Catalytic activity of activated carbon supported tungstosilicic acidin synthesizing 2-methyl-2-ethoxycarbonylmethyl1,3-dioxolane, 2,4-dimethyl-2-ethoxycarbonylmethyl-l,3-dioxolane, cyclohexanone ethylene ketal, cyclohexanone 1,2-propanediol ketal, butanone ethylene ketal, butanone 1,2-propanediol ketal, 2-phenyl-1,3-dioxolane, 4-methyl-2-phenyl-1,3-dioxolane,2-propyl-1,3-dioxolane, 4-methyl-2-propyl-1,3-dioxolane was reported. It has been demonstrated that activated carbon supported tungstosilicic acid is an excellent catalyst. Various factors involved in these reactions were investigated. The optimum conditions found were: molar ratio of aldehyde/ketone to glycol is 1/1.5, mass ratio of the catalyst used to the reactants is 1.0%, and reaction time is 1.0 h. Under these conditions, the yield of 2-methyl-2-ethoxycarbonylmethyl-l,3-dioxolane is 61.5%, of 2,4-dimethyl2-ethoxycarbonylmethyl-1,3-dioxolane is 69.1%, of cyclohexanone ethylene ketal is 74.6%, of cyclohexanone 1,2-propanediol ketal is 80.1%, of butanone ethylene ketal is 69.5%, of butanone 1,2-propanediol ketal is 78.5%, of 2-phenyl-1,3-dioxolane is 56.7%, of 4-methyl-2-phenyl- 1,3-dioxolane is 86.2%, of 2-propyl-1,3-dioxolane is 87.5%, of 4-methyl-2-propyl-1,3-dioxolane is 87.9%.

OBJECTIVETo investigate the absorption mechanism of genistein self-microemulsifying system in rat intestines.

METHODThe concentrations of phenol red and genistein by in situ perfusion in rats were determined by UV and HPLC, respectively. The effects of drug concentrations, pH, various intestinal segments and P-glycoprotein (P-gp) inhibitor verapamil on the absorption had been studied.

RESULTThe absorption rate constant (Ka) of genistein had no significant difference at concentrations of 0.05-0.5 mg x mL(-1) and pH of 5.4-7.8 in perfusion. It was Ka of jejunum > ileum > duodenum > colon. The absorption of genistein in jejunum had significant difference (P < 0.05) compared with other parts of intestines. Ka was increased obviously when verapamil was coper-fused with genistein (P < 0. 05).

CONCLUSIONThe absorption of genistein self-microemulsifying system is a first order process with passive diffusion mechanism related to P-gp efflux. It can be absorbed at all segments of rat intestine, and the jejunum is the best absorption segment, pH had no special effect on the absorption of genistein self-microemulsifying system in rat intestine.

ATP Binding Cassette Transporter, Sub-Family B ; antagonists & inhibitors ; Animals ; Chromatography, High Pressure Liquid ; Emulsions ; Genistein ; analysis ; metabolism ; pharmacokinetics ; Hydrogen-Ion Concentration ; Intestinal Absorption ; drug effects ; Intestines ; drug effects ; metabolism ; Male ; Organ Specificity ; Rats ; Rats, Wistar ; Temperature ; Verapamil ; pharmacology

