To compare the difference of total phenol of magnolia solid dispersion prepared by different methods. Hot melt extrusion, solvent evaporation method, and fusion-cooling method were used to prepare total phenol of Magnolia accessory solid dispersion, Plastone S-630 and HPC. The drug dispersion state in the prepared solid dispersion was evaluated with DSC and X-ray diffraction; FT-IR method was used to analyze the possible connections between drug and accessories. Finally, accelerated stability-in vivo dissolution test was use to compare the stability differences between these three processes. The results of DSC and X-ray diffraction showed that all of the drug in solid dispersion processed by three processes can exist in amorphous form; FT-IR results also could not distinguish the difference between the three processes; accelerated stability-in vivo dissolution test showed the stability of solid dispersion prepared by HPC was better than Plastone S-630, and the same kinds of materials solid dispersion prepared by hot melt extrusion showed a better stability than the other two processes.
Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; Magnolia ; chemistry ; Phenol ; chemistry ; Spectroscopy, Fourier Transform Infrared ; X-Ray Diffraction

HPLC analysis was performed to study the changes in chemical composition of ginseng extracts prepared from high quality ginseng with 0, 2, 4, 8 h of steamed times. An UFLC-MS/MS multiple-reaction monitoring (MRM) quantitative analysis was made to investigate the pharmacokinetic behavior differences of ginsenosides in mice ig administered of ginseng extracts with different steamed times in the negative ion mode, with Digoxin as the internal standard substance. The mice were injected with LPS to establish inflammation model after ig administration of ginseng for a week and the contents of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in mice plasma were detected by ELISA, in order to study on anti-inflammatory effects of ginseng with different steamed times. It was determined that levels of TNF-α and IL-1β were significantly decreased in inflammation model group ig administered of ginseng extracts with 8h of steamed time. The results showed that the chemical components in ginseng changed after steaming and the components into the blood changed, correspondingly. Ginseng with steamed 8 h contributes to anti-inflammatory effects. These results provided an experimental basis for revealing the active substance basis and dose-effect relationship of ginseng on anti-inflammatory effect.
Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacokinetics ; Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Ginsenosides ; chemistry ; pharmacokinetics ; Hot Temperature ; Humans ; Inflammation ; drug therapy ; Male ; Mice ; Mice, Inbred ICR ; Panax ; chemistry ; Time Factors

Objective To construct a short hairpin RNA (shRNA) adenovirus vector targeting Aktl (protein kinase B1, PKBI/Aktl) and cyclooxygenase-2 (COX-2) and study its effects on the invasion and metastasis of SGC-7901 human gastric adenocarcinoma cells. Methods Aktl and COX-2 shRNA expression frames were subcloned to pGSadeno adenovirus vector by homologous recombination technology to construct pGSadeno-Aktl+COX-2 (rAdS-A+C) vector. After screening and amplification, the recombinant adenovirus vector was digested with PacI and transfected into SGC-7901 cells, the titer and transfection efficiency were detected by fluorescent microscopy. Aktl and COX-2 mRNA and protein expression was identified by real-time PCR and Western blot. MMP-2 and MMP-9 contents in control group SGC-7901、rAd5-HK and treatment group rAdS-A+C were detected by ELISA assay and transwell assay analyzed cell invasion and metastasis ability. Results Adenovirus vector rAdS-A+C was successfully constructed and it dramatically down-regulated Aktl and COX-2 mRNA and protein expression in SGC-7901 gastric cancer cells. MMP-2 and MMP-9 contents in treatment group rAd5-A+C were respectively (39.7± 1.7) ng/ml, (31.3±3.6) ng/ml, and they were lower than those in control group SGC-7901 (278.4± 15.5) ng/ml, (225.4±15.1) ng/ml and rAd5-HK (275.5±2.1) ng/ml, (226.0±23.3) ng/ml (P= 0.01, P=0.021). Transwell assay showed treatment group rAd5-A+C significantly inhibited the invasion and metastasis of SGC-7901 gastric adenocacinoma cells. Conclusions Adenovirus-mediated targeting Aktl and COX-2 shRNA can inhibit the invasion and metastasis of SGC-7901 human gastric adenocarcinoma cells.

