Objective To obtain two types of optical isomers from 1-(Benzamidomethyl)-1,2,3,4-tetrahydro-isoquinoline (BTIQ). Methods ( ±) BTIQ as raw materials , optically pure camphor sulfonic acid as resolution agent was used and repeated resolution in acetone , And the resolution product was detected by specific optical rotation .The product of BTIQ was hydrolyzed , and the ratio of ATIQ was compared with that of the literature .ResuIts After two repeated chemical resolutions , the specific rotations of both enantiomers are no longer changed .It was showed that the products of higher optical purity.The specific rotation of both isomers are -35.65°(CH2Cl2, C=0.5)with the yield of 27.52%,and +35.17°(CH2Cl2, C =0.5) with the yield of 31.55% respectively.The specific rotation value of chiral 1,2,3,4-tetrahydroisoquino line ( ATIQ) which was the hydrolysis product of BTIQ consistent with values reported in the literature .ConcIusion The (-) BTIQ and ( +) BTIQ enantiomers were successfully obtained by the method of resolution , and the yield and optical purity of the obtained products are higher , laying the foundation for the further development of high efficiency , low toxicity of chiral schistosomicide ( praziquantel ) and other containing tetrahydroisoquinoline structure of chiral drugs .

AIM To study whether cyproheptadine(Cyp) affects endocrine functions in reproductive system with gender difference. METHODS Sixty SD rats were randomly distributed into 3 groups according to gender, respectively, and they were administered NS(5 mL*kg-1*d-1), Cyp 2.4, 4.8 mg*kg-1*d-1 accordingly by ig for 14 d or 21 d. The serum levels of luteinizing hormone(LH), follicle stimulating hormone(FSH), testosterone(T), progesterone(P), estrodiol(E2) were measured by radio-immunoassay and the ultrastructure of gonadotropin-releasing hormone(GnRH) cells, gonadotropin cells, Leydig cells, Sertoli cells, luteal cells, granulocytes and so on were observed by electronmicroscopy and microscopy. The calmodulin(CaM) mRNA expression in hypothalamus-pituitary-testis axis(HPTA) was detected by reverse transcriptase-polymerase chain reaction. RESULTS Cyp(2.4 mg*kg-1*d-1×14 d, ig) increased serum LH concentration while decreased serum FSH, P concentrations in female rats. Cyp(4.8 mg*kg-1*d-1×14 d, ig)increased serum LH, T concentrations in males, and increased serum LH concentration while decreased serum FSH, E2 and P concentrations significantly in females. The retrograde changes of ultrastructure were observed in part of gonadotropin and ovary endocrine cells, while a stimulating one in testis endocrine cells. CaM mRNA expression levels were elevated in testis but not in hypothalamus and pituitary in male rats. CONCLUSIONCyp had a negative effect on endocrine function in females, but a positive one in males. The ultrastructure showed relevant changes in target gland. Cyp promoted CaM mRNA expression in testis,which had close connections with Cyp′s stimulative effect in HPTA.

Objective To observe the clinical efficacy of percutaneous vertebroplasty (PVP) with percutaneous kyphoplasty (PKP) in the treatment of osteoporotic vertebral compression fracture(OVCF) by systematic review. Methods From September 2005 to March 2009,46 cases of fresh OVCF were treated. Patients were divided into 2 groups (A, B), according to Jikei grade, Genant semiquantitative method, injury vertebra number. Twenty-five cases(group A)were treated by PVP,8 males and 17 females with the age of 52 - 78 years (average 69). Vertebra segment of fracture was within T6 - L5 (14 in case thoracical vertebrae and 11 lumbar vertebrae). Twenty-one cases(group B)were treated by PKP,There were 6 males and 15 females with the age of 54 - 82 years (average 71). Vertebra segment of fracture was within T6 - L4 (12 in case thoracical vertebrae and 9 lumbar vertebrae). The clinical efficacy, incidence rate of complication, the anterior height of vertebrae body,visual analogue pain scale(VAS) ,ease of pain were measured preoperatively and at 6 weeks, 3 and 6 months and 1 year postoperatively between the two groups. Results All the patients were followed up for 12 -45 months with an average of 23.5 months. The average recovery of anterior height of vertebrae body was respectively(85.95 ± 4.31) % in group A and (93.64 ± 3.35) % in group B,which statistically difference in vertebral height between two groups (P ＜ 0.05). No statistical significant difference was seen in VAS, analgesic durg (AID) and ease of pain complication between two groups (P ＞0. 05). Statistical significant difference was noted in pre-postoperatively between intra-two groups (P ＜0. 05). Conclusions PVP and PKP can quickly relieve pain and enhance vertebral stability in treating thoracolumbar OVCF according to evaluation parameter, and have the similar therapeutic efficacy in treatment of OVCF with minimal invasion. However, PKP is superior in the recovery of vertebral height.

