Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
Antineoplastic Agents ; chemical synthesis ; chemistry ; Artemisinins ; chemical synthesis ; chemistry ; Breast Neoplasms ; pathology ; Cell Proliferation ; Doxorubicin ; Drug Design ; HL-60 Cells ; drug effects ; Humans ; MCF-7 Cells ; drug effects

OBJECTIVETo assess the efficacy and safety of percutaneous cryoablation (PCC) and (125)I seed implantation combined with chemotherapy for advanced pancreatic cancer.

METHODSSixty-seven patients with advanced pancreatic cancer (6 in stage III, 61 in stage IV) received PCC and (125)I seed implantation combined with concomitant gemcitabine hydrochloride and DDP chemotherapy. The clinical benefit response (CBR), survival rate and therapy-related complications were assessed.

RESULTSAll patients except one were followed up over 1 year. The 6-month and 1-year survival rates were 84.8% and 33.4%, respectively. The median progression free survival were 6.3 months and 5.5 months in the group stage III and group stage IV (P > 0.05), respectively, while the overall survival was 9.1 months in the group stage III and 11.0 months in the group stage IV (P > 0.05). CR,PR and SD were achieved in 5, 8, 54 patients, respectively. Fifty-four and 50 in the 67 patients experienced a ≥ 50% reduction of pain score and analgesic consumption, respectively, 18 patients experienced a ≥ 2 kg weight gaining, and KPS was increasing from 71.2 ± 0.4 to (90.0 ± 0.3, P < 0.05), the overall benefit rate was 80.6%. No serious therapy-related complications except pancreatic fistula accompanied abdominal hemorrhage, bile leakage, acute pancreatitis and needle track seeding in 1, 1, 2 and 1 case, respectively.

CONCLUSIONPercutaneous cryoablation and (125)I seed implantation combined with chemotherapy are effective and safe for the treatment of advanced pancreatic cancer.

Adult ; Aged ; Aged, 80 and over ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Brachytherapy ; methods ; Cisplatin ; administration & dosage ; Combined Modality Therapy ; Cryosurgery ; methods ; Deoxycytidine ; administration & dosage ; analogs & derivatives ; Disease-Free Survival ; Female ; Follow-Up Studies ; Humans ; Iodine Radioisotopes ; therapeutic use ; Liver Neoplasms ; secondary ; Male ; Middle Aged ; Neoplasm Staging ; Pancreatic Neoplasms ; pathology ; surgery ; therapy ; Survival Rate ; Young Adult

Objective To investigate the relationship between expressions of mammalian target of rapamycin (mTOR) and vascular endothelial growth factor (VEGF) and pathological grading of meningiomas. Methods Seventy-six specimens of meningiomas, performed resection in our hospital from January 1995 to August 2010, were chosen, in which, 40 were of WHO grade Ⅰ, 24 of WHO grade Ⅱ, and 12 of WHO grade Ⅲ. The expressions of mTOR and VEGF were immunohistochemically studied with SABC method. Results The protein expressions of mTOR and VEGF mainly located in cytoplasm of meningioma cells, and these proteins were granular materials colored from pale yellow to dark yellow. The expressions of mTOR and VEGF were significantly different among meningiomas of grade Ⅰ,Ⅱ and Ⅲ (P<0.05);the expressions of mTOR and VEGF had a positive correlation (r=0.440, P=0.000). Conclusion The expressions of mTOR and VEGF are positively correlated with the tumor grades.

OBJECTIVETo evaluate the effectiveness of free graft transplantation two-stage urethroplasty for hypospadias repair.

METHODSFifty-eight cases with different types of hypospadias including 10 subcoronal, 36 penile shaft, 9 scrotal, and 3 perineal were treated with free full-thickness skin graft or (and) buccal mucosal graft transplantation two-stage urethroplasty. Of 58 cases, 45 were new cases, 13 had history of previous failed surgeries. Operative procedure included two stages: the first stage is to correct penile curvature (chordee), prepare transplanting bed, harvest and prepare full-thickness skin graft, buccal mucosal graft, and perform graft transplantation. The second stage is to complete urethroplasty and glanuloplasty.

RESULTSAfter the first stage operation, 56 of 58 cases (96.6%) were successful with grafts healing well, another 2 foreskin grafts got gangrened. After the second stage operation on 56 cases, 5 cases failed with newly formed urethras opened due to infection, 8 cases had fistulas, 43 (76.8%) cases healed well.