Objective To construct a short hairpin RNA (shRNA) adenovirus vector targeting P85 and protein kinase B1 (PKB1/Akt1) and study its effects on the growth of SGC-7901 human gastric adenocareinoma cells. Methods P85 and Aktl shRNA expression frames were subcloned to pGSadeno adenovirus vector with homologous recombination technology to construct pGSadeno-P85 + Akt1 (rAd5-P + A) vector. After screening and amplification, the recombinant adenovirus vector was digested with PacI and transfected into SGC-7901 cells and then its titer and transfection efficiency were detected with fluorescent microscope. P85 and Akt1 mRNA protein expression was identified with real-time PCR and Western blot. The proliferative activity of tumor cells was evaluated with MTr assay and flow cytometry in vitro, rAd5-HK and rAd5-P + A mediated by adenovirus were injected into the established subcutancous SGC-7901 gastric adenocarcinoma in nude mice. During the observation period of 21 days, tumor volume was measured every 3 days to further testify the anti-tumor effect of rAd5-P + A on the SGC-7901 gastric adenocarcinoma cells and cell in situ apoptosis was detected with TUNEL assay. Results The adenovirus vector rAd5-P + A was successfully constructed and it dramatically downregulated P85 and Akt1 mRNA expression in SGC-7901 gastric adenocarcinoma cells. Compared with a control group of SGC-7901 cells and cells transfected with general adenovirus rAd5-HK as control, P85 and Akt1 protein expression 48 h and 72 h after rAd5-P + A transfection was decreased by 57.5% and 63. 7%, 67. 8% and 75.6% with statistical significance(P = 0. 005, P = 0. 003). Cell proliferative activity in rAd5-P + A transfected cells was suppressed from the second day (P <0. 001) and the decreased P85 and Akt1 expression was accompanied by 5.9% -7. 1% decrease of S phase fraction and 12. 1% - 13.7% increase of G0/G1 phase. The tumor volume of rAd5-P + A treated group was smaller than that of the control and rAd.5-HK group with statistical significance (F = 9. 871, P = 0. 025) . Moreover, rAd5-P + A could induce cell in situ apoptosis. Conclusions Adenovirus-mediated targeting P85 and Akt1 shRNA can inhibit the growth of SGC-7901 human gastric adenocarcinoma cells and this may provide a new strategy of combination gene therapy in gastric adenocarcinoma.

Objective To study changes of the autoimmune antibody level in patients after autologous hematopoietic stem cell transplantation(CD_(34)~+).Methods Twelve patients with SLE received autologous hematopoietic stem cell transplantation.All they survived and their immune system were recoverd after a period of time.The serum autoimmune antibody levels were measured before and after the transplantation,Results The antibody levels became normal 6 months after transplantation.Conclusion Autologous hematopoietic stem cell transplantation can effectively reduces the level of autoimmune antibody in patients with SLE.

Objective To observe the changes of magnetoencephalography (MEG) during stretching and flexing forefinger in one hemiplegic patient before and after rehabilitation training.MethodsThe cerebral electromagnetic wave of one hemiplegic patient during stretching and flexing both forefingers was recorded by MEG and superposed with magnetic resonance imaging (MRI) to form magnetic source imaging (MSI). The changes of MEG before and after rehabilitation training were analyzed.ResultsThere was no movement evoking magnetic fields in right hemisphere motor cortex at two MSI detections, but detected in left hemisphere motor cortex. The latent period of the first and the second detection was -34.2 ms and -61.7 ms respectively. The exiting motor cortex was located in precentral gyrus. The exiting motor cortex at the second detection was located more front medial and low than at the first detection. The volume of the exiting motor cortex (9569.6 m3) at the second detection was more larger than the first detection (2309.7 m3). There was no movement evoking somatosensory magnetic fields in right hemisphere motor cortex at first MSI detection, but found at the second detection, the latent period was 91.1 ms, and the exiting cortex was located in postcentral gyrus.ConclusionThe cortex somatosensory function of patient with stroke recovers early than the motor function and the uninjured hemisphere function can improve obviously after rehabilitation training.

