OBJECTIVE:To investigate the permeability of lomefloxacin through blood-pancreatic barrier in rats.METHO-DS:Lomefloxacin(20mg/kg body weight) was injected through caudal vein.At the given time points,the samples were collected.The concentrations of lomefloxacin in the serum,pancreatic tissue and liver tissue were measured by HPLC.RESULTS:The concentration-time profiles of lomefloxacin could be described as two-compartment model in rats.The peak concentrations in serum,pancreatic tissue and liver tissue were 65.550?g/ml,48.801?g/g and 84.121?g/g at 5 min post-injection respectively.Then the concentrations decreased quickly in all of them.Concentrations in pancreatic tissue were higher than those in serum at 10 min and even at 480 min post-injection.The permeation ratio (PR) through blood-pancreatic barrier was 0.744 at 5 min and rose to 3.817 at 480min.CONCLUSION:After intravenous injection,lomefloxacin can permeate blood-pancreatic barrier satisfactory,therefore it is worthy of being recommended for prevention and treatment of pancreatic infections.

Psoriasis is a chronic,refractory,inflammatory skin disease that occurs in young adults.The traditional animal model cannot simulate the skin characteristics of patients with psoriasis effectively, so it is difficult to be used for in-depth study of psoriasis mechanism. Immortalized human epidermal cells (HaCaT)is a non-tumor,immortalized human epidermal cell which is widely used in the study of dermatosis.HaCaT cells are the best choice for the study of psoriasis mechanism because their immu-nological characteristics and reproductive ability are coincide with the pathological features of psoriasis. This article reviews the specific methods such as establishment of cell method, cytokine and chemo-kine analysisin the pathogenesis study of psoriasis based on HaCaT cells, hoping to provide some thoughts for drug′s pharmacological activity research.

Coronavirus disease 2019 (COVID-19) is a highly contagious disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). More than one-third of patients with COVID-19 experience neurological symptoms, including confusion, headaches, and decreased/disordered taste. Alzheimer's disease (AD) is a slowly progressive neurodegenerative disease and the most common type of dementia. Alzheimer's disease patients are at high risk and susceptible to infection with COVID-19, which may cause severe illness and even death. There appears to be an interaction between AD and COVID-19, and on the one hand, patients with COVID-19 seem to be more likely to develop AD. AD patients, on the other hand, may be more susceptible to severe COVID-19. Therefore, understanding the common link between COVID-19 and AD may help to develop treatment strategies. Risk factors common to AD and COVID-19 are aging, ApoE ε4 allele, β-amyloid (Aβ) deposition, angiotensin-converting enzyme (ACE), neuroinflammation, oxidative stress. Here, this article focuses on the relationship between COVID-19 and AD, explores common risk factors and potential pathogenesis, and provides help for early prevention, treatment and recovery.

The excipient processing is an essential part of traditional Chinese medicine processing, and understanding its scientific connotations is a critical scientific issue that urgently needs resolution. Building upon a foundation where the composition of traditional Chinese medicine substances is fundamentally clear, this paper applies the techniques and methods of chemoinformatics to the study of the excipient processing mechanism. Relevant information on traditional Chinese medicines processed with four kinds of excipients (wine, vinegar, salt and honey) was collected, including properties, taste, meridian tropism, chemical components, etc. Molecular descritors and skeletons corresponding to each chemical component were calculated using chemoinformatics to characterize the properties and structural features of the components. Characteristic components associated with the four excipients (wine, vinegar, salt and honey) were explored through multivariate statistical analysis and Murcko skeleton analysis. Further analysis, taking honey-processed Astragali Radix as an example, the focus was on the impact of the processing excipient honey on the solubility and permeability of its characteristic pharmacologically active components (isoflavones). It was discovered that the excipient honey can increase their solubility and permeability, emphasizing that the impact of processing excipients on the pharmacological classification properties is a key breakthrough in elucidating the mechanism of excipient processing. In summary, this study analyzed the characteristic components associated with the processing excipients "wine, vinegar, salt and honey" based on their composition characteristics, providing data support for the research on the mechanism of excipient processing from a biopharmaceutical perspective.

