Spinosyns are secondary metabolites from the aerobic fermentation of saccharopolyspora spinosa Spinosyn is a kind of broad spectrum insecticide, which has contact and ingestion toxicity on insects On lepidopteran insects, spinosad (a mixture of spinosyn A and spinosyn D) is one of the most selective compounds ever discovered In this paper, the structure, biosynthesis, property and process of spinosyns are reviewed

This study is to investigate the anti-tumor activities of a novel cyclophosphamide derivate 4, 6-diphenyl cyclophosphamide (9b) in vivo and in vitro, and its possible mechanism of action. The inhibitory effects of 9b on human hepatoma cell line HepG2, human breast carcinoma cell line MCF-7 and human myeloid leukemia cell line K562 were measured by MTT assay in vitro. Cell cycle distribution and apoptotic rate were evaluated by flow cytometry. To evaluate the anti-tumor effect of 9b in vivo, mouse model bearing inoculated H22 tumor was established. The results indicated that 9b could inhibit the proliferation of HepG2, MCF-7 and K562 cells in a dose and time dependent manner. The ICo50 values of 9b were 32.34 micromol.L-1 to HepG2 cells, 87.07 micromol.L-1 to MCF-7 cells and 149.10 micromol.L-1 to K562 cells after incubation for 48 h. The results of flow cytometry indicated that after being treated for 48 h with different concentrations of 9b, the ratios of HepG2, MCF-7 cells at the Go/G1 phase and K562 cells at the G0/Gl phase and G2/M phase increased significantly compared with control group, and the apoptotic rate increased with the increase of the concentration of 9b. 9b could significantly reduce tumor weight of H22 solid tumor mouse model in vivo. To summarize, 9b showed significantly anti-tumor activity in vivo and in vitro, of which the mechanism might be associated with the change of cell cycle distribution and induction of tumor cell apoptosis.
Animals ; Antineoplastic Agents, Alkylating ; chemistry ; pharmacology ; Apoptosis ; drug effects ; Cell Cycle ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cyclophosphamide ; analogs & derivatives ; chemistry ; pharmacology ; Dose-Response Relationship, Drug ; Female ; Humans ; Inhibitory Concentration 50 ; Liver Neoplasms, Experimental ; pathology ; Male ; Mice ; Molecular Structure ; Random Allocation ; Tumor Burden ; drug effects

To construct a secretory-expression vector of antimicrobial peptide Bactenecin 7(Bac7),and identify the secretory-expression product in L.lactis MG1363 and its bioactivity.The splicing primers of regulation elements and Bac7 gene,which designed according to codon usage preferences of L.lactis MG1363,were chemically synthesized,and the overlap-extension PCR method was used to splice the full length of Bac7 gene.Then the Bac7 gene was linked to expression vector pMG36e to construct pMG36e/Bac7 vector,and pMG36e/Bac7 was transformed into L.lactis MG1363 by electrophoration.RT-PCR and Western blot assays were applied to investigate the expression of the Bac7 gene in L.lactis,and bioactivity of Bac7 in culture supernatant of L.lactis was tested with plate-diffusion method.The results showed that the Bac7 gene and its regulation elements was amplified and cloned in the vector pMG36e successfully,The secretory-expressed Bac7 in L.lactis MG1363 harboring pMG36e/Bac7 was identified by Western blot,and it had high bacteriostatic activity against E.coli.These results indicate that the recombinant L.lactis MG1363 could express bioactive Bac7,which lays a foundation for further study of oral administration of a Bac7-secreting L.lactis to treat intestinal bacteria infection.

OBJECTIVETo observe the clinical efficacy difference between segmentation scraping and conventional acupuncture for cervical spondylosis (CS) so as to provide effective treatment method.

METHODSEighty-five cases of cervical type of CS were randomly divided into a scraping group (44 cases) and an acupuncture group (41 cases). The segmentation scraping therapy was used in the scraping group. The scraping group was treated with focusing on scraping the head and joint part of neck and occiput in the upper cervical spine injury, and focusing on scraping the lower section of cervical and shoulder in the lower cervical spine injury, once every seven days, totally for 3 times. In the acupuncture group, Fengchi (GB 20),Wangu (TE 5), Tianzhu (BL 10),Neck-Jiaji (EX-B 2), etc. were selected,once daily,for 15 days. The visual analogue scale (VAS) was used to evaluate the immediate analgesic effect after the first treatment and the clinical efficacy was observed after the end of treatment.

