Objective To compare the value of 99m Tc-DTPA dynamic renal imaging and intravenous pyelography(IVP) in assessing renal function. Methods The results of 99m Tc-DTPA dynamic renal imaging and IVP in 117 patients with renal diseases confirmed by clinical examinations, abdominal ultrasonography, CT and blood biochemical markers were analysed retrospectively. Results Out of 234 kidneys,101 were clearly visualized by IVP, which were indicated normal renal uptake by 99m Tc-DTPA dynamic renal imaging, and the GFR value was (60.13?16.85)ml/min. 48 kidneys were poorly visualized by IVP, their uptake detected by dynamic renal imaging was between grade 1 to 3, and the GFR value was (23.06?10.61)ml/min. 85 kidneys were not visualized by IVP, 71.8% of which(61/85kidneys) were indicated uptake of radionuclide by dynamic renal imaging with the (20.39?12.54)ml/min GFR value, and uptake of 8 kidneys among the 61 kidneys was normal. The functional kidneys detected by dynamic renal imaging were more than those detected by IVP(P

Objective To observe the protective effect of levo-anlodipine on the calcium overload in the anoxic myocardial cells. Methods Myocardial cells were cultured, and in vitro model of anoxic myocardial cells was established. Fura2/am fluorescent probe was used to measure the free calcium concentration of the myocardial cells by spectrofluorometer. The expression of Ca~2+ ATPase of cellular membrane was detected by RT-PCR, and the content of calcium pump in sarcoplasmic reticulum was measured by western blot. Results The levo-anlodipine could decrease the free calcium concentration of the anoxic myocardial cells markedly(359.06?75.00nM), and increase the expression of Ca~2+ ATPase of cellular membrane and the content of calcium pump of sarcoplasmic reticulum in the anoxic myocardial cells. Conclusion Levo-anlodipine could enhance the resistance to calcium overload in anoxic myocardial cells through increasing the expression of Ca~2+ ATPase.

Objective: To investigate the inhibitory effect of Dahuangzhechong pill to platelet activation.Methods: The blood platelet were incubated with the medicated blood plasma with Dahuangzhechong pill,and then activated with ADP and marked with PAC-1 monoclonal antibody.The activation rate of blood platelet was analyzed by flow cytometer.The patients with coronary heart disease or cerebral infarction took Dahuangzhechong pill,after one course of treatment,the patients,blood platelet were separated and then incubated with PAC-1 monoclonal antibody.The activation of blood platelet was detected by ? ow cytometer.Results: Compared with aspirin group(51.7%),the activation rate(20.82%) of blood platelet in Dahuangzhechong pill group decreased(P

Objective To observe the impact of lysophosphatidyl choline(LPC) on the expression of scavenger receptor class B type Ⅰ(SRBI) in L-20 cells and the impact of simvastatin.Methods Cultured hepatocytes were randomly assigned to normal group,LPC-damaged group and simvastatin group.The changes of mRNA and protein expression of SRBI in hepatic tissue were assayed by RT-PCR,immunocytochemistry and Western blot,respectively.Results The expression of SRBI was higher in LPC-damaged hepatocytes than that in normal cells at both mRNA and protein level(P

AIM: To compare the components of crude and processed Dryopteris Crassirhizoma Nakai by different kinds of cutting and carbonizing. METHODS: UV-spectrometry was utilized to analyze the yield and extract content. RESULTS: Dryopteris Crassirhizoma Nakai after being curshed has the maximum in the yield, the total phenol of carbonized products, the water extract and alcohol extract. CONCLUSION: There are significant differences in intrinsic quality among various processed products of Dryopteris Crassirhizoma nakai, among them the crushed one has the highest quality, which conforms to China pharmacopeia 2000 VolⅠ.

Eighteen novel levofloxacin-thiadiazole HDACi conjugates were designed and synthesized from levofloxacin. The chemical structures of all conjugates were confirmed by ¹H NMR, ¹³C NMR and HR-MS spectra. The inhibitory activities of new conjugates were evaluated in an assay with a HDACs reagent kit, and their anti-tumor activities were tested in CCK-8 assay. The results showed that these new conjugates displayed potent inhibitory activity against HDACs, and the hydroxamate conjugates exhibited more potent activity than carboxylic acid and benzamide derivatives. Specifically, conjugate 5d exhibited the most potent anti-HDAC1 (IC₅₀=0.031±0.011 μmol·L^-1) and HDAC6 (IC₅₀=0.019±0.006 μmol·L^-1) activities, which was more potent than SAHA. Molecular docking studies suggest that the hydroxamate group of conjugate 5d was deeply inserted into the active site to interact with the residues in coordination with the zinc ion. Additionally, the thiadiazole group of conjugate 5d also engaged in hydrogen bonding with F679 in HDAC6, which had been linked to the selectivity of the HDAC isoforms. Moreover, these conjugates displayed significant antiproliferative effects on SW620, MGC-803, PC-3, NCIH460, MCF-7 and HepG2 cells, in particular, conjugate 5d showed the greatest potency against MGC-803 (IC₅₀=0.7±0.05 μmol·L^-1), NCIH460 (IC₅₀=2.3±0.421 μmol·L^-1), MCF-7 (IC₅₀=1.6±0.56 μmol·L^-1) and HepG2 (IC₅₀=3.9±0.26 μmol·L^-1), which was >3-fold more potent than SAHA. Additionally, all conjugates were nontoxic to health GES-1 cells, while SAHA showed some toxicity.

