Herpetin (HPT) is an active monomer constituent isolated from lignanoid in seeds of Herpetospermum caudigerum. HPT shows inhibitory effects in hepatic injury and HBV-DNA and the replication. In the study, we successfully prepare herpetin liposomes by film dispersion method for the first time. The prescription process was optimized, with the entrapment efficiency as the index. According to the optimized prescription, the mass ratio of HPT: phospholipids: cholesterol was 2.44:78.05: 19.51, the hydration and de-molding process was performed with 0.5% F68 solution at 50 degrees C, and the water-bath ultrasonic time was 20 min. The HPT liposomes prepared by this method showed an average entrapment efficiency of (94.50 +/- 2.15)% and a particle size of (119.2 +/- 10.7) nm, which was consistent with the trial expectations and will lay a solid foundation for the hepatic targeting delivery system in future.
Chemistry, Pharmaceutical ; methods ; Cholesterol ; chemistry ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Lignans ; chemistry ; isolation & purification ; Liposomes ; chemistry ; Phospholipids ; chemistry ; Ultrasonics

Objective To study the effect of intensive trunk muscle training on balance and walking in pa- tients with hemiplegia caused by stroke.Methods A total of 90 stroke patients were recruited and randomly divid- ed into a treatment group(45 cases)and a control group(45 cases).All the patients were given conventional reha- bilitation training.Meanwhile,intensive trunk muscle training was also administered for those in the treatment group as well.The trunk control function,balance ability and walking ability were assessed by using the trunk control test, Berg Balance Scale and the balance subscale of the Fugl-Meyer physical performance test,and Holden's functional ambulation classification,respectively,before and after 6 weeks of training.Results It was found that all the pa- tients scored better with the trunk control test,Berg's balance scale,the balance subscale of the Fugl-Meyer physical performance test and Holden's ambulation classification after treatment,and there were significant differences between the two groups after treatment(P

Objective To assess the liver histopathological characteristics of chronic hepatitis B (CHB) patients with alanine aminotransferase(ALT)lower than 2 times the upper limit of normal (ULN) through liver biopsy, and try to provide subjective evidence for clinical anti-viral treatment.Methods From October 2005 to August 2010, patients accepted liver biopsy in department of infectious disease, Sichuan provincial people's hospital were enrolled. The criteria for liver biopsy was as follow, (1) HBsAg-positive for more than 6 months, (2) HBeAg-positive patients with HBV DNA ≥103 copies/ml or HBeAg-negative patients with HBV DNA≥ 104copies/ml, (3) ALT was lower than 2 times ULN for more than 6 months,and without any hepatic protectants, (4) never accepted any antiviral treatment before, including IFN or nucleoside analogues, (5) willing to accept liver biopsy. Before liver biopsy, routine blood test, prothrombin time, liver function test, hepatitis B antigen and antibody test, HBV DNA quantification were examined. The biopsy position was located under routine ultrasound, liver biopsy were performed to assess the grading of inflammation and necrosis and the degree of fibrosis. The correlation between all the factors and liver inflammation and fibrosis were analyzed. Results Totally 383 cases (240 males and 143 females) met the diagnostic criteria, aged from 16 to 59 years old and the mean age was 28.0 years old. Cases of liver inflammation in G0, G1, G2, G3andG4 grade was 2 cases (0.5％), 165 cases (43.1％), 191 cases (49.9％), 25 cases (6.5 ％ ) and 0 cases (0 ％ ) respectively, cases≥G2 grade accounted 56.4 ％ of total. Meanwhile,stage of fibrosis in S0, S1, S2, S3 and S4 was 103 cases (26.9％), 265 cases (69. 2％), 13 cases (3.4％), 2 cases (0.5％) and 0 cases (0％) respectively, percentage of liver fibrosis in S2stage and over was only 3.9％. The occurrence of serious liver inflammation was associated with age, ALT levels, HBV DNA levels and HBeAg status (P＜0.05). There was no obvious association between HBV DNA level and liver fibrosis (P＞0.05). Conclusions There were obvious liver inflammation and different degree of liver fibrosis in CHB patients with alanine aminotransferase(ALT)lower than 2 times ULN. The degree of liver injury assessed by liver biopsys is recommended as an evaluation for the necessary of anti-viral therapy.

