The optimum conditions of baicalin hydrolysis into baicalein by immobilized beta-glucosidase in a two-phase system was studied and the yield was observed. A two-phase system comprising of sodium acetate buffer and chloroform was determined by comparing the solubleness of baicalein in different solvents and partition coefficient of baicalein in related aqueous-organic two-phase system. beta-Glucosidase was immobilized by the crosslinking-embedding method using sodium alginate as the carrier The optimum reaction temperature, pH value, Michaelis constant, the thermal stability and pH stability were assayed. By comparing the yield of baicalin hydrolysis into baicalein by immobilized beta-glucosidase in two-phase system, the optimum reaction conditions were determined-the optimum reaction temperature, pH value and time were 50 degrees C, 5.0 and 10 h, respectively. The yield of baicalein was 85.28%. Compare with one-phase system, two-phase system had an advantage in reaction rate and yield.
Biocatalysis ; Drugs, Chinese Herbal ; chemistry ; Enzyme Stability ; Enzymes, Immobilized ; chemistry ; Flavanones ; chemistry ; Flavonoids ; chemistry ; Hydrolysis ; beta-Glucosidase ; chemistry

Aged ; Female ; Femoral Neck Fractures ; diagnostic imaging ; surgery ; Fracture Fixation, Internal ; methods ; Humans ; Male ; Middle Aged ; Radiography ; Retrospective Studies ; Treatment Outcome

AIMTo evaluate the effect of in vitro and in vivo treatment with mitomycin C (MMC) on activities of CYP2D1/2, CYP2C1 , and CYP1A2 in the liver of male rats.

METHODSUsing HPLC to determine the activities of the three isoenzymes in rat liver microsomes by detecting the specific metabolites of their substrates after treatment with inducers in vivo or inhibitors in vitro.

RESULTSIn vitro, MMC inhibited the activity of CYP2D1/2, CYP2C11, and CYP1A2 in dexamethasone-induced microsomes by (19 +/- 6)% (P < 0.05), (85 +/- 10)% (P < 0.01), and (36 +/- 6)% (P < 0.05), respectively, and decreased the activity of CYP1A2 in beta-naphthoflavone-induced microsomes by (58 +/- 6)% (P < 0.01). Rats were injected intraperitoneally with 20% of the LD50 of MMC for 3 or 6 d. The treatment showed no significant effect on microsomal activities of CYP2D1/2, CYP2C11 or CYP1A2.

CONCLUSIONMMC can inhibit the activities of CYP2D1/2, CYP2C11, and CYP1A2 in rat liver microsomes in vitro, but it showed no significant effect on the activities of the three isoenzymes in vivo.

Alcohol Oxidoreductases ; Animals ; Antibiotics, Antineoplastic ; pharmacology ; Aryl Hydrocarbon Hydroxylases ; metabolism ; Biotransformation ; Cytochrome P-450 CYP1A2 ; metabolism ; Cytochrome P450 Family 2 ; Male ; Microsomes, Liver ; enzymology ; Mitomycin ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Steroid 16-alpha-Hydroxylase ; metabolism

Craniofacial Dysostosis ; Humans ; Receptors, Fibroblast Growth Factor

BACKGROUNDPemetrexed is a novel folic acid antagonist with multiple targets, which has been widely used in the treatment of non-small cell lung cancer (NSCLC). The objective of this study was to compare the effects and toxicities in NSCLC patients treated with pemetrexed monotherapy versus pemetrexed plus a platinum combination agent, so as to provide a basis for standard second-line chemotherapy.

METHODSThe clinical data of 52 patients with NSCLC who were admitted to Shanghai Chest Hospital from August 2006 to October 2008 were retrospectively analyzed. Ten of the 52 patients received pemetrexed monotherapy, and the other 42 patients received the pemetrexed plus platinum regimen. The primary end point was overall survival (OS). The progression-free survival time (PFS) was analyzed and the effects and toxicities were assessed. Survival analysis was evaluated by Kaplan-Meier method. Single factor analysis and the COX regression model were done to analyze the relationship between the influential factors and the prognosis of disease. The elderly patients (> or = 60 years old) were analyzed separately as a subgroup.

RESULTSNo statistically significant increase in OS (chi(2) = 0.09, P = 0.76), PFS (chi(2) = 0.15, P = 0.70), disease control rate (DCR) (chi(2) = 0.06, P = 0.81) or 1-year survival rate (chi(2) = 0.33, P = 0.57) was found between the two regimens. Single factor analysis showed that the factors including surgery history, PS score before treatment, clinical stage, and response to second-line treatment influenced the prognosis of NSCLC (all P < 0.05). COX regression analysis demonstrated that surgery history (P = 0.041) and performance status (PS) score before treatment (P = 0.043) may be associated with survival. The toxicity of the two regimens was similar. In the subgroup of elderly patients, no significant difference in OS (chi(2) = 0.01, P = 0.94), PFS (chi(2) = 0.14, P = 0.70), DCR (chi(2) = 0.004, P = 0.95), or 1-year survival rate (chi(2) = 0.03, P = 0.87) was found between the two regimens. The toxicity of combination therapy was significantly higher in terms of hematologic (chi(2) = 9.95, P = 0.01) and gastrointestinal adverse events (chi(2) = 7.66, P = 0.03).