BACKGROUND: The contact lenses were easily contaminated by adsorbing components from the tear film, particularly protein after wearing for a period of time. Lysozyme adsorption dynamics of fluorosilicone acrylate contact lenses has been studied in order to further improve data of protein adsorption, reduce adsorbing amount of surface protein, and prevent surface contamination of contact lenses.OBJECTIVE: To investigate the adsorption dynamics of fluorosilicone acrylate contact lenses to lysozyme in vitro. METHODS: A stock solution of lysozyme was prepared in Hanks balanced salt solution (2.0 g/L, solution Ⅰ) and different trifluoroacetic acid (TFA) concentrations were prepared. Recovery experiment, the contact lenses were placed in shaking incubator at 37 ℃ for varying time intervals. After incubation there was a single rinsing in Hanks balanced salt solution. Contact lenses in control group were placed in diluted water, and contact lenses in the other group were placed in different concentrations of TFA. For deposition, FSA contact lenses in experimental group were placed in shaking incubator at 37 ℃ for varying time intervals. After incubation there was a single rinsing in Hanks balanced salt solution. Then FSA contact lenses were immersed in 0.2% TFA solution. The amount of lysozyme was assayed with BCA method.RESULTS AND CONCLUSION: Lysozyme which attached to fluorosilicone acrylate contact lenses could be resolved by TFA, and the recovery was influenced by the immersed time and the concentration of TFA. The optimal time was 1 hour, and the optimum concentration was 0.2%. The adsorption dynamics of lysozyme on FSA contact lenses was a second-phased process, i.e., lysozyme adsorption increased rapidly during 10 minutes-1 hour, reached a plateau at 1 hour, stably adsorbed during 1-24 hours, and reached a saturation of 0.349 mg/cm~2. The recovery of lysozyme was lower at 10 and 30 minutes, but reached 90%-100% while the time of incubation was between 40 minutes and 24 hours.

Objective To investigate the mechanism of acute inflammatory response and tissue repair when rats accepted transplanted bone marrow mesenchymal stem cells (MSC) in severe acute pancreatitis (SAP).Methods A total of 40 rats were randomly divided into 4 groups which included the normal group (n=10),the model severe acute pancreatitis group (n=10),the transplanted bone marrow mesenchymal stem cells group (n =10),and the combination of bone marrow mesenchymal stem cells and granulocyte colony-stimulating factor (G-CSF) group (n=10).To cure the acute severe pancreatic injury caused by SAP,rats were injected with EDU-labeled MSCs and granulocyte colonystimulating factor (Gr-CSF).The conversion rate of MSCs to pancreatic cells or MSCs to endothelial cells was detected to assess the role of MSCs in tissue regeneration and repair.The expression of amylase,interleukin-6 (IL-6),and interleukin-10 (IL-10) in serum was detected to assess the role of MSCs in an acute inflammatory response.Results The concentrations of amylase and IL-6 were reduced and the concentration of IL-10 was increased in MSC and MSC+G-CSF groups after the onset of SAP.Flow cytometry showed a small amount of MSCs converting to endothelial or pancreatic cells,but the conversion rate was relatively low.Conclusions MSCs can play an important role in the antipre-release of inflammatory mediators,reducing acute immune response to control the acute inflammatory response in SAP.Moreover,MSCs can repair a damaged pancreas by converting into both pancreatic and endothelial cells.

OBJECTIVEThe present study investigated the effects of rapamycin on Aβ1-42-induced deficits in working memory and synaptic plasticity.

METHODSAfter bilateral hippocampal injection of Aβ1-42 and rapamycinin rats, spontaneous alternation in Y-maze and in vivo hippocampal long-term potentiation (LTP) of rats were recorded. All data were analized by two-way repeated measures analysis of variance (ANOVA).

