OBJECTIVE: To improve the synthetic technology of nateglinide so as to increase yield and promote industrial production.METHODS: The improvement was conducted from aspects of reagent,catalyst,crystal form transformation etc in which the sodium hydride reported in literature was substituted by sodium hydrate in cis-trans transformation,and phosphorus trichloride or phosphorus pentachloride was substituted by thionyl chloride for the chlorination,and PtO2 or Raney Ni was substituted by RuNiAlC as catalytic agent.In H form crystal form transformation,fine seed-crystal was obtained by low temperature crushing,which was added with seed-crystal to induce crystallization to obtain H form crystal.The structure of the crystal form of the product obtained using the improved technology was characterized and its yield was computed.RESULTS: The crystal form characterization results demonstrated that the product was H form crystal and its yield reached 72%,higher than that reported in literature(50%).CONCLUSION: The improved technology of nateglinide contributed to the increase of its yield;Therefore,this technology is suitable for industrial production.

OBJECTIVE:To improve the production technology of prulifloxacin.METHODS:The primary synthetic process of prulifloxacin was improved from aspects of raw material,agents,reaction method,reaction condition etc by referring to literature together with our experience in and considerable experiments on the production of pruliflorxacin.RESULTS & CONCLUSIONS:The improved production technology of prulifloxacin is simple in operation,obtainable in raw material,high in yield and low in cost,it also meets the requirement on environmental protection,and which is thus suitable for the industrial production of prulifloxacin.

Objective To investigate the expression of high mobility group A1 (HMGA1) in patients with lung squamous cancer and its clinical significance.Methods The expression of HMGA1 in 76 patients with lung squamous cancer (lung squamous cancer group) and 30 cases of control lung tissue (control group) was detected by SP method of immunohistochemistry and its correlation with clinical-pathological parameter was analyzed statistically.Results The positive expression rate of HMGA1 was 68.4％ (52/76)and 16.7％ (5/30) in lung squamous cancer group and control group respectively,and the difference was significant(P＜ 0.01).HMGA1 expression showed significant correlation with lymph metastasis and degree of differentiation in patients with lung squamous cancer (P ＜ 0.05).Conclusions The progression of lung squamous cancer may correlate with the increase of HMGA1 expression.It's promising for HMGA1 to become a new marker for diagnosis of lung squamous cancer.Clinical detecting of HMGA1 could help with prognosis and treatment-guiding of lung squamous cancer.

Objective:Comparative analysis of imaging features of abdominal CT, B ultrasound and magnetic resonance cholangiopancreatography in three different methods for detection of extrahepatic bile duct stones. Methods: A random sample of extrahepatic bile duct stones were a sample of 150 cases as the object of study, patients in the endoscopic retrograde cholangiopancreatography after diagnosis, followed by B ultrasound examination, the implementation of CT scanning and MRI imaging in 142 cases, including 78 cases of B ultrasound detection, CT detection, 118 cases underwent MRI examination. Results: The detection results were recorded and compared the 3 imaging methods. Results: The positive rate of B ultrasound 39.4%, the positive rate of CT was 53.8%, MRI positive rate was 86.4%, the positive rate of MRI was significantly higher than that of B ultrasound and CT (x2=59.725, x2=25.595; P<0.01), the detection rate of CT was significantly higher than that of B ultrasound(x2=4.231, P<0.05). Diameter less than 8 mm of extrahepatic bile duct stones with B ultrasound and positive rate of 25%, the positive rate of CT was 33.3%, MRI positive rate was 60%, the positive rate of MRI was significantly higher than that of B ultrasound and CT(x2=7.789, x2=7.789;P<0.01), the detection rate of CT with no significant differences between the B ultrasound. Conclusion:MRI of extrahepatic bile duct stones with B ultrasound and the positive rate of CT is higher, but the clinical needs according to the comprehensive evaluation of individual patients, economic status, symptoms, diagnosis method for selecting suitable.

Objective To investigate the protection of renal function and the prevention of acute renal failure (ARF) in patients with malignant obstructive jaundice in perioperative period of radical resection. Methods A series of clinical interventions had been taken since 2004 in our treatment team, including control of endotoxemia, depression of biliary tract before operation, maintenance of adequate effective blood volume, nutritive support, administration of mannitol and low dose of furosemide, and avoidance of disseminated intravascular coagulation. The incidence of perioperative ARF in 206 patients with malignant obstructive jaundice who had been radically resected from 2000 to 2007 was retrospectively studied, and the RIFLE criteria was used for ARF classification. This study was progressed in two periods. The first one was from Jan. 2000 to Dec. 2003, and the second one was from Jan. 2004 to Dec. 2007. Results After 2003, the proportion of radical resection rose from 44.8% to 57.1% (P

