OBJECTIVETo synthesize venlafaxine with an improved novel method.

METHODSp-methoxypheny lethyl-acid was reacted with SOCl(2) to produce acyl chloride which was reacted with N,N-dimethylamine solution to get amide; then through Ivanov reaction and reduction by KBH(4)/BF(3).Et(2)O to yield venlafaxine.

RESULTVenlafaxine was successfully synthesized by using this method with an yield rate of 50.3%.

CONCLUSIONThe improved method is suitable for industrial production of venlafaxine.

Antidepressive Agents, Second-Generation ; chemical synthesis ; Cyclohexanols ; chemical synthesis ; Venlafaxine Hydrochloride

OBJECTIVETo modify the synthetic method of fluvoxamine.

METHODSFluvoxamine was synthesized from 4-trifluoromethylbenzonitrile by the steps of Grignard reaction, hydrolysis and oximation.

RESULTThe chemical structure of the synthesized product was confirmed by (1)HNMR, and the total yield reached to 36.16%.

CONCLUSIONThe results indicate that the synthetic route is practical.

Fluvoxamine ; chemical synthesis ; Serotonin Uptake Inhibitors ; chemical synthesis

OBJECTIVETo investigate the role of perindopril for prevention and treatment of glucocorticoid-induced osteoporosis (GIOP) in rabbits.

METHODSA total of 45 male New Zealand white rabbits (10 months old, weight 3.0 to 3.5 kg) were randomly divided into 3 groups involving normal control group (muscle injection of saline solution, n = 15, group NC), model group (muscle injection of dexamethasone, n = 15, group GIOP), and treatment group (muscle injection of dexamethasone combined with oral perindopril, n = 15, group GIOP+ACEI). All rabbits put to death after 12 weeks' treatment. The changes of bone mass and strength were observed and analyzed by bone histomorphology, biomechanics, metabolic bone related serological indexes and mRNA expression.

RESULTSAt 12 weeks, the analysis of bone histomorphology and biomechanics results showed that the bone mass and bone strength of group GIOP were significantly lower than that of group NC (P < 0.05); after perindopril treatment, the bone mass and bone strength of group GIOP+ACEI were higher obviously than that of group GIOP (P < 0.05). Mineralizing surface,mineral apposition rate and serum osteocalcin in group GIOP decreased than group NC; however, osteoclast number, osteoclast surface, eroded surface, and urinary deoxypyridinoline in group GIOP increased than group NC (P < 0.05); these changes were inhibited after perindopril treatment (P < 0.05). Quantitative RT-PCR revealed that after dexamethasone treatment, the ratio of SOST mRNS expression and RANKL/OPG mRNA expression obviously increased than that of group NC (P < 0.05); and Runx2 expression decreased significantly (P < 0.05); while the changes of mRNA expression were improved by perindopril treatment.

CONCLUSIONPerindopril can promote bone formation and inhibit bone resorption to deduce glucocorticoid-induced osteoporosis. This study provides a new method for prevention and treatment of GIOP.

Animals ; Biomechanical Phenomena ; Glucocorticoids ; adverse effects ; Male ; Osteoporosis ; chemically induced ; prevention & control ; Perindopril ; therapeutic use ; Rabbits

OBJECTIVETo investigate the effects and underlying mechanism of notoginsenoside R1 on amyloid-β (1-42) (Aβ(1-42)) induced mitochondrial apoptotic death in SH-SY5Y cells.

METHODCell viability was assayed by MTT, apoptotic rates were analyzed with PI/Annexin V flow cytometry, Bax and Bcl-2 expression were detected with Western blotting, enzymatic activity of caspase-3, caspase-8 and caspase-9 were measured by ELISA assay.

RESULTThe 6.25-100 nmol x L(-1) of notoginsenoside R1 attenuate Aβ(1-42) induced apoptotic death of SH-SY5Y in dose dependent manner. The ratio of Bcl-2/Bax was elevated in SH-SY5Y with notoginsenoside R1 treatment. Caspase-3 and caspase-9 were activated with notoginsenoside R1 treatment while caspase-8 was not affected.