CONCLUSIONSFree graft transplantation two-stage urethroplasty for hypospadias repair is a kind of effective treatment with broad indication, comparatively high success rate, less complications and good cosmatic results, indicative of various types of hypospadias repair.

Adolescent ; Adult ; Child ; Child, Preschool ; Humans ; Hypospadias ; surgery ; Male ; Mouth Mucosa ; transplantation ; Penis ; abnormalities ; surgery ; Retrospective Studies ; Scrotum ; abnormalities ; surgery ; Skin Transplantation ; Treatment Outcome ; Urethra ; surgery ; Urologic Surgical Procedures, Male ; methods

OBJECTIVETo evaluate the relationship between A46G and C79G polymorphisms in the β2-adrenergic receptor (ADRB2) gene and the incidence of essential hypertension (EH) among the Han Chinese population.

METHODSWe conducted a computer retrieval of PUBMED, EMBASE, CNKI, Wanfang and VIP databases prior to May 2010. Articles investigating the relationship of EH and ADRB2 gene polymorphism of Han group were found through literature search, including 15 articles on A46G and 10 articles on C79G. According to the including and excluding criteria, a Meta-analysis was conducted in EH and ADRB2 gene polymorphism of A46G and C79G. The association was examined by RevMan4.2 software through quantitative analysis.

RESULTSEight articles on A46G polymorphism (including 1078 EH cases and 788 control subjects) and six articles on C79G polymorphism (including 1367 EH cases and 1006 control subjects) were included in the current study. Meta-analysis showed that there was a significant association between A46G polymorphism and EH: genotype GG/(AA + AG) (fixed-effected model, OR = 1.35, 95%CI = 1.04 - 1.74, P = 0.02), genotype GG/AA (fixed-effected model, OR = 1.41, 95%CI = 1.06 - 1.89, P = 0.02). No significant association was found between C79G polymorphism and EH of Han group in China: G/C allele comparison (random-effected model, OR = 0.88, 95%CI = 0.55 - 1.39, P = 0.57).

CONCLUSIONSignificant association was found between A46G polymorphism of ADRB2 gene and EH, whereas no association could be found between C79G polymorphism and EH among Han Chinese population.

Alleles ; Asian Continental Ancestry Group ; genetics ; China ; epidemiology ; Gene Frequency ; Genotype ; Humans ; Hypertension ; epidemiology ; genetics ; Polymorphism, Single Nucleotide ; Receptors, Adrenergic, beta-2 ; genetics ; Risk Factors

BACKGROUNDSentinel lymph node (SLN) biopsy has become a common procedure for early breast cancer patients. The GeneSearch(TM) Breast Lymph Node (BLN) Assay is a real-time RT-PCR assay for the detecting nodal metastases larger than 0.2 mm. China Breast Cancer Clinical Study Group (CBCSG)-001a is a prospective multi-center clinical trial that was conducted to validate the GeneSearch(TM) BLN Assay in China.

METHODSThe SLNs from 90 consecutive patients were identified and dissected, and then sectioned along the short axis into multiple blocks. Intra-operatively, the odd blocks were tested by BLN assay and the even ones were used for frozen section, while all the blocks were evaluated by touch imprint cytology. Post-operatively, the remaining tissues were assessed by histological evaluation.

RESULTSA total of 189 SLNs was tested by BLN assay. The sensitivity, specificity, positive predictive value, and negative predictive value were 88.9%, 97.4%, 88.9% and 97.4%, respectively, for BLN assay, 75.0%, 100%, 100% and 94.4%, respectively, for frozen section, and 63.9%, 100%, 100% and 92.2%, respectively, for touch imprint cytology. The sensitivity of BLN assay was higher than that of touch imprint cytology (P = 0.01) and frozen section (P = 0.13). When assessing the nodes with micro-metastases, BLN assay had a significant higher sensitivity than frozen section (P = 0.023) and touch imprint cytology (P = 0.005).

CONCLUSIONThe GeneSearch(TM) BLN Assay is an accurate and rapid intra-operative assay for breast SLNs and it is suitable for application in general medical practice.

Adult ; Aged ; Breast Neoplasms ; complications ; Female ; Humans ; Lymph Nodes ; pathology ; Lymphatic Metastasis ; diagnosis ; Middle Aged ; Sentinel Lymph Node Biopsy ; methods

OBJECTIVEAdhesive or too highly located folds upper eyelid and even blepharoptosis are common complications of double eyelid operation. To correct such deformities.

