AIMTo study the synthesis and antitumour activities of some aryl-substituted pteridines.

METHODSA series of aryl-substituted pteridines were synthesized from 4, 6-diamino-5-nitrosopyrimidines by cyclization with 4-aminophenylacetonitriles. The antitumour activities were tested by MTT method.

RESULTSNine new compounds (I-III) were synthesized and their structures were characterized by EA, IR, 1HNMR and MS spectra. Compounds I-III showed antitumour activities in vitro.

CONCLUSIONCompounds I-III showed remarkable antitumour activities in vitro. No interaction was determined between the title compounds and calf thymus DNA. It indicated that these compounds possibly inhibit dihydrofolate reductase (DHFR) or other enzymes on which folic acid depends.

Adenocarcinoma ; pathology ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; drug effects ; Humans ; KB Cells ; drug effects ; Lung Neoplasms ; pathology ; Molecular Structure ; Pteridines ; chemical synthesis ; chemistry ; pharmacology

OBJECTIVETo prepare cryptotanshinone (CT)-cyclodextrin inclusion compound and improve dissolution of CT.

METHODInclusion ratio was determined by plotting the phase solubility curve of CT versus hydroxypropyl-beta-cyclodextrin (HPCD). CT-cyclodextrin inclusion compound was made by wet grinding method. Properties of the inclusion compound was investigated by in vitro dissolution test, DTA and IR spectrum.

RESULTInclusion ratio of CT versus HPCD was 1:1. Dissolution of CT-HPCD inclusion compound at 45 min was 21.6 times of material drug.

CONCLUSIONDissolution of CT was improved remarkably in CT-HPCD inclusion compound. The complexation force of the inclusion compound was hydrogen bond formed by carbonyl group of CT and hydroxyl group of HPCD.

2-Hydroxypropyl-beta-cyclodextrin ; Biological Availability ; Drug Carriers ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; isolation & purification ; Salvia miltiorrhiza ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods ; Time Factors ; beta-Cyclodextrins ; chemistry

AIMTo determine the effects of azide methyl anthraquinone derivative (AMAD) on growth inhibition and inducing apoptosis of multidrug resistant (MDR) KBv200 cells and parental drug-sensitive KB cells.

METHODSCytotoxicity was determined by tetrazolium (MTF) assay. Reactive oxygen species (ROS) levels and mitochondrial membrane potential (deltapsi(m)) in cells were labeled with DCFH-DA and DiOC6 and tested by flow cytometry. Annexin V stain and DNA ladder were used to examine the apoptosis of KB and KBv200 cells induced by AMAD.

RESULTSAMAD was shown to inhibit the growth of KB and KBv200 cells significantly in a concentration-dependent manner, with mean IC50 of 0.36 and 0.45 micromol x L(-1), respectively. The generation of ROS increased obviously after the cells were treated with AMAD for 12 h, up to the peak in 24 h, meanwhile the levels of deltapsi(m) were time-dependently decreased. DNA fragmentation appeared on the agarose gel. Annexin V stain showed AMAD induced apoptosis of KB and KBv200 cells also in a concentration-dependent manner.

CONCLUSIONAMAD showed inhibitory effect on both MDR KBv200 cells and parental drug-sensitive KB cells. The mechanism of action was associated with the increase of the cellular ROS level and the decrease of the mitochondrial membrane potential induced by AMAD, which result in cell apoptosis.

Anthraquinones ; administration & dosage ; chemistry ; pharmacology ; Antineoplastic Agents ; administration & dosage ; chemistry ; pharmacology ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Dose-Response Relationship, Drug ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Humans ; KB Cells ; Mitochondria ; physiology ; Molecular Structure ; Mouth Floor ; Mouth Neoplasms ; pathology ; Reactive Oxygen Species ; metabolism ; Vincristine ; pharmacology

OBJECTIVETo evaluate medium-long term patency of below-knee bypass on patients who suffered from diabetic lower limb ischemia.

METHODSClinical and follow-up data of 51 patients was retrospectively analyzed who underwent 56 below-knee bypass because of diabetes from November 2001 to December 2006. There were 35 male and 16 female with an average age of 68 years. They endured 26 months ischemic time lag in average, and had suffered from diabetes for 11 years. All of the patients were performed bypass to below-knee (posterior tibial, anterior tibial or peroneal) arteries. Kaplan-meier method was applied. The subgroups of different operative methods and different out-flow vessels were compared by Log-rank tests.

RESULTSAn average follow-up time of 23 months was achieved, and lost-follow-up rate was 15%. The total 1- and 5-year primary patent rates were 68% and 54% respectively, secondary patent rate were 70% and 60% respectively, limb salvage rates were 69% and 65%, survival rates were 82% and 60%. One year (3 years) of patent rate(s) of operative method subgroups of femoral-popliteal-infrageniculate bypass with composite grafts, femoral/popliteal-infrageniculate bypass with artificial grafts and femoral/popliteal-infrageniculate bypass with autologous veins were 70% (50%), 33% (33%) and 70% (70%) respectively. One year (4 years) of patent rate(s) of out-flow vessel subgroups of posterior tibial artery, anterior tibial artery and peroneal artery were 65% (60%), 80% (53%) and 77% (66%) respectively. However, both subgroups did not show any statistic differences by log-rank tests.

