AIMTo investigate the effects of sodium sulfonate daidzein (SSD) on stress-induced gastric ulcer and explore its possible mechanism.

METHODSUsing exhausted swimming and counting the number of gastric ulcer to establish the model of stress-induced gastric ulcer. Mouse experience intraperitoneal injection of different doses of SSD and L-NAME, and NDP histochemical method was used to detect the changes of nitric oxide synthase (NOS) positive neurons in stomach.

RESULTSSSD had dose-dependent protective effect on gastric mucosa. L-NAME could prevent stress induced gastric lesion. After combined injection of L-NAME and effective dose of SSD, the protective effect of SSD on gastric mucosa was reinforced. The number of NOS ganglion was constant, and effective dose of SSD had slight effect on NOS-positive neurons in normal mouse while it decreased NOS positive neurons in per area and in per ganglia after stress.

CONCLUSIONThe increased nitric oxide (NO) leads to gastric ulcer during stress, SSD has protective effect on gastric mucosa and this effect may be mediated by inhibiting NOS and restricting the overproduction of NO during stress.

Animals ; Gastric Mucosa ; drug effects ; pathology ; Isoflavones ; pharmacology ; Male ; Mice ; Mice, Inbred ICR ; Nitric Oxide ; metabolism ; Stomach Ulcer ; Stress, Physiological

Using chrysin as a leading compound, intermediate 5, 7-dihydroxy-6, 8-bis (hydroxymethyl) flavone (1) was synthesized by hydroxymethylation. The intermediate reacted with different alcohols to afford 5, 7-dihydroxy-6, 8-bis ( methoxymethyl) flavone (2), 6, 8-bis (ethoxymethyl) -5, 7dihydroxyflavone (3), 6, 8-bis-(butoxymethyl)-5, 7-dihydroxyflavone (4), 6, 8-bis (pentyloxymethyl) -5,7-dihydroxy flavone (5) and 6, 8-bis-(ethoxymethyl) -5-hydroxy-7-methoxyflavone (6). These compounds were characterized by IR, 1H NMR, 13C NMR and element analysis. The crystal structure of 6 was determined by X-ray crystal diffraction. The interaction of the derivatives with CT-DNA was studied by fluorescent spectroscopy. According to the Stern-Volmer equation, the quenching constants of the compounds 1 - 4 were measured, separately, they were K(q1) = 9.71 x 10(3) L x mol(-1), K(q2) = 2.25 x 10(4) L x mol(-1), K(q3) = 1.03 x 10(4) L x mol(-1) and K(q4) = 7.96 x 10(3) L x mol(-1). Compounds 1-4 showed higher binding affinity with DNA than chrysin did. The results provided the experimental basis for developing a more effective flavonoid and worthing further thoroughly study.
Animals ; Crystallography ; DNA ; metabolism ; Drug Interactions ; Flavones ; chemical synthesis ; chemistry ; Flavonoids ; chemical synthesis ; chemistry ; metabolism ; Magnetic Resonance Spectroscopy ; Molecular Structure ; X-Ray Diffraction

A water-soluble compound, sodium formononetin-3'-sulfonate with good lipid-lowering and liver-protection activities was synthesized. It was synthesized by sulfonation reaction, and its structure was characterized by IR, NMR and elemental analyses. The solubility of sodium formononetin-3'-sulfonate in water and n-octanol/water partition coefficient were determined by UV spectrophotometry. The lipid-lowering and liver-protection activities of sodium formononetin-3'-sulfonate were tested by using rat's high fat model induce by feeding with high fat food. The results showed that sodium formononetin-3'-sulfonate not only had favorable water, solubility but also had good lipid-lowering and liver-protection activities.
Adipose Tissue ; drug effects ; Alanine Transaminase ; metabolism ; Animals ; Aspartate Aminotransferases ; metabolism ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Cholesterol, LDL ; blood ; Hypolipidemic Agents ; chemical synthesis ; chemistry ; pharmacology ; Isoflavones ; chemical synthesis ; chemistry ; pharmacology ; Lipids ; blood ; Liver ; enzymology ; pathology ; Male ; Molecular Structure ; Protective Agents ; chemical synthesis ; chemistry ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Solubility ; Triglycerides ; blood

