In order to identify ceftriaxone and its analogs whether has the function of anti-tolerance of morphine and study the dose-effect relation of ceftriaxone in mice, hot plate method to measure pain threshold of mouse and naloxone withdrawal models were carried out and compared with normal saline group. Ceftriaxone and cefotaxime had the effect of anti-tolerance and anti-dependence of morphine notably. And ceftriaxone has the effect of anti-tolerance of morphine in a dose dependent manner.
Animals ; Anti-Bacterial Agents ; pharmacology ; Cefotaxime ; pharmacology ; Ceftriaxone ; pharmacology ; Dose-Response Relationship, Drug ; Drug Tolerance ; Female ; Mice ; Morphine ; pharmacology ; Morphine Dependence ; prevention & control ; Pain Threshold ; drug effects ; Random Allocation ; Substance Withdrawal Syndrome ; physiopathology

OBJECTIVETo explore the mRNA expressions of IL-10, IL-18 and Fas in peripheral blood mononuclear cells (PBMCs) in systemic lupus erythematosus (SLE) patients of various Chinese medicine syndrome types in order to seek the objective indices for syndrome differentiation of SLE.

METHODSSLE patients were sorted into various syndrome types by Chinese medicine syndrome differentiation. In them, patients with the 4 often encountered types were selected, i.e. the qi-xue excessive heat type (Group A, 12 patients), the Pi-Shen yang-deficiency type (Group B, 19 patients), the qi-yin deficiency with blood stasis type (Group C, 23 patients), and the qi stagnation and blood stasis with gan stagnation type (Group D, 28 patients). The mRNA expressions of IL-10, IL-18 and Fas in PBMCs were detected by SYBR Green I real time PCR.

RESULTSThe mRNA expressions of IL-10, IL-18 and Fas in PBMC of all SLE patients (0.40 +/- 0.53, 1.41 +/- 1.93 and 0.33 +/- 0.70) were significantly higher than those in the normal control group (0.07 +/- 0.11, 0.24 +/- 0.25, 0.08 +/- 0.21, P<0.01, P<0.05), their levels in different syndrome types decreased in order of type A-->B-->C-->D. The levels of the three indices in patients of type A and B were obviously higher than those in patients of type C and D (P<0.01), while no significant difference was found between type A and B (P>0.05), and between type C and D (P>0.05).

CONCLUSIONThe mRNA expressions of IL-10, IL-18 and Fas in PBMCs could be taken as the objective indices for reference in syndrome differentiation of SLE.

Adolescent ; Adult ; Aged ; Child ; Female ; Humans ; Interleukin-10 ; blood ; Interleukin-18 ; blood ; Leukocytes, Mononuclear ; metabolism ; Lupus Erythematosus, Systemic ; blood ; diagnosis ; therapy ; Male ; Medicine, Chinese Traditional ; methods ; Middle Aged ; RNA, Messenger ; genetics ; Yang Deficiency ; diagnosis ; Yin Deficiency ; diagnosis ; Young Adult ; fas Receptor ; blood

No abstract available.

To study the toxicokinetics of bakuchiol, hepatic and renal toxicity in rats after single oral administration of Psoraleae Fructus and combined with Glycyrrhizae Radix et Rhizoma, in order to provide scientific evidences for clinical safe medication use. A total of 35 SD rats were randomly divided into seven groups: vehicle (distilled water) control group, Glycyrrhizae Radix et Rhizoma group, positive control (aristolochic acid A) group, Psoraleae Fructus (40 g x kg(-1)) group( both male and female rats), Psoraleae Fructus and Glycyrrhizae Radix et Rhizoma (40 +20) g x kg(-1) group (both male and female rats). HPLC-UV method was used to determine the concentration of bakuchiol in rat plasma at different time points after single oral administration. Plasma alanine transaminase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), plasma creatinine (Cr), N-acetyl-β-D-glucosaminidase (NAG) and kidney injury molecule 1 (Kim-1) were measured after administration for 24 h. The main toxicokinetics parameters of bakuchiol in rats exert significantly gender difference. When Psoraleae Fructus combination with Glycyrrhizae Radix et Rhizoma, the total area under the plasma concentration-time curve( AUC), C(max), and plasma clearance (CL) of bakuchiol were increased, respectively; CL, half-life (t½) were decreased, and T(max) were prolonged. The biochemical indicators (including ALT, AST, BUN, Cr and KIM-1 level) in different dose of Psoraleae Fructus groups, were found no statistically significant difference when compared with vehicle control group. The level of NAG in both Psoraleae Fructus and compatibility with Glycyrrhizae Radix et Rhizoma groups were significant increased (P < 0.05). There are obvious effects on toxicokinetics of bakuchiol in rats when Psoraleae Fructus combined with Glycyrrhizae Radix et Rhizoma. Renal toxicity induced by Psoraleae Fructus at high dose was observed after single oral administration and no liver damage in rats was found.
Administration, Oral ; Animals ; Female ; Glycyrrhiza ; toxicity ; Kidney ; drug effects ; Liver ; drug effects ; Male ; Phenols ; pharmacokinetics ; toxicity ; Psoralea ; toxicity ; Rats ; Rats, Sprague-Dawley ; Rhizome ; toxicity ; Toxicokinetics