RESULTSAfter the first treatment, the score of VAS was decreased significantly in the scaping group (P < 0.01), but there was no significant difference in the acupuncture group compared with those before treatment (P > 0.05); the score of VAS in the scaping group after the first treatment was lower than that in the acupuncture group (3.66 +/- 0.74 vs 5.43 +/- 0.35, P < 0.01). Compared with before treatment, the scores of VAS were decreased significantly after treatment in two groups (both P < 0.01), but without significant difference between two groups (P > 0.05); the effective rate was 95.5% (42/44) in the scaping group and 87.8% (36/41) in the acupuncture group, the curative effects were similar (P > 0.05).

CONCLUSIONBoth of scraping and acupuncture therapies have good analgesic effect for cervical spondylosis, and overall effects are similar, but the immediate analgesic effect of scraping thrapy is better than that of conventional acupuncture.

Acupuncture Points ; Acupuncture Therapy ; Female ; Humans ; Male ; Medicine, Chinese Traditional ; Neck Pain ; therapy ; Spondylosis ; therapy ; Treatment Outcome

OBJECTIVETo observe the differences in onset time and the overall efficacy of the acupuncture therapy of dredging Governor Vessel and regulating mentality combined with fluoxetine and the fluoxetine for post-stroke depression(PSD).

METHODSSixty-three patients were randomly divided into an acupuncture intervention of dredging Governor Vessel and regulating mentality group(acupuncture and medication group, 33 cases) and a control group (medication group, 30 cases). In the medication group, 20 mg fluoxetine was used by oral administration, once a day at 7:00 in the morning, continuously for 4 weeks. In the acupuncture and medication group, based on the oral administration of fluoxetine, the acupuncture intervention of dredging Governor Vessel and regulating mentality was applied mainly at Baihui(GV 20), Fengfu(GV 16), Shenting(GV 24), Shuigou(GV 26), Dazhui(GV 14) and Shendao(GV 11), once a day, 6 times a week, continuously for 4 weeks. Twenty-four items in Hamilton Depression Scale(HAMD), modified Edinburgh Scandinavia Stroke Scale(MESSS) and activity of daily life scale(ADL, Barthel index, BI) were used before and after 2-week and 4-week treatment. The efficacy was compared between the two groups.

RESULTSAfter 2-week treatment, the HAMD score and the MESSS score in the acupuncture and medication group were obviously decreased and the BI score was apparently increased(all P<0. 01). In the medication group, however, the score of every scale was not statistically different from that before treatment(P'>0. 05). After 4-week treatment, HAMD scores and MESSS scores in the two groups were obviously decreased and the BI scores I were apparently increased(all P<0. 01). After 2-week and 4-week treatment, the HAMD scores and the MESSS scores in the acupuncture and medication group were lower than those in the medication group and the BI scores were higher than those in the medication group(P<0. 01, P<0. 05). The total effective rate of anti-depression (97. 0%, 32/33) the total effective rate of nerve function impairment(90. 9%, 30/33) and the total effective rate of daily life activity(97. 0% 32/33) in the acupuncture and medication group were better than 80. 0% (24/30), 80. 0%(24/30), 83. 3%(25/30) in the medication group(all P<0. 05).

CONCLUSIONThe acupuncture therapy of dredging Governor Vessel and regulating mentality could reduce the onset time of anti-depression medicine treatment of PSD and enhance the overall efficacy. Therefore, it enhances the clinical compliance.

Acupuncture Therapy ; Adult ; Aged ; Antidepressive Agents ; administration & dosage ; Combined Modality Therapy ; Depression ; drug therapy ; etiology ; therapy ; Female ; Humans ; Male ; Meridians ; Middle Aged ; Stroke ; complications ; psychology

It was estimated that about 428 species of genus Corydalis are distributed all worldwide, with about 298, especially 10 groups and 219 species being uniquely spread in China. The genus Corydalis have been widely employed as folk medicines in China, especially as traditional Tibetan medicines, for treatment of fever, hepatitis, edema, gastritis, cholecystitis, hypertension and other diseases. The phytochemical studies revealed that isoquinoline alkaloids are its major bioactive ingredients. The extensive biological researches suggested its pharmacological activities and clinic applications against cardiovascular diseases and central nervous system, antibacterial activities, analgesic effects, anti-inflammatory, anti-oxidation and anti-injury for hepatocyte, and so on. As an effort in promoting the research of pharmacodynamic ingredients, this article presents an overview focusing on the distribution, phytochemical and pharmacological results of Corydalis species that have been applied in traditional Tibetan medicinal, hopefully to provide a reference for the new Tibetan medicine development from Corydalis plant resource.
Alkaloids ; chemistry ; pharmacology ; Animals ; Anti-Infective Agents ; chemistry ; pharmacology ; Corydalis ; chemistry ; classification ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Mice ; Molecular Structure ; Phytotherapy