RESULTS(Hippocampal injection of Aβ1-42 alone impaired working memory of rats; (2) Rapamycin did not affect working memory of rats, but alleviated Aβ1-42-induced working memory deficits, compared with Aβ1-42 alone group; (Aβ1-42 remarkably suppressed in vivo hippocampal LTP of fEPSPs in the CA1 region; (4) Pretreatment with rapamycin prevented Aβ1-42-induced suppression of LTP.

CONCLUSIONThese data indicates that rapamycin could protect against Aβ1-42-induced impairments in working memory and synaptic plasticity in rats.

Amyloid beta-Peptides ; adverse effects ; Animals ; Hippocampus ; drug effects ; Long-Term Potentiation ; Maze Learning ; Memory, Short-Term ; drug effects ; Neuronal Plasticity ; drug effects ; Peptide Fragments ; adverse effects ; Rats ; Sirolimus ; pharmacology

To prepare ginseng saponin Compound K with ultrasound-assisted total zymolytic ginseng saponins. The conversion rate was taken as the index to detect the pre-treatment factors such as ultrasonic power and ultrasonic time, as well as the impact of enzymatic factors, such as pH value, temperature, concentration of substrate, dosage of enzyme and reaction time, on the conversion rate. The response surface method was used to optimize the preparation conditions. The enzymolytic products were identified with MS, 1H-NMR and 13C-NMR. The results showed that the optimum conditions of the ultrasound-assisted enzymolysis were 250 W for ultrasonic power, 15 min for ultrasonic time, 5.5 for enzymolytic pH, 50 degrees C for enzymolytic temperature, 36 h for enzymolytic time, 4:5 for enzymolytic dosage: substrate and 1.0 g x L(-1) for concentration of substrate. The relative molecular mass of reaction products was 622.4. Therefore, the nuclear magnetic map verified that the reaction product was rare ginseng saponin Compound K. Under the above conditions, based on the total zymolytic ginseng saponins, the conversion rate of rare ginseng saponin Compound K was 6.91% in proportion to the total of ginsenosides. The process features gentle reaction conditions, high conversion rate and simple and reliable process, which is suitable for industrial production.
Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Enzymes ; chemistry ; Panax ; chemistry ; Plant Roots ; chemistry ; Saponins ; chemistry ; isolation & purification ; Ultrasonics ; methods

Objective To explore the therapeutic effect of lipid emulsion on acute organophosphorus poisoning and its consequence of acute lung injury. Methods A total of 48 sealant - grade Sprague-Dawley (SD) rats were randomly divided into four groups A,B,C,D,namely saline control group,lipid emulsion control group,the conventional therapy group and lipid emulsion administration group. After dichlorvos (DDVP) 11 mg/kg was given by intra-peritoneal injection,if there was no loss of DDVP during the injection process,the model of poisoning was considered to be made successfully.Then the rat models in four groups were respectively treated:with normal saline (5 ml/kg) intravenous injection in group A,lipid emulsion (5ml/kg) intravenous injection in group B,atropine (5 mg/kg) and pralidoxime chloride (40 mg/kg) intramuscular injection in group C,and combined use of lipid emulsion (5 ml/kg) with atropine and pralidoxime chloride in group D after administration of DDVP by intra-peritoneal injection.The activity of cholinesterase (CHE) in blood was detected before and 0.5 h,2 h and 4 h after DDVP poisoning. The clinical manifestations,the survival of rats,the wet weight of rat' s lung and the pathological changes of the lung tissue were observed within following 24 h. The rates of survival and symptoms of rats were compared between paired groups by using the x2 test,and the mean values of biomarkers were compared paired groups by using t test. Results In groups A and B,the intensity of muscular fasciculation and salivation were more severe and appeared sooner after DDVP exposure in comparison with groups C and D leading to lower survival rates in group A and B. Compared with group C,the rate of 24 h survival was higher and the intensity of muscular fasciculation was weaker in group D ( P ＜ 0.05 ).In group A and group B,the 24-hour survival rates were 1/12 and 2/12,respectively ( P ＜ 0.05 ).The levels of CHE in blood significantly decreased after DDVP poisoning ( P ＜ 0.05 ).There was no significant difference in activity of CHE between group B and group A,and in groups C and D,the levels of CHE in blood were not significantly higher than that in the group B 0.5 h after DDVP poisoning ( P ＜ O.05 ).In groups C and D,the activity of CHE in blood was significantly higher compared with group A and B,and that in group D was higher compared with C,and that in group B was higher compared with A 2 and 4 hours after DDVP poisoning ( P ＜ 0.05 ).In groups C and D,the wet weight of rat lung was significantly lighter compared with groups A and B,and that in group D was lighter compared with C,and that in group B was lighter compared with A 24 h after DDVP poisoning P ＜ 0.05 ).The electron microscopic findings showed the combined use of lipid emulsion with atropine and pralidoxime chloride obviously lessened the lung histopathologic changes after DDVP poisoning.Conclusions The lipid emulsion combined with atropine and pralidoxime chloride can be beneficial to controlling the toxic symptoms,reduce the death rate,accelerate the resume of the activity of CHE in blood,and relieve the lung injury induced by acute organophosphorus poisoning.