Objective To discuss the clinical influence and advantages of applying the local flap of finger tip lateral skin to repair the fingertip defective injuries.Methods From August,2013 to December,2015,used the way of local the flap of finger tip lateral skin to repair the first-fourth fingertip defects for 32 cases and 32 fingers,among which there were 20 males and 12 females;finger categories:11 thumbs,9 index fingers,8 middle fingers and 4 ring fingers.The defective area of fingertips was 0.5 cm×0.8 cm-1.0 cm×1.5 cm,all with bone exposure,23 cases had defects at the end part of phalanx,32 cases had different extent of nail bed defects.Reasons for the injuries:13 cases of grind injuries,11 cases of punch pressing injuries,8 cases of sharp tool cutting injuries.The time from injury to the treatment was 0.5-3.0 h,all of them had no associated injuries.Results Thirty-two cases of finger flaps all survived,with the follow-up for 3-24 months and average follow-up of 6 months,the flaps were slightly bloated after 3 months comparing with the normal skin,there was no contracture in the flap area and pedicle scars,two-point discrimination was 4-5mm,the farinterphalangeal joint flexion was normal.Conclusion The local flap of fingertip lateral skin can repair the defects of fingertip with less scar,not bloated flap,satisfying appearance,operation is simple,and good function,so it's the ideal way to repair the defects of fingertip.

Objective To evaluate the relationship between ultrasound-assayed detrusor thickness and bladder outlet obstruction (BOO) in old men with benign prostatic hyperplasia (BPH).Methods The 106 BPH patients underwent the urodynamic examination on which the diagnosis of BOO was dependent. The obstruction was defined as the Abrams-Griffiths nomogram (A-G index)≥40 and the grade of linear passive urethral resistance relation (LinPURR)≥Ⅱ . When bladder capacity reached 150 ml, the detrusor thickness was measured by abdominal ultrasound. Results Compared with unobstructed group, the maximum flow rate and average flow rate were both lower in obstructed group [(10.1±3.0) ml/s vs. (17.4±3.1) ml/s, (5.5±2.2) ml/s vs. (11.2±2.2) ml/s, t= 10.26and 11.03, both P＜0.01]. And the residual urine volume and maximum detrusor pressure were significantly higher in obstructed group than in unobstructed group [(47.6 ± 24.3) ml vs. (17.0 ±5.6) ml, (39.3±14.4) cm H2Ovs. (26.8±8.0) cm H2O, t=6.32 and 4.07, P＜0.01 or 0.05].Detrusor thickness was positively correlated with maximum detrusor pressure (r= 0.419, P＜0.01),but negatively correlated with maximum flow rate (r =- 0.749, P＜ 0.01 ), mean flow rate (r=-0.853, P＜0.01) and voided volume (r=-0.556, P＜0.01). There was significant difference in detrusor thickness between obstructed group and unobstructed group [(3.0± 0.2) mm vs. (2.5 ±0.2) mm, t= 11.2,P＜0.05]. According to the diagnostic standard of detrusor thickness≥3.0 mm,it had a sensitivity of 90% and a specificity of 84.6%, a positive predictive value of 93.1% and a negative predictive value of 78.6%. Conclusions Detrusor thickness of 3.0 mm or greater has a certain predictive value for BOO in old men.