Objective To overcome the fact that SRV-NM virus can only multiple and amplify through partially pu-rified jaagsiekte retrovirus inoculated intratracheally in sheep but it cannot be augmented using in vitro cell culture, we con-structed JSRV-NM pseudovirions based on high efficiency packing system of lentivirus. Methods Lentivirus of three high efficiency packing plasmids system pMD.G, pCMV-HIV 8.2 and pHIV-eGFP was developed, and JSRV-NM-env coated plasmid pCMVJSRV-NM was used to substitute VSV-G virus coated plasmid pMD.G then co-transfected into 293T cells to replicate, package and produce restructured JSRV-NM pseudovirions. Gene expression of pseudovirion was determined through WPRE using real time PCR; Virus infectivity was detected through inoculating JSRV-NM pseudovirions into 24 pore plates. Results We construct JSRV-NM pseudovirions successfully based on the lentivirus system. JSRV-NM pseudo-virions can also be concentrated to higher titer (108 TU/mL detected by real time PCR by ultracentrifugation without signifi-cant loss of activity. JSRV-NM and VSV-G pseudovirions infected on Hela cells (both MOI= 3) respectively and no obvi-ous difference were shown on their infection efficiency detected by real time PCR. Conclusion Based on lentivirus system, JSRV-NM pseudovirions can be multipled and amplified in 293T cell culture in vitro. JSRV-NM pseudovirions is stable without loss its infection activity and the requirements of biological laboratory safety II was also met. JSRV-NM pseudoviri-ons will provide a useful tool for further study of JSRV-NM-env infection across species or its induction of lung adenocarci-noma.

Objective: To study the formation regularity and kinetic parameters of advanced glycation end-products during the processing of boiled Cervi Cornu Pantotrichum (CCP). Methods: UV-visible spectrophotometry and UPLC-MS/MS method were used to determine the change of browning index and content of typical advanced glycation end-products, Nε-(carboxymethyl) lysine and Nε-(carboxyethyl) lysine, of the processing system of simulated boiled CCP. The formation regularity and kinetic parameters of advanced glycation end-products during the processing of boiled CCP were discussed by constructing glucose and lysine to simulate the Maillard reaction system of CCP processing. Results: The activation energy of browning reaction, Nε-(carboxymethyl) lysine and Nε-(carboxyethyl) lysine reaction during processing of boiled CCP were 5.07, 40.44 and 78.47 kJ/mol, respectively, and all of them were zero-order kinetics. The activation energies of the above reactions in the baking process were 6.72, 89.34 and 164.77 kJ/mol, respectively, and all of them were zero-order kinetics. Compared to the formation of Nε-(carboxymethyl) lysine, the formation of Nε-(carboxyethyl) lysine required higher activation energy and was more difficult to occur. Conclusion: The temperature changed in the baking process has a significantly higher effect on the kinetic parameters of the advanced glycation end-products than in the boiling process. Long-term higher baking temperature resulted in more advanced glycation end-products produced in the boiled CCP. This study provides a solid theoretical basis for the blocking and inhibition strategies of advanced glycation end-products in the processing of CCP, which is also a great significance for the production of green safety CCP and strengthening the safety of traditional Chinese medicine.