Objective To investigate the curative effect of brucellar spondylitis,so as to provide scientific proof for improving the curative level of the disease.Methods Epidemiological information was collected from 113 patients diagnosed as brucellar spondylitis,who were divided into 5 groups according to different drugs and drug combinations of doxycycline,gentamicin,sulfamethoxazole and rifampicin.Then the curative effect was investigated.Twenty-one patients who had greater paoas muscle abscess or Para vertebral abscess,intraspinal abscess of spinal canal,necrotic intervertebral disk and major osteolasia received the minimal invasive surgery and the focus removal surgery.Results The occurrence of the disease in female was much higher than that in male.Grazing and breeding beasts was the principal route of infection.Lumbars was mostly involved.they usually was infected in the adjacent 2 piece.L4 was the most common and seriuous one.The curative effect of doxycycline group was better than that without doxycycline(72.60% vs 35.00%,X2=15.14,P＜0.05).Doxycyeline+gentamicin+sulfamethoxazole was reeommended as the first choice.However,the curative effect did not increase despi~course of the treatment prolonged.The heMing rate and effective rate after 1 course was 52.21%(59/113)and 92.04%(104/113).that after 2 courses 58.41%(66/113)and 95.58%(108/113),that after 3 courses 59.29%(67/113)and 95.58%(108/113).The healing rate in different course did not present differences(P＞0.05).21 patients undergoing surgery were followed-up,12 patients were after 2 years and 9 patients were between 1-2 years.The healing rate was 95.24%(20/21),1 case was healed basically,the effective rate was 100%.None reoccurred.Conclusions There are characterized features in clinical epidemiology of the brucell spondylitis.Long term,adequate in dosage,combination and multi-approach use of antibiotics is the most reliable way to treat and prevent it from recurring.But fof the patients soitable for surgery.the minimal invasive surgery or the focus removal could shorten the course of therapy,decrease the complications and increase the cure rate.

0.05);2)After 12,24,36 months' treatment,BP was decreased significantly in each group (P0.05).Conclusion Both combined spirono- lactone/HCTZ and captopril/HCTZ significantly reduced BP and LVMI or LVMI and the maguitude of reduction was further enhanced after prolonged treatment.

Zuotai (gTso thal) is a typical representative of Tibetan medicines containing heavy metals, but there is still lack of modem safety evaluation data so far. In this study, acute toxicity test, sub-acute toxicity test, one-time administration mercury distribution experiment, long-term mercury accumulative toxicity experiment and preliminary study on clinical safety of Compound Dangzuo were conducted in the hope of obtain the medicinal safety data of Zuotai. In the acute toxicity test, half of KM mice given the lethal dose of Zuotai were not died or poisoned, and LD50 was not found. The maximum tolerated dose of Zuotai was 80 g x kg(-1). In the subacute toxicity test, Zuotai could reduce ALT, AST, Crea levels in serums under low dose (13.34 mg x kg(-1) x d(-1)) and medium dose (53.36 mg x kg(-1) x d(-1)), with significant difference under low dose, and increase the levels of ALT, AST, MDA, Crea in serums under high dose (2 000 mg x kg(-1) x d(-1)); besides, the levels of BUN and GSH in serums reduced with the increase in dose of Zuotai, indicating a significant dose-effect relationship. In the one-time administration distribution experiment, the content of mercury in rat kidney, liver and lung increased after the one-time administration with Zuotai, with a significant dose-dependent relationship in kidney. In the long-term mercury accumulative toxicity experiment, KM mice were administered with equivalent doses of Zuotai for 4.5 months and then stopped drug administration for 1.5 months. Since the 2.5th month, they showed significant mercury accumulation in kidney, which gradually reduced after drug withdrawal, without significant change in mercury content in liver, spleen and brain and ALT, AST, TBIL, BUN and Crea in serum. At the 4.5th month after drug administration, KM mice showed slight structural changes in kidney, liver and spleen tissues, and gradually recovered to normal after drug withdrawal. Besides, no significant difference in weight gain was found between the Zuotai group and the control group. According to the findings of the clinical safety study of Dangzuo, after subjects administered Dangzuo under clinical dose for one month, their serum biochemical indicators, blood routine indicators and urine routine indicators showed no significant adverse change. This study proved that traditional Tibetan medicine Zuotai was slightly toxic, with a better safety in clinical combined administration and no adverse effects on bodies under the clinical dose and clinical medication cycle. However, long-term high-dose administration of Zuotai may have a certain effect on kidney.
Adult ; Animals ; Clinical Trials as Topic ; Drugs, Chinese Herbal ; analysis ; pharmacokinetics ; toxicity ; Female ; Humans ; Kidney ; drug effects ; Liver ; drug effects ; Male ; Medicine, Tibetan Traditional ; Mice ; Middle Aged ; Rats ; Rats, Wistar ; Young Adult