AIM: The study was undertaken to investigate the effort of Dexamethasone (DEX) on cultured rabbit corneal epithelial (RCE) cells and rabbit corneal epithelial wound healing.METHODS: For the in vitro experiments, primary cultures of RCE cells were used. DEX in different concentrations was added to cultured RCE cells. The effects were measured with tetrazolium salt (MTT)method and flow cytometry. For the in vivo wound-healing experiments, a central corneal deepithelialization was created and were treated with 0.1g/L DEX eyedrop randomly explain how randomly. Epithelial wound healing was evaluated clinically and analyzed histopathologically using light microscopy along with immunohistochemical staning and electronic microscopy.RESULTS: Less than 0.1g/L DEX didn't influence survival rate in cell culture conditions by MTT assay. Flow cytometric studies revealed that 0.1g/L DFX had no effect on cellular growth phase in cultured rabbit corneal epithelial cells. The mean time of the epithelial healing was significantly shorter in the DEX-treated group than in the control group at 24h. There were strong proliferative-cell-nuclear-antigen(PCNA) expressions in newly generated epithelial cells of both groups. The Dex-treated group had a more regular architecture of stromal lamella and significantly less inflammatory response than the control group under electronic microscopy.CONCLUSION: Less than 0.1g/L DEX had no inhibiting effect on cultured rabbit corneal epithelial cell growth.0.1g/L DEX eye drops can effectively promote epithelial growth and reduce inflammatory response, which may have useful clinical application at the early stage of corneal wound healing process.

OBJECTIVEThe relationship between the mode of tumor invasion in the tumor-host borderline and the frequency of cervical lymph node metastasis was investigated in squamous cell carcinoma of the oral cavity.

METHODS200 cases with histologically proven squamous cell carcinoma of the oral cavity were studied by histological method with HE stained. The mode of invasion in the tumor-host relationship was classified into five grades by Yamamoto's criteria.

RESULTSWith regard to the relationship between the mode of invasion and metastasis, the more invasive the tumor tissue was, the more frequent the metastasis formed (P < 0.001). The frequency of metastasis in grades 1 and 2 was low (0 and 5.9%, respectively), The frequency of metastasis in grades 3 was moderate (14.3%), and that in grades 4c and 4d was highly rapid (63.0% and 82.9%, respectively). Single node metastases were frequent in grade 3 and grade 4c (66.7% and 58.8%, respectively), while plural node metastases were frequent in grade 4d (70.6%, P < 0.05). Moreover, the distribution of metastasized lymph nodes was focused on level 1 (41.2%) or level 1 and 2 (79.4%) in grade 4c and was dispersed from level 1 to 4 in grade 4d (P < 0.05). In the present study, the degree of differentiation did not correlate well with the frequency of metastasis.

CONCLUSIONThese results indicate that the more invasive the tumor cells were to the host, the more frequent the metastasis formed. The different mode of invasion would accompany with different frequency of metastasis, different number and distribution of metastasized lymph nodes.

Aged ; Carcinoma, Squamous Cell ; Cell Differentiation ; Female ; Humans ; Lymph Nodes ; Lymphatic Metastasis ; Middle Aged ; Mouth Neoplasms ; Neck ; Neoplasm Invasiveness

OBJECTIVETo evaluate the prognostic significance of various clinicopathologic parameters in gastrointestinal stromal tumor (GIST), and to study the frequency of c-kit exon 11 mutations in this tumor.

METHODSOne hundred and fifty-six cases of gastric or small intestinal GIST were retrieved from the archival files of the Department of Pathology, Chinese PLA General Hospital. The clinical features, site of occurrence, tumor diameter, mitotic index, coagulative tumor necrosis, and risk grade were studied and analyzed statistically. Tumor DNA was extracted and c-kit exon 11 was amplified. Upon detection by denaturing high-performance liquid chromatography, the amplified exon 11 was sequenced.