A series of 6 novel 2-amino-4, 5-diarylpyrimidines were synthesized by the reaction of isoflavones with guanidine. They were identified by the spectra of IR, 1H NMR, 13C NMR and elemental analysis. The protective effects of 2-amino-4, 5-diarylpyrimidines against oxygen-glucose deprivation leading by sodium hydrosulfite in PC12 cells were studied by MTT method. It was shown that 2-amino-4, 5-diarylpyrimidines exhibited neuroprotective effects against oxygen-glucose deprivation injury in PC12 cells, which could increase the amount of survival PC12 cells and reduce their injured degree in the model.
Animals ; Cell Hypoxia ; drug effects ; Cell Survival ; drug effects ; Glucose ; deficiency ; Molecular Structure ; Neuroprotective Agents ; chemical synthesis ; chemistry ; pharmacology ; PC12 Cells ; Pyrimidines ; chemical synthesis ; pharmacology ; Rats

To explore new biflavones, 7-hydroxy-8-hydroxymethyl-4'-methoxyisoflavone (1), (5, 7-dihydroxyflavone-8-yl)-(7'-hydroxy-4"-methoxyisoflavone-8'-yl)methane (2), bis(7-hydroxy-4'-methoxyflavone-8-yl) methane (3), bis(3', 5'-diisopropyl-7, 4'-dihydroxy-isoflavone-8-yl)methane (4), and bis(7-hydroxy-isoflavone-8-yl) methane (5) were designed and synthesized from chrysin, formononetin, 7, 4'-dihydroxy-3', 5'-diisopropyl-isoflavone and 7-hydroxy-isoflavone. Their structures were identified with IR, 1H NMR, 13C NMR and elemental analysis. The binding of 1-5 with DNA was studied with fluorescent spectroscopy. Compounds 2-5 showed higher binding affinity with DNA than 1. According to the Stern-Volmer equation, the binding constants of 2, 3 were determined at 35 degrees C and 25 degrees C respectively, they were Kq2 (25 degrees C) = 1.95 x 10(4) Lx mol(-1) and Kq2 (35 degrees C) = 1.67 x 10(4) L x mol(-1); Kq3 (25 degrees C) = 1.89 x 10(4) L x mol(-1) and Kq3 (35 degrees C) = 1.58 x 10(4) L x mol(-1). The quenching mechanism of 2, 3 was suggested as static quenching.
Biflavonoids ; chemical synthesis ; chemistry ; DNA ; chemistry ; Flavonoids ; chemical synthesis ; chemistry ; Molecular Structure

Objective To examine the effects of application of ultrasonography guided water injection for inser-tion of naso-jejunal tubes. Methods Hospitalized patients in ICU who needed naso-jejunal tubes were recruited from one tertiary hospital in Beijing from November 2016 to April 2017. Ultrasonography guided water injection was used to assist insertion of naso-jejunal tubes. Meanwhile,we conducted semi-structured interviews to learn feel-ings and suggestions from the patients. Results A total of 40 patients were included in this study,37 patients (92.5%) were successfully inserted with the tubes at the first attempt. The duration of insertion of naso-jejunal tubes was 25 (20,38.75) min. Conclusion Ultrasonography guided water injection is a simple and convenient method to guide the placement of naso-jejunal tubes for critical ill patients,which provides guarantee for early en-teral nutrition.

The solubility/dissolution, hygroscopicity and mechanical properties of drug candidates have a profound effect on oral bioavailability, processability and stability. The physicochemical properties of crystalline drug are closely related to inner crystal structure. Crystal engineering technologies, as strategies of altering the crystal structure and tailoring physicochemical properties at molecular level, possess the potential of enhancing the pharmaceutical performance of product. The current article reviewed the modification of drug solubility/dissolution, hygroscopicity and mechanical properties by crystal engineering technologies through polymorphic selection, amorphization/co-amorphization, as well as co-crystallization, which provided a reference for the applications of pharmaceutical crystallography in improving physicochemical properties and druggability.

