To discuss the availability of evaluation on the dissolution studies of the multicomponents in traditional Chinese medicine, the in vitro dissolution of total composition of the tablet of rhizomes of Ligusticum chuanxiong components and its correlation with the in vivo were studied by the method of area under the absorbance-wavelength curve (AUAWC). Taken the tablet of rhizomes of Ligusticum chuanxiong components which is composed of sodium ferulate and ligustrazine hydrochloride as subject model, the dissolution tests were carried out with basket method. The plasma concentrations of tablets in different rats were determined by AUAWC at different interval times. The in vivo absorption percentage was calculated by Wagner-Nelson equation to evaluate the in vitro and in vivo correlation. According to the results, the cumulative dissolution in vitro of total composition of tablets of rhizomes of Ligusticum chuanxiong components at 60 min was 90.65% in water by AUAWC. The in vivo pharmacokinetics is fitted with an one-compartment model. The linear equation based on the cumulative dissolution rate (fr) and absorption percentage (fa) at 5, 10, 20, 30 and 60 min was fa = 0.819 7 fr+0.183 and the correlation coefficient was 0.959 5, which showed a good correlation between the in vitro dissolution and the in vivo absorption percentage. The method of AUAWC can be used accurately, feasibly and conveniently to evaluate the in vitro and in vivo correlation of total composition of tablets of rhizomes of Ligusticum chuanxiong components, which will provide better guidance to study the in vitro and in vivo correlation of sustained release preparation etc under complex system of traditional Chinese medicine in the future.
Animals ; Coumaric Acids ; chemistry ; Delayed-Action Preparations ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Ligusticum ; chemistry ; Rats ; Rhizome ; chemistry ; Solubility ; Tablets

Objective To investigate the value of MR imaging methods for the quantification of fat content in a customized lipid phantom at 3.0 T.Methods Eleven homogeneous fat-water phantoms (50 ml)with fat volume percentages from 0 to 100％ were constructed with reference to Bernard's methods.Fat tractions of the lipid phantom were acquired using water selective saturation (WS),fat selective saturation (FS),in-and out-of-phase imaging (IOP),iterative decomposition of water and fat with echo asymmetry and least-squares estimation (IDEAL) gradient echo imaging and IDEAL Quant imaging methods on a 3.0 T MRI system.For statistical comparisons,paired-sample t test,Pearson correlation test,and Bland-Ahman maps were applied.Results Evaluated fat fractions acquired by WS,IDEAL Gradient echo imaging and IDEAL Quant were (49.6±28.8)％,(46.0±28.4)％,(51.0±32.0)％,the result has no significant difference with the true fat contents(t values were-0.186,-2.218,2.713;P values were 0.856,0.051,0.055).Evaluated fat fractions acquired by FS,corrected algorithm and IOP were (64.2±26.7)％,(58.9±31.9)％ and (45.3±32.3)％,these three kinds of methods have significant difference with the true fat contents (t values were 5.168,4.273,-6.441;P＜0.01).All the chemical shift imaging methods correlated with the true phantom model fat fractions,r values were 0.977(FS),0.978 (corrected algorithm),0.982 (WS),0.99 8(IOP),0.993 (IDEAL Gradient echo imaging),0.999 (IDEAL Quant) (all P＜0.01).Each method's 95％ confidence interval of the mean difference acquired by Bland-Altman map was WS (-14.7％ to 13.8％),FS (-3.6％ to 32.0％),corrected algorithm (-4.6％ to 22.5％),IOP(-9.4％ to 0.0％),IDEAL gradient echo imaging (-15.9％ to 7.8％),IDEAL Quant(-2.0％ to 4.0％).IDEAL Quant had the best correlation and confidence with the true fat fraction.Conclusions Chemical shift imaging methods (IOP,IDEAL Gradient echo imaging,IDEAL Quant) can acquire more accurate fat quantification results than chemical saturation imaging methods (FS,Corrected algorithm,WS) in a customized lipid phantom at 3.0 T.IDEAL Quant can acquire the best fat quantification result compared with the other imaging methods.