RESULTSFor the 83 cases of gastric GIST studied, the mean age of patients was 55.4 years. Follow-up information was available in 62 cases, with 17 cases having local recurrence or distant metastasis. The 5-year survival rate was 66.5% +/- 17.1%. For the 73 cases of small intestinal GIST studied, the mean age of patients was 50.6 years. Follow-up information was available in 43 cases, with 22 cases having local recurrence or distant metastasis. The 5-year survival rate was 61.8% +/- 18.3%. In general, for gastric GIST, age younger than 50 years (P = 0.046), advanced clinical stage (P = 0.0001), large tumor size (P = 0.0001), high mitotic index (P = 0.0001), presence of coagulative tumor necrosis (P = 0.0001), and high risk grade (P = 0.004) were associated with lower survival rate. COX hazard proportional model revealed that advanced clinical stage (P = 0.001), large tumor size (P = 0.001), high mitotic index (P = 0.002) and high risk grade (P = 0.018) indicated worse prognosi. For small intestinal GIST, advanced clinical stage (P = 0.010) and presence of coagulative tumor necrosis (P = 0.036) were associated with lower survival rate. Advanced clinical stage was an independent prognostic factor. A total of 25 cases harbored c-kit mutations. The frequency of c-kit mutations was 32% and 22.5% for gastric and small intestinal GIST respectively. For gastric GIST, c-kit mutations occurred mainly in patients older than 50 years. In contrast, c-kit mutations in small intestinal GIST occurred in the age group of 40 to 49 years.

CONCLUSIONSFor gastric GIST, advanced clinical stage, tumor diameter, mitotic index and risk grade are the main prognostic indicators. For small intestinal GIST, advanced clinical stage and presence of coagulative tumor necrosis indicate poor prognosis. In general, small intestinal GIST is more frequently associated with metastasis and tumor relapse than gastric GIST. The occurrence of c-kit mutations also correlates with age of patients.

Adolescent ; Adult ; Age Factors ; Aged ; Aged, 80 and over ; Bone Neoplasms ; secondary ; DNA, Neoplasm ; genetics ; Disease-Free Survival ; Exons ; Female ; Follow-Up Studies ; Gastrointestinal Stromal Tumors ; genetics ; pathology ; Humans ; Liver Neoplasms ; secondary ; Male ; Middle Aged ; Mutation ; Neoplasm Recurrence, Local ; Neoplasm Staging ; Proportional Hazards Models ; Proto-Oncogene Proteins c-kit ; genetics ; Survival Rate ; Tumor Burden ; Young Adult

OBJECTIVETo compare the reactogenicity and serology between influenza subunit vaccine and split vaccine.

METHODSA randomized, double-blind study was carried out among children (age 6 - 12 years) in order to compare the safety and immunogenicity of an influenza inactivated subunit vaccine (Agrippal, Chiron Vaccines) with that of a split vaccine (Flurix, GSK).

RESULTSA total of 499 subjects were vaccinated and included in the safety analysis. A total of 249 subjects received Agrippal and 250 received Flurix. All subjects were kept under medical observation for 30 minutes in order to check the evidence of having any immediate local and systemic reaction. Daily observation records were collected during the 3-day follow-up after vaccination. 6.4% of the cases with fever >or= 37.5 degrees C was reported in the Flurix group, but 2.4% in Agrippal group which was significantly less than the former group (P > 0.05). Blood samples (the D0 pre- and D23 post-vaccination sera) were collected from 224 of Agrippal group and 223 of Flurix group and analysed by the haemagglutination inhibition (HI) assay. Agrippal and Flurix induced similar seroprotection (HI titer >or= 1:40, H1N1 99.6% vs 100.0%; H3N2 99.1% vs 99.1%) and seroconversion (4-fold increase, 95.1% vs 97.8%; H3N2 74.5% vs 79.8%) rates and geometric mean titer (GMT) increase (16.0 vs 21.0; 5.4 vs 6.4) against the two A subtypes. A similar seroprotection rate (94.2% vs 96.4%) and GMT increase (21.2 vs 18.2) against the influenza B strain were also noticed in both vaccines. No significant difference was found in the results of immunological assay between the two vaccines (P < 0.05). A lower seroconversion rate against B strain was observed in Agrippal group than in Flurix group (91.1% vs 97.3%).

CONCLUSIONIn terms of safety, both vaccines were generally well tolerated. The fever reaction was less frequently seen in the Agrippal group. Both vaccines induced an effective immune response in the vaccines.

Antibodies, Viral ; blood ; Child ; Double-Blind Method ; Female ; Fever ; chemically induced ; Hemagglutination Inhibition Tests ; Humans ; Influenza A virus ; immunology ; Influenza B virus ; immunology ; Influenza Vaccines ; adverse effects ; classification ; immunology ; Influenza, Human ; prevention & control ; Male ; Safety ; Vaccination ; Vaccines, Inactivated ; adverse effects ; immunology ; Vaccines, Subunit ; adverse effects ; immunology