Theacrine is one kind of natural purine alkaloids, which mainly exists in an unusual Chinese tea known as Kucha. It shows various biological activities, such as anti-depression, sedative and hypnotic effects and anti-inflammatory and analgesic activi-ties. The study on theacrine dates back to a few decades ago. According to the references published in recent years, the resource, preparation, characterization and pharmacological effects of theacrine were reviewed, and its application prospect was also explored.

Objective To evaluate the outcome of reoperation(after I stage anterior/posterior operation)for thoracolumbar fractures combined with kyphosis and spinal cord injury. Methods A retrospective study was done on the medical records of 12 patients who underwent two-stage decompression with kyphosis and neurologic deficit due to single-stage approach(anterior or posterior) operation of thoracolumbar fractures combined with spinal cord injury between January 2005 and April 2009.There were 9 males and 3 females,at mean age of 34.6 years(range,19-57 years).According to the Denis classification,there were five patients with burst fractures,five with compression fractures and two with fracture dislocation.All the patients had couns medullaris injury.Of all the patients,five underwent one stage anterior approach surgery and the others underwent posterior approach operation.All the patients had vailous degrees of neurological symptoms.The patients treated with one stage anterior surgery were treated with two stage posterior surgery and the patients treated with one stage posterior surgery were treated with the two stage anterior operation.The mean interval from one stage operation to two stage decompression was 13.4 months(range,12-18 months).The radiologic,neurologic and functional outcomes were assessed through observation of the Cobb angle,Frankel spinal cord injury grading and Japanese Orthopaedic Association Scores(JOA). Results AIl the patients were followed up for mean 25 months (12-48months),which showed primary healing of the incisions in all the patients.The average anterior and posterior heisht of the vertebrae wers corrected from preoperative 42.6%and 70.5%to postoperative 92.5%and 95.7%and to 87.3%and 92.2%at the final follow-up respectively.Neurologic status was improved at least one Frankel grade in the patients who had preoperative incomplete paraplegia.The Cobb angle was corrected from preoperative 36.3°to postoperative 5.8°and to 5.9°at the final follow-up(P<0.05).No patient had any notable loss of correction between discharge and final follow-up.According to JOA coring,the results were excellent in nine patients,good in two and fair in one,with excellence rate of 92%. Conclusions Two stage decompression for epiconus and cauda equina syndrome resulted from one stage approach(anterior or posterior)operation of thoracolumbar fractures combined with spinal cord injury call attain satisfactory correction of the kyphosis and nerve decompression as well as various degrees of nerve function recovery.

Objective To explore the efficacy and safety of double dosage of SHUGANJIEYU capsule on mod?erate depression. Methods The study was conducted by a multicenter, random, double-blind and parallel-controlled trial. Trial group received SHUGANJIEYU capsules 4# twice a day. Control group got two SHUGANJIEYU capsules and two simulated ones twice a day. The study lasted 56 days (8 weeks) for both groups. Primary efficacies were evalu? ated by the total score and score changed rate of Hamilton depression scale-17 (HAMD-17)and Hamilton anxiety scale (HAMA) as well safety by reported adverse events and laboratory tests for patients. Results One hundred twenty patients were recruited in trial group and 120 patients in control group. After a 8-week treatment, the remission ratio was 84.2% and 63.3% for the trial group and the control group, respectively according to the HAMD-17. The differ?ence in the remission ratio was significant (P<0.05). Furthermore, the reduction rate of the total scores of HAMD-17 was 35.4% and 27.1% for the trial group and the control group at the 14th day of treatment, respectively, whereas 79.0%and 65.9%for the trial group and the control group at the 56th day. The reduction ratio was significantly higher in trial group than control group (P<0.01). The median time to response was 14 days in both groups. Based on the HA?MA, the remission ratio was 93.3%and 77.5%for the trial group and the control group respectively after 8 weeks and the difference in the remission ratio was significant between the two groups (P<0.05). Incidences of adverse effect were not significantly different between the two groups (17.5%vs. 11.7%, P>0.05). Conclusion SHUGANJIEYU capsule ex?hibits a good therapeutic effect on the depressive symptoms and anxiety symptoms in patients with moderate depres?sion. Double doses of SHUGANJIEYU capsule can increase the effect of SHUGANJIEYU and accelerates SHUGAN?JIEYU-induced improvement of depression symptoms with an acceptable safety.