Objective: The absolute bioavailability of the preparation of Chuanxiong Radix components in rats was simultaneously studied by two methods of area under absorbance-wavelength curve (AUAWC) and high performance liquid chromatography (HPLC), which would confirm the feasibility that AUAWC could be used to determine the absolute bioavailability of components of Chinese materia medica (CMM). Methods: Based on the random two-way cross-over design, 60 SD rats were given the injection of Chuanxiong Radix components by iv and the same amount of drug suspension of the tablet of Chuanxiong Radix components by ig, respectively. Blood samples were collected at various time points after the administration. Plasma concentration of the total components, sodium ferulate, and ligustrazine hydrochloride of the two preparations of Chuanxiong Radix components in rats was measured by AUAWC combined with HPLC. Pharmacokinetic parameters and absolute bioavailability were calculated by DAS 2.0 program and the data obtained by the two methods were compared. Results: After ig administration, AUC0-∞ of total components was (77.218±13.492) mg·min/L by AUAWC and AUC0-∞ of total component was (169.775±18.252) mg∙min/L for iv injection. The absolute bioavailability of tablet of ligustrazine hydrochloride were (69.134±4.853) and (16.422±2.584) mg∙min/L, respectively by HPLC. As for iv injection, AUC0-∞ of sodium ferulate and ligustrazine hydrochloride were (155.244±28.994) and (36.754±6.645) mg∙min/L, respectively. The absolute bioavailabilities of ig administration were 44.53% and 44.68%, respectively. The data obtained by AUAWC were similar to by HPLC. Conclusion: The method of AUAWC can be used to determine the absolute bioavailability on the mixed drugs in the tablet of Chuanxiong Radix components, which will be helpful to solve the problem that the total and individual drugs of the preparation can be coanalyzed together under the combination method of HPLC. It will provide better enlightenment to study the absolute bioavailability of the mixed drugs from Western compound chemicals or complex components in CMM.

Animals ; Apoptosis ; Azoxymethane ; Colorectal Neoplasms ; chemically induced ; metabolism ; pathology ; Cytoskeletal Proteins ; metabolism ; Precancerous Conditions ; chemically induced ; metabolism ; pathology ; Rats ; Rats, Inbred F344 ; Trans-Activators ; metabolism ; beta Catenin

This study investigated the effect of arctigenin (Arc) on the cell activation, cytokines expression, proliferation, and cell-cycle distribution of mouse T lymphocytes. Mouse lymphocytes were prepared from lymph node and treated with Phorbol-12-myristate-13-acetate (PMA)/Ionimycin (Ion) and/or Arc. CD69, CD25, cytokines, proliferation and cell cycle were assayed by flow cytometry. The results showed that, at concentrations of less than 1.00 micromol x L(-1), Arc expressed non-obvious cell damage to cultured lymphocytes, however, it could significantly down-regulate the expression of CD69 and CD25, as well as TNF-alpha, IFN-gamma, IL-2, IL-4, IL-6 and IL-10 on PMA/Ion stimulated lymphocytes. At the same time, Arc could also inhibit the proliferation of PMA/Ion-activated lymphocytes and exhibited lymphocyte G 0/G1 phase cycle arrest. These results suggest that Arc possesses significant anti-inflammatory effects that may be mediated through the regulation of cell activation, cytokines expression and cell proliferation.
Animals ; Anti-Inflammatory Agents ; isolation & purification ; pharmacology ; Antigens, CD ; metabolism ; Antigens, Differentiation, T-Lymphocyte ; metabolism ; Arctium ; chemistry ; Cell Cycle Checkpoints ; drug effects ; Cell Proliferation ; drug effects ; Cytokines ; metabolism ; Female ; Furans ; isolation & purification ; pharmacology ; Interferon-gamma ; metabolism ; Interleukin-10 ; metabolism ; Interleukin-2 ; metabolism ; Interleukin-2 Receptor alpha Subunit ; metabolism ; Interleukin-4 ; metabolism ; Interleukin-6 ; metabolism ; Ionomycin ; pharmacology ; Lectins, C-Type ; metabolism ; Lignans ; isolation & purification ; pharmacology ; Lymphocyte Activation ; drug effects ; Mice ; Mice, Inbred BALB C ; Plants, Medicinal ; chemistry ; T-Lymphocytes ; cytology ; drug effects ; immunology ; Tetradecanoylphorbol Acetate ; pharmacology ; Tumor Necrosis Factor-alpha ; metabolism

OBJECTIVETo measure the stability of Evans procedure and Chrisman-Snook technique in the treatment of II degree lateral collateral ligament of ankle joint, and provide basis for treatment and prognosis.