CONCLUSIONSThere is no significant difference in survival or side effects between these two regimens. For elderly patients (> or = 60), pemetrexed monotherapy shows similar efficacy and a better safety profile when compared with pemetrexed combination therapy.

Aged ; Aged, 80 and over ; Antineoplastic Agents ; therapeutic use ; Antineoplastic Combined Chemotherapy Protocols ; Carcinoma, Non-Small-Cell Lung ; drug therapy ; Female ; Glutamates ; therapeutic use ; Guanine ; analogs & derivatives ; therapeutic use ; Humans ; Lung Neoplasms ; drug therapy ; Male ; Middle Aged ; Pemetrexed ; Platinum ; therapeutic use ; Retrospective Studies ; Treatment Outcome

OBJECTIVETo compare the characteristics of interbody fusion achieved using hat type cervical intervertebral fusion cage (HCIFC) with those of an autologous tricortical iliac crest graft, Harms cage and Carbon cage in a goat cervical spine model.

METHODSThirty-two goats underwent C(3, 4) discectomy and fusion in which the following were used: Group 1, autologous tricortical iliac crest bone graft (8 goats); Group 2, Harms cage filled with autologous iliac crest graft (8 goats); Group 3, Carbon cage filled with autologous iliac bone (8 goats); Group 4, HCIFC filled with autologous iliac graft (8 goats). Radiography was performed pre- and postoperatively and after 1, 2, 4, 8, and 12 weeks. At the same time points, disc space height, intervertebral angle, and lordosis angle were measured. After 12 weeks, the goats were killed and fusion sites were harvested. Biomechanical testing was performed in flexion, extension, axial rotation, and lateral bending to determine the stiffness and range of motion. All cervical fusion specimens underwent histomorphological analysis.

RESULTSOne week after operation, the DSH, IVA and LA of HCIFC and Carbon cage were statistically greater than those of autologous iliac bone graft and Harms cage. Significantly higher values for disc space height, intervertebral angle and lordosis angle were shown in cage-treated goats than in those that received bone graft over a 12-week period. The stiffness of Harms cage in axial rotation and later bending were statistically greater than that of other groups. Radiographic and histomorphologic evaluation showed better fusion results in cage groups than in autologous bone group.

CONCLUSIONSHCIFC can provide a good intervertebral distractability and enough biomechanical stability for cervical fusion.

Animals ; Biomechanical Phenomena ; Bone Transplantation ; methods ; Cervical Vertebrae ; diagnostic imaging ; physiopathology ; surgery ; Goats ; Ilium ; transplantation ; Internal Fixators ; Male ; Materials Testing ; Radiography ; Random Allocation ; Spinal Fusion ; instrumentation ; methods ; Transplantation, Autologous

Objective To analyze the cause, prevention and treatment of complications related to endovascular embolotherapy for ruptured intracranial aneurysms. Methods Sixty-eight patients with ruptured intracranial aneurysms received early endovascular embolization. Intraoperatively, artery spasm was relieved by papaverine infusion through microcatheter or balloon dilatation; parent artery occlusion by coils was treated by anticoagulation or antiplatelet treatment; ruptured aneurysms were embolized using mixed heparin; arterial thrombosis after embolization was ameliorated by the micro-catheter infusion of r-tPA thrombolytic. Results In the 68 cases, 8 cases suffered from complications, accounting for 11.77%. Among them, 1 case of extensive spasm of middle cerebral artery developed cerebral infarction and mild hemiplegia; 2 cases of localized spasm were improved well without sequelae; 1 case in which partial coils entered middle cerebral artery achieved a satisfied therapeutic outcome without infarction; 1 case with cerebral infarction due to coil dropping and 1 case with aneurysm rupture during operation received secondary embolotherapy without adverse consequences; one week after operation, 1 case died from aneurysm re-rupture; 1 case had hemiplegia owing to massive cerebral infarction. Conclusions It will do much benefit to secure the success of the operation by displaying the location, shape and size of the aneurysms as well as the relationship with the parent artery. Moreover, the proper choice of coils and well mastering of operative skills can decrease the incidence of complications, and adequate and prompt treatment of intraoperative complications can improve the prognosis of the patients obviously.