Objective To study the CT and MR imaging features of skull epidermoid cyst. Methods CT and MR findings of 4 cases of pathologically proved skull epidermoid cyst were analyzed and correlated with operative and pathologic reports.Results CT and MR appearances of skull epidermoid cyst were as follows:(1)crater-form or scalloping deossification with sclerotic border and fatty density focus was detected on CT.(2)The lesions were isointense to hypointense relative to normal white matter in T1-weighted image,prominent hyperintense in T_2-weighted image,mild to moderate hyperintense in diffusion-weighted imaging(DWI),and isointense to hypointense in apparent diffusion coefficient(ADC) map on MR.Proton MRS revealed lactate(Lac)peaks at 1.3 ppm and amino acids(AAs)at 0.9 ppm. (3)No enhancement was found in substance region of all tumors on both enhanced CT and enhanced MR examinations.Conclusion CT and MR appearances of skull epidermoid cyst have unique features which are very helpful in the diagnosis of skull epidermoid cyst.

Maillard reaction is a non-enzymatic browning reaction which is ubiquitous in the food industry and processing of Chinese materia medica (CMM). Maillard reaction can not only change the color and aroma of CMM, extend the shelf life of CMM, but also produce new active substances in CMM. In addition, a small amount of toxic and harmful substances such as 5-hydroxymethylfurfural and advanced glycation end-products produced by Maillard reaction have been given increasingly attention. It is of great significance to control the quality of CMM by changing the reaction temperature, time, potential of hydrogen, adding inhibitors, and anti-oxidants to regulate Maillard reaction. This paper reviews the general situation of Maillard reaction research and its research progress on the quality and regulation of CMM, and provides a reference for further research on the regulation of Maillard reaction for the quality control of CMM.

Objective: To investigate the causes and influencing factors of 5-hydroxymethylfurfural (5-HMF) during the processing of Cervi Cornu Pantotrichum (CCP). Methods: HPLC was used to determine the content of 5-HMF in CCP with different processing methods and different parts. Moreover, the contents of total sugar, reducing sugar, amino acid, and Ca, Mg, Fe, and Cu in velvet antler were determined, and the effects of several factors on 5-HMF production during processing were discussed by comparing the contents of above mentioned substances in velvet antler with different processing methods. Results: The contents of 5-HMF of boiled CCP were significantly higher than that of freeze-dried CCP (P < 0.05) in same parts, indicating that high temperature intensified caramelization reaction and Maillard reaction to produce more 5-HMF in boiled CCP; The contents of 5-HMF of CCP with blood were significantly higher than that of CCP without blood (P < 0.05), CCP with blood was rich in total sugar, reducing sugar and amino acid and these substances can provide sufficient substrate to produce more 5-HMF; The content of 5-HMF in wax slices was significantly higher than other parts (P < 0.05), and rich content of total sugars, reducing sugars, amino acids, and differentially distributed mineral elements all contribute to the production of 5-HMF in wax slices. Conclusion: The production of 5-HMF in processing CCP is the result of the combined action of total sugar, reducing sugar, amino acid, and mineral elements at different temperatures.

In this study, we designed and synthesized 12 novel aloperine derivatives with different core structures. Among them, compound 3 with a ten-membered ring core was obtained through a special ring expansion reaction after γ-H Huffman elimination of quaternary ammonium salt, and the structure was verified by X-single crystal diffraction. Furthermore, their antiviral activity against human β-coronavirus HCoV-OC43 was evaluated by CCK-8 assay. Quaternary ammonium salt 2a and 3 had a good inhibitory effect against HCoV-OC43, and 2a had the highest anti-HCoV-OC43 activity with an EC₅₀ values of 3.77 μmol·L^-1 and a SI value of over 53.1. Schrӧdinger molecular docking results showed that both 2a and 3 might display their anti-HCoV-OC43 activity by directly acting on host TMPRSS2 and SR-B1. The results expanded the structural types of endocyclic aloperine and the function against coronavirus, and provided useful scientific data for the development of pharmaceutical applications of these compounds.