CONCLUSIONNotoginsenoside R1 could protect SH-SY5Y cells from Aβ(1-42) induced apoptosis via mitochondria related apoptotic pathway.

Amyloid beta-Peptides ; antagonists & inhibitors ; Apoptosis ; drug effects ; Caspases ; metabolism ; Cell Line, Tumor ; Cell Survival ; drug effects ; Cytoprotection ; Ginsenosides ; pharmacology ; Humans ; Mitochondria ; drug effects ; Peptide Fragments ; antagonists & inhibitors

AIMTo identify the commercial drugs collected from 11 different areas with name of "Baitouweng", in order to understand the homonym status of Baitouweng in markets.

METHODSBased on macroscopic identification, we further studied the microscopic structures of the collected samples by digital imaging technique.

RESULTSNine species belong to 4 different families have been found out from the commercial drugs of "Baitouweng". There are the roots of Pulsatilla chinensis (Bunge) Regel (recorded in Chinese Pharmacopoeia with name "Baitouweng"), P. cernua (Thunb.) Bercht et Opiz, P. turczaninovii Kryl. et Serg., P. dahurica (Fisch.) Spreng., Anemone tomentosa (Maxim.) Pei, Rhaponticum uniflorum (L.) DC. and the herbs of Potentilla chinensis Ser., Po. discolor Beg. and Polycarpaea corymbosa Lam..

CONCLUSIONThe original plants of the crude drug "Baitouweng" were still promiscuous in the market because there are different medicinal usages in different areas resulting in the phenomenon of homonym for Baitouweng. Otherwise, the digital photographs offered by the paper visually reflected the main microscopic characteristics of the commercial "Baitouweng", can be used for the identification of the above drugs.

Anemone ; anatomy & histology ; cytology ; Drug Contamination ; Image Processing, Computer-Assisted ; methods ; Pharmacognosy ; Plant Roots ; anatomy & histology ; cytology ; Plants, Medicinal ; anatomy & histology ; cytology ; Potentilla ; anatomy & histology ; cytology ; Pulsatilla ; anatomy & histology ; cytology ; Quality Control ; Species Specificity

Objective To investigate the diagnostic value of Multislice CT scanning in patients with acute thoracic trauma. Methods151 patients with chest wound admitted after Multislice CT scanning were reviewed and analyzed. ResultsThis group of 151 patients with chest wound after X-ray and CT inspection were as follows:lungs were damaged in 139 cases including 52 cases with traumatic wet lung,94 cases with lung rip,28 cases with lacerated wound and 7 cases with tracheal bronchial tube damage.Damages outside the lungs were found in 108 patients including 83 patients with trauma in pleural membrane(hemothorax 27 cases,pneumothorax 32 cases and blood pneumothorax 24 cases),mediastinum damage in 9 cases(vertical mediastinal pneumatosis 6 cases,hematocele 4 cases and traumatic disphragmatic hernia 2 cases),thoracic wall damage in 76 cases(rib bone fracture 59 cases,breast bone fracture 18 cases and costal cartilages damage 5 cases).Clavicle and scapula fracture in 31 cases. ConclusionMultislice CT scanning was principal method for the diagnosis of chest wound,it had the advantages of scanning range,quick scanning and characteristics of high sensitivity,and it would certainly play a vital role in first aid process in emergency medical treatment of wound.

Purpose To detect the expression of CD90 in invasive ductal breast carcinoma with different molecular subtypes and to explore its clinical significance.Methods The expression of CD90,ER,PR,Ki-67 and HER-2 were detected in 80 cases of invasive ductal breast carcinoma tissue and 20 cases of breast benign lesion with immunohistochemical method.The relationship between CD90 and clinicopathological parameters were analyzed.Results The positive expression rate of CD90 in invasive ductal breast carcinoma and breast benign lesion tissues were 62.5％ and 20.0％,respectively (P ＜0.001).The expression of CD90 in invasive ductal breast carcinoma was correlated with lymph node metastasis (P ＜ 0.05),but not with age,tumor size,TNM staging and histological grade (P ＞ 0.05).Among different molecular subtypes,CD90 expression level in Luminal A type was the lowest (40.0％),and the level in triple negative type was the highest (82.4％) (P ＜0.05).CD90 expression level was negatively correlated with ER (r=-0.342,P＜0.05) orPR (r=-0.374,P＜0.05) expression level,but not with Ki-67 (r =0.084,P ＞ 0.05).Condusion The over-expression of CD90 is related with molecular subtypes of breast carcinoma,and its high expression suggests a poor prognosis.