METHODSFrom July 2008 to June 2009,18 frozen corpes were collected, including 10 males and 8 females, with an average age of fresh 39.3 +/- 11.2 years. The frozen corpes were randomly divided into three group, including normal controls(group A), Evans procedure (group B) and Chrisman-Snook technique ( group C), 6 specimens in each group. Anterior talofibular ligament and calcaneofibular ligament were cut off to cause II degree lateral collateral ligament in group B and C. Evans procedure or Chrisman-Snook technique were applied to restore lateral collateral ligament, and measure biomechnics. The displacement of tibiotalar joint and subtalar joint were observed.

RESULTS(1) The lateral stress results of tibiotalar joint showed the displacement by Evans procedure (group B) was greater than other groups (P < 0.0001). There were no significant differences between group A and C (P > 0.05). (2) The lateral stress results of subtalar joint showed the displacement by Evans procedure (group B) was greater than other groups (P< 0.0001). There were no significant differences between group A and C (P > 0.05).

CONCLUSIONAnkle instability is caused by ankle joint lateral collateral ligament injury. Chrisman-Snook technique is better than Evans procedure in stability on the early stage of ankle joint restoration, and conform to principle of biomechanics.

Adult ; Ankle Joint ; Biomechanical Phenomena ; Female ; Humans ; Lateral Ligament, Ankle ; diagnostic imaging ; injuries ; surgery ; Male ; Mechanical Phenomena ; Prognosis ; Radiography ; Reconstructive Surgical Procedures ; methods

Objective Benzothiazole derivative BD960 has immunosuppressive activity after cell -based assays for high-throughput screening.The paper aimed to investigate the involved mechanism of BD960 on T cell proliferation. Methods Human peripheral blood T-lymphocytes were isolated and purified by the immunomagnetic microbeads.Then the T cells were activated by anti-CD3/anti-CD28 mAbs or alloantigen.The effect of BD960 on activa-ted T cell proliferation, the cytotoxic effect BD960 on resting T cells and the expression of activated T cells marker CD25 were measured by flow cytometer.Cytokine levels, including IL-2, IL-4, IL-6, IL-10, IL-17A and IFN-γ, were determined by ELISA. Results BD960 significantly inhibited the proliferation of T cells stimulated by anti-CD3/anti-CD28 mAb or alloantigen in a dose-dependent manner.The IC50 value is (2.3 ±0.3)μmol/L or (2.5 ±0.3)μmol/L, respectively.Moreover, BD960 had no obvious cytotoxic effects on rest-ing T cells and peripheral blood mononuclear cells, even at a high concentration ( up to 100μmol/L) .The ratio of CD25 expression on T cell was 69.7%after stimulated by Anti-CD3/CD28 mAbs with 72 h, the concentration (0.625、2.5、10)μmol/L of BD960 also had no potent effects on the ratio, but 0.1μmol/L FK506 could inhibit CD25 expression as low as 9.4%.The G0/G1 phase of activated T cells was 58.5%after stimulated by BD960 with 96 h.BD960 could induce cell cycle arrest at the G0/G1 phase in activated T cells with the increase of concentration and RAPA in the concentration of 0.1 μmol/L was 91.5%.In addition, BD960 (0.625、2.5、10)μmol/L could inhibit the secretion of IFN-γ, IL-6 and IL-17 in activated T cells with the increase of concentration, without any effects on the secretion of IL-2, IL-4 and IL-10. Conclusion BD960 not only exerts the inhibition on the late stage of T cell activation of cell proliferation but also inhibits the secretion of inflammatory cytokines, such as IL-6, IL-17 and IFN-γ, while the mechanism of BD960 on T cell proliferation was not the same as FK506.As a result, BD960 has the potential to be the lead compound to develop a new immunosuppressant.

OBJECTIVETo explore and sum up the characteristics of infection after cardiac transplantation and to discuss the prophylaxis and management.

METHODFrom May 2000 to April 2003, 36 patients received orthotopic heart transplantation, the clinical data were observed and analyzed.

RESULTSInfection occurred in 2 (6%) cases, both belonged to lung infection caused by human cytomegalovirus. The 2 cases were cured by ganciclovir intravenously.