Objective To explore the regulatory effects of HTLV-1 ( human T-cell leukemia virus type 1 ) Tax protein on the expression of HMGB 1 ( high mobility group box 1 ) gene in T cells .Methods Total RNA and protein were extracted from Tax +-T cells ( TaxP ) , Tax--T cells ( TaxN ) and Jurkat cells which were stably transfected with pCMV-Tax and pCMV-Neo, respectively.Then, the expression levels of HMGB1 mRNA and protein in different CD 4+T cells were analyzed by real-time PCR and Western blot (WB).By using liposome-mediated method, pGL3-HMGB1-luc reporter genes and pGL3-neo-luc were tran-siently transfected into TaxP and TaxN cells and the basal transcriptional activity was observed in different T cells.Additionally, pCMV-Tax and pGL3-HMGB1-luc reporter genes were also co-transfected into Jurkat cells and the regulatory effects of Tax protein on HMGB 1 gene was detected .The chromatin immunoprecipi-tation (ChIP) assay was used to identify HMGB1 genomic sites directly targeted by Tax .Results The ex-pression levels of HMGB1 mRNA and protein in Tax+-T cells ( TaxP) were higher than those in Tax--T cells (TaxN).The transcription regulation trends for HMGB1 gene in TaxN and TaxP cells were similar but not identical in diverse T cells.pHLuc3 (containing -504-+83 HMGB1) showed the highest transcriptional ac-tivity of HMGB1 gene in both TaxP and TaxN cells , but HMGB1 transcriptional activity of pHLuc 6 in TaxP cells was significantly stronger than that in TaxN cells .Luciferase assays also showed that Tax protein promo-ted the transcription of HMGB1 gene in a dose-dependent manner .The ChIP assay further confirmed that Tax protein enriched at the HMGB1 region of -1163--1043.Conclusion The region of nt -504--383 is essen-tial for the basal promoter activity of -1163-+83 HMGB1 gene originated from pHLuc 6 reporter plasmid , and Tax protein enriched probably at the HMGB 1 site of -1163--1043 enhances HMGB1 transcription.

Oleanolic acid (OA) has a wide variety of bioactivities such as hepatoprotective, anti-inflammatory and anti-cancer activity and is used for medicinal purposes in many Asian countries. In the present study, the effect of OA on induction of autophagy in human hepatocellular carcinoma HepG2 and SMC7721 cells and the related mechanisms were investigated. MTT assay showed that OA significantly inhibited HepG2 and SMC7721 cells growth. OA treatment enhanced formation of autophagic vacuoles as revealed by monodansylcadaverine (MDC) staining. At the same time, increasing punctuate distribution of microtubule-associated protein 1 light chain 3 (LC3) and an increasing ratio of LC3-II to LC3-I were also triggered by OA incubation. In addition, OA-induced cell death was signifi cantly inhibited by autophagy inhibitors 3-methyladenine (3-MA) and chloroquine (CQ) pretreatment. And we found out that OA can suppress the PI3K/Akt1/mTOR signaling pathway. Furthermore, our data suggested that OA-triggered autophagy was ROS-dependent as demonstrated by elevated cellular ROS levels by OA treatment. When ROS was cleared by N-acetylcysteine (NAC), OA-induced LC3-II convertsion and cell death were all reversed. Taken together, our results suggest that OA exerts anticancer eff ect via autophagic cell death in hepatocellular carcinoma.
Acetylcysteine ; Asian Continental Ancestry Group ; Autophagy* ; Carcinoma, Hepatocellular* ; Cell Death ; Chloroquine ; Humans ; Microtubule-Associated Proteins ; Oleanolic Acid* ; Vacuoles