Objective To investigative CT findings of gastrointestinal neurilemmoma,and to improve the recognition and diagnosis ability of the disesase.Methods Twelve cases of gastrointestinal neurilemmoma proven surgically and pathologically were included.The unenhanced CT and double phase enhanced CT were performed in all patients.The clinical feature and CT findings with regard to the location, size,contour,margin,growth type,contrast enhancement pattern,contrast enhanced degree,presence or absence of ulcer were retrospectively reviewed by two experienced radiologists.Results On unenhaneed CT, all the patients present masses with homogeneous attenuation in the wall of gastrointestinal tract,compared with muscle.Three of the gastric neurilemmoma showed endoluminal growth pattern,and 6 had a predominantly exophytic growth pattern,the tumor had both endoluminal and exophytic growth pattern in 3 cases.The tumors were round or oval with distinct margin in 10 of 12 gastrointestinal neurilemmoma,and lobulated with indistinct margin in 2 cases.Three of the gastric neurilemmoma had ulceration.On contrast- enhanced CT,all the tumors showed homogeneously solid mass.No obvious enhancement on the arterial phase showed moderate enhancement on portal vein phase in 10 cases,2 of gastrointestinal neurilemmoma which manifested mild enhancement on the arterial phase showed obvious enhancement on portal vein phase. Conclusion CT findings of most gastrointestinal neurilemmoma have characterstic,which appeared as round or oval,distinct margin,and homogeneously solid tumors,slow but fairly uniform and moderate enhancement throughout the mass.

OBJECTIVETo compare the liver pathohistological and clinical features between chronic HBV carriers and chronic hepatitis B patients with mild elevated in ALT.

METHODS128 patients were divided into 3 groups according to the ALT: group A: ALT is less than or equal to 0.5*ULN, group B: 0.5*ULN less than ALT is less than or equal to 1*ULN, group C: 1*ULN less than ALT less than 2*ULN. The age, sex, serum HBV DNA, HBeAg status, expression of HBcAg in liver, thickness of spleen, breadth of portal vein ,blood stream speed of protal vein, right liver obliqua diameter, grade of liver inflammation and stage of liver fibrosis were compared in the three groups.

RESULTSAmong 128 patients, 57(44.5%) patients had G1 hepatitis and 71 (55.5%) had G2 hepatitis, no G0 hepatitis was found in these patients; 72 patients (56.3%) had S1 fibrosis, 30 (23.4%) patients had S2 fibrosis, and 26 (20.3%) patients did not have liver fibrosis. The liver inflammation in group C was more aggravated than that in group A (P less than 0.05). And there were significant differences in thickness of spleen and right liver obliqua diameter between group C and group A, as well as between group C and B (P all less than 0.01). With the aggravating of liver inflammation, the serum ALT, thickness of spleen, breadth of portal vein and expression of HBcAg in liver were increased obviously (P less than 0.05). With the aggravating of liver fibrosis, the thickness of spleen, breadth of portal vein, right liver obliqua diameter and HBeAg negative patients were increased obviously, while the blood stream speed of portal vein was decreased obviously (P less than 0.01).

CONCLUSIONAmong the chronic HBV infection patients whose ALT less than 2*ULN, there were 55.5% patients had G2 of liver inflammation and 23.4% patients had S2 of liver fibrosis. The serum ALT, thickness of spleen, breadth and blood stream speed of portal vein, right liver obliqua diameter and expression of HBcAg in liver are associated with pathohistological changes in these patients.

Adult ; Alanine Transaminase ; blood ; Biopsy, Needle ; Carrier State ; blood ; pathology ; virology ; DNA, Viral ; blood ; Female ; Hepatitis B Core Antigens ; metabolism ; Hepatitis B e Antigens ; blood ; Hepatitis B, Chronic ; blood ; pathology ; virology ; Humans ; Liver ; metabolism ; pathology ; virology ; Liver Cirrhosis ; pathology ; Male ; Polymerase Chain Reaction ; methods ; Retrospective Studies ; Virus Replication

China ; Clinical Trials as Topic ; Drugs, Chinese Herbal ; adverse effects ; therapeutic use ; Humans ; Kidney Diseases ; drug therapy ; Prospective Studies ; Retrospective Studies ; Tripterygium

The progress in the research of the active ingredients of licorice flavonoid and the pharmacological activities was reviewed. Licorice flavonoid constituents mainly included flavones, flavonals, isoflavones, chalcones, bihydroflavones and bihydrochalcones. Pharmacological investigation concluded that they had antioxidant, antibacterial, antitumer and inhibiting HIV activities. It is important to study further the flavonoid constituents and pharmacological activities.
Animals ; Anti-HIV Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Antioxidants ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; Glycyrrhiza ; chemistry ; Humans ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry

AIMTo design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C3'-N of taxol side chain.

