Animals ; Antineoplastic Agents ; pharmacology ; therapeutic use ; Cell Cycle ; drug effects ; physiology ; Cyclin-Dependent Kinases ; antagonists & inhibitors ; metabolism ; Cyclins ; metabolism ; Flavonoids ; pharmacology ; therapeutic use ; Humans ; Neoplasms ; drug therapy ; metabolism ; pathology ; Piperidines ; pharmacology ; therapeutic use ; Purines ; pharmacology ; therapeutic use ; Staurosporine ; analogs & derivatives ; pharmacology ; therapeutic use

This is designed to analyze and summarize medication rules for treating senile dementia with Chinese medicine in CNKI according to the traditional Chinese medicine (TCM) inheritance auxiliary system. Collect documents in CNKI that account treating senile dementia with Chinese formula; filter and establish a formula database, and then to search for medication rules on the TCM inheritance auxiliary system. It is filtered that 104 formulas are used for treating senile dementia screening treat senile dementia, involving 147 kinds of Chinese medicine. Tonic medicine are most frequently used, followed by the medicine of activating blood circulation and resuscitating; medicine pair most used is Ligusticum chuanxiong Hort-Acorus tatarinowii, accounting for 27.9% of all formula. And then 8 core pairs and 4 new formulas are evolved. Analysis on formulas for treating senile dementia filtered form CNKI by TCM inheritance auxiliary system shows prescription is mainly tonifying, activating blood circulation and resuscitating, that reveals prescription rules, to provide a reference for clinical treatment.
Databases, Factual ; Dementia ; drug therapy ; Drug Prescriptions ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; chemistry ; therapeutic use ; Humans

This study is to establish the characteristic HPLC chromatogram of phenols in Ephedrae Herba, from which to pick out the marker peaks, followed by the analysis of the regularity of their distribution and content in the herbaceous stems of Ephedra sinica, E. intermedia and E. equisetina. The HPLC-DAD method for the characteristic chromatogram as well as quantitative analysis was established. The separation was carried out on a YMC-Pack ODS-A column (4.6 mm x 250 mm, 5 µm), eluted with the mobile phases as 0.01% formic acid aqueous solution (A) and acetonitrile (B) in a linear gradient (0-10 min, 17% B; 10-25 min, 17%-19% B; 25- 33 min, 19%-48% B; 33-35 min, 48%-51% B; 35-44 min, 51% B). The flow rate was kept at 1.0 mL · min⁻¹. The column tem- perature was 40 °C, and the detection wavelength was set at 350 nm (0-16 min) and 330 nm (16-44 min). Forty-six batches of collected samples from three official origins of Ephedrae Herba were detected, whose liquid chromatograms proven to be helpful to the differentiation of different origins. With principal component analysis and the analysis of distribution of peak area, twelve key peaks from the chromatogram were discussed in details on their contributions to the characteristics and differences of three official origins of the herb: peak area of peak 10, 11, 12 were found out to be significantly higher in E. equisetina than in other two origins, whose sum (higher than 146 mAU in E. equisetina) was useful for the discrimination between E. equisetina and the other two origins; peak area of 1 and 4 were respectively higher in E. sinica and E. intermedia than in other official origins, indicating their important effect on the differen- tiation of corresponding origins; peak 8 and 9 were picked out as two characteristic common peaks in three official origins of the herb, whose peak area showed little difference among different origins; further, peak area of other key peaks in the chromatogram also showed some difference among three origins, which make contributions to the differentiation of origins as well. Then, four phenols as 2"-O-α- L-rhamnosyl-isovitexin (1), vitexin (2), pollenitin B (5) and herbacetin-7-O-β-D-glucoside (6) were quantitative analyzed with the above-mentioned method, with good linear relationship and accuracy (recoveries in a range of 97.8%-102.5%). The content of the four phenols were firstly reported in Ephedrae Herba from official origins, which were respectively trace-1.55 (1), trace-0.160 (2), trace-0.284 (5) and trace-0.620 (6) mg · g⁻¹ in all of the tested samples. In addition, the content of these phenols showed differences in three official origins, especially 1, whose content in E. sinica [(0.670 ± 0.88) mg ± g⁻¹] were significantly higher than in other two origins (lower than 0.16 mg ± g⁻¹ besides sample Ei-060630-2-2), and 6, whose average content in E. equisetina [(0.260 ± 0.039 2) mg · g⁻¹] were twice as high as in E. sinica [(0.120 ± 0.270) mg · g⁻¹] and E. intermedia [(0.136 ± 0.485) mg g⁻¹], indicating the important effects of the two constituents on the differentiation among three official origins of the herb. The method established for the characteristic HPLC chromatogram and quantitative analysis of phenols was simple and accurate, and the marker constituents selected may provide new guides for the discrimination of official origins as well as the improvement of quality criteria of EphedraeHerba.
Chromatography, High Pressure Liquid ; methods ; Ephedra ; chemistry ; Phenols ; analysis