Animals ; Cell Proliferation ; drug effects ; Diabetic Nephropathies ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; Male ; Mesangial Cells ; cytology ; drug effects ; metabolism ; RNA, Messenger ; analysis ; Rats ; Rats, Sprague-Dawley ; Transforming Growth Factor beta ; genetics

Catalytic activity of activated carbon supported tungstosilicic acid in synthesizing 2-methyl-2-ethoxycarbonylmethyl- 1,3-dioxolane, 2,4-dimethyl-2-ethoxycarbonylmethyl-1,3-dioxolane, cyclohexanone ethylene ketal, cyclohexanone 1,2-propa- nediol ketal, butanone ethylene ketal, butanone 1,2-propanediol ketal, 2-phenyl-1,3-dioxolane, 4-methyl-2-phenyl-1,3-dioxolane, 2-propyl-1,3-dioxolane, 4-methyl-2-propyl-1,3-dioxolane was reported. It has been demonstrated that activated carbon supported tungstosilicic acid is an excellent catalyst. Various factors involved in these reactions were investigated. The optimum conditions found were: molar ratio of aldehyde/ketone to glycol is 1/1.5, mass ratio of the catalyst used to the reactants is 1.0%, and reaction time is 1.0 h. Under these conditions, the yield of 2-methyl-2-ethoxycarbonylmethyl-1,3-dioxolane is 61.5%, of 2,4-dimethyl- 2-ethoxycarbonylmethyl-1,3-dioxolane is 69.1%, of cyclohexanone ethylene ketal is 74.6%, of cyclohexanone 1,2-propanediol ketal is 80.1%, of butanone ethylene ketal is 69.5%, of butanone 1,2-propanediol ketal is 78.5%, of 2-phenyl-1,3-dioxolane is 56.7%, of 4-methyl-2-phenyl-1,3-dioxolane is 86.2%, of 2-propyl-1,3-dioxolane is 87.5%, of 4-methyl-2-propyl-1,3-dioxolane is 87.9%.

Objective: To analyze the current status of anticoagulant therapy for in-hospital patients with acute coronary syndromes (ACS) at county hospitals of China and to explore the relationship between anticoagulant therapy and clinical outcomes in real medical environment. Methods: 99 county hospitals from15 provinces of China were selected for this prospective registry study and 12373 eligible ACS patients without interventional therapy admitted from 2011-09 to 2014-06 were enrolled. The basic condition, previous history, initial assessment, anticoagulants (unfractionated heparin/low molecular weight heparin) application, severe bleeding events and in-hospital mortality were collected in all patients. Multiple logistic regression analysis was conducted to explore the relationship between anticoagulant therapy and clinical outcomes including in-hospital mortality, severe bleeding events and combined endpoints; meanwhile, possible confounders were adjusted. Results: A total of 9985/12373 ACS patients received anticoagulant therapy and 2388 did not. Anticoagulant therapy was conducted in 92.7% (4237/4570) patients with ST-segment elevation myocardial infarction (STEMI), 90.8% (1639/1805) with non-ST-segment elevation myocardial infarction (NSTEMI) and 68.5% (4109/5998) with unstable angina (UA); there were differences by regions and genders,P<0.01and no difference by age. Multivariable analysis indicated that anticoagulant therapy decreased the risk of in-hospital mortality in ACS patients at 53% (OR= 0.47, 95% CI 0.36-0.62), such reduction in STEMI patients was at 55% (OR=0.45, 95% CI 0.32-0.64), in NSTEMI patients was at 58% (OR=0.42, 95% CI 0.24-0.75); while it had no real effect in UA patients,P>0.05. Meanwhile, it did not increase the risk of severe bleeding events in ACS patients,P>0.05. Conclusion: Anticoagulant therapy has been widely used in STEMI and NSTEMI patients at county hospitals of China and obviously decreased the in-hospital mortality; while the application rate was relatively low in UA patients. The general safety of anticoagulant therapy has been good in ACS patients.

