OBJECTIVETo prepare the quercetin self-emulsified formulation and evaluate its quality.

METHODThe quercetin self-emulsified formulation was optimized based on the quercetin solubility in different oils, and the self-microemulsified efficiency of various combinations of emulsifier and co-emulsifier evaluated using the pseudo-ternary phase diagram. The microemulsion of morphology, size and zeta potential were examined. The quercetin of solubility in self-emulsified system was tested and the formulation stability was investigated by accelerated experiment.

RESULTThe blank self-emulsified system was composed of ethyl oleate/Cremophor EUL/butanol with weight ratio of 10: 54: 36. After being dilutied with water, the morphology of microemulsion was homogeneous small spherical drops observed under the electro-microscopy. The particle size and the zeta potential were 16.3 +/- 4.6 nm and 2.1 +/- 0.8 mV, respectively. The solubility of quercetin in self-emulsifing system was (62.42 +/- 0.11) mg x mL(-1), increased 2 229 folds compared with that of in water. The quality of quercetin self-emulsified formulation was stable during the 3 months storage at 40 degrees C.

CONCLUSIONThe solubility of quercetin is significantly increased in self-emulsified system and the formulation is stable and easy to prepare.

Antioxidants ; administration & dosage ; chemistry ; Butanols ; chemistry ; Chromatography, High Pressure Liquid ; Drug Delivery Systems ; Drug Stability ; Emulsions ; Glycerol ; analogs & derivatives ; chemistry ; Oleic Acids ; chemistry ; Particle Size ; Quercetin ; administration & dosage ; chemistry ; Solubility ; Solvents ; Technology, Pharmaceutical ; methods

AIMTo observe possible mechanism that endurance training can enhance anti-fatigue capability, and that blood redistribution by analyzing some biochemical indexes of endurance-trained mice after exhaustive exercise.

METHODSThe model was set up by exhaustive exercise. The indexes include the activity of SOD, CAT and POD and the MDA content in serum and the NO content in liver, muscle, heart and serum.

RESULTSAfter exhaustive exercise, the SOD activity in serum and the NO content in liver significantly decrease (P < 0.05 - 0.01), and the activity of POD and CAT, the NO content in serum and muscle significantly increase (P < 0.05 - 0.01), but the rest insignificantly change in non-endurance (P > 0.05). In endurance group, the CAT activity in serum are significantly higher than in non-endurance (P < 0.05), and the NO content in serum is significantly lower than in non-endurance (P < 0.01), but the rest are insignificantly different between two groups (P > 0.05). After 24h restoration, in non-endurance group, the CAT activity and the MDA content in serum and the NO content in liver significantly rise (P < 0.05-0.01), and the NO content in muscle and serum significantly decrease (P < 0.05), but the rest insignificantly change (P > 0.05). In endurance group, the SOD activity in serum and the NO content in liver, serum and heart significantly rise (P < 0.05), and the CAT activity in serum significantly decreases (P < 0.05), but the rest insignificantly change (P > 0.05). In endurance group, the CAT activity and the MDA content in serum are significantly lower than in non-endurance (P < 0.05), but the NO content in heart is higher than in non-endurance (P < 0.05). The rest are insignificantly different between two groups (P > 0.05).

CONCLUSIONThe possible mechanism, which endurance training can enhance anti-fatigue capability, is relative to enhance the capability to resume balance. Blood redistribution are possibly relative to change to the NO content.

Animals ; Catalase ; blood ; Liver ; chemistry ; Male ; Malondialdehyde ; blood ; Mice ; Muscles ; chemistry ; Nitric Oxide ; analysis ; blood ; Peroxidase ; blood ; Physical Conditioning, Animal ; physiology ; Physical Endurance ; physiology ; Superoxide Dismutase ; blood

OBJECTIVETo understand the influence of different sleep stages on respiratory regulation in normal people.