Adult ; Antiviral Agents ; adverse effects ; therapeutic use ; Hepacivirus ; Hepatitis C, Chronic ; drug therapy ; Humans ; Liver Cirrhosis ; drug therapy ; Middle Aged ; Postoperative Period ; Splenectomy

OBJECTIVE Based on the methods of microdialysis,HPLC-MS/MS and gene chip tech-nology,the mechanism of Baicalin and Geniposide(BC/GP)against excitatory amino acid toxicity in ce-rebral ischemia was studied. This will provide guidance for the clinical application of BC/GP and the study of excitatory amino acid toxicity in cerebral ischemia.METHODS (1)Microdialysis technique and HPLC-MS/MS was performed to study the pharmacodynamics of BC/GP against cerebral ischemia. ①18 SD rats with body weight of(280±20)g were randomly divided into control group,treatment groups with BC/CP at low dose,medium dose and high dose(equal to the dosage of crude drugs for 30 mg·kg-1, 45 mg·kg-1and 60 mg·kg-1respectively).Rats in each group were given intragastric administration for seven days to establish cerebral ischemia model. Then, microdialysis probe was applied to collect cerebrospinal fluid from hippocampus before and after cerebral ischemia. ② First, we established the HPLC-MS/MS method for measuring drugs and excitatory amino acids.Then we detected the microdi-alysis samples and observed their changes in animals.(2)The mechanism of BC/GP against excitatory toxicity of cerebral ischemia were observed at gene level by chip technique. ① 16 SD rats with body weight of 240±20 g were randomly divided into sham group, model group, treatment group of BC(60 mg·kg-1),treatment group of GP(60 mg·kg-1)and treatment group of BC/GP(7:3)(60 mg·kg-1).Rats in eachgroup were given intragastric administration for seven days to establish cerebral ischemia model. Then the rats were sacrificed,and the hippocampus were rapidly harvested and stored at-80℃for further detection. ②After the quality inspection of the hippocampal,the qualified samples were subjected to detect the levels of neurotransmitter receptor gene in the ischemic of rats by gene chip technology.Finally,the results were analyzed by the method of Δ ΔCt.RESULTS (1)Only three compounds includ-ed GP,glutamic acid and aspartic acid were detected in microdialysis samples by HPLC-MS/MS.The concentration of GP increased and lasted for 120 min with a significant dose-dependent after cerebral ischemia.Compared with low dose group,the AUC(0-t),MRT(0-∞),Cmaxand t1/2zin high-dose group showed significant difference(P<0.01).Compared with the model group,the levels of glutamic acid and aspartic acid in the treatment groups decreased significantly,especially in the middle and high dose groups.(2) 89 genes in the neurotransmitter receptor gene signaling pathway were detected by gene chip technol-ogy. There were 22 genes with |Fold Regulation|>1.5 in the model group, compared with the sham group.Five of the 22 genes showed statistically significant differences,including Grin2c(2.9026),Chrna7 (-1.5877), and Tacr2 (-1.7695). Htr3a (-1.8172) and Grm6 (-2.3527). There were 5 genes with |Fold Regulation|>1.5 in the BC group, compared with the model group, Two of them exhibited statistically significant differences,including Brs3(1.797)and Grin2c(-1.7979).There were 14 genes with|Fold Reg-ulation|>1.5 in the GP group, compared with the model group. Three of them displayed statistically significant differences,including Hcrtr2 (-1.6584), Sctr (-3.8524) and Grin2c (-4.8408). Compared with model group, the genes of |Fold Regulation|>1.5 in BC/GP (7:3) group are 5, and only one of them showed a significant differences. CONCLUSION (1)After administration of BC and GP,GP can cross the blood-brain barrier and reduce the release of excitatory amino acids in the hippocampus. (2) BC/GP can inhibit the interaction between excitatory amino acids and excitatory amino acid receptors and attenuate the toxicity of excitatory amino acids by down-regulating the expression of glutamic acid receptor Grin2c gene.(3)BC/GP may exert their brain protection effect by reducing the release of excit-atory amino acids and inhibiting the expression of excitatory amino acid receptors.