CONCLUSIONGood prophylactic method may decrease post cardiac transplantation infection significantly. It is very important to early diagnose and treat infection.

Adolescent ; Adult ; Aged ; Antibiotic Prophylaxis ; Antiviral Agents ; therapeutic use ; Cytomegalovirus Infections ; drug therapy ; Female ; Follow-Up Studies ; Heart Transplantation ; Humans ; Male ; Middle Aged ; Postoperative Complications ; Postoperative Period

BACKGROUNDThe relationship between inflammatory markers and the characteristics of coronary atherosclerosis plaques is uncertain. The aim of the present study was to evaluate the relationship between the characteristics of coronary atherosclerosis plaques and inflammatory markers such as high sensitivity C-reactive proteins (Hs-CRP) and interleukin-6 (IL-6).

METHODSAll patients suspected of having coronary heart disease (CHD) underwent Siemens 64-slice CT angiography (64-SCTA) to distinguish the quality of plaque of coronary artery lesions. Blood samples were taken to measure levels of serum Hs-CRP and IL-6 in different plaque groups and the control group and compared with the value of 64-SCTA for detection of coronary artery plaque.

RESULTSThe sensitivity of detecting coronary artery plaque by 64-SCTA was 87.4%, the specificity was 87.1%, the positive predictive value was 82.2%, and the negative predictive value was 91.0%. Comparing the levels of serum Hs-CRP and IL-6 among plaque groups, the mean levels of serum Hs-CRP and IL-6 in three plaque groups were significantly higher than those in the control group (P < 0.01). The mean levels of serum Hs-CRP and IL-6 in the soft plaque group and mixed plaque group were significantly higher than those in hard plaque group (P < 0.01). Plaque burden in the soft plaque group and mixed plaque group was significantly higher than in the hard plaque group (P < 0.01), but there was no statistical difference between the soft plaque group and mixed plaque group (P = 0.246). There was a negative correlation between the CT scale and Hs-CRP and IL-6 levels in the soft plaque group (r = -0.621, P < 0.01, and r = -0.593, P < 0.01 respectively). There was a positive correlation between the plaque burden and Hs-CRP and IL-6 levels in the soft plaque group (r = 0.579, P < 0.05 and r = 0.429, P < 0.05 respectively).

CONCLUSIONS64-SCTA is an effective way to distinguish the different quality of coronary atherosclerosis plaque. Serum Hs-CRP and IL-6 levels can be considered as the indexes to judge the degree of CHD and may reflect the activity of plaque in CHD patients. Thus it is important for clinical diagnosis and risk evaluation of acute coronary syndrome (ACS) patients.

Aged ; C-Reactive Protein ; metabolism ; Coronary Artery Disease ; blood ; diagnostic imaging ; metabolism ; Female ; Humans ; Interleukin-6 ; blood ; metabolism ; Male ; Middle Aged ; Tomography, Spiral Computed

OBJECTIVETo detect the germline polymorphic variations of Bat26 in Chinese and its significance in microsatellite instability (MSI) study of gastric cancers.

METHODSBat26 was analyzed by PCR-based denatured polyacrymide gel electrophoresis-silver stain method in peripheral blood from 389 healthy people and 34 gastric cancers with matched normal mucosa. Eleven other microsatellite loci were also detected for gastric cancers.

RESULT(1) No Bat26 variations were identified in 423 genomic DNA from peripheral blood or normal mucosa by polyacrymide gel electrophoresis. (2) Two MSI-H cancers, oth Bat26+, were detected in 34 cases of gastric cancer. The alterations of Bat26 and MSI-H status were identical (P<0.05). (3) Compared with those of RER-cancers, MSI-H (RER+)cancers showed more obvious infiltration of intraepithelial lymphocytes and peri-tumoral lymphocytes, and more pushing borders (P<0.05).

CONCLUSION(1) The germline polymorphisms of Bat26 in Chinese people are quasimonomorphic. Thus, no matched genomic DNA is needed while Bat26 was selected for tumor MSI analysis. (2) Bat26 is an independent indicator of MSI-H gastric cancers with distinct clinicopathological features.

Chromosomal Instability ; genetics ; Humans ; Microsatellite Repeats ; genetics ; Polymorphism, Genetic ; Stomach Neoplasms ; genetics ; pathology