Ten novel conjugates with ursolic acid core and different chalcone ligands were synthesized via esteri-fication using the natural ursolic acid as starting material. The structures of these conjugates were confirmed by 1 H NMR, 13 C NMR and HRMS. The preliminary biological results showed that these compounds displayed signifi-cant antiproliferative effect on CNE2, KB, MCF-7, A549 and HepG2 cells. These compounds were more effective than ursolic acid and tamoxifen against MCF-7 cells. Especifically, compound 11e ( IC50 =4. 7 μmol/L) showed the greatest potency against MCF-7, which was about 3-times more potent than tamosifen ( IC50 =15. 2 μmol/L) . Additionally, all conjugates were nontoxic to health MCF-10A and VERO cells, and had higher security than tamoxifen.

Objective To observe the recovery efficiency of sufentanil and oxycodone hydrochloride in neurosurgical operation.Methods Total of 120 patients scheduled for microvascular decompression under general anesthesia were randomly divided into 4 groups to receive 0.03 mg·kg-1 oxycodone (group H1), 0.05 mg·kg-1 oxycodone (group H2), 0.08 mg·kg-1 oxycodone (group H3), and 0.08 μg·kg-1 sufentanil (group S).Each patient accepted 4 ng·mL-1 of remifentanil and 5-6 mg·kg-1·h-1 of propofol after induction to maintain bispectral index (BIS) value at 40-60.On starting to suture dura mater, oxycodone or sufentanil was given in various doses through intravenous route.The BIS value, the amount consumption of propofol, anesthesia and operation duration, and the drug delivery time of each group were recorded.The time of spontaneous breath recovery, awaking and extubation, verbal rating score (VRS) and sedation score (SS) at 10 min, 20 min, 30 min after operation as well as side-effects were also recorded.Results The VRS scores had no statistic difference among the groups at 10 min after operation, while the average scores of H1 were higher than those of H2 and H3 at 20, 30 min after operation.No statistic difference of the SS scores was showed among 4 groups at 10 min after operation, but it was lower in group H1 than those in group H3, and lower in group S than those in H2 at 20 min after operation;group H3 had a significantly higher SS scores than H1, H2 and S at 30 min after operation.Conclusion Oycodone hydrochloride 0.05 mg·kg-1 or sufentanil 0.08 μg·kg-1 can both provide satisfactory recovery quality in neurosurgical operation.

Objective To explore the clinical characteristics of chronic obstructive pulmonary disease (COPD)in the patients with pulmonary interstitial fibrosis.Methods Twenty-seven COPD patients with pulmonary fibrosis and thirty patients with COPD who were diagnosed from July 2001 to October 2010 were analyzed for their clinical symptoms,physical signs,pulmonary function,arterial blood-gas,radiographic features,CT and high resolution computed tomography(HRCT)of the chest.Results The clinical features of COPD with pulmonary fibrosis shared that of the two diseases.Eighteen cases of COPD with pulmonary fibrosis had mixed ventilatory dysfunction(P ＜ 0.01).COPD were all obstructive ventilatory dysfunction(P ＜ 0.01).For arterial blood-gas test,PF-COPD showed progressing hypoxemia and little PaCO2 retention,but no significant difference was observed.Chest X-ray showed that 30 cases in the COPD group had an increased anteroposterior diameter of the thorax,while it was 14 cases in the PF-COPD group(P ＜0.05).Twenty four cases in the PF-COPD group showed nodular,meshy or honeycomb-like lesions,but none in COPD group(P ＜ 0.01).Chest CT and HRCT showed that there were higher chances of frosted glass-like and grid-like nodular lesions in the lungs of PF-COPD group than in COPD group(9 vs.0,19 vs.0 ;x2 =10.85,17.36,P ＜ 0.01).Conclusions Patients with chronic obstructive pulmonary disease and pulmonary fibrosis sharing the clinical features of both diseases.Chest HRCT can provide important information for clinical diagnosis.