CONCLUSIONSPartial or whole autologous veins as bypass grafts should be chosen when infrageniculate bypass is considered in diabetic patients. Considerable patent rates are acceptable no matter what kinds of out-flow vessels are chosen.

Aged ; Diabetic Angiopathies ; surgery ; Female ; Femoral Artery ; surgery ; Follow-Up Studies ; Humans ; Ischemia ; etiology ; surgery ; Lower Extremity ; blood supply ; Male ; Middle Aged ; Popliteal Artery ; surgery ; Retrospective Studies ; Saphenous Vein ; transplantation ; Tibial Arteries ; surgery ; Vascular Surgical Procedures ; methods

BACKGROUND: Inferior vena cava filter is an effective way to prevent fatal pulmonary embolism. The existing filters have some shortcomings that limit the clinical application. OBJECTIVE:To evaluate the feasibility and capture efficiency of a new self-convertible inferior vena cava filter(SCF)in vitro. METHODS: The biodegradable switch was constructed of a copolymer of ε-caprolactone and L-lactide (75%/25%, PCLA75). The biodegradable switch bound together with the apices of the convertible struts to make the self-convertible filter. The deformability and capture efficiency of the filter were tested in an in-vitro flow model with three different diameters (22, 25, 28 mm). A total of 15 filters were implanted both in the vertical and horizontal positions, and the tilt angle of the filter was tested after release. To accelerate switch degradation, a lipase perfusate was injected into the flow model and refreshed every 8 hours until conversion. RESULTS AND CONCLUSION: (1) All the filters were successfully implanted without tilting, both in the vertical and horizontal positions in the three different diameter models. (2) All the 15 SCFs were converted successfully without tilting, structural damage, and displacement. (3) The capture efficiency of the SCF had significant difference between the different diameter of the models, the size of the embolus and the position of the two models (P < 0.001). The mean capture efficiency was 82.5%, and the capture efficiency exhibited a downward trend with the increase of pipe diameter, the decrease of emboli size, and the position of pipeline changing from vertical to horizontal. All these results show that the SCF is feasible and highly efficient.

BACKGROUND:An inferior vena cava filter is an effective tool to prevent fatal pulmonary embolism. The existing filters have some shortcomings that limit their clinical application. OBJECTIVE:To evaluate the feasibility and capture efficiency of a new self-convertible inferior vena cava filter (SCF)in vivo. METHODS:L-lactide and ε-caprolactone were fused and polymerized to act as a degradable deformable switch of the filter. Medical stainless steel wire as the metal structure of the filter was combined with the degradable deformable switch to make the SCF. Eight SCFs were implanted into the inferior vena cava of eight adult Beagle dogs. The inferior vena cava angiography was performed to evaluate the release process, morphology and location of the filter. Venous angiography was performed 2 weeks later to evaluate the morphology and location of the filter and inferior vena cava patency. Detection of pulmonary embolism or other complications was performed at autopsy. RESULTS AND CONCLUSION:Eight SCFs were successfully implanted and positioned accurately with no tilt, and they were converted successfully at 2 weeks after the implantation, as assessed by the venous angiography. One of the eight SCFs migrated to the orifice of the right atrium, and caused asymptomatic inferior vena cava obstruction. The remaining SCFs were normally positioned with no tilt and local lesion or obstruction after deformation. No marked filling defect in the trunk of the pulmonary artery was shown by the pulmonary artery angiography. The autopsy report revealed that the filter arm had been endothelialized, and the inferior vena cava that was in contact with the filter arm had no obvious stenosis. Mild intimal hyperplasia, less than 1 mm in thickness, was found in the bottom of the filter arm, but it did not cause a stenosis in the lumen. No vena cava perforation, retroperitoneal hemorrhage, and injury of the surrounding viscera were found. Overall, the design of the SCF is feasible.

OBJECTIVETo explore the management of cerebral ischemia caused by Takayasu's arteritis.

METHODSOne hundred and three cases treated from 1984 to 2003 were reviewed including 92 females. Seven cases underwent ascending aorta to bilateral internal carotid artery (ICA) bypass, 38 cases to the axillary artery with graft to single ICA bypass. Six cases underwent ascending aorta to axillary bypass with 3 graft to single ICA bypasses as the second stage surgery. Three cases underwent ascending aorta to right ICA bypass with 2 graft to left ICA bypasses as well as 6 subclavian to carotid bypass, PTA in 5 and stenting in 3 cases, etc.

RESULTSTwenty-seven patients with less clinical severity received conservative therapy, 9 of them had mostly temporarily improvement, 15 had slight improvement or basically no change, 1 had hemiplegia and 2 died of stroke and myocardial infarction respectively. Surgically, the short-term effective rate was 87% and operative death 7.8%. Fifty-five patients were followed up, a mean follow-up time was 48 months, and the follow-up rate was 80.9%. The excellently, good, fair, no change and death rate were 36.4%, 38.2%, 20.0%, 3.6% and 1.8% respectively. All patients with PTA or stent had an immediate good response and all recurred within 3 to 5 months.