METHODWe shifted down the double eyelid line, removed adhesion thoroughly, relieved orbital fat and restarted the volume with infraorbicularis oculi fat flap.

RESULTWe had treated 32 case in past two years. The results were satisfying.

CONCLUSIONThe method are acted easy and gained fine result, so behaving to extend application.

Adipose Tissue ; transplantation ; Adult ; Blepharoplasty ; methods ; Eye Abnormalities ; etiology ; surgery ; Eyelids ; abnormalities ; pathology ; Female ; Humans ; Oculomotor Muscles ; surgery ; Postoperative Complications ; surgery ; Tissue Adhesions ; Young Adult

OBJECTIVESTo study the effect of antisperm antibody(AsAb) on human sperm acrosin activity.

METHODSAsAb and sperm acrosin activity were measured and analyzed in 3,432 infertile men and 65 fertile volunteers.

RESULTSAsAb positive rate was 10.20% in 3,432 case of male infertility, and 9.37% in 2,882 infertile males who received tests of sperm acrosin activity. Acrosin activity of infertility cases were lower than those of fertile cases(P < 0.001). The comparison between AsAb positive group and AsAb negative group infertility cases showed no significant differences of acrosin activity (P > 0.05). Between normal acrosin activity group and abnormal acrosin activity group, there was no significant difference of AsAb positive rate (P > 0.05).

CONCLUSIONSAntisperm antibody could not affect acrosin activity.

Acrosin ; metabolism ; Adult ; Autoantibodies ; analysis ; Case-Control Studies ; Humans ; Infertility, Male ; immunology ; Male ; Semen ; chemistry ; Spermatozoa ; enzymology ; immunology

BACKGROUNDCoronary endothelial shear stress (ESS) triggered the development of atherosclerosis. However, the effect of calcium channel antagonist on the distribution of ESS remained unclear.

METHODSTwenty consecutive patients with acute coronary syndrome (ACS) 48 hours after maximal medication with single left anterior descending artery stenosis < 50% were studied. Nicardipine was intravenously injected at 1 µg/kg after a bolus of 10 mg in order to achieve mean blood pressure (MBP) reduced by 10% or more, or the heart rate increased by 10 - 15 beats/min. Hemodynamic variables and angiogram at baseline and during injection of nicardipine were recorded, respectively. Coronary artery 3-D reconstruction was used for the analysis of ESS.

RESULTSDistal reference-vessel-diameter and minimal lumen diameter decreased significantly from (2.42 ± 0.41) mm and (1.47 ± 0.49) mm at baseline to (2.22 ± 0.35) mm and (1.35 ± 0.49) mm at maximal drug-dosage (P = 0.018 and 0.020, respectively). Nicardipine did not change blood velocity. Lowest mean shear stress at segments 2-mm distal to plaque increased significantly from (0.034 ± 0.519) Pa at baseline to (0.603 ± 0.728) Pa (P = 0.013) at peak effect of drug.

CONCLUSIONSNicardipine was associated with the constriction of diseased vessel segment that adapted to the reduction of blood pressure, without dynamic change of blood velocity at each stage of whole cardiac cycle. Increased ESS value at segments distal to plaque reflected the cardioprotection by nicardipine (ChiCTR-TRC-10000964).

Acute Coronary Syndrome ; Aged ; Angina, Unstable ; diagnostic imaging ; drug therapy ; Blood Pressure ; drug effects ; Coronary Angiography ; Coronary Vessels ; drug effects ; Female ; Heart Rate ; drug effects ; Hemodynamics ; drug effects ; Humans ; Male ; Middle Aged ; Nicardipine ; therapeutic use

OBJECTIVETo evaluate the aesthetic outcome after application of rectangle periosteous flap to cover corrugator.

METHODSOn the basis of regular rhytidectomy, a inter-eyebrow periosteous flap is applied to cover the fascia flap of corrugator by means of turnover. This manipulation helps to separate the skin from the muscle and prevent the re-adherence between the skin and muscle.

RESULTSThe approach was applied on 15 cases. The follow-up ranged from 6 months to 1 year. The results were satisfactory.

CONCLUSIONSThe method is effective in elimination of inter-eyebrow crease.

Adult ; Female ; Humans ; Middle Aged ; Muscle, Skeletal ; transplantation ; Periosteum ; transplantation ; Reconstructive Surgical Procedures ; methods ; Rhytidoplasty ; methods ; Skull ; Surgical Flaps ; Treatment Outcome