Objective: To develop a suitable method for the large-scale separation of quinolone alkaloids from the fruits of Evodia rutaecarpa by high-speed counter-current chromatography (HSCCC). Methods: Two solvent systems were developed for the separation method. The upper phase was used as the stationary phase, and the lower phase was used as the mobile phase at 35 °C with the flow rate of 2 mL/min and rotation speed of 855 r/min. Results Using the described method, 1-methyl-2-undecyl-4(1H)-quinolone (1), evocarpine (2), 1-methy-2-[(6Z,9Z)]-6,9-pentade-cadienyl-4-(1H)-quinolone (3), dihydroevocarpine (4), and the mixture (5) of 1-methyl-2-[(Z)-10-pentadecenyl]-4(1H)-quinolone (Va) and 1-methyl-2-[(Z)-6-pentadecenyl]-4(1H)-quinolone (Vb) could be isolated from a petroleum ether extract. They were identified by 1H-NMR, 13 C-NMR, and MS/MS, and the purities were 94.3%, 95.2%, 96.8%, 98.3%, and 96.8%, respectively. Conclusion: Five quinolone alkaloids from the fruits of E. rutaecarpa could be systematically isolated and purified using HSCCC. The presented method is simple and efficient with good potentials on the preparation of reference substances, especially on the quality control of Chinese materia medica. © 2014 Tianjin Press of Chinese Herbal Medicines.

Objective To assess the effects of different doses of oxycodone hydrochloride on spontaneous breathing and consciousness level of patients,so as to provide theoretical basis for its clinical application.Sixty patients undergoing elective surgery were randomly divided into 3 groups:0.05 mg · kg-1 oxycodone group (group P1),0.1 mg· kg-1 oxycodone group (group P2),0.2 mg· kg-1 oxycodone group (group P3).Changes of respiratory rate (RR),end tidal carbon dioxide partial pressure (PETCO2),saturation of blood oxygen (SpO2) and bispectral index (BIS) were recorded in patients before injection (t0) and 1-15 min after injection (once per min);the Observer's Assessment of Alertness/Sedation Scale (OAA/S) were recorded.At the same time,the adverse reactions were observed after drug injection in each group.Results In 10 min after injection there were no significant differences in the RR,SpO2,PETCO2,BIS and OAA/S in group P1 as compared with those before injection (P＞0.05).The patients had no respiratory depression in group P1.In group P2,RR had a significant decrease (P＜0.05),BIS had decreased but were greater than 85;there were no significant differences in the SpO2,PETCO2 and OAA/S (P＞0.05).The P2 group had 3 cases with respiratory frequency＜10 per min,but SpO2 were all greater than 94％.In group P3,There were significant differences in the RR,SpO2,PETCO2,BIS and OAA/S (P＜0.05).The P3 group had 12 cases of respiratory frequency ＜10 per min,at the same time there were 8 patients with SpO2 less than 94％.With the increasing dose,the frequency of respiratory inhibition increased,and there were statistical differences (P＜ 0.05).In 15 min after injection,RR,SpO2,PETCO2,BIS and OAA/S were not significantly different in group P1 and P2 as compared with those before injection (P＞0.05).In group P3,RR was significantly different after injection (P＜0.05).There were no significant differences in the SpO2,PETCO2,BIS and OAA/S in group P3 after injection (P＞0.05).No patients complained with chest wall stiffness,nausea and vomiting,cough and other adverse reactions in group P 1 and P2.In group P3,three patients had nausea 5 min after injection,two patients complained of chest skin itching but no skin flushing.Conclusion With the increasing dose,effect of oxycodone hydrochloride on breathing and consciousness level of patients gradually increased.Injection of oxycodone hydrochloride 0.05 mg · kg-1 had no obvious effect on breathing and consciousness.After injection of oxycodone hydrochloride 0.1 and 0.2 mg · kg-1 for 5 to 10 min,respiration inhibition and sedative effect were the most obvious.Fifteen min after injection,the 0.1 mg · kg-1 dose group recovered to the level before,the respiratory rate of the 0.2 mg · kg-1 dose group was still lower than that before the injection.

