OBJECTIVE: To design and synthesize two kinds of allyl-substituted quercetin and investigate their anti-oxidation and anti-tumor activities in vitro. METHODS: The target compounds 1 and 2 were first synthesized from quercetin by hydroxyl protection, allylation,Claisen rearrangement and deprotection. The anti-oxidation and anti-tumor activities of the target compounds and intermediate products were evaluated by DPPH and MTT assay. RESULTS: Eight compounds were synthesized,including six intermediates and two target compounds,in which four were new compounds. All of them were confirmed by 1H-NMR,13C-NMR and LC-MS spectra. The anti-oxidation and anti-tumor tests showed that compounds 1,2,5,6,8 and 9 had anti-oxidation activities and compound 5 inhibited A549 lung cancer cell proliferation. Compound 9 could inhibit the proliferation of lung cancer A549 cells and HepG2 cells. CONCLUSION: The compounds with electron-donating groups have significant anti-oxidant activity. When acetyl and methyl ether groups are used as the protecting groups,the position of introducing allyl group to quercetin has obvious impact on the anti-tumor activity.

Objective To investigate the clinical outcomes of minimally invasive percutaneous nephrolithotomy(MPCNL)in the treatment of lower caliceal calculi.Methods We retrospectively re- viewed the clinical outcomes and complications of 33 patients who underwent MPCNL for lower caliceal cal- culi from March 2001 to April 2005.The average diameter of the calculi was 2.8 cm.Single tract nephrosto- my was performed in all 33 cases;among them renal access was obtained through a middle calyx in 10 cases and a lower calyx in 23.Nine cases had F14 renal access;and 24 cases,F16.Results Of 33 cases,28 (85%)achieved stone-free at 1 session.A second-look was needed in 3 cases due to intraoperative bleed- ing;ESWL,in 1 case with residual,calculi;no treatment,in 1 case with residual calculi＜4 ram.The mean operative time was 93 min;mean blood loss was 113 ml;mean hospital stay was 11 d.Blood transfusion was needed in 1 patient who suffered from hepatic cirrhosis preoperatively;another experienced severe bleeding 7 d after operation and was cured with hyperselective spongia gelatinosa embolization of the renal artery.Fol- low-up was available in 19 cases for 2-48 months,and no recurrence of renal calculi was noted.Conclu- sions Minimally invasive percutaneous nepbrolithotomy has advantages of safety,less invasion,and easy re- covery for the treatment of lower caliceal calculi.

The aim of this study was to develop the data element standard directory of traditional Chinese medicine (TCM) clinical pharmacy information, to provide application standards and models of TCM clinical pharmacy for the electronic medical record (EMR). The developed line of work is as follows: initially establish research through four forms: literature analysis, questionnaires, discussion groups, expert advice. The research range from the Chinese herbal medicine research, herbal origin, harvesting, processing, identification of traits, physical and chemical identification, modern research, character, taste, Indications, clinical application, processing, dispensing medicine, Chinese medicine specifications, usage, dosage, caution, efficacy indications to small packaging applications, drug research, management and other related issues, including traditional Chinese medicine theory, application and hospital management information; according to the general and part 16 content of the national "Health Information Data Element Standards", and the basic method of extracting data element to study and develop the data element of TCM clinical pharmacy information from the defining content. Correspondingly propose the ideas and methods of construction of the "Data Element Standard Directory of TCM Clinical Pharmacy Information", sort out medicine clinical information data element standard catalog, divided into basic categories, clinical application class, management class three parts, and set norms and standards of identifying data elements, definitions, allowable value of traditional Chinese medicine clinical information, and discuss the sources and standards of information collection, leaving the interface, standardized and scientific terminology, docking with the existing standards, maintenance and management program and oter issues.
China ; Data Mining ; methods ; statistics & numerical data ; Database Management Systems ; standards ; statistics & numerical data ; Electronic Health Records ; standards ; statistics & numerical data ; Evidence-Based Medicine ; methods ; statistics & numerical data ; Humans ; Information Dissemination ; methods ; Medicine, Chinese Traditional ; methods ; Phytotherapy ; methods ; statistics & numerical data