AIM: To investigate the antitumor activity and mechanism of Paecilomyces tenuipes polysaccharide(PTPS).METHODS: PTPS-I was obtained by water extraction and alcohol precipitation,and purified by DEAE-cellulose and Sephadex G-100 chromatography.Human erythroleukemia cell line K562,laryngocarcinoma cell line Hep2 and hepatic carcinoma cell line SMMC-7721were co-cultured with PTPS-I or the conditioned medium which prepared with PTPS-I-stimulated human mononuclear cells(PTPS-I-MNC-CM),and the proliferation of tumor cells was determined.The cell counting kit-8(CCK-8) was used to determine the proliferation of MNCs.The FQ-RT-PCR was applied to investigate the expression of TNF-? and IL-6 mRNA in MNCs.RESULTS: PTPS-I-MNC-CM inhibited the proliferation of K562,Hep2 and SMMC-7721 cells in vitro(P

BACKGROUNDThis study investigated the inhibitory effect of berberine (BBR) on lipopolysaccharide (LPS) induced cyclooxygenase-2 (COX-2) expression via the mitogen activated protein kinase (MAPK) signalling cascade pathways in human peripheral blood monocytes (PBMC).

METHODSPBMC from whole blood were isolated and cultured for up to 24 hours after division into 5 groups treated with LPS, LPS + BBR 25 micromol/L, LPS + BBR 50 micromol/L or LPS + BBR 100 micromol/L and untreated. Monocytes were extracted for RT-PCR and Western blot analyses to examine COX-2 mRNA and protein activated expression of p38 mitogen activated protein kinase (p38MAPK), Jun N-terminal kinase (JNK) and extracellular regulated kinases 1/2 (ERK1/2) signalling pathways.

RESULTSCOX-2 mRNA and protein expression decreased to a minimum at 12 hours after BBR treatment (P < 0.05). With the increasing concentration of BBR treatment, the COX-2 expression decreased progressively (P < 0.01). With BBR treatment for 6, 12 or 24 hours at three doses, ERK1/2 protein expression was significantly inhibited. For the JNK pathway, only with the treatment of BBR at the concentration of 100 micromol/L was JNK protein expression inhibited compared with the LPS stimulation group (P < 0.01). Irrespective of the BBR concentration, no difference was shown between the BBR group and the LPS group for p38MAPK protein expression. Human monocytes COX-2 mRNA, by RT-PCR, and protein expression, by Western blot analysis, were inhibited when incubated with PD98059, SP600125 and SB203580 (P < 0.05).

CONCLUSIONSBerberine inhibits COX-2 expression via the ERK1/2 signalling pathway and, possibly, at a high dosage via the JNK pathway. P38MAPK may have no relationship with the effect of BBR in PBMC. Berberine inhibited COX-2 mRNA and protein expression in a dose dependent manner and suppressed COX-2 expression to a minimal level after 12 hours of berberine treatment.

Atherosclerosis ; drug therapy ; Berberine ; pharmacology ; therapeutic use ; Cells, Cultured ; Cyclooxygenase 2 ; genetics ; Cyclooxygenase 2 Inhibitors ; pharmacology ; Dose-Response Relationship, Drug ; Extracellular Signal-Regulated MAP Kinases ; antagonists & inhibitors ; Humans ; JNK Mitogen-Activated Protein Kinases ; antagonists & inhibitors ; Lipopolysaccharides ; pharmacology ; MAP Kinase Signaling System ; Time Factors

AIMTo search for new artemisinin derivatives with higher immunosuppressive activity.

METHODSTwo kinds of new artemisinin derivatives containing polyethylene glycol group were synthesized from dihydroartemisinin via condensation and esterification. These compounds were assayed for their inhibitory activity on ConA-induced T cell proliferation and LPS-induced B cell proliferation.

RESULTSTwenty three new compounds (2a - 2f, 3a - 3d, 4a - 4f, 6a, 6b and 7a - 7g) were synthesized and identified by 1H NMR and elemental analysis.

CONCLUSIONThese compounds had immunosuppressive activity in vitro. Among them, the symmetrical substituted compound 2 and 6 had higher activity than mono-substituted compound 3, 4 and 7. Especially, compounds 2a - 2f remarkably exhibited higher inhibition in comparison with artemisinin and artesunate.