The global pandemic of coronavirus disease 2019 (COVID-19) has brought great challenges to the traditional medical model. During the outbreak of COVID-19 in Shanghai, China, from March to May, 2022, there was a significant increase in the number of pediatric cases due to high transmissibility, immune escape, and vaccine breakthrough capacity of Omicron variants. The designated hospitals for children with COVID-19 served as a connecting link between children's specialized hospitals and mobile cabin hospitals. From April 7 to June 2, 2022, a total of 871 children with COVID-19 were admitted to Renji Hospital, Shanghai Jiao Tong University School of Medicine (South Branch), a designated hospital for children with COVID-19. Among these patients, 568 (65.2%) were children under 3 years old, 870 (99.9%) were mild or moderate, and 1 was severe. This article reports the experience in the management of pediatric cases in this designated hospital, which included the following aspects: establishing an optimal case-admission process; strengthening multidisciplinary standardized diagnosis and treatment; optimizing the management, warning, and rescue system for severe COVID-19; implementing family-centered nursing care; formulating an individualized traditional Chinese medicine treatment regimen; optimizing the discharge process and strengthening bed turnover; implementing strict whole-process control to reduce the risk of nosocomial infection; constructing a structured medical record system and using information platforms to adapt to the work mode of large-volume cases; conducting scientific research and sharing the experience in diagnosis and treatment.
COVID-19 ; Child ; Child, Preschool ; China ; Hospitals, Pediatric ; Humans ; SARS-CoV-2

Background: Youths are disproportionally affected by the human immunodeficiency virus (HIV) infection. We aimed to assess antiretroviral therapy (ART) initiation and viral suppression rates among student and non-student youths in Hangzhou, China. Methods: Data were taken from the Chinese HIV/acquired immune deficiency syndrome Comprehensive Response Information Management System. Youths aged 15 to 24 years who were newly diagnosed with HIV between 2012 and 2016 and were living in Hangzhou were included in the study. Comparisons between student and non-student youths were made for ART initiation within 30 days, 90 days, and 12 months of HIV diagnosis, and the viral suppression rate at 12 months of HIV diagnosis and at 12 months of ART initiation. Results: A total of 707 cases met inclusion criteria, 29.6% of which were students and 70.4% were non-student youths. The student group had a higher proportion of ART initiation compared with the non-student group within 30 days of diagnosis (45.5% vs. 37.0%, P = 0.044), and a slightly higher but not statistically significant proportion at 90 days (67.0% vs. 62.7%), and 12 months (83.7% vs. 78.5%) of HIV diagnosis. ART initiation within 30 days improved from <15% in 2012 to over 65% in 2016 in both groups, and ART initiation within 90 days improved from <30% in 2012 to >90% in 2016. A smaller proportion of students experienced viral suppression compared with the non-student group (9.6% vs. 17.1%, P = 0.011) at 12 months after HIV diagnosis, but the suppression rate was similar at 12 months of ART initiation (69.9% vs. 71.1%, P = 0.743). Conclusions ART initiation in both student and non-student youths has significantly improved between 2012 and 2016. However, the viral suppression rate remained unacceptably low at 12 months of HIV diagnosis in both student and non-student groups. Specific intervention strategies must be taken to address this challenge.

Realgar nanoparticles (NPs) are increasingly used as therapeutic agents for their enhanced anti-proliferation effect and cytotoxicity on cancer cells. However, the alteration of particle size may enhance biological reactivity as well as toxicity. A LC/MS and GC/MS based metabolomics approach was employed to explore the mechanism of realgar NPs-induced hepatotoxicity and identify potential biomarkers. Male Sprague-Dawley rats were administrated intragastrically with realgar or realgar NPs at a dose of 1.0 g·kg·d for 28 days and toxic effects of realgar NPs on liver tissues were examined by biochemical indicator analysis and histopathologic examination. Increased levels of serum enzymes and high hepatic steatosis were discovered in the realgar NPs treated group. Multivariate data analysis revealed that rats with realgar NPs-induced hepatotoxicity could be distinctively differentiated from the animals in the control and realgar treated groups. In addition, 21 and 32 endogenous metabolites were apparently changed in the serum and live extracts, respectively. Realgar NPs might induce free fatty acid and triglyceride accumulation, resulting in hepatotoxicity. In conclusion, the present study represents the first comprehensive LC/MS- and GC/MS-based metabolomics analysis of realgar NPs-induced hepatotoxicity, which may help further research of nanotoxicity.
Animals ; Biomarkers ; blood ; chemistry ; Chromatography, Liquid ; methods ; Fatty Acids ; metabolism ; Gas Chromatography-Mass Spectrometry ; methods ; Liver ; chemistry ; drug effects ; metabolism ; Male ; Mass Spectrometry ; methods ; Metabolomics ; methods ; Nanoparticles ; toxicity ; Rats ; Rats, Sprague-Dawley ; Triglycerides ; metabolism