OBJECTIVE:To improve the synthesis technology of sorafenib tosylate (Ⅰ). METHODS:The intermediate N-methyl-(4-chlorpyridin-2-yl)carboxamide(Ⅳ)was obtained by chlorination and amidation with 2-picolinic acid as the starting com-pound. Meanwhile,N-[4-chloro-3-(triflouromethyl)phenyl]-N′-(4-hydroxyphenyl)urea (Ⅶ) was prepared from aminophenol and 4-chloro-3-trifluoromethyl phenyl isocyanate,which was obtained from 4-chloro-3-(trifluoromethyl)aniline(Ⅴ)by reaction with initiator triethylamine. Sorafenib tosylate was synthesized from Ⅳ and Ⅶ with potassium tert-butoxide by condensation and salt for-mation. The target compound was characterized by 1H-NMR. RESULTS:The target compound was confirmed as Ⅰ,with the over-all yield of 74% [based on 4-chloro-3-(trifluoromethylanilin)]. The purification of chromatogram was 94%. Optimized technology improves yield and simplifies multi-step intermediate decompression,distillation and purification process;the application of initia-tor shortens the duration of reaction. CONCLUSIONS:Ⅰ is prepared successfully,and raw material can be obtained easily and is easy to operate with high yield.

Objective To develop the human colon carcinoma(HT-29) liver metastasis model in nude mice,and to detect the expression of human telomerase reverse transcriptases(hTERT) mRNA in liver of nude mice. Methods Liver metastases were established in 30 Balb/c nude mice by intrasplenic injection of colonic cancer cells(HT-29),and the spleens were resected.After being sacrificed,the tumor growth was observed,and the pathological examinations were performed.The expression of hTERT mRNA in the livers of nude mice was detected by RT-PCR technique. ResultsHuman colon carcinoma(HT-29) liver metastasis model was developed in all the 30 nude mice,with the liver metastasis rate of 100%.The pathological results revealed the occurrence of liver metastases,and the expression of hTERT mRNA was positive in the liver tissues. Conclusion Intrasplenic injection of HT-29 cell is a reliable way for producing colonic cancer liver metastasis model,and the positive expression of hTERT mRNA in liver tissues indicates the significance of hTERT in the early diagnosis and treatment of colon carcinoma liver metastasis.

Objective To compare the clinical effects of electroacupuncture at antagonistic motor points and at acupoints on ankle varus post stroke. Methods 96 patients with ankle varus post stroke were randomly divided into treatment group (n=48) and control group (n=48). All the patients accepted Bobath approach. The treatment group accepted electroacupuncture at antagonistic motor points, while the control group at antagonistic acupoints. They were assessed with Holden functional ambulation category, modified Ashworth scale and dorsiflexion- eversion grade of ankle before and after 4 weeks of treatment. Results The ambulation, spasticity of ankle, and dorsiflexion-eversion of ankle improved in both groups after treatment (P<0.05), and improved more in the treatment group than in the control group (P<0.05). Conclusion Electroacupuncture at antagonistic motor points may release spasticity of ankle post stroke more effective than at acpoints

The paper is aimed to identify SNP in Sarcandra glabra and Chloranthus spicatus, and authenticate S. glabra from Ch. spicatus and the mixture by using PCR amplification of specific alleles. SNPs in the ITS sequences of S. glabra and Ch. spicatus were found by ClustulX 2. 1 program and Bioedit software. Primers for authentic S. glabra and Ch. spicatus was designed according to the SNP site, and ITS sequence universal primers plus to the authentic primer to construct a multi-PCR reaction system, and then optimized the PCR reaction system. Five hundred and eighty band special for S. glabra and 470 bp band special for Ch. spicatus were found by using multi-PCR reaction. The multi-PCR reaction system could be applied to identify S. glabra and Ch. spicatus's leaves.
DNA, Plant ; analysis ; genetics ; DNA, Ribosomal ; genetics ; DNA, Ribosomal Spacer ; analysis ; genetics ; Magnoliopsida ; classification ; genetics ; Plant Leaves ; genetics ; Polymerase Chain Reaction ; Polymorphism, Single Nucleotide ; RNA, Ribosomal ; genetics ; RNA, Ribosomal, 18S ; genetics ; RNA, Ribosomal, 5.8S ; genetics ; Species Specificity