METHODSWe measured ventilation (VE) and occlusion pressure (P0.1) responses to hyperoxia hypercapnia (deltaVE/deltaPaCO2, deltaP0.1/deltaPaCO2) and isocapnic hypoxia (deltaVE/deltaSaO2 and deltaP0.1/deltaSaO2) in eleven non-snoring healthy people during wakefulness and during non-rapid eye movement (NREM) I + II, NREM III+IV, and rapid eye movement (REM) sleep stages.

RESULTSDuring NREM I + II and NREM III+IV, the normal subjects showed no significant decrease in P0.1, deltaP0.1/deltaSaO2 and deltaP0.1/deltaPaCO2 (P > 0.05), but deltaVE/ deltaSaO2 and deltaVE/ deltaPaCO2 decreased significantly (P < 0.05). During REM sleep, P0.1 maintained the level during wakefulness, but both hypoxic and hypercapnic responses decreased significantly (P < 0.05).

CONCLUSIONSSleep has significant influence on respiratory regulation in normal people. The respiratory drive (P0.1) in both NREM and REM sleep stages could maintain the awake level due to an effective compensation to the increase of upper airway resistance. The P0.1 responses to both hypoxia and hypercapnia decrease only in REM sleep stage, which is in consistent with the clinical phenomenon that sleep disordered breathing occurs in REM in normal people.

Adult ; Female ; Humans ; Hypercapnia ; physiopathology ; Hypoxia ; physiopathology ; Male ; Respiration ; Respiratory Physiological Phenomena ; Sleep Stages ; physiology ; Sleep, REM ; physiology ; Wakefulness ; physiology

OBJECTIVETo prepare the alpha-asarone reservoir patch and investigate its release and transdermal absorption characteristics in vitro. The efficient enhancers were chosen to improve the drug's permeation rate.

METHODThe alpha-asarone reservoir patch was prepared using 1% hydroxypropyl methylcellulose (HPMC) of ethanol solution as medium and ethylene vinyl acetate (EVA) membrane to control the release of drug. The Franz diffusion cells were used and several permeation enhancers were evaluated. High performance liquid chromatorgraphy (HPLC) was used to determine alpha-asarone's content and permeation rate.

RESULTThe release mechanisms of alpha K-asarone patch in vitro coincided with zero-order kinetic. 30% ethanol cooperates with 1% Isopropyl Myristate (IPM) have the best effect on permeation of the patch. The permeation rate reaches (20.67 +/- 1.33) microg x cm(-2) h(-1).

CONCLUSIONEthanol combined with IPM is good permeation enhancer, which facilitated the permeation of alpha K-asarone to fit the clinical requirements. However, the further studies of the skin's stimulation and bioavailability are needed.

Acorus ; chemistry ; Administration, Cutaneous ; Anisoles ; administration & dosage ; isolation & purification ; pharmacokinetics ; Delayed-Action Preparations ; administration & dosage ; pharmacokinetics ; Ethanol ; pharmacology ; Humans ; Hypromellose Derivatives ; In Vitro Techniques ; Methylcellulose ; analogs & derivatives ; chemistry ; Myristates ; pharmacology ; Plants, Medicinal ; chemistry ; Polyvinyls ; chemistry ; Skin ; drug effects ; metabolism ; Skin Absorption ; drug effects

BACKGROUNDRegulatory T cells (Tregs) may play an important role in immunopathology during HIV-1 infection. Transcription factor forkhead box P3 (FoxP3) orchestrates the development of Tregs and is a useful marker to identify this population. Using a FoxP3 phenotype to define Tregs, we investigated the level and phenotype of peripheral blood natural CD4(+)Tregs and assessed the relationship between the frequencies and absolute numbers of CD4(+) Tregs and disease progression among untreated HIV-infected men who have sex with men (HIV(+) MSM) in China.

METHODSFifty-two untreated HIV(+) MSM with CD4(+) T-cell counts of ≤ 350 cells/µl or > 350 cells/µl were compared in a cross-sectional study. Twelve age-matched HIV-uninfected MSM and nine patients receiving antiretroviral therapy for at least 1 year were also included. Expression of CD25, CD127, CD45RA, CCR7 and CTLA-4 was assessed on CD4(+) Tregs using polychromatic flow cytometry.