Objective To investigate the changes in auditory evoked potential index (AEPI) during endotracheal intubation and the effects of intravenous lidocaine or topical anesthesia of larynx and vocal cords with tetracaine on intubation response. Methods Thirty-six patients classified as ASA physical status and Mallampati intubation status I or II , aged 19-55 yr scheduled for elective surgery under general anesthesia were randomly divided into 3 groups with 12 patients in each group: (1) control group (C) ; (2) intravenous lidocaine group (L) and (3) topical tetracaine group (T). The patients were premedicated with intramuscular atropine 0.01 mg?kg-1 and phenobarbital 0.1 g. Anesthesia was induced with midazolam 30 ?g ? kg-1, fentanyl 3 ?g ? kg-1 and propofol 1.5-2.0 mg?kg-1 . Direct vision tracheal intubation was performed at 3 min after vecuronium 0.1 mg?kg-1 . In group L 1 % lidocaine 1 mg ? kg-1 was given i. v. after propofol injection. In group T the suproglottic area and vocal cords were sprayed with 1% tetracaine 3-5 ml before intubation. All intubations were performed by the same anesthesiologist. BP, HR, SpO2 and AAI value were recorded 1 min before and 1 min after intubation. The time between vecuronium injection and tracheal intubation was also recorded.Results AAI value, MAP and HR significantly increased after endotracheal intubation in all 3 groups. The increase in AAI value in group T was significantly larger than that in group C and L. The increase in MAP and HR in group L after intubation was significantly smaller in group L than in group C and T. There was no significant difference in MAP and HR between group C and T after intubation. Conclusion AAI is more sensitive than MAP and HR in terms of detecting the increase in AAI value induced by responses to tracheal intubation. Neither intravenous lidocaine nor tetracaine topical anesthesia of vocal cords inhibits the intubation. Intravenous lidocaine can attenuate the cardiovascular response to intubation.

Abstract?AlM:To compare the effects of different adjustable suture in glaucoma trabeculectomy on early tear film function.?METHODS:Sixty-eight cases of primary glaucoma ( 76 eyes) during January 2012 to June 2014 in our hospital were selected and divided into exposure conjunctival suture group ( 34 cases, 36 eyes ) and embedded conjunctival suture group ( 34 cases, 40 eyes ) according to treatment. Adjustable suture exposed conjunctival suture and embedding conjunctival suture was given to two groups, respectively. lntraocular pressure ( lOP ) before and after treatment 7, 14, 30d were observed and Schirmer test, tear break-up time, No Hikaru sensitivity and the occurrence of adverse reactions after treatment 1, 30d were recorded.?RESULTS: After the treatment, the mean lOP of two groups were decreased significantly ( P < 0. 05 ). The average lOP after treatment of 1d in the two groups were not statistically different (P>0. 05), after treatment 7, 14, 30d embedded conjunctival suture group was significantly higher than that of exposure conjunctival suture group ( P<0. 05). After 1d of treatment, Schirmer test, tear break-up time, No Hikaru sensitivity of two groups compared no significant difference (P<0. 05). After treatment 7, 14, 30d embedded conjunctival suture group Schirmer test, tear break- up time, was significantly superior to expose conjunctiva suture group (P<0. 05). The 30d package after treatment of conjunctival suture group buried adverse reaction rate was significantly lower than that of exposed conjunctival suture group (P<0. 05).? CONCLUSlON: Trabeculectomy operation with adjustable thread embedding conjunctival suture has few effects on the tear film function in patients with early postoperative complications, lower, and operation effect is better than that of exposed conjunctival suture.

Erythropoiesis ; physiology ; Humans ; Mitochondria ; physiology ; Mitochondrial Degradation

OBJECTIVETo establish the steriod-induced osteoporosis model with the type of Kidney-Yin deficiency.

METHODSTotally 45 female Kunming mice were randomly divided into normal group,model group and Liuwei Dihuang pills(Chinese character: see text)group. The model was established by intramuscular injecting of Dexamethasone. Liuwei Dihuang pills (Chinese character: see text) group was administered orally with Liuwei Dihuang pills (Chinese character: see text). The signs and symptoms of mice were observed dynamically. All the animals were sacrificed at the end of the 6th weeks. The level of ACTH, cAMP, cGMP, TSH and E2 in serum were detected to evaluate deficiency of Kidney-Yin. Morphological changes and bone density were observed to evaluate osteoporosis.