Animals ; Artemisinins ; chemical synthesis ; pharmacology ; B-Lymphocytes ; drug effects ; Cell Proliferation ; drug effects ; Humans ; Immunosuppressive Agents ; chemical synthesis ; pharmacology ; Molecular Structure ; Polyethylene Glycols ; Sesquiterpenes ; chemical synthesis ; pharmacology ; T-Lymphocytes ; drug effects

OBJECTIVETo study the validity of criteria currently used in China for the classification of symmetric small for gestational age infants (SGA) as compared with its definition.

METHODSThis study included 417 inpatients diagnosed as SGA in authors' hospital from January 1998 to June 2002. Symmetric SGA was diagnosed by the following three criteria: (1) the Ponderal Index (PI), (2) the crown-heel length-to-head circumference ratio (BL/HC) issued in Chin J Pediatr (1988;26:164 - 165), as well as (3) the SGA definition. The definition criterion was considered as the "gold standard". The sensitivity, specificity, false positive and negative values, positive and negative predictive values, exact agreement ratio, diagnosis index, and Cohen's Kappa value were used to evaluate the validity and agreement of the methods of PI and BL/HC. Receiver Operating Characteristic (ROC) analysis was used to evaluate the validity of the diagnosis.

RESULTSOf 417 SGA infants, 376 (90.17%), 376 (90.17%) and 187 (44.84%) subjects were diagnosed as symmetric type with PI, BL/HC and the definition criteria, respectively. (2) The agreement rate and Kappa value between PI and BL/HC was 80.82% and -0.093 (SEM 0.026), respectively. And the agreement rates between PI or BL/HC and the definition criterion were 49.88% and 50.84%, respectively. As compared with the definition criterion, the PI and BL/HC methods had sensitivities of 91.8% - 96.4%, specificities of 9.3% - 25.9%, positive predictive values of 45.8% - 51.1%, negative predictive values of 72.7% - 82.8%, diagnosis indices of 4.9% - 17.7% and Kappa values of 0.070 - 0.167. (3) The areas under the ROC curves in full-term and preterm infants by PI method were 0.635 (95% CI, 0.573 - 0.697) and 0.698 (95% CI, 0.622 - 0.725), respectively. PI cutoffs at 2.47 in full-term SGA, at 2.43 in preterm SGA, and BL/HC cutoff at 1.43 produced the maximum diagnosis indices that were 24.7%, 39.6% and 33.7%, respectively. When the PI at 2.50 (full-term), PI at 2.31 (preterm) and BL/HC values at 1.46, the sensitivity closed mostly to the specificity. The sensitivities and specificities in full-term and preterm infants were 59.4% and 59.3%, 65.3% and 65.5%, and 66.3% and 65.5%, respectively.

CONCLUSIONIn the classification of SGA, the results showed a poor agreement between PI or BL/HC and the definition criterion. The results suggested that the current cutoffs of PI and BL/HC might not be appropriate for the diagnosis of symmetric SGA. Low AUC suggested that PI and BL/HC could not give a valid diagnosis at any cutoffs.

Anthropometry ; methods ; Birth Weight ; Body Height ; China ; Female ; Gestational Age ; Humans ; Infant, Newborn ; Infant, Premature ; Male ; Reproducibility of Results ; Sex Factors

BACKGROUND:Polylactic acid and its copolymers have been widely used in biomedical fields because of their good biocompatibility and biodegradability, which have become a hotspot in the research of biomaterials. OBJECTIVE:To review the biocompatibility of fully degradable polylactic acid and its copolymers. METHODS:A computer-based online retrieval of PubMed and CNKI was performed to search relevant papers published from 2006 to 2016, with the key words of "polylactide, polylactic acid, copolymer, biodegradability, biocompatibility, animal" in English and Chinese, respectively. RESULTS AND CONCLUSION:Polylactic acid and its copolymers as polyester compounds are approved by the US Food and Drug Administration for use in the biomedical field because of their good biocompatibility mainly as drug delivery carriers and temporary implants. Moreover, their side effects in clinical application have attracted attentions. Polylactide copolymers can cause some adverse reactions when used in drug delivery systems, orthopedic and skin care, and other clinical medical fields. These copolymers are deemed to have no impact on the central nervous system, eyes, cardiovessels and other tissues and organs. They also have no virtually genotoxic and carcinogenic effects. Currently, the polylactide copolymer implant mainly results in local reactions in the surrounding tissues, and no systemic reactions have been found.