Objective: To observe the clinical efficacy of sinew-bone balancing manipulation in treating lumbar disc herniation (LDH) and offer clinical evidence to support the concept of paying equal attention to sinew and bone. Methods: Sixty LDH patients were randomized into an observation group and a control group, with 30 cases in each group. The observation group was treated with the sinew-bone balancing manipulation, and the control group received conventional Tuina (Chinese therapeutic massage) manipulation. The clinical efficacy and posterior muscle chain tone effect were compared between the two groups by observing the visual analog scale (VAS) score, Japanese Orthopaedic Association (JOA) score, and posture-associated indicators. Results: The total effective rate was 86.7％ in the observation group, higher than 76.7％ in the control group, but the between-group difference in efficacy was statistically insignificant (P>0.05). After treatment, the VAS and JOA scores, angle-dependent muscle tone indicator of the posterior muscle chain, and lumbar posture symmetry showed significant changes in both groups (P<0.05). The VAS and JOA scores, angle-dependent muscle tone indicator of the posterior muscle chain, and lumbar posture symmetry in the observation group were significantly different from those in the control group after treatment (P<0.05), but the between-group difference in the general posture symmetry was statistically insignificant (P>0.05). Conclusion: Both the sinew-bone balancing and conventional Tuina manipulations can reduce pain in LDH patients, improve lumbar function, and adjust the angle-dependent muscle tone coefficient of the posterior muscle chain and lumbar posture symmetry; except for the general posture symmetry of the posterior muscle chain, the sinew-bone balancing manipulation wins out over the conventional Tuina manipulation.

Anesthesia, General ; Animals ; Central Venous Pressure ; physiology ; Heart Function Tests ; Hemodynamics ; physiology ; Respiration, Artificial ; Shock, Septic ; pathology ; Swine ; physiology ; Venae Cavae ; physiology

OBJECTIVETo explore the potential biochemical mechanisms of neuromuscular junction transmission (NMJT) dysfunction induced by organophosphorus insecticides.

METHODSTen rats were dosed with phoxim (1,144 mg/kg) and 5 of them developed myasthenia. The NMJT function was evaluated by the mean consecutive differences (MCD) measured by stimulation single fiber electromyography (SSFEMG) with the frequency of stimuli at 20 Hz. The activity of Ca(2+)-ATPase, Na(+), K(+)-ATPase, cAMP dependent protein kinase (PKA), Ca(2+)/phospholipid dependent protein kinase (PKC), and tyrosine protein kinase (TPK) were determined.

RESULTSIn comparison with the control and non-myasthenic rats, the results in myasthenic rats showed that: (1) the MCDs increased; (2) the activities of Ca(2+)-ATPase, Na(+), K(+)-ATPase and PKA decreased and were negatively correlated with MCD; (3) the activities of PKC and TPK increased, and were positively correlated with MCD; (4) the phosphorylation of serine residuals in sarcolemma was weaker and the phosphorylation of tyrosine residuals was stronger.

CONCLUSIONSThe NMJT dysfunction is likely associated with the decrease in Ca(2+)-ATPase and Na(+), K(+)-ATPase activity. The acceleration of desensitization and prolongation of resensitization of nicotinic acetylcholine receptors occur following the increase in tyrosine phosphorylation and the decrease in serine phosphorylation induced by OPs poisoning.

Animals ; Calcium-Transporting ATPases ; metabolism ; Cyclic AMP-Dependent Protein Kinases ; Electromyography ; drug effects ; Insecticides ; pharmacokinetics ; toxicity ; Myasthenia Gravis ; chemically induced ; enzymology ; Organothiophosphorus Compounds ; pharmacokinetics ; toxicity ; Protein Kinase C ; metabolism ; Protein-Serine-Threonine Kinases ; metabolism ; Rats