RESULTS(1) Compared with control group, mice in model group appeared obvious Kidney-Yin deficiency symptoms, including hair dry, restlessness, excitability, hard stool, and yellow. (2) Compared with control group,the weight of mice in model group gained slower (P<0.01); the index of adrenal gland,liver and spleen decreased (P<0.01, P<0.01 ,P<0.01); the level of ACTH and TSH increased (P<0.01 ,P<0.01), the level of E2 decreased (P<0.01) and the ratio of cAMP/cGMP increased (P< 0.05). (3)Compared with control group,the bone density of lumbar vertebra and femur in model group were significantly decreased (P<0.01, P<0.05); HE staining revealed osteoporosis in model group mice. (4)However, the Liuwei Dihuang pills (Chinese character: see text) group can partly antagonize the inhibition of the HPA axis, alter the disordered sex hormone and the ratio of cAMP/cGMP, and reverse the osteoporosis partly.

CONCLUSIONthe model of osteoporosis with type of Kidney-Yin deficiency could be established by Dexamethasone intramuscular injection. With less interference, it wight be a stable and reliable modeling method for integration of disease and syndrome in TCM.

Animals ; Bone Density ; Dexamethasone ; toxicity ; Disease Models, Animal ; Female ; Kidney Diseases ; etiology ; Medicine, Chinese Traditional ; Mice ; Osteoporosis ; chemically induced ; Yin Deficiency ; complications

OBJECTIVETo observe effects of serum Bushen Huoxue prescription(Chinese characters) on classic Wnt/β-catenin signaling pathways of osteoblasts, and explore mechanism of Bushen Huoxue prescription (Chinese characters) for preventing osteoporosis.

METHODSTwenty health female rats were randomly divided into two groups, including Bushen Huoxue (Chinese characters) group and saline group,10 in each group. Bushen Huoxue (Chinese characters) group and Saline group were gavaged Bushen Huoxue and saline every day for 1 week. Bushenhuoxue containing serum and saline containing serum were got according to methods of serum preparation of drug-containing. The osteoblasts was cultured with neonatal rat skull according to Enzyme Consumer Law, and was identified by Wright-Giemsa staining (R-J) and alkaline phosphatase staining (ALP). The third generation of osteoblasts was divided into three groups, including saline group, normal group,Bushen Huoxue (Chinese characters) group. Each group were added to 15% appropriate medium. ALP activity of osteoblasts and osteoblasts proliferation rate were tested, mineralized nodules were observed, the expression of β-catenin, Runx2, Osx mRNA of osteoblasts were tested by RT-PCR.

RESULTSThere was blue granules in cytoplasm, cell nucleus was flint with 1 to 3 nucleoli showed by R-J staining, morphology of osteoblasts were cultured. ALP staining showed cytoplasm with purple granules, the results showed that the cultured cell was osteoblasts. The content of ALP in Bushen Huoxue (Chinese characters)group was (6.272±0.131) ,appreciation rate was (0.81? 0.172), and could significantly improve differentiation and proliferation activity of osteoblasts compared with Saline group (P< 0.01). There were four different size orange nodules, the Maximun nodule was 1.0 x 1.0 cm in Bushen Huoxue (Chinese characters) group after Alizarin red staining, the results showed Bushen Huoxue (Chinese characters)group could obviously improve mineralization of osteoblasts. The expression of mRNA of β-catenin, Runx2 and Osx in Bushen Huoxue (Chinese characters)group were (1.782±0.944), (1.935±0.994) and (1.610±0.811) by RT-PCR,it was significantly increased compared with saline group (P<0.01), but there was no difference between Bushen Huoxue (Chinese characters)group and normal group (P>0.05).

CONCLUSIONBushen Huoxue (Chinese characters)group could obviously promote differentiation, proliferation and mineralization of osteoblasts through activation of Wnt, β-catenin signaling pathway. It suggested that the mechanism of action of Bushen Huoxue (O'f f Il.t)particle clould prevent osteoporosis through the activation of Wnt, β-catenin signaling pathway.

Animals ; Cell Differentiation ; drug effects ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Female ; Humans ; Osteoblasts ; cytology ; drug effects ; metabolism ; Osteoporosis ; drug therapy ; genetics ; metabolism ; physiopathology ; Rats ; Rats, Sprague-Dawley ; Wnt Proteins ; genetics ; metabolism ; Wnt Signaling Pathway ; drug effects ; beta Catenin ; genetics ; metabolism