The study is to establish an HPLC method using fluorescence detector for the determination of doxazosin enantiomers and investigate their chiral inversion in vitro and in vivo. Ultron ES-OVM was taken as the chiral chromatographic column, and the column temperature was 30 degrees C. Isocratic elution using a mobile phase of phosphate buffer-acetonitrile (85 : 15, v/v) at a flow rate of 0.8 mL x min(-1) was done. The fluorescence detection was set at lambda(Ex) = 255 nm and lambda(Em) = 385 nm. Prazosin was used as the internal standard. (-) Doxazosin or (+) doxazosin added into rat plasma in vitro was determined after incubating in 37 degrees C water bath for 2, 5 and 10 days. (-) Doxazosin or (+) doxazosin was administered orally to the rats for one months. Plasma samples were taken at 8 h after the last administration. A good linear relationship was achieved when the concentration of doxazosin enantiomers was within the range of 4 - 2 000 ng x mL(-1). The average recovery for (-) doxazosin was 99.5% with RSD 3.6%, and for (+) doxazosin was 99.3% with RSD 4.3%. Chiral inversion was observed neither in vitro nor in vivo studies. The method is selective, accurate and reproducible, which is suitable for the detection of doxazosin enantiomers in rat plasma. The in vitro and in vivo studies indicate that chiral inversion occurs uneasily between (-) doxazosin and (+) doxazosin in the rat.

Flavonoids baicalin is the main bioactive component extracted from Scutellaria baicalensis Georgi. Baicalin has high medicinal value and shows extensive pharmacological effects including antitumor, antibiosis, anti-inflammatory, antioxidation, neuro-protection, and significant potential in tumor treatment. Recent studies have shown that baicalin suppresses the growth of many kinds of human cancer. The underlying mechanisms include induction of apoptosis, induction of cell cycle arrest, inhibition of tumor metastasis, suppression of angiogenesis, and so on. This article reviewed the research progress of baicalin on its antitumor pharmacology and possible mechanisms at home and abroad, and provided the basis for its further research.

Objective To investigate the therapeutic effect of the Hubei Wingnut ( Malus hapehensis ) leaf decoction (MHD) against conjunctivitis infected with human simplex virus type I (HSV-1). Methods Malus hupehcnsis decoction was used as the active treatment and ribavirin ( RBV) eye drop was used as the positive control. Both of the Vero cells and rabbit eye conjunctiva were infected with HSV-1. The effect and mechanism of the MHD on viral replication was determined by observing the cytopathic effect ( CPE) . The efficacy of MHD at different doses on the rabbit viral conjunctivitis was examined by pathological changes of eye conjunctiva tissues. Results MHD did not inhibit the proliferation of HSV-1 in vitro. The inflammatory reactions of rabbit viral conjunctivitis caused by HSV-1 were obviously attenuated or disappeared after treatment with MHD at 6 kg·L-1 and 3 kg·L-1 for 7 consecutive days,compared with the negative control of 0. 9% NaCl. The curative rate of MHD at the middle and high doses was 83. 3% and 100. 0%, respectively. Conclusion MHD has the potential for treating eye conjunctivitis caused by HSV-1 by relieving inflammation.

This article dealed with the effects of processing method and duration on the major bioactive components (sinigrin and sinapine thiocyanate) in Brassica juncea. The contents of sinigrin and sinapine thiocyanate in decoctions of raw and processed B. juncea were determined and compared by high performance liquid chromatography on a Alltima C18 column (4.6 mm x 250 mm, 5 microm) at 35 degrees C with the acetonitrile-0.1% phosphoric acid as the mobile phrase in gradient elution. The detection wavelength of sinigrin and sinapine thiocyanate was set at 227 nm and 326 nm, and the flow rate was 1.0 mL x min(-1). It was found that with the extended processing duration, the contents of sinigrin and sinapine thiocyanate first increased and then decreased: i.e., 0-2 minutes they increased gradually (for sinigrin, by 9.65% in processed products and 356. 10% in powder; for sinapine thiocyanate, by 12.82% in processed products and 3.41% in powder), and achieved their highest content at 2 min; then, decreased during the next 5 minutes (for sinigrin, by 80.35% in processed products and 82.09% in powder; for sinapine thiocyanate, by 14.29% in processed products and 17.54% in powder), suggesting that processing duration could significantly affect the contents of bioactive components in B. juncea, enzymatic hydrolysis of sinigrin when the seed is crushed in the present of moisture may be responsible for the content change. It is recommended that the slow fire should be the best processing method and the raw seed could be used directly in the water extracts related industrial production.
Brassica ; chemistry ; Choline ; analogs & derivatives ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Glucosinolates ; chemistry ; Powders ; chemistry ; Thiocyanates ; chemistry