A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

OBJECTIVE:To study the purification technology of Sanhuang yishen formula. METHODS:Using retention rate and impurity rate of purified total polysaccharide,astragaloside and calycosin glucoside as index,the purification effects of water extraction and alcohol precipitation method (50%,60%,70% ethanol) and clarifying agent method (101 juice clarifying agent, ZTC natural clarifying agent,chitosan clarifying agent) were respectively detected to screen the purification method;orthogonal test was used to optimize the technology parameters(mass concentration of liquid,amount of clarifying agent and pH of liquid)by the optimized purification method,and the verification test was conducted. RESULTS:The purification was better when using chito-san as clarifying agent with comprehensive score of 98.62;the purified technology parameters were mass concentration of liquid 1 g/mL,1% chitosan solution amount of 2 mL/g,pH 5.1;the average value of retention rate and impurity rate of purified total poly-saccharide, astragaloside and calycosin glucoside in verification test were 79.56%(RSD=1.24%, n=3), 78.11%(RSD=0.97%,n=3),79.46%(RSD=1.03%,n=3)and 32.18%(RSD=1.16%,n=3),respectively. CONCLUSIONS:Using chito-san as clarifying agent shows good purification effect for Sanhuang yishen formula,which is simple. The optimized technology is stable and feasible.

Traditional Chinese medicine (TCM) has its advantages in a combination of multi-target and multi-channel overall treatment. However, its mechanism is still unclear. This article elaborated upon prior research results by analyzing the effect of property, efficacy of Chinese materia medica (CMM), acupuncture and moxibustion on mitochondria. TCM can improve the morphology and structure of mitochondria. It was involved in a series of metabolic processes, which included the energy metabolism regulation, inhibition of cell apoptosis, and resistance of oxygen free radicals in mitochondria. The results showed that there existed a certain correlation between intracellular targets of TCM and mitochondria.

Objective To evaluate the effects of serum procalcitonin (PCT)-guided antibiotic therapy in elderly patients with early-onset stroke-associated pneumonia (EOP).Methods Totally 179 eligible elderly patients with EOP were randomly devided into 2 groups:standard therapy group (standard group,n=88) and PCT-guided group (PCT group,n=91).Patients in standard group received antibiotics according to antibiotics guidelines in China by the treating physicians.Patients in PCT group were treated with antibiotics for 5 days,then the antibiotic treatment was based on serum PCT levels as follows:discouraged if PCT＜0.25 μg/L and encouraged if PCT≥0.25 μg/L.Length of hospitalization,duration of antibiotics,costs of hospitalization and antibiotics,clinical efficacy,andmortality,National Institutes of Health Stroke Scale (NIHSS) score and Barthel index (BI) on the 28th day were observed.Results There were no significant differences in clinical efficacy,mortality,NIHSS score and BI between the two groups on the 28th day [(85.7％ vs.86.3％),(8.8％ vs.7.9％),10.1 (7.8,16.2) vs.9.8 (6.0,15.5),60.1(42.5,82.3) vs.57.9 (39.2,84.8),respectively,all P＞ 0.05].The length of hospitalization,antibiotic duration,costs of hospitalization and antibiotics were lower in PCT group than in standard group [19 (10,38) d vs.26(17,42) d,10 (7,14) dvs.15 (6,21) d,3350 (2052,6163) yuanvs.10355 (6877,15421) yuan,7532 (4810,12116) yuan vs.5358 (3089,8144) yuan,respectively,all P＜0.05].Conclusions PCT guidance of antibiotic therapy is effective and safe for the treatment of early-onset stroke associated pneumonia in elderly patients.It can reduce the antibiotic duration and costs of hospitalization.

OBJECTIVETo observe the regulatory effects of electroacupuncture with different acupoints combinations on blood lipid and atherosclerosis index (AI) in rats with hyperlipemia, so as to make a preliminary screening for the optimal acupoints combination for hyperlipemia.

METHODSOne hundred and five clean-grade SD male rats were randomly divided into 9 groups, including a normal group, a model group, a Quchi group, a Zhongwan group, a Fenglong group, a Quchi+Zhongwan group, a Quchi+Fenglong group, a Zhongwan+Fenglong group and a Quchi+Zhongwan+Fenglong group (three acupoints group), 17 rats in the normal group and 11 rats in the rest groups. The normal group was fed with normal diet, while the rest groups were fed with high-fat diet for 3 weeks to prepare the hyperlipemia model. All the rats were given unlimited water. After the establishment of model, the normal group was fed freely without any treatment; the model group was bundled and immobilized everyday; the rest groups were bundled, immobilized and treated with electroacupuncture at corresponding acupoints with disperse-dense wave, 20 min per time, once a day. After 4 weeks, the blood examples were collected from abdominal aorta to measure the total cholesterol (TC), triglyceride (TG), high-density lipoprotein (HDL-C) and low-density lipoprotein (LDL-C), and analyzed the AI in each group.

