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.

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

With low molecular weight chitosan and poloxamer 188 as the joint carriers, ginsenoside Rg3 solid dispersions were prepared by using the solvent evaporation method for an in vitro dissolution test. Subsequently, differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray diffraction (X-RD) were adopted for a phase analysis. The results showed that the 60 min in vitro cumulative dissolution rate of ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 at the ratio of 2:1 exceeded 90%, and the drug was dispersed in carriers in an amorphous state. Therefore, ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 could help significantly improve the drug dissolution, with a practical application value.
Chitosan ; chemistry ; Drug Compounding ; methods ; Ginsenosides ; chemistry ; Molecular Weight ; Poloxamer ; chemistry ; Solvents ; chemistry

Based on the transcriptome data, we cloned the open reading frame of IiHCT gene from Isatis indigotica, and then performed bioinformatic analysis of the sequence. Further, we detected expression pattern in specific organs and hairy roots treated methyl jasmonate( MeJA) by RT-PCR. The IiHCT gene contains a 1 290 bp open reading frame( ORF) encoding a polypeptide of 430 amino acids. The predicted isoelectric point( pI) was 5.7, a calculated molecular weight was about 47.68 kDa. IiHCT was mainly expressed in stem and undetectable in young root, leaf and flower bud. After the treatment of MeJA, the relative expression level of IiHCT increased rapidly. The expression level of IiHCT was the highest at 4 h and maintained two fold to control during 24 h. In this study, cloning of IiHCT laid the foundation for illustrating the biosynthesis mechanism of phenylpropanoids in I. indigotica.
Acyltransferases ; chemistry ; genetics ; metabolism ; Amino Acid Sequence ; Cloning, Molecular ; Gene Expression Regulation, Plant ; Isatis ; chemistry ; classification ; enzymology ; genetics ; Models, Molecular ; Molecular Sequence Data ; Open Reading Frames ; Phylogeny ; Plant Proteins ; chemistry ; genetics ; metabolism ; Quinic Acid ; metabolism ; Sequence Alignment ; Shikimic Acid ; metabolism

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.

BACKGROUND:There are reports concerning differentiation of adipose-derived mesenchymal stem cells(ADSCs)into chondrocytes using gene transfection technique.However,the transfection of adenovirus and adeno-associated virus into ADSCs is various.It is controversial whether adeno-associated virus(AAV)can transfect ADSCs.OBJECTIVE:To observe the enhanced green fluorescent protein(EGFP)expression following Ad5-EGFP and rAAV2-EGFP transfection into ADSCs,and investigate the cell proliferation ability following transfection.METHODS:ADSCs were isolated from the adipose tissue,which was from 6-month-old New Zealand albino rabbit back and neck by mechanical digestion and enzyme digestion,then ADSCs were cultured and amplified in vitro.ADSCs were infected with Ad5-EGFP and rAAV2-EGFP,and the EGFP expression was observed.A total of 2 μL sodium butyrate(1 mol/L)was added into the medium after rAAV2-EGFP transfection.MTT assay was used to detect the gene transfection effects on reproductive activity of ADSCs.RESULTS AND CONCLUSION:ADSCs isolated and cultured in vitro were flat,long-spindle and amplified stabry.The cell morphology was uniform.Many green fluorescent cells were observed in Ad5-EGFP and rAAV2-EGFP groups.Transfection efficiencies were about 88% and 83%.Adenovirus and adeno-associated virus vector can be transfected with ADSCs,and transfection efficiency is high.Adeno-associated virus needs sodium butyrate to increase its level of gene expression.