Effect of Pien Tze Huang against EV71 / 中国中药杂志

This study aims to investigate the inhibitory effect of Pien Tze Huang(PZH) on enterovirus 71(EV71). To be speci-fic, chemiluminescence method was adopted to evaluate the toxicity of PZH to African green monkey kidney(Vero) cells and human rhabdomyosarcoma(RD) cells, and cytopathic effect(CPE) method to assess the inhibition on EV71-GFP reporter virus and EV71 C4 wild-type virus. The results showed that PZH had low cytotoxicity to Vero cells and RD cells, with the half-maximal cytotoxic concentration(CC_(50)) of about 0.691 3-0.879 2 mg·mL~(-1) for the two. In addition, PZH can effectively inhibit the replication of EV71 within the non-cytotoxic concentration range, and dose-dependently alleviate the cytopathic changes caused by virus infection, with the half-maximal effective concentration(EC_(50)) of 0.009 2-0.106 3 mg·mL~(-1). On the basis of the above results, the green fluorescent protein(GFP), indirect immunofluorescence assay(IFA), and median tissue culture infective dose(TCID_(50)) were employed to assess and verify the anti-EV71-GFP and anti-EV71 C4 activity of PZH. The results demonstrated that PZH can dose-dependently lower the expression of GFP by EV71-GFP and structural protein VP-1 by EV71 C4 and decrease the production of progeny infectious viruses. The EC_(50) of PZH for EV71-GFP and EV71 C4 was about 0.006 0-0.006 2 mg·mL~(-1) and 0.006 6-0.025 6 mg·mL~(-1), respectively. This study suggested that PZH may exert antiviral activity by acting on EV71 and interfering with the expression of VP-1. At the moment, there is still a lack of specific anti-EV71 drugs. This study proposed a new idea for the symptomatic treatment of EV71 infections such as hand-foot-mouth disease and verified an effective drug for the treatment of EV71 infections.

Application of zebrafish in drug screens for active ingredients / 中国中药杂志

Zebrafish has unique advantages over other animal models in the aspect of drug screens for active ingredients and gains more and more attentions in drug research and development recently. Thus, this article reviews the recent advance of zebrafish-based drug screens in Chinese traditional medicine (TCM) effective part research, monomer drug screening, activity evaluation of natural products, discovery of new uses for old drugs, and toxicity assessment in early-phase drug discovery.

Pharmacokinetics, tissue distribution and magnetic resonance's response characterstics of folic acid-O-carboxymethyl chitosan ultrasmall superparamagnetic iron oxide nanoparticles in mice and rats / 药学学报

Folic acid-O-carboxymethyl chitosan ultrasmall superparamagnetic iron oxide nanoparticles (FA-OCMCS-USPIO-NPs) are a novel molecular targeting MR contrast agent. This paper reperts the pharmacokinetics and magnetic resonance response characteristics of FA-OCMCS-USPIO-NPs in normal rats and mice, and discussed its distributing regularity in animals, providing basis for tumor targeting imaging. O