RESULTSAfter the treatment, TC, TG, HDL-C, LDL-C and AI in each acupuncture group were all lower than those in the model group (P<0.05, P<0.01). Compared with single acupoint group and the Quchi+Zhongwan group, the content of TC in the three acupoints group was lower (P<0.01). The differences of content of TG among each acupuncture group were not significant (all P>0.05). Compared with the rest 6 acupuncture groups, the content of HDL-C and AI in the three acupoints group were significantly different (all P<0.05). The content of LDL-C in the three acupoints group was decreased as compared with the Quchi group and the Zhong-wan group.

CONCLUSIONThe electroacupuncture at "Quchi" (LI 11), "Zhongwan" (CV 12) and "Fenglong" (ST 40) has more advantages on regulating the content of HDL-C and LDL-C as well as improving AI in hyperlipemia rats, and it has superior effects on blood lipid metabolism.

Acupuncture Points ; Animals ; Electroacupuncture ; Humans ; Hyperlipidemias ; blood ; therapy ; Lipids ; blood ; Male ; Rats ; Rats, Sprague-Dawley

Objective To investigate the effects of the microbubbles combined with different mechanical index ultrasound irradiation on ultrastmcture and migration of colon cancer cells.Methods The experimental study was conducted.Colon cancer cells inn vitro (Lovo ceils) were cultured and divided into 4 groups,ceils in the A group were not treated and cells in the B,C and D groups were treated by microbubbles combined with different mechanical index ultrasound irradiation (mechanical index were 0.20,0.80 and 1.45).The changes of ultrastructure and migration of cells were observed using laser scanning confocal microscope and MilliceIl-PCF cell culturechamber method,respectively.Measurement data with normal distribution were represented as (x)±s.Comparisons among groups were analyzed by the one-way ANOVA.Pairwise comparisons were done by the t test.Results (1)Effects of the microbubbles combined with different mechanical index ultrasound irradiation on ultrastructure of Lovo cells:Lovo cells in the A group showed big nucleus,less plasma,regular arrangement,jagged-like or more irregular varicosity surrounding nucleus,twisted euchmmatin,expansion of nucleus cisternal space,homogeneous distribution and normal development of granular soil and clear mitochondrial ridge-like structures.Lovo cells in the B group showed big nucleus with regular arrangement,obvious nucleolus margination,endoplasmic reticulum dilatation,normal development of mitochondrion and clear mitochondrial ridge-like structures.Lovo cells in the C group showed broadening nucleus space,abnormal nucleus with karyopycnosis,chromatin condensation,a few remaining or obvious dilatation of rough endoplasmic reticulum,typically consisting of different fragments or bubbles,cytoplasmic vacuoles changes and decreasing mitochondrial ridge-like structures.Lovo cells in the D group showed big and irregular nucleus,nucleolus margination,obvious endoplasmic reticulum dilatation,fewer mitochondrion with extended cell area and swelling shape,rare mitochondrial ridge-like structures with disordered or broken arrangement,even disappearing.(2) Effects of the microbubbles combined with different mechanical index ultrasound irradiation on migration of Lovo cells:Millicell-PCF cell culture chamber method showed that number of migration of Lovo cells were respectively 63±7,61±4,21±3 and 19±5 in the A,B,C and D groups,with a statistically significant difference (F=55.040,P＜0.05).There were no statistically significant difference in migration of Lovo cells between group A and B (t =1.571,P＞0.05) and between group C and D (t =2.013,P＞0.05).There were statistically significant differences in migration of Lovo cells between group A and C or D (t=7.861,10.652,P＜0.05) and between group B and group C or D (t=7.161,10.453,P＜0.05).Conclusion Microbubbles combined with high mechanical index ultrasound irradiation can make the ultrastructural alterations in the cancer cells,resulting in tumor cell degeneration and death,ultimately inhibit tumor cell migration and metastasis.

Objective To observe the changes of rotation behavior and tyrosine hydroxylase immunopositive neurons and investigate how Mrh-aFGF affects them in substantia nigra of Parkinson disease rats. Methods After building a rat model of Parkinson disease by injecting 6-OHDA into substantia nigra and ventral tegmental area,we used Mrh-aFGF to intervene rats by lateral ventricle injection to observe how behavior of rats induced by apomorphine and tyrosine hydroxylase immunopositive neurons in substantia nigra of rats changes,then quantitatively analyzed the change of tyrosine hydroxylase immunopositive neurons. Results Rotation behavior was not found in control group,otherwise,actuation time was shorted,time length was prolonged,and average velocity of rotation was accelerated in Parkinson disease rats(P