RESULTSThe percentage of CD4(+) Tregs was increased significantly, whereas CD4(+) Tregs expressed less CTLA-4 in HIV(+) MSM compared with controls. CD4(+) Tregs displayed predominantly an effector memory phenotype (CD45RA(-) CCR7(-)), phenotypically distinct from conventional CD4(+) T cells. Moreover, the expansive frequencies of CD4(+) Tregs coincided with lower CD4(+) T-cell counts and higher viral loads whereas the absolute numbers of CD4(+) Tregs were associated with higher CD4(+) T-cell counts and lower viral loads. The expansion of Tregs was also associated with CD8(+) T-cell activation.

CONCLUSIONIncreased proportions and decreased numbers of CD4(+) Tregs are associated with HIV progression, and their functions may impair with the progression of HIV infection.

Acquired Immunodeficiency Syndrome ; immunology ; Adult ; CD4 Lymphocyte Count ; CTLA-4 Antigen ; analysis ; Cross-Sectional Studies ; Disease Progression ; HIV-1 ; Homosexuality, Male ; Humans ; Immunologic Memory ; Lymphocyte Activation ; Male ; Middle Aged ; RNA, Viral ; blood ; T-Lymphocytes, Regulatory ; immunology

To explore a new lyophilized preservation methods for human platelets, platelets were pre-treated with aldehyde, human albumin or trehalose was added to the system of condensed cooling as protectant to stabilize the structure of platelets. The optimal resuspending buffer was also selected in the study. The morphological changes of platelets were observed by using electron microscopy after lyophilization, and the expression of membrane proteins on platelets was detected also after lyophilization. The results indicated that the recovery rate of platelets treated with aldehyde was generally more than 60%. Aggregative ability was reduced a little than the platelet untreated. 5% of human albumin had an advantage over 40 mmol/L of trehalose in respect of the preservation effect. In the way of keeping aggregative ability, PPP was obviously better than PBS. The results of electron microscopy displayed that organelles including mitochondria and excreted granules could be observed distinctly. Whereas, expression of membrane proteins of platelet treated with aldehyde was evidently dropped as compared with those of the fresh platelet. In conclusion, aldehyde as a novel protective agent, has excellent effects on lyophilization of platelets and is worthy to be further studied.
Albumins ; pharmacology ; Aldehydes ; pharmacology ; Blood Platelets ; cytology ; drug effects ; Blood Preservation ; methods ; Freeze Drying ; Humans ; Reproducibility of Results ; Trehalose ; pharmacology

ObjectiveTo construct geographic information database of drinking water type of endemic arsenism at village level with Google Earth and provide scientific basis for prevention and management of endemic arsenism.MethodsDrinking water samples were collected in the field of Shilegetu village,Tuoketuo county,Inner Mongolia in 2008.Arsenic concentrations were determined by high-performance liquid chromatography-hydride generation-atomic fluorescence spectrometry.Global positioning system(GPS) was performed to obtain the geographic information of the water sources.Google Earth was applied to establish the geographic information database.Results There were 5 drinking water resources in this village.They were located between 40°29′09″ N and 40°29′36″ Nlatitude and 111°28′00″ E and 111°29′02″ E longitude,with the altitude between 1010 m and 1021 m.For all drinking water resources,four water arsenic concentrations was beyond 0.05 mg/L and one below 0.05 mg/L.In addition,one water source had been abandoned and the remaining four were providing daily drinking water for residents of the villages.ConclusionsThe geographic information database,established by Google Earth,can intuitively reflect the real situation of the endemic village.It can provide more useful information for field epidemiological research.It is an effectively tool in control and management of endemic arsenism.

