OBJECTIVE:To optimize the formulation of Asiaticoside cationic liposomes,and to investigate the characteristics of drug release in vitro. METHODS:The thin film dispersion method was used to prepare liposome;using encapsulation efficiency and drug-loading amount as index,the formulation of Asiaticoside liposomes was optimized by central composite design-response surface method with the ratio of drug to lipid(X1),the ratio of cholesterol to lipid(X2)and the concentration of D-mannose(X3) as factors. Using sodium lauryl sulfate as medium,in vitro release characteristics of cationic liposomes prepared with 1%octadecyl-amine was investigated by bag filter method,and compared with those of Asiaticoside solution and common liposome. RESULTS:The optimal formulation was X1 0.07,X2 0.17 and X3 0.03 g/ml. The encapsulation efficiency was (75.529 ± 1.071)%,and drug-loading amount was(2.539±0.029)%(n=3);the deviation from the predicted values were -0.217% and 0.205%;1% oc-tadecylamine was add into formulation to obtain cationic liposomes,and the Zeta potential had changed from -5.6 mV to 20.8 mV. in vitro accumulative release rates of Asiaticoside solution,common liposomes and cationic liposomes were 89.13%(12 h), 87.58%(72 h) and 94.46%(72 h),and the latter was in line with Weibull model. CONCLUSIONS:Asiaticoside cationic lipo-somes have high encapsulation efficiency,and can releases for 72 h.

Objective To detect the mutations of pigment epithelium derived factor (PEDF) gene in a human malignant melanoma cell line A375. Methods A375 cells and control melanocytes obtained from circumcised prepuce were cultured, genomic DNA was extracted from these cells. All eight exons of PEDF gene were scanned by single strand conformation polymorphism analysis ofpolymerase chain reaction products (PCR-SSCP) in both A375 cells and control melanocytes. DNA sequencing was performed for the PCR products separated into electrophoretic bands with altered mobility. Results Altered mobility was observed with SSCP analysis in amplicons of exon 3, 4, 5, 6 and 7, with the most obvious alteration occurred in exon 5 and 6. DNA sequencing revealed mutations in both exon 5 and 6. The common type of mutations was single base-deletion in exon 5 and single base-substitution in exon 6. Conclusion Mutations of PEDF gene may contribute to the development of human malignant melanoma.

BACKGROUND:Apoptosis of chondrocytes eventualy leads to osteoarthritis. New studies find many mechanisms of chondrocyte apoptosis, but the mechanism of endoplasmic reticulum stress-induced chondrocyte apoptosis is stil in the first stage. OBJECTIVE: To review how the endoplasmic reticulum stress causes the chondrocyte apoptosis and to explore a new method of treatment for osteoarthritis. METHODS: A computer-based online search of PubMed database, CNKI database and Wangfang database between January 2000 and January 2015 was performed to search related articles with the key words of “endoplasmic reticulum stress, chondrocyte, apoptosis” in English or in Chinese, respectively. The word “AND” was used for the connection between the word retrieval. Literatures related to osteoarthritis were selected; the articles published lately in authoritative journals were preferred. RESULTS AND CONCLUSION: A total of 62 literatures were primarily selected, and 57 documents were involved in result analysis according to inclusion criteria. PERK, IRE1 and ATF6 play an important role in the chondrocytes. Endoplasmic reticulum stress-mediated apoptosis mechanisms include two kinds, UPR and Ca2+start signal, but the specific mechanism and the interactions between apoptosis pathway are unclear. Inhibitory molecules for chondrocyte apoptosis in these signaling pathways as treatment targets for osteoarthritis may provide new methods for the treatment of osteoarthritis.

30 ml) undergoing minimally invasive evacuation of intracranial hematoma from January 1999 to October 2002 in our department were analyzed retrospectively. The changes of IL 1, IL 6, and IL 8 in hematoma fluid were observed continuously. The content of IL 1 was determined by radioimmunassay and IL 6, IL 8 by ELISA methed. Results IL 1, IL 6, and IL 8 were observed at 6 12 h after hypertensive cerebral hemorrhage, and showed different changes in acute stage. Conclusion Inflammatory cytokines are involved in the pathological process of cerebral hemorrhage.

It is important to pay more attention to students’ basic skills training and their comprehensive abilities cultivating in microbiology experiment teaching. Explorations and reforms in enforcing the students’ base and cultivating their abilities were carried out in order to improve teaching quality and train specialized talents with high quality.

Objective To evaluate the left ventricular rotation and twist in the cardiac allograft by speckle tracking echocardiography.Methods Twenty-six heart transplant recipients underwent echocardiographic studies at 1st,3rd,6th and 12th month after heart transplantation.Twenty-six healthy subjects served as controls.Parasternal basal and apical short-axis images of left ventricle were recorded and then were analyzed using EchoPAC software.The curves of basal and apical rotation and left ventricular twist were obtained,Peak values of basal and apical rotation and left ventricular twist were measured and then statistically analyzed.Results There were no significant differences in left ventricular ejection fraction (LVEF) and fractional shortening (LVFS) between heart transplant recipients and controls (P ＞0.05).The left ventricular twist,apical rotation were significantly lower in heart transplant recipients at 1 st,3rd,6th and 12th month after surgery than those in controls (P ＜0.05) ;while basal rotation in heart transplant recipients had no significant difference when compared with controls (P ＞0.05).The left ventricular twist,apical and basal rotation in heart transplant recipients among 1 st,3rd,6th and 12th month after surgery had no significant difference (P ＞ 0.05).Conclusions Although the LVEF and LVFS of cardiac allograft seemed normal,the left ventricular twist,apical rotation were still significantly lower in heart transplant recipients than those in controls.Speckle tracking echocardiography can be used for accurate assessment of left ventricular twist in heart transplant recipients.