AIM:To explore the effect of sesamin on blood fat,blood glucose and vascular remodeling in rats fed with high-fat,refined-sugar diet.METHODS:A high-fat,refined-sugar diet was given to rats for 24 weeks.Sesamin(120,60,30 mg?kg-1?d-1)was given by intragastric administration to the rats at 9th week,which lasted for 16 weeks.After 24 weeks,blood glucose,blood fat,blood pressure,activity of total anti-oxidation capacity(T-AOC)and concentration of hydrogen peroxide in serum and aorta were determined.Changes of histology and collagen fibers were observed in aorta by HE and Masson' staining,respectively.Immunohistochemical method was used to examine iNOS protein expression in aorta.In mesenteric arteries,media thickness(M),luminal radius(L)and ratio of media to lumen(M/L)were measured.RESULTS:Compared to model group,sesamin(120,60 mg?kg-1?d-1)obviously decreased the levels of blood glucose,blood fat,blood pressure and concentration of hydrogen peroxide in serum and aorta.Sesamin also markedly enhanced the activity of T-AOC in serum and aorta and reduced collagen deposition and iNOS protein expression in the vascular wall.In addition,proliferation of intima and vascular smooth muscle cells were improved.In mesenteric arteries,sesamin lessened M and M/L and increased L of mesenteric arteries.CONCLUSION:Sesamin ameliorates disorders of glucose and lipid metabolism and inhibits vascular remodeling in rats caused by chronic high-fat,refined-sugar diet.

AIM:To explore the effects of sesamin on blood glucose,blood lipids and vascular cell adhesion molecule-1(VCAM-1)protein expression of aorta in rats with metabolic syndrome.METHODS:A high-fat,refined-carbohydrate diet was given to rats to induce metabolic syndrome for 24 weeks.Sesamin(120,60,30 mg?kg-1?d-1)were given to the metabolic syndrome rats at the ninth week by intragastric administration,which were lasted for 16 weeks.Then,the body weight and abdominal fat of all rats were weighed and the levels of blood lipid,blood glucose,the total anti-oxidation capacity(T-AOC)and the hydrogen peroxide concentration in the serum were determined.In addition,the pathological change and the VCAM-1 protein expression of aorta were observed by H-E staining and immunohistochemical method respectively.RESULTS:Compared with those in model group,the body weight and abdominal fat of sesamin(120,60 mg?kg-1?d-1)groups were obviously decreased,the levels of serum TG,TC,LDL-C and blood glucose were markedly decreased and the level of HDL-C was increased.The VCAM-1 protein expression of aorta was depressed.The pathological change was improved;The T-AOC and hydrogen peroxide concentrations of serum and aorta were decreased.CONCLUSION:Sesamin can obviously descrease the levels of blood lipid,blood glucose and depress the VCAM-1 protein expression of aorta,improve the pathological change of aorta and protect against the progression of atherosclerosis.

Many datas show that thrombosis related events during chemotherapy in patients with cancer increase obviously.Thromboprophylaxis in patients receiving chemotherapy has been shown to not only improve the hypercoagulable states and effectively prevent thrombosis,but also have the potential antitumor effect and prolong the patients over survival.

Arthroplasty, Replacement, Hip ; methods ; Bone Transplantation ; Femur ; surgery ; Humans

Objective To investigate the security and efficacy in the elderly patients with acute myeloid leukemia (AML) treated by decitabine based regimen. Methods A retrospective analysis was carried out on 12 elderly patients with AML who were treated by decitabine alone or with low-dose chemotherapy in Beijing Luhe Hospital, Capital Medical University from June 2014 to December 2015. Results There were 6 patients of complete remission (CR), 5 patients of partial remission (PR), 1 patient of none remission (NR) after one course of chemotherapy. 1 case of 6 CR patients relapsed after 6 cycles of chemotherapy , others remained CR during the follow-up . Among 5 PR patients , 2 cases achieved CR , 1 patient relapsed after 2 cycles of chemotherapy and 2 patients relapsed after 3 cycles of chemotherapy. 1 patient remained NR after 2 cycles of chemotherapy and died of severe pulmonary infection. 3 of 4 complex karyotype patients had poor efficiency, and only 1 patient achieved CR but relapsed eventually. 7 patients achieved CR in patients with +8, -X or normal karyotype in the near future. The main adverse effects were bone marrow suppression and infection. All patients could tolerate. Conclusion Elderly patients with primary AML treated by decitabine alone or with low-dose chemotherapy show good effects, well tolerance and high safety, which could serve as the front-line treatment.