BACKGROUNDThere are few studies for evaluating wall characteristics of intracranial vertebral artery hypoplasia (VAH). The aim of this study was to determine wall characteristics of VAH with three-dimensional volumetric isotropic turbo spin echo acquisition (3D VISTA) images and differentiate between acquired atherosclerotic stenosis and VAH.

METHODSThirty patients with suspicious VAH by luminograms were retrospectively enrolled between January 2014 and February 2015. The patients were classified as "acquired atherosclerotic stenosis" or "VAH" based on 3D VISTA images. The wall characteristics of VAH were assessed to determine the presence of atherosclerotic lesions, and the patients were classified into two subgroups (VAH with atherosclerosis and VAH with normal wall). Wall characteristics of basilar arteries and vertebral arteries were also assessed. The clinical and wall characteristics were compared between the two groups.

RESULTSFive of 30 patients with suspicious VAH were finally diagnosed as acquired atherosclerotic stenosis by 3D VISTA images. 25 patients were finally diagnosed as VAH including 16 (64.00%) patients with atherosclerosis and 9 (36.00%) patients with normal wall. In the 16 patients with atherosclerosis, plaque was found in 9 patients, slight wall thickening in 6 patients, and thrombus and wall thickening in 1 patient. Compared with VAH patients with normal wall, VAH patients with atherosclerosis showed atherosclerotic basilar arteries and dominant vertebral arteries more frequently (P = 0.000).

CONCLUSIONSThree-dimensional VISTA images enable differentiation between the acquired atherosclerotic stenosis and VAH. VAH was also prone to atherosclerotic processes.

Aged ; Female ; Humans ; Imaging, Three-Dimensional ; methods ; Magnetic Resonance Imaging ; methods ; Male ; Middle Aged ; Plaque, Atherosclerotic ; pathology ; Retrospective Studies ; Vertebral Artery ; abnormalities ; pathology

OBJECTIVETo investigate the changing regular of specific cytokeratin (CK) markers expressing in human pseudoepitheliomatous hyperplasia (PEH), keloids (Ke) and hypertrophic scar (HS) lesion, and to explore the correlation between such changes and the different outcomes of wound repair.

METHODSHistopathology and immunohistochemistry (IHC) double staining methods were used in samples of human PEH, Ke, HS and NS to determine the distribution characteristics and changing regularity of CKs in epidermal tissues.

RESULTSNo CK8&18 and CK17 expressed in epidermis of NS group, while CK8&18(+) cells and CK17(+) cells were detected in epidermis of active-stage Ke, HS and PEH. The quantities of CK8&18(+) cells and CK17(+) cells ranked as follows: PEH > Ke > HS and HS > Ke > PEH (P < 0.05). CK19(+) cells and CK5&6(+) cells expressed similar changing trend, while reverse trend of CK10(+) cells was detected in epidermal cells, with local epidermal hyperplasia, cells morphological changes and sub-epidermal inflammatory reaction.

CONCLUSIONDifferent degree of de-differentiation and terminal differentiation imbalance are found in epidermal cells of active-stage PEH, Ke and HS, which hint the correlation between the abnormal proliferation and differentiation of epidermal cells and the different outcomes of wound repair.

Adolescent ; Adult ; Aged ; Cell Differentiation ; Cell Proliferation ; Child ; Child, Preschool ; Cicatrix ; metabolism ; pathology ; Epidermis ; metabolism ; pathology ; Epithelial Cells ; metabolism ; pathology ; Female ; Humans ; Hyperplasia ; metabolism ; pathology ; Infant ; Keratins ; metabolism ; Male ; Middle Aged ; Wound Healing ; Young Adult