The study is aimed to assess the genetic diversity and genetic relationship of 18 Sarcandra glabra resources from different populations,and guide parent selection of cross breeding between these resources. The molecular marker technique ISSR was used to investigate the genetic diversity of the 18 resources. Data was analyzed by POPGEN 32, and a cluster diagram was presented by UPGMA. One hundred and ninety-eight amplified fragments were obtained using 23 ISSR primers. One hundred and eighty-four polymorphic loci were identified. Nei's genetic diversity index (h) was 0.32, Shannon diversity index (I) was 0.485 4. The genetic similarity coefficient among the resources ranged from 0.383 8 to 0.878 8 in an average of 0.661 2. The genetic distance between sample S2 and sample S18 was the farthest, so as between sample S3 and sample S18 both Nei's genetic distance was 0.957 5, The genetic distance between sample S4 and sample S5 was the closest, the Nei's genetic distance was 0.129 2,and the sample S1, S2, S3, S7, S10 were significantly different from the others based on the clustering analysis, the three groups S2 vs S3, S2 vs S6, S2 vs S18 were the best parent group selection. There was a middle level of genetic differentiation in the resources. The genetic distance between resources gives useful information to guide parent selection of cross breeding.
Conservation of Natural Resources ; DNA Primers ; genetics ; Genetic Variation ; Magnoliopsida ; classification ; genetics ; Microsatellite Repeats ; Phylogeny

Objective To evaluate the CT findings and classification of the Le Fort fracture. Methods Sixty-two cases with Le Fort fractures were studied with thin-slice high-resolution CT scanning and analyzed with three-dimensional(3D)imaging reconstruction.Results Of the 62 patients,10 had Le Fort type Ⅰ fracture,9 had Le Fort type Ⅱ fracture,8 had Le Fort type Ⅲ fracture,and 35 had various combinations of the three types of Le Fort fractures,including 18 Le Fort Ⅰ+Ⅱ fracture,7 Le Fort Ⅰ+ Ⅱ+Ⅲ fracture and 10 Le Fort Ⅱ+Ⅲ fracture.Fifty-five cases had associated multiple fractures in the maxillofacial region.On 2D CT images,Le Fort fracture manifested as multiple and complex fractures. Though 2D image was better than 3D image in accurately defining tiny fractures and fractures of deep structures,the diagnosis of Le Fort fracture could not be correctly made solely on 2D image.3D CT clearly and stereoscopically demonstrated the entire shape and orientation of Le Fort fracture,thus facilitating the correct classification of Le Fort fracture.Conclusion 3D CT image is important in providing information about the space relationship of Le Fort fracture,thus very valuable for the preoperative planning.

OBJECTIVETo investigate the effects of Salvia miltiorrhiza (SM) on oxidative stress and microinflammatory state in patients undergoing continuous hemodialysis (CHD).

METHODSThirty-six patients who had received CHD for over half a year were assigned into the routine CHD group (18 cases) and the treated group treated with routine CHD plus SM (18 cases). Meanwhile, 18 healthy adults were taken as the normal control. Indexes related with oxidative stress [malondialdehyde (MDA), advanced oxidative protein products (AOPP) and superoxide dismutase (SOD)) and microinflammation C-reactive protein (CRP), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-alpha) were detected before and after 1, 2 and 3 months of treatment.

RESULTSThe levels of AOPP, MDA, CRP, IL-6 and TNF-alpha in patients were higher and SOD was lower than those in the normal control at all the time points (P < 0.01). Compared with the baseline, the levels of AOPP and MDA in the routine CHD group significantly increased and SOD decreased after 3 months of treatment (P < 0.05), but changes of CRP, IL-6 and TNF-alpha showed no significance though there were somewhat increment (P > 0.05). The levels of AOPP and MDA were lower and SOD was higher after 1, 2 and 3 months of SM combined treatment, and CRP was lower after 3 months of treatment in the treated group than those of baselines and those at the corresponding time points in the routine CHD group (P < 0.01), but IL-6 and TNF-alpha reduced insignificantly (P > 0.05).

CONCLUSIONHemodialysis may aggravate the oxidative stress and microinflammation in patients, which could be obviously alleviated by SM.

Adult ; Aged ; C-Reactive Protein ; metabolism ; Female ; Humans ; Interleukin-6 ; blood ; Kidney Failure, Chronic ; blood ; therapy ; Male ; Malondialdehyde ; blood ; Middle Aged ; Oxidative Stress ; Phytotherapy ; Renal Dialysis ; adverse effects ; Salvia miltiorrhiza ; Superoxide Dismutase ; blood ; Tablets ; Treatment Outcome ; Tumor Necrosis Factor-alpha ; blood

OBJECTIVETo explore the correlation between Chinese medical (CM) syndrome types of chronic atrophic gastritis (CAG) patients and Helicobacter pylori (Hp) infection, polymorphisms of IL-1B, and IL-1β.

METHODSTotally 192 CAG patients and 202 healthy subjects (as the healthy control group) were recruited in this case-control study. The Hp infection was tested by 13C-urea breath test and colloidal gold-labeled assay (GICA). The concentration of peripheral blood IL-1β was measured by ELISA. The polymorphisms of IL-1B gene in the promoter region were analyzed using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP).