METHODSProtective side chain acid VI (4'S,5'R) was prepared from optically active (2'R,3'S) methyl beta-phenyl glycidate I in five steps. The desired acids were coupled with cephlotaxine and drupacine respectively in the presence of 2-DPC/DMAP, followed by acidic hydrolysis and acylating to give novel alkloid esters with different substitutes on C3'-N.

RESULTSThe seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C3'-N.

CONCLUSIONIt might provide some rational basis for further structral modification.

Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Colonic Neoplasms ; pathology ; Esters ; Harringtonines ; chemical synthesis ; chemistry ; pharmacology ; Humans ; KB Cells ; Liver Neoplasms ; pathology ; Molecular Structure

Objective To evaluate the efficacy and safety of continuous erythropoietin receptor activator (C.E.R.A.) once every 4 weeks by subcutaneous administration on hemoglobin (Hb)maintenance in dialytic patients with chronic renal anemia who had been treated with stable dose of erythropoietin (EPO).Methods This was an open,randomized,controlled,multi-center trial.All the hemodialysis or peritoneal dialytic patients in EPO maintenance treatment received subcutaneous EPO-β during the 6-week pre-treatment period to maintain Hb level between 100 g/L and 120 g/L.Eligible patients were randomized (2∶1 ) to accept either C.E.R.A.once every 4 weeks by subcutaneous administration ( C.E.R.A.group,n =187 ) or subcutaneous EPO-β 1-3 times weekly ( EPO group,n =94) for 28 weeks (including 20-week dose titration period and 8-week efficacy evaluation period ). The starting dose of C.E.R.A.was converted according to the dose of EPO-β administered in the week preceding the first study drug administration.The primary outcome was the change of Hb level between the baseline and that in the efficacy evaluation period.Results Totally 253 patients completed the whole 28-week treatment.The change of baseline-adjusted mean Hb was +2.57 g/L for C.E.R.A.group and + 1.23 g/L for EPO group,resulting in a treatment difference of 1.34 g/L (95％ CI - 1.11-3.78 g/L).Since the lower limit of 95％ CI was greater than the pre-defined non-inferiority margin -7.5 g/L( P ＜ 0.0001 ),C.E.R.A.once every 4 weeks by subcutaneous administration was clinically non-inferior to EPO regarding the maintenance of stable Hb level.The proportion of patients maintaining Hb level within the range of 100-120 g/L through efficacy evaluation period was similar between the two groups ( 69.0％ for C.E.R.A.group vs 68.9％ for EPO group,P ＞0.05 ).The overall incidence of adverse events was similar between the C.E.R.A.(41.7％)and EPO (46.2％ ) groups ( P ＞ 0.05 ).The safety findings were in accordance with the patients' primary diseases rather than the administration.Conclusions Conversion from EPO to C.E.R.A.once every 4 weeks by subcutaneous injection could maintain the Hb in target level in dialytic patients with renal anemia,and it was non-inferior to EPO.In general,subcutaneous administration of C.E.R.A.is well tolerated in dialytic patients with chronic renal anemia.

OBJECTIVETo study the effect of aldosterone on cell proliferation, alkaline phosphatase (AKP) activity and osteogenic gene expression in rat osteoblasts and explore the mechanisms.

METHODSOsteoblasts isolated from the skull of neonatal SD rats by enzyme digestion were cultured and treated with different concentrations of aldosterone. The cell proliferation and AKP activity were evaluated using CCK-8 assay kit and AKP assay kit, respectively. The effects of aldosterone on mRNA and protein expressions of the osteogenic genes and epithelial sodium channel (ENaC) gene were investigated using semi-quantitative PCR and Western blotting.

RESULTSCompared with the control cells, the cells treated with 0.01-1.0 µmol/L aldosterone showed obviously enhanced proliferation while lower (1×10µmol/L) or higher (10 µmol/L) concentrations of aldosterone did not significantly affect the cell proliferation. Aldosterone within the concentration range of 1×10to 10 µmol/L did not cause significant changes in AKP activity in the osteoblasts. Treatment with 0.01 to 1.0 µmol/L aldosterone significantly upregulated the expressions of the osteogenic genes and α-ENaC gene at both the mRNA and protein levels.

CONCLUSIONAldosterone within the concentration range of 0.01-1.0 µmol/L stimulates the proliferation and osteogenic gene expressions and enhances α-ENaC gene expression in rat osteoblasts in vitro, suggesting the possibility that ENaC participates in aldosterone-mediated regulation of osteoblast functions.