Objective To evaluate the efficacy and safety of oxiracetam in the treatment of neurological deficits resulting from brain injury through the comparison of oxiracetam for injection and piracetam for injection in clinical trials. Methods A multiple-center, randomized, double-blind,parallel study was performed on 239 patients; these patients were divided into experimental group (oxiracetam for injection, n=120) and control group (piracetam, n=119). National institutes of health stroke scale (NIHSS), Glasgow coma scale (GCS), myodynamia grading, mini-metal state examination (MMSE) were employed to evaluate the therapeutic effects; electrocardiogram and laboratory examination were performed, and the side effects were also observed. Results The scores of NIHSS,GCS and myodynamia grading after treatment in the 2 groups were all significantly higher than those before treatment (P＜0.05); however, no significant differences on these scores were noted between the experimental group and control group (P＞0.05). No serious adverse events were noted in both groups.Conclusion Oxiracetam, the same as piracetam, is safe and effective in the treatment of neurological deficits secondary to brain injury.

OBJECTIVETo identify the uptake and biological distribution of technetium galactosyl human serum albumin diethylenetriamine pentaacetic acid injection (99mTc-GSA) in three mouse models with different degrees of hepatic injuries.

METHODSThree mouse models including hepatic fibrosis, hepatic cholestasis, and liver cancer were established. Hepatic fibrosis model was established by intraperitoneal injection of carbon tetrachloride, 0.4 ml 10%, every 48 hours for 48 days. Hepatic cholestasis model was set up by ligature of the common bile duct for 72 hours, and liver cancer model by implantation of H22 tumor cells underneath liver capsule for 10 days. On measurement, each mouse in different models and normal controls was injected with 0.1 ml (0.37 MBq)99mTc-GSA (2 microg) into vena caudalis, and 5 minutes later sacrificed by decapitation. Important organs and tissues including liver, heart, lungs, kidney, spleen, stomach, blood, bones, muscles, and intestines were taken and their different radio countings were measured. The hepatic injuries were evaluated with serum and pathological examinations.

RESULTS99mTc-GSA was concentrated in the liver in all three models and the control mice ( >40% ID x g(-1)). Compared with the control mice (90.05 +/- 10.55)% ID x g(-1), the density of 99mTc-GSA was significantly lower in the models with hepatic injuries (P < 0.001). The liver function test indicated that the injury in hepatic fibrosis model was less serious than those in the other two models. However, the concentration of 99mTc-GSA in hepatic fibrosis model [(72.20 +/- 2.13)% ID x g(-1)] was significantly higher than those in the models with cholestasis [(56.72 +/- 5.92)% ID x g(-1)] and liver cancer [(42.80 +/- 6.05)% ID x g(-1)] (P < 0.001).

CONCLUSIONS99mTc-GSA may well concentrate in liver and its concentration degree is adversely correlated with hepatic injuries. Therefore 99mTc-GSA may be clinically used as liver imaging agent. When combined with three-dimensional scanning technique, it may facilitate constructing a new three-dimensional imaging method to demonstrate the function of designed liver segments.

Animals ; Disease Models, Animal ; Female ; Humans ; Liver ; diagnostic imaging ; drug effects ; injuries ; Liver Diseases ; diagnosis ; diagnostic imaging ; Mice ; Mice, Inbred BALB C ; Radiography ; Radionuclide Imaging ; Radiopharmaceuticals ; administration & dosage ; pharmacokinetics ; Random Allocation ; Technetium Tc 99m Aggregated Albumin ; administration & dosage ; pharmacokinetics ; Technetium Tc 99m Pentetate ; administration & dosage ; pharmacokinetics

OBJECTIVELeber's hereditary optic neuropathy (LHON) is a maternally inherited degeneration of the optic nerve caused by point mutations of mitochondrial DNA (mtDNA). Many unsolved questions regarding the penetrance and pathophysiological mechanism of LHON demand efficient and reliable mutation testing. This study aims to develop a minor groove binder (MGB) probe assay for rapid detection of mtDNA11778 mutation and heteroplasmy in Chinese LHON patients by real-time polymerase chain reaction (PCR).

METHODSForty-eight patients suspected of having LHON and their maternal relatives underwent a molecular genetic evaluation, with 20 normal individuals as a control group at the same time. A real-time PCR involving two MGB probes was used to detect the mtDNA11778 mutation and heteroplasmy. A linear standard curve was obtained by pUCmLHONG and pUCmLHONA clones.

RESULTSAll 48 LHON patients and their maternal relatives were positive for mtDNA11778 mutation in our assay, 27 heteroplasmic and 21 homoplasmic. Eighteen cases did not show an occurrence of the disease, while 9 developed the disease among the 27 heteroplasmic mutation cases. Eleven did not show an occurrence of the disease, while 10 cases developed the disease among 21 homoplasmic mutation cases. There was a significant difference in the incidence between the heteroplasmic and the homoplasmic mutation types. The time needed for running a real-time PCR assay was only 80 min.

CONCLUSIONThis real-time PCR assay is a rapid, reliable method for mtDNA mutation detection as well as heteroplasmy quantification. Detecting this ratio is very important for predicting phenotypic expression of unaffected carriers.

China ; DNA Probes ; analysis ; genetics ; DNA, Mitochondrial ; analysis ; genetics ; Humans ; Mutation ; genetics ; Optic Atrophy, Hereditary, Leber ; blood ; genetics ; Polymerase Chain Reaction ; methods ; Time Factors