OBJECTIVE: To investigate the effect and possible mechanism of lidocaine precondition on calcium overload and apoptosis of the hepatocytes induced by cell hypoxia-reoxygenation. METHODS: The cultured L02 hepatocytes were randomly divided into 3 groups: a hypoxia-reoxygenation group (Group I), a lidocaine precondition group (Group II), and a normal control group (Group III). After 4 hours of cell hypoxia and 10 hours of reoxygenation, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) concentrations in the nutritive medium were detected. The cytoplasm ionic calcium concentration was measured by fluoro spectrophotometer. The apoptosis was measured by flow cytometry and fluorescent microscope. The appearance and ultra-microstructure changes of hepatocytes were observed by inverted microscope and electronic microscope. RESULTS: Cytoplasm ionic calcium concentration and apoptosis was positively correlated (r=0.7652, R(2)=0.5855, P< 0.05). The ALT concentration in the nutritive medium, AST concentration in the nutritive medium, cytoplasm ionic calcium concentration and the ratio of apoptosis of Group I and II were significantly higher than those of Group III(P< 0.05).The appearance and ultra-microstructure changes of Group I and II were worse than those of Group III. The ALT concentration in the nutritive medium, AST concentration in the nutritive medium, cytoplasm ionic calcium concentration and the ratio of apoptosis of Group II were significantly lower than those of Group I (P< 0.05). The ultra-microstructure injury of hepatocytes of Group II were less serious than those of Group I. CONCLUSION Precondition with lidocaine can attenuate calcium overload of hepatocytes induced by hypoxia-reoxygenation in vitro,and decrease the ratio of apoptosis.
Apoptosis ; drug effects ; Calcium ; metabolism ; Cell Hypoxia ; drug effects ; Cells, Cultured ; Hepatocytes ; cytology ; drug effects ; metabolism ; Humans ; Lidocaine ; pharmacology ; Oxygen ; metabolism

ObjectiveTo investigate the value of 18F-FDG SPECT myocardial imaging in evaluating haemodynamic change,treatment outcome and prognosis for idiopathic pulmonary arterial hypertension (IPAH).MethodsAll 24 patients with IPAH underwent 18 F-FDG SPECT myocardial imaging.Right ventricle/left ventricle (RV/LV)-FDG uptake was calculated by ROI method drawing over the central areas of left and right ventricular free walls.All patients underwent right heart catheterization within 3 days after imaging studies.Mean pulmonary artery pressure (mPAP) and pulmonary vascular resistance (PVR) were recorded.After six month pharmaceutical treatment,15 IPAH patients were re-examined with 18F-FDG SPECT myocardial imaging followed by repeated right heart catheterization within 3 days.Plasma N-terminal pro-brain naturetic peptide (NT-proBNP) and endothelin-1 ( ET-1 ) were measured in 17 patients using electrochemiluminescent immunoassay and enzyme immunoassay respectively.All patients were followed up for 12 months at least.Correlations between RV/LV-FDG uptake and mPAP and PVR were determined by simple linear regression analysis.Change of RV/LV-FDG before and after treatment was calculated using Student's t-test.Survival in groups with RV/LV FDG uptake ≥ 1.15 and RV/LV-FDG uptake ＜ 1.15 were compared using Log-rank test.ResultsSignificant correlations were found between RV/LV-FDG uptake and mPAP (r =0.562,P ＜ 0.01 ),and between RV/LV-FDG uptake and PVR ( r =0.574,P ＜ 0.01 ).There were no significant correlation between RV/LV-FDG uptake and NT-proBNP( r =0.18 1,P ＞ 0.05 ),but a significant correlation between RV/LV-FDG and ET-1 was observed (r =0.669,P ＜ 0.01 ).The RV/LV-FDG uptake in patients with positive treatment outcome ( n =6) decreased from 1.38 ± 0.52 to 0.92 ±0.26 (t =4.018,P ＜ 0.05) after 6 months treatment.In contrast,no significant change of RV/LV-FDG uptake was seen in those patients (n =9) with negative treatment outcome ( t =1.861,P ＞ 0.05 ).The mean follow-up time was (21 ±8) months.Mean survival time for the patients with RV/LV- FDG uptake ≥ 1.15was 28 months (95％ confidence interval:24-32 months),which was significantly lower than 34 months survival (95％ confidence interval:33-35 months) for the patients with RV/LV-FDG ＜ 1.15 (x2 =3.956,P ＜0.05 ).Conclusions Detection of right ventricle myocardial glucose metabolism level with 18F-FDG SPECT may be a practical method for evaluating haemodynamic change,treatment outcome and prognosis of IPAH.