Objective To investigate whether three-dimensional speckle tracking imaging ( 3D-STI) combined with conventional echocardiography can identify cardiac functional characteristics and predict adverse cardiovascular events in patients with hypertrophic cardiomyopathy ( HCM ) . Methods One hundred and eighty HCM patients were involved in the study . All patients were followed up to March 2017 after comprehensive evaluation of 3D-STI and conventional echocardiography for endpoint events . The endpoint events were divided into the primary and secondary endpoints . The primary endpoints included sudden cardiac death ( SCD ) , survival after cardioversion and appropriate implantable cardioverter-defibrillator( ICD) discharge ;the secondary endpoints included acute myocardial infarction ,heart failure hospitalization ,thromboembolism and endstage HCM . The composite endpoints contained primary or secondary endpoints . Results ①Totally 175 HCM patients completed the follow-up [ ( 435 ± 204) days] . During follow-up ,25 patients ( 14 .3% ) reached composite endpoints :8 cases of the primary endpoints ( 3 cases of sudden cardiac death ,3 cases of survival after defibrillation ,and 2 cases of appropriate implantable cardioverter-defibrillator discharge ) ; 17 cases of the second endpoints ( 14 cases of heart failure hospitalization ,2 cases of thromboembolism ,and 1 case of end-stage HCM ) . ② Patients with primary endpoints had higher NYHA class ,reduced systolic and early diastolic mitral annular velocities (MV s′and MV e′) ,decreased systolic tricuspid annular velocity ( TV s′) ,and impaired 3D left ventricular global longitudinal strain ( GLS ) ,as compared to those without primary endpoints ( n ＝ 167 ) ( P ＜ 0 .05 ) . Impaired 3D GLS ( hazard ratio was 0 .72 ,95% CI was 0 .53 －0 .98 , P ＝ 0 .035) and decreased TV s′( hazard ratio was 0 .70 ,95% CI was 0 .54－0 .91 , P ＝0 .007) were independent predictor factor for primary endpoints . 3D GLS≤11 .7% or TV s′≤12 .7 cm/s raised the risk of primary endpoints . ③Similarly ,HCM patients with composite endpoints ( n ＝25) had higher NYHA class ,enlarged left atrial diameter ( LAD) , reduced MV s′,MV e′ and TV s′,as well as impaired 3D GLS ( P ＜ 0 .05) ,when compared to those without composite endpoints ( n＝150) . Moreover ,impaired 3D GLS ( hazard ratio was 0 .68 ,95% CI was 0 .56－0 .81 , P ＝0 .000) was independent predictor for composite endpoints ;and patients with 3D GLS≤12 .9% was more susceptible to composite endpoints . Conclusions 3D GLS combined with TV s′ are of value in predicting adverse cardiovascular events .

Objective To diagnose Kennedy's disease (KD) via molecular analysis of the androgen receptor gene with suspected KD.Methods Two patients with suspected KD were reported.We analyzed their clinical features and investigated the number of CAG repeats in the androgen receptor genes. Results Both of the patients were characterized by slow progression of predominant proximal and bulbar muscle weakness.Patient 2 had oligospermatism.Serum creatine kinase and triglyceride levels were found markedly increased.The exact number of CAG was 52 in patient 1 and 48 in patient 2,respectively.These 2 patients were finally diagnosed as Kennedy's disease through the analysis of androgen receptor gene by PCR and direct sequencing.Conclusions The method of molecular analysis for KD had been copied in China.The clinical and molecular biological features of 2 Chinese patients with KD had been discussed.KD is a neurodegenerative disorder by proximal limb muscular atrophy and weakness with lower motor neuron signs,bulbar involvement.Dyscrinism and metabolic abnormalities may also be observed.Gene analysis is the unique and reliable methods to diagnose KD.