The present study is aimed to study the effect of sarcoplasmic reticulum Ca(2+)-ATPase 2a (SERCA2a) gene transfer on the contractile function of isolated cardiomyocytes of canines. The cardiomyocytes were isolated with collagenases. The isolated cardiac cells were divided into untransfected group, empty vector group and SERCA2a-transfected group. Recombinant adenovirus vector carrying enhanced green fluorescent protein gene was used for SERCA2a gene delivery. The expression of SERCA2a protein in cardiomyocytes was determined by Western blot. Contractile function of cardiomyocytes was measured with motion edge-detection system of single cell at 48 h after transfection. The results showed, compared with untransfected group, SERCA2a protein level, percentage of peak contraction amplitude under normal condition, percentages of peak contraction amplitude under Ca(2+) or isoproterenol stimulation, time-to-peak contraction (TTP) and time-to-50% relaxation (R50) in SERCA2a-transfected group all increased significantly. While all the above indices in empty vector group did not show any differences with those in untransfected group. These results suggest that the overexpression of SERCA2a by gene transfer may enhance the contraction function of canine myocardial cells.
Adenoviridae ; genetics ; metabolism ; Animals ; Dogs ; Male ; Myocardial Contraction ; drug effects ; physiology ; Myocytes, Cardiac ; metabolism ; Recombinant Proteins ; genetics ; metabolism ; Sarcoplasmic Reticulum Calcium-Transporting ATPases ; genetics ; metabolism ; Transfection

AIMTo investigate the relations between left ventricular hypertrophy and systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP), neuropeptide Y (NPY) during cardiac hypertrophy and regression.

METHODSBlood pressure and heart rate were recorded with polygraph channel biologic message system. NPY in plasma and myocardium were measured with Radioimmunoassay. Correlation coefficient were calculated with SPSS software.

RESULTSThere were positive correlations between SBP, DBP, MAP, NPY in the cardiac tissue and cardiac coefficient (LVW/BW). There was no correlations between cardiac coefficient and heart rate (HR), NPY in plasma.

CONCLUSIONHypertension is one of cardiac hypertrophy factors, SBP correlate better with LVW/ BW than DBP. SBP, DBP, MAP, NPY in cardiac tissue has correlative tendency with LVW/BW.

Animals ; Blood Pressure ; Heart Rate ; Hypertension ; metabolism ; physiopathology ; Hypertrophy, Left Ventricular ; metabolism ; physiopathology ; Male ; Neuropeptide Y ; metabolism ; Rats ; Rats, Wistar

OBJECTIVETo assess the clinical value of three-dimensional contrast-enhanced magnetic resonance angiography (3D-CE-MRA) in the diagnosis of mesenteric arteriosclerosis.

METHODS3D-CE-MRA of the mesenteric arteries was performed in 21 patients with 23 healthy subjects as the control. After 3D image reconstruction and maxi intense projection, and the abnormalities of the mesenteric arteries were observed and analyzed. The diameter and number of the arterial branches were compared between the patients and the control subjects.

RESULTSAll the 21 patients suffered arteriosclerosis in the arteries other than the mesenteric arteries. On 3D-CE-MRA, mesenteric arteriosclerosis was characterized by thinning of the arterial trunk, luminal stenosis, irregular arterial margins and homo- or heterogeneous thickening of vascular walls. Multiple filling defects were found in the mesenteric artery lumens with reduced second order branches, which showed rigid lining with dashed line appearance or disappeared in some cases. The inferior mesenteric arteries were seen in only 2 patients. The diameters of superior and inferior mesenteric arteries were 3.8-/+0.32 mm and 1.20-/+0.12 mm in the patients, significantly smaller than those of in the control subjects (6.51-/+1.01 mm and 2.90-/+0.90 mm, respectively, P<0.01). The number of the mesenteric artery branch of the patients was also significantly reduced as compared with that in the control subjects (P<0.05). In som cases, the intestinal enhancement was attenuated with the intestinal contraction, dilatation and lowering of the intestinal tension.

CONCLUSION3D-CE-MRA can clearly display mesenteric arteriosclerosis and secondary intestinal changes, and provides a useful means for the diagnosis and assisting the therapy of mesenteric arteriosclerosis.

Aged ; Aged, 80 and over ; Arteriosclerosis ; diagnosis ; pathology ; Case-Control Studies ; Contrast Media ; Female ; Humans ; Image Enhancement ; Imaging, Three-Dimensional ; Magnetic Resonance Angiography ; methods ; Male ; Mesenteric Arteries ; pathology ; Middle Aged