? AIM: To investigate health - related quality of life ( HRQOL ) state in children with intermittent exotropia using the Intermittent Exotropia Questionnaire ( IXTQ ) and research the effect of strabismus surgeries on HRQOL.?METHODS: In this prospective study, we chose 42 patients with intermittent exotropia ( aged 5-17 years) as case group, and 42 patients ( aged 5-17 years) as control group. The Chinese IXTQ was used to evaluate HRQOL at 1d preoperatively and 3mo postoperatively in the two groups, and the differences of the two groups before and after surgery and the effect of strabismus surgery on HRQOL were analyzed.?RESULTS:The scores of HRQOL in control group were statistically significant higher than that of case group ( P<0. 01 ). Every items showed a statistically significant difference except on “Kids tease me because of my eyes”and “ My eyes make it hard for me to make friends” ( P<0.05). At 3mo postoperatively ,the scores of HRQOL in case group significantly increased than that at 1d preoperatively(P<0. 01). Child IXTQ of case group was lower on every items than those of control group after surgery(P<0. 05).?CONCLUSION:Intermittent exotropia could affect the HRQOL in psychosocial and visual functional. The greatest HRQOL concerns for children with intermittent exotropia were shutting one eye when sunny, waiting for their eyes to clear up instead of taunts and friendship. The surgical treatment could improve HRQOL in children with intermittent exotropia.

Objective To investigate the protective effects of electroacupuncture on the endothelial tissues of microvessels in the basal ganglia in the rats with cerebral ischemia-reperfusion.Methods The MCAO model was established by using Longa's method.The immunohistochemistry SABC(strepto-avidin-biotin-peroxidase complex) method was employed to detect the expression of ICAM-1,P-selectin in the microvessel of rats'ipsilateral basal gan- glia.Results The number of positive ICAM-1 and P-selectin endothelial cells of model group were significantly in- creased,as compared to normal group and sham operated group(P

Early diagnosis and intervention is an important way to delay the progress of Alzheimer′s disease (AD).Compared with cerebrospinal fluid, blood sampling is not invasive and easy to be obtained in clinic practice.In this study, the serum samples of 9 controls, 10 AD and 12 mild cognitive dysfunction (MCI) patients were analyzed and compared through one by one analysis to screen potential markers for AD diagnosis.The experimental results showed that VGFYESDVMGR of α-2-macroglobulin peptide was closely related to the late stage of AD disease, and the large amount degradation of apolipoprotein C-Ⅲ, histone H1.2 and histone H1.4 was significantly related to early stages of AD progression.The characteristics of serum peptidome were different for the early and late AD, and these four proteins may be used as potential biomarkers of AD disease.In addition, the obvious ladder sequence characteristic was observed for apolipoprotein C-Ⅲ and histone H1, which could partly explain why the peptides distribution in different samples was somewhat contingent.On the contrary, the distribution at protein level was more stable.Finally, it was confirmed that the peptides of proteins such as fibrinogen α-chain, thymosin β-4 and patchy proteins were the dominant peptides in all serum samples.Overall, this study showed that the method of using serum peptidomics to diagnose AD was possible.The results may provide evidence and references for the large-scale clinical validation of AD.