RESULTSPi-Wei weakness syndrome (PWWS) was dominant in CAG patients (31.77%, 61/192 cases). The Hp infection ratio in CAG patients was 53.65% (103/192 cases), of which, Pi-Wei damp-heat syndrome(PWDHS, 64.86%, 24/37 cases) and Gan-Wei disharmony syndrome (GWDS, 66.67%, 24/36 cases) were dominant. Compared with the health control group, the plasma concentration of IL-1β was obviously elevated in CAG patients with PWDHS, GWDS, and static blood obstructing collaterals syndrome (SBOCS) (all P < 0.05). Additionally, there was no difference in the distribution of polymorphisms in the promoter region of IL-1 B gene between the CAG patients and the healthy control group (P > 0.05).

CONCLUSIONSThe incidence risk of CAG was not associated with IL-1B polymorphism. But CM syndrome types of CAG patients was associated with Hp infection and peripheral blood IL-1β levels.

Case-Control Studies ; Gastritis ; Gastritis, Atrophic ; genetics ; Helicobacter Infections ; genetics ; metabolism ; Humans ; Incidence ; Interleukin-1beta ; genetics ; Medicine, Chinese Traditional ; Polymorphism, Genetic

OBJECTIVETo investigate the correlation of the deleted azoospermia (DAZ) gene copy related to gr/gr and b2/b3 deletions in the AZFc region with male spermatogenic impairment.

METHODSThis study included 121 infertile men with different de- grees of spermatogenic impairment and 95 healthy donors from the sperm bank. Using PCR, PCR-RFLP, and Y chromosome specific sequence tagged sites (STS) , we analyzed the association of DAZ gene copy deletions related to gr/gr and b2/b3 deletions in the AZFc region with spermatogenic impairment.

RESULTSThere were 15 cases of gr/gr deletion (12. 40% ) and 6 cases of b2/b3 deletion (4.96%) in the infertility group as compared with 13 cases of gr/gr deletion (13.68%) and 1 case of b2/b3 deletion (1.05%) in the control. Analysis of the DAZ-specific single nucleotide variant (SNV) loci revealed 11 gr/gr-DAZI/DAZ2 deletions (9.09%), 4 gr/gr-DAZ3/DAZ4 deletions (3.31%), and 6 b2/b3-DAZ1/DAZ2 deletions (4.96%) in the infertile men in comparison with 3 gr/ gr-DAZ1/DAZ2 deletions (3.16%), 10 gr/gr-DAZ3/DAZ4 deletions (10.53%), and 1 b2/b3- DAZ3/DAZ4 deletion (1.05%) in the control.

CONCLUSIONPartial deletions of gr/gr and b2/b3 exist in both healthy men and male patients with different degrees of spermatogenic impairment and cannot be considered as a risk factor for spermatogenesis impairment. However, deletions of different DAZ duplicons in gr/gr and b2/b3 deletions have different effects on spermatogenesis. DAZ1/DAZ2 instead of DAZ3/DAZ4 deletions might be associated with spermatogenesis impairment.

Deleted in Azoospermia 1 Protein ; Gene Deletion ; Gene Dosage ; Humans ; Male ; RNA-Binding Proteins ; genetics ; Spermatogenesis ; genetics

Objective To investigate the aging-related changes in gap junction protein-connexin 43 (Cx 43) in rats and their effect on the high incidence rate of ventricular arrhythmia in aged rats. Methods The 64 healthy male Fischer 344 (F344) rats were randomly divided into four age groups (n=16,each): 3-6 months (juvenile), 9-12 months (young-adult), 18-21 months (middle-aged) and 24-26 months (aged). The incidence rate of ventricular arrhythmia was recorded by monitoring their limb-lead Electroa rdiogram(ECG). Morphological changes of ventricular myocardium were observed under optical microscope in Hematoxylin (HE) and Masson's stain. The distribution of connexins 43 (Cx43) and deophosphatase (NP) Cx43 was observed by confocal immunofluorescence microscopy and the Cx43 and NP-Cx43 protein expression was assessed by Western-Blot. Results The incidence rate of ventricular arrhythmia was much higher in aged group (75.0%) than in other three groups (0%,0%,12.5%), all P＜0.05, and the aged group showed that ventricular muscle cells were hypertrophy and arrayed sparsely and disorderly with hyperplasia of connective tissues. The distribution of Cx43 changed from end-to-end to disordered arrangement and the total expression amount of Cx43 decreased as age increased (P＜0.05). The expression amount of NP-Cx43 in middle-aged rats was notably decreased than in juvenile and aged rats (P＜0.05). Conclusions For aged rats, the high incidence rate of ventricular arrhythmia may be associated with ventricular myocardium reconstruction, disarrangement of ventricular muscle cells and gap junction proteins, decreased expression amount of Cx43 and relatively increased NP-Cx43.