facile method for the synthesis of 2-[3-hydroxy-1-adamantyl]-2-oxoacetic acid and it’s optimization

2-[3-hydroxy-1-adamantyl]-2-oxoacetic acid [IV], a key intermediate of saxagliptin for type 2 diabetes mellitus [T2DM], was prepared from 1-adamantanecarboxylic acid[I] via oxidation by potassium permanganate[KMnO4] to afford 3-hydroxy-1-adamantanecarboxylic acid [II], which was treated with a one-pot method to give 1-acetyl-3-hydroxyadamantane [III] followed by oxidation. Some key steps were optimized and the overall yield was about 51%

Effect of a selective inducible nitric oxide synthase inhibitor on cell growth in human colorectal cancer Lovo cell line / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To investigate the effect of a selective inducible nitric oxide synthase(iNOS) inhibitor, aminoguanidine (AG), on the proliferation and apoptosis of human colorectal cancer (CRC) Lovo cell line, and explore its possible mechanism.</p><p><b>METHODS</b>MTT assay was used to detect the inhibition of Lovo cell growth by aminoguanidine. Apoptosis and cell cycle of Lovo cells were examined by flow cytometry (FCM). Morphologic change of Lovo cell treated by AG was observed with AO/EB staining.</p><p><b>RESULTS</b>There were significant differences in 0.5 mmol/L and 1.0 mmol/L AG groups as compared to the control group (P<0.05). The absorbance (A) values of Lovo cells in each time point were significantly different (P<0.05). Growth of Lovo cells was inhibited by aminoguanidine in a dose- and time-dependent manner. FCM analysis showed that the cell ratio of G(0)/G(1) phase increased with the increasing of the concentration of aminoguanidine, but the cell ratio of S-and G(2)/M phase decreased correspondingly (P<0.05). S phase fraction and proliferation index (PI) decreased remarkably, and the apoptotic rate of Lovo cells increased. After AG treatment, AO/EB staining revealed some apoptotic morphological features such as cell shrinkage, nuclear condensation, DNA fragmentation, and formation of apoptosis bodies.</p><p><b>CONCLUSIONS</b>Aminoguanidine inhibits the proliferation and facilitates the apoptosis of human CRC Lovo cells. One of the mechanisms may be explained as blocking the progress of cell cycle of CRC Lovo cells by aminoguanidine.</p>

Comparative study on three types of digestive reconstruction after total gastrectomy / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To investigate the rational digestive reconstruction after total gastrectomy for gastric malignancy.</p><p><b>METHODS</b>Three types of digestive reconstruction were performed after total gastrectomy in 189 cases with gastric carcinoma. The operating time, morbidity and mortality, food intake, digestive tract symptoms, nutritional status at 1 and 3 years after surgery and 1-, 3-, 5-year cumulative survival were compared.</p><p><b>RESULTS</b>There were no significant differences among the three procedures in operative morbidity and mortality, postoperative food intake, nutritional status (Hemoglobin, total protein and labium), and incidences of diarrhea and dumping syndrome (P > 0.05). The overall 1-, 3-, 5-year survival rates were 75.3%, 38.2% and 20.5% respectively, and there were no significant differences among the three groups (P > 0.05). Orr-type and P-type esophagojejunostomy had an advantage of anti-esophageal reflux, and were obviously superior to Moynihan-type anastomosis (P< 0.01). Compared with P-type reconstruction, Orr-type reconstruction was simpler with shorter operating time, and less complications.</p><p><b>CONCLUSIONS</b>Orr-type Roux-en-Y esophagojejunostomy can be recommended as an adaptable method of digestive reconstruction after total gastrectomy for gastric cancer because of its avoiding reflux esophagitis, maintaining better nutritional status and quality of life, and simpler procedure.</p>

A case-control study on the mxA polymorphisms and susceptibility to severe acute respiratory syndromes / 中华流行病学杂志

<p><b>OBJECTIVE</b>To investigate the association between the genetic polymorphisms of myxovirus resistance 1 (MxA) gene and susceptibility to severe acute respiratory syndromes (SARS).</p><p><b>METHODS</b>A case-control study was conducted and polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) was used to detect the T/G polymorphism at position-88 in the mxA gene promoter. Information on related factors of SARS was collected using a pre-testing questionnaire. Univariate and multivariate logistic analyses were conducted with SPSS software package.</p><p><b>RESULTS</b>Sixty-six cases and sixty-four controls were selected for the study. Comparing with GG genotype, the proportion of GT genotype were significantly higher in the case group (81.3%) than that in the control group (62.5%)) with an OR (95% CI) of 2.700 (1.208-6.037). Multivariate logistic regression analysis revealed that the significant association remained after factors as wearing masks, protection gowns and eye-protection when contacting with SARS patient etc. were adjusted with an OR (95 % CI) of 2.911 (1.027-8.250).</p><p><b>CONCLUSION</b>mxA promoter-88G/T SNP might be confered to host genetic susceptibility to SARS in Chinese Han population.</p>