Objective To discuss the effect of Montelukast (Mont) on MDA,SOD,W/D,TNF-α,IL-10 and NF-κBp65 in lung tissue of Wistar rats poisoned by paraquat (PQ) and also to observe the pathological changes of the lung tissue.Methods A total of 104 Wistar rats were divided into 3 groups in random (random number),namely PQ group (n =40),Mont group (n =40) and control group (n =24).PQ (20 mg/kg) was administered by intra-peritoneal route to rats of PQ group and Mont group and narcotics were used for 2 hours.Mont in dose of 50 mg/kg was administered intra-gastrically to rats of Mont group per day and saline instead were administered to PQ group and control group per day until they were sacrificed for experiment.Of both PQ group and Mont group,10 rats were sacrificed at each interval of 1,3,5 and 7 days respectively after modeling,whereas 6 rats of control group were sacrificed at each interval.The levels of MDA and SOD in lung tissue and W/D of lung tissue,the levels of serum TNF-α and IL-10 and the level of NF-κBp65 in lung tissue were determined.Further,the specimen of lung tissue was prepared for electron microscopy observation.Results The level of MDA in lung tissue of PQ group was (8.19 ± 0.53) nmol/mg prot,which was significantly higher than that of control group on the 7th day.The level of SOD in lung tissue of PQ group was (128.76 ± 10.18) U/mg prot,which was significantly lower than that of control group.In PQ group,the W/D of lung tissue (6.62 ±0.42),level of serum TNF-α (156.16 ± 11.13) pg/ml,level of IL-10 (43.63 ±4.44) pg/ml and level of NF-κBp65 in lung tissue (0.23 ±0.02) were significantly higher than those in control group (P ＜0.01).In Mont group on the 7th day,the level of serum TNF-α (129.99 ±13.13) pg/ml,level of serum IL-10 (34.28 ± 3.80) pg/ml and level of NF-κBp65 in lung tissue (0.20 ±0.02) were significantly lower than those in PQ group (P ＜ 0.01).In the PQ group,pathological changes of lung tissue under the light and electron microscopes were acute diffused lung injury manifested itself in hemorrhage,effusion and infiltration of inflammatory cells inside the alveolar space,and the necrosis and defluxion of Ⅰ type and Ⅱ type epithelia cells.The pathological changes in Mont group were localized with infiltration of scanty inflammatory cells,and Ⅰ type epithelia cells were intact and there was no obvious necrosis of Ⅱ type epithelia cells.Conclusions Mont has protective effects on acute lung injury caused by PQ poisoning in rats.