhanced ultrasound for characterizing thyroid nodules.

METHODSForty thyroid nodules from 35 patients were studied both by conventional techniques and gray-scale contrast-enhanced ultrasound. Of the nodules examined, 15 were benign and 25 malignant. The enhancement of echogenicity was evaluated. The diagnosis was confirmed by surgical biopsy and histopathological examination.

RESULTSThe study using gray-scale contrast-enhanced ultrasound showed absent contrast-enhancement in 9 of 25 malignant nodules and 1 of 11 benign solitary nodules; intense enhancement in 6 of 25 malignant nodules, with perfusion defect in the center; diffuse faint enhancement in 10 of 25 malignant nodules and 10 of 11 benign solitary nodules. Benign cystic nodules all showed absent enhancement in the cystic components and 2 of 4 intense enhancement in the solitary components.

CONCLUSIONSGray-scale contrast-enhanced ultrasonography imaging may be a useful tool for evaluating the perfusion of thyroid nodules. Solitary nodules showing absent enhancement or intense enhancement with absent enhancement in the nodular center may suggest malignant.

Contrast Media ; Diagnosis, Differential ; Female ; Humans ; Image Enhancement ; methods ; Male ; Thyroid Neoplasms ; diagnostic imaging ; pathology ; Thyroid Nodule ; diagnostic imaging ; pathology ; Ultrasonography ; methods