CONCLUSIONSFor treating severe cerebral ischemia caused by Takayasu's arteritis, the ascending aorta to axillary and single ICA reconstruction or the ascending aorta-bilateral axillary bypass for patients with subclavian steal syndrome is advocated; second stage operation from graft to contralateral ICA can be carried out if necessary.

Adolescent ; Adult ; Angioplasty, Balloon ; Brain Ischemia ; etiology ; therapy ; Carotid Artery, Internal ; surgery ; Cerebral Revascularization ; methods ; Child ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Stents ; Takayasu Arteritis ; complications ; Treatment Outcome ; Vascular Surgical Procedures

OBJECTIVETo investigate the management of complicated, severe or recurrent Budd-Chiari syndrome.

METHODSFrom February 2004 to August 2007, 28 patients with complicated, severe or recurrent Budd-Chiari syndrome were treated. In this series, 16 patients relapsed after treated with percutaneous transluminal angioplasty or stent deployment, 2 cases relapsed after surgery; and the other 10 were under severe conditions and hard to treat, including malignancy of the inferior vena cava and right atrium. Meso-cavo-atrial shunt was carried out in 10 cases, meso-cavo-jugular shunt in 6 (capitis medusa was used in one case), cavoatrial shunt in 2 and cavo-jugular shunt in 1, mesocaval shunt in 2, and radical or extended radical correction in 7.

RESULTSOne patient (3.6%) died in 24 hours after operation. Graft infection occurred in 1 case. Excellent, good, fair, poor and death rate were 22.2%, 55.5%, 14.8%, 3.7% and 3.7%, respectively, the overall effective rate was 92.5%.

CONCLUSIONTo select personalized treatment according to the disease status brings hopes to difficult, severe, recurrent Budd-Chiari syndrome.

Adolescent ; Adult ; Blood Vessel Prosthesis Implantation ; Budd-Chiari Syndrome ; surgery ; Child ; Child, Preschool ; Critical Illness ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Portacaval Shunt, Surgical ; Recurrence ; Retrospective Studies ; Treatment Outcome

BACKGROUNDTotally laparoscopic aortic surgery is still in its infancy in China. One of the factors preventing adoption of this technique is its steep learning curve. The objective of this study was to evaluate the feasibility and safety of laparoscopic surgery for aortoiliac occlusive disease (AIOD).

METHODSFrom November 2008 to November 2012, 12 patients were treated for severe AIOD with a totally laparoscopic bypass surgery at our university hospital. The demographic data, operative data, postoperative recovery data, morbidity and mortality were analyzed and compared with those of conventional open approach.

RESULTSTwelve totally laparoscopic aortic surgery procedures, including two iliofemoral bypasses (IFB), three unilateral aortofemoral bypasses (UAFB), and seven aortobifemoral bypasses (ABFB), were performed. Conversion to open procedures was required in three patients. The mean operation time was 518 (range, 325-840) minutes, mean blood loss was 962 (range, 400-2500) ml, and mean aortic anastomosis time was 75 (range, 40-150) minutes. Compared with conventional open approach for aortofemoral bypasses performed concomitantly during this period, laparoscopic patients required fewer narcotics and a shorter in-hospital stay and earlier recovery. Postoperative complications developed in four patients, including a single patient with transient left hydronephrosis, ischemic colonic fistula and pneumonia, residual aortic stenosis proximal to the anastomotic site, and asymptomatic partial left renal infarction. All patients recovered and were discharged on postoperative Days 7-14 except one patient that died of respiratory failure on Day 46. All grafts were patent with follow-up imaging performed by Duplex examination, with a mean follow-up time of 10.7 (range, 2-61) months.

CONCLUSIONTotally laparoscopic bypass surgery is a feasible and safe procedure for AIOD, but attention needs to be paid to improve laparoscopic skills of vascular surgery in order to minimize morbidity during the learning curve of this advanced procedure.

Adult ; Aged ; Aortic Diseases ; surgery ; Arterial Occlusive Diseases ; surgery ; Female ; Humans ; Iliac Artery ; surgery ; Laparoscopy ; adverse effects ; methods ; Male ; Middle Aged ; Postoperative Complications ; etiology

A 68-year-old female patient was treated for unhealed ulcer in the fourth toe of the left foot. Clinical examinations identified severe stenosis of the proximal segment and occlusion of the distal segment of the left anterior tibial artery, and occlusion of the left posterior tibial artery and the peroneal artery. The proximal stenotic segment of the left anterior tibial artery was dilated, but the distal occlusive part failed to be re-canalized. Left anterior tibial artery to dorsal pedal artery bypass was performed on the patient with an epoxide-crosslinked, special radicals antigen-sealed, porcine-derived biological graft; debridement of the left 4th digiti pedis was also performed. Postoperation course was uneventful. The pulse of the left dorsal pedal artery was strong. The ankle brachial index (ABI) increased from 0.60 to 1.09. Warfarin and two antiplatelet drugs were given after the operation. Six months after operation, computed tomographic angiogram (CTA)identified the patent graft.