To discover novel dihydropyridin-2-one derivatives with higher HDAC inhibitory activity and subtype selectivity, twenty-seven dihydropyridin-2-one derivatives containing triazole unit were synthesized via click chemistry. The structures of these compounds have been confirmed by IR, ¹H NMR and HR-MS spectra. Preliminary in vitro pharmacological tests showed that these compounds potently inhibited HDAC1 and HDAC6, which also displayed significant antiproliferative effect on five cancer cells, and most of them were better than that of the parent compound 1A and drug SAHA. Specifically, compound 18g exhibited most potent anti-HDAC1 activity, and also showed the greatest potency against PC-3 and HepG2. Additionally, all compounds were nontoxic to health RWPE-1 and VERO cells, while SAHA showed essential toxicity.

AIM　To study the pharmacokinetics and bioavailability of clinafloxacin in rats. METHODS　The drug concentration was determined by HPLC. The main pharmacokinetic parameters were obtained by 3P87 program. An RP-C18 was used as the stationary phase. The mobile phase was a mixture of acetonitrile-0.05 mol*L-1 citric acid triethylamine (pH 2.5) (20∶80). The flow rate was 1.0 mL*min-1. The UV absorbance detector was set at 300 nm. RESULTS　A good linearity was obtained from 0.03-20 μg*mL-1 of clinafloxacin in rat plasma with γ=0.9998. The plasma concentration-time curve of clinafloxacin conformed to one compartment open model. After ig administration of 50 mg*kg-1 and 100 mg*kg-1 dose of clinafloxacin in six rats, mean Cmax and AUC values increased in proportion to dose. Mean T1/2 appeared to be independent of dose. Mean AUC was 65±6 and 27±4 μg*h*mL-1 respectively after iv and ig adminostration of 100 mg*kg-1 dose. The extent of bioavailability (F) of clinafloxacin was 42%. CONCLUSION　The results of the pharmacokinetic study of clinafloxacin showed that it exhibited first order kinetic characteristics and the bioavailability is low.

Objective To study the relationship between the OATP1B1 521T ＞ C genetic polymorphism and essential hypertension.Methods 164 essential hypertension subjects and 159 normotensive subjects were detected by the TaqMan-MGB probe real-time fluorescence quantitative PCR,and the results were compared with those of DNA sequencing.Results The frequencies of T/C genotype and C allele of OATP1B1 521T ＞ C gene of the essential hypertension subjects were obviously lower than those of the normotensive subjects(T/C genotype:0.16 vs 0.25,P ＜0.05 ;C allele:0.10 vs 0.17,P ＜0.05),The difference was significant.Binary logistic stepwise regression analysis was used for evaluatine the risk factors of essential hypertension,there was significant relationship between OATP1 B1 52IT ＞ C gene polymorphism and essential hypertension.Conclusion The SLCO1 B1 521T ＞ C variant was common in Chinese essential hypertension population,but the difference of frequency of SLCO1B1 52IT ＞ Cmuton between the essential hypertension patients and the normotensive controls was of obviously statistical significance,which indicates that the SLCO1B1521T ＞ C variant maybe associate with essential hypertension.

OBJECTIVE: To investigate the effect of Dahuang Zhechong pills (DZ) on arterial thrombotic model in vivo. METHODS: Sixty-five rabbits were randomly divided into 7 groups: normal, model (collagen encapsulated thread-drawing),model+aspirin (ASA), model+clopidogrel (CP),model+ASA+CP, model+ low dosage DZ (DZL), and model+high dosage DZ (DZH). All rabbits except the normal group were fed with the drugs repectively for 8 days,and sacrificed at 2 hours after the last feeding, obtained aortae. The pathological changes in the aortae were observed under microscope,and the level of FDP, D-dimer and tissue factor (TF) were measured by enzyme-linked immunosorbent assay (ELISA). RESULTS: The vascular vessels were filled with thrombi in the model group and the elastic membranes of the vessel wall were seriously injured. The arterial thrombi were observed around the vascular wall in the DZL group, but some of the thrombi were dissolved. The number of thrombi was remarkably decreased in the DZH group, and most thrombi were dissolved and the vascular intimal membranes were intact. Compared with the model group, the dry and wet weight of the thrombi and the level of D-dimer, FDP, and TF in the plasma were significantly attenuated (P<0.01) in all the treatment groups. There were no significant difference between the DZL group and the ASA group in the dry weight, D-Dimer, and FDP (P>0.05). The pathological changes in the vascular vessel and the elevation of plasma parameters in the DZL group were similar to those in the ASA and CP groups (P>0.05). The dry and wet weight, D-dimer, FDP, and TF in the plasma in the DZH group were significantly lower than those in the DZL group (P<0.01 or P<0.05, separatively), and closed to those in the ASA+CP group. CONCLUSION Dahuang Zhechong pills are potential novel anti-thromobotic agent for arterial thrombosis.
Animals ; Carotid Artery, Common ; metabolism ; pathology ; Drugs, Chinese Herbal ; therapeutic use ; Fibrinolytic Agents ; therapeutic use ; Male ; Phytotherapy ; Rabbits ; Random Allocation ; Thromboplastin ; metabolism ; Thrombosis ; drug therapy