Objective To evaluate the diagnostic value of 64 multidetector-row CT angiography for internal carotid artery(ICA)stenosis and the application in the follow-up of carotid endarterectomy and percutaneous transluminal stenting.Methods Forty transient ischemie attack(TIA)patients with interpretable CTA and DSA of the cervical carotid arteries were selected from May 2005 to December 2005. This yielded a total of 80 vessels.The CTA curved planar reformations(CPR)and DSA images referenced to the distal cervical internal carotid were graded by two senior neuroradiologists blindly,according to the North American Symptomatic Carotid Endarterectomy Trial(NASCET)guidelines.The paired-t test was used to verify the statistical significant difference between pre-operating and post-operating of carotid endarterectomy or percutaneous transluminal stenting in measuring the vascular diameter and area of cross section using CTA.Results When the 70% stenosis was used as the cut-off value,the seasitivity,specificity,negative predictive value,and the positive predicting value were 97%,95%,95%,and 98%,respectively.There was statistically significant difference in measuring the vascular diameter(P

Objective To investigate the dynamic changes of adenosine receptors, A1 (A1R) and A2a (A2aR) in the brain from the acute to chronic phase after kindling and to explore the correlation between seizure and expression level of A1R and A2aR. MethodsRats were randomly selected into the testing model, reference and normal control groups.Testing rats were kindled by lithium choride-pilocarpine, reference rats were treated with saline, and no treatment was given in normal control group. The dynamic expression of A1R and A2aR were detected by RT-PCR, immunofluorescence staining and Western blot at time-points of 24 hours, 1 month and 6 months post-kindling. Results In the acute phase of 24 hours after kindling, the A1R expression level (mRNA level was (1. 1483 ±0. 1182); Western blot result was ( 0. 7872± 0. 0621 ) ; immunofluorescence staining count was ( 76. 17 ± 4. 62 )/HP) was increased and A2aR (mRNA level was (0. 8338±0. 0572) ; Western blot result was (0. 2098 ±0. 0257) ; immunofluorescence staining count was (43. 83 ± 5. 12 )/HP) was decreased.The results showed statistically difference compared with the reference and normal groups (P< 0. 05 ). In the later chronic phase of 1 month and 6 months after kindling, the expression level of A1R was decreased and A2aR was increased. These data revealed statistically significant difference (P <0. 01 ). Furthermore, the comparison of the results in 1 month and 6 months after kindling found that the expression of AIR was lower in 6 months (mRNA level was (0. 5682 ±0. 0443) ; Western blot result was (0. 7749 ±0. 0262) ; immunofluorescence staining count was (38. 50 ±4. 81 )/HP) than in 1 month and that of A2aR was higher in 6 months (mRNA level was (1. 2169±0. 0332) ; Western blot result was (0. 7080 ±0. 0371 ); immunofluorescence staining count was (114. 50 ± 4. 04)/HP). The differences were statistical significant (t = - 19. 02--13.28, P < 0. 05). ConclusionsThe expressions of A1R and A2AR during and after kindling presents a bidirectional change. In the acute phas the expression of AR is regulated to suppress seizures. While in the chronic phase, the repeated seizures result in the change of A1R and A2aR expression in the opposite direction. This mechanism plays an important role in refractory seizures.

To investigate the anticancer effects of ring C in 18β-glycyrrhetinic acid (GA), a series of GA derivatives featured with 9(11)-ene moiety in ring C were designed and synthesized. The structures were confirmed by IR, LC-MS and 1H NMR. Their inhibitory effects towards human prostate cancer PC-3 and leukemia HL-60 cell lines were determined. Most of the derivatives displayed stronger antiproliferative activities than GA. Particularly, compound 14 showed promising anticancer activity with the GI50 values of 4.48 µmol · L(-1) and 1.2 µmol · L(-1) against PC-3 and HL-60 cells respectively, which is worth further study.
Antineoplastic Agents ; chemistry ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; drug effects ; Drug Design ; Glycyrrhetinic Acid ; analogs & derivatives ; chemistry ; HL-60 Cells ; drug effects ; Humans ; Male ; Prostatic Neoplasms ; pathology

Objective To explore the expression of transforming growth factor ?1(TGF-?1)in the mucosa of guinea pigs with otitis media with effusion(OME)and the role of TGF-?1 in the development of OME.Methods 70 guinea pigs were randomly devided into 7 groups,each with 10 animals.OME was produced by injecting deactivated streptococcus pneumoniae into the typmpanic cavity of guinea pigs.The expression of TGF-?1 was examined by means of immunohistochemistry 6 h,1 d,3 d,7 d,14 d and 30 d after injection.Results TGF-?1 expression could be detected in the middle ear mucosa at 7 d after injection and reached maximum at 30 d.Conclusion TGF-?1 is expressed in the middle ear mucosa of the guinea pigs with OME induced by deactivated streptococcus pneumoniae,and this indicates that TGF-?1 may play a role in the chronic protraction of OME.