A novel probe (DNSBN) towards biothiols on the basis of 4-hydroxynaphthalimide as fluorophores and 2, 4-dinitrobenzenesulfonyloxy group as specific recognition site was designed and synthesized.The result of absorption and fluorescence spectral analyses indicated that the probe had high sensitivity and selectivity towards cysteine (Cys), homocysteine (Hcy) and glutathione (GSH), and the detection was not affected by other 17 kinds of natural amino acids.Meanwhile, it was confirmed that DNSBN was a ratiometric probe through the fluorescence titration experiment, and the fluorescent intensity at 555 nm had a high linear relationship with biothiols concentration in the range of 0-20 μmol/L.The detection limits (3σ) of Cys, Hcy and GSH were 25.9, 92.0 and 77.9 nmol/L, respectively.The absorption, emission and mass spectra indicated that biothiols could be engaged in nucleophilic substitution reaction with 2,4-dinitrobenzenesulfonate, which induced the sulfonic esters decomposed.With the departure of receptor unit, the d-PeT progress (donor-excited photoinduced electron transfer) was blocked with an obvious colorimetric and fluorescence change.Finally, HeLa cell imaging experiments verified that DNSBN had good biocompatibility and could be used to detect exogenous biothiols.

ObjectiveTo analyze the status of DACH1 gene promoter methylation and explore its association with the expression of DACH1 gene promoter methylation and clinical significance of endometrium carcinoma(EC).Methods From February 2004 to August 2008,a total of 80 EC tissue samples with comprehensive surgical pathology staging were collected and used for this study.Twenty normal endometrium tissues in 2008 were abtained from the fractional curettage because of dysfunctional uterine bleeding as control.All samples were confirmed pathologically.Methylation specific PCR (MSP) was performed to detect the promoter methylation of DACH1 gene,and analyze its influence on the expression of DACH1 and the relationship between DACH1 promoter methylation and clinicopathological factors in EC.DACH1 protein expression was detected by western blot.Chi-square test and Pearson test were used for statistical analysis.ResultsThe rate of promoter methylation of DACH1 gene in the EC tissues was significantly higher than that in the normal endometrium issues (30％ vs.5％,P ＜ 0.05).There was an association between the expression of DACH1 and DACH1 gene promoter methylation ( r =- 0.30,P ＜ 0.01 ).There was statistical difference between the methylation of DACH1 and the pathological grade ( P ＜ 0.05 ) or histological type ( P ＜0.05).But DACH1 gene methylation was not related with the age,stage,myometrial invasion depth and lymphnode metastasis (P ＞ 0.05 ).Conclusions DACH1gene promoter methylaion could lead to a decrease or absence in the DACH1 expression in EC.The promoter methylation of DACH1 gene may induce the inhibition of DACH1 expression,which might be one of the mechanisms of DACH1 gene inactivation in human EC.

ObjectiveTo evaluate the impact of compliance with antihypertensive therapy in pailents with essential hypertension on risk for their first-ever cerebral infarction.MethotisQuestionnaire survey and auxiliary examinations were conducted in 114 patients with essential hypertension hospitalized for acute cerebral infaretion at the First Hospihal Affiliated to Harbin Medical University during December 2006 to December 2007,as well as in another 114 patients with essential hypertensive without history of cerebral infarction as controls during the sanle period.Univariate and multivariate 10gistic regression analyses were performed to study the relationship between first-ever cerebral infarction and compliance with antihypertensive agents and other relevant factors.ResultsAntihypertensive agents compliance,course of hypertension,and history of smoking and alcohol drinking could significantly affect their first occurrence of cerebral infarction in patients with essential hypertension(P＜0.05),with odds ratios(OR)of 0.429(95%C10.186-0.993) and 2.142(95% CI 1.052-4.364)for good and poor compliance with antihypertensive agents,respectively,as compared to those without antihypertensive treatmenL Mild drinking was a protective factor for cerebral infarction with an OR of 0.494(95%CI 0.252-0.968).kngth of hypertension with 10-19-years and more than or equal to 20 years.as compared to those with le88 than five years of hypertension,was also a risk factor for it,with an OR of 2.118(95% CI 1.075-4.174).ConclusionsCompliance of essential hypertensive patients with antihypertensive therapy was an important factor that affect their contracting first-ever cerebral infarction.Good compliance could obviously refrain them from it.Patients with poor-compliance or without treatment prone to contract cerebral infarction more easily than those with good compliance.It is necessary to improve compliance with antihypertensive agents in patients with essential hypertension as soon as possible.as well as quitting smoking and limiting alcohol drinking for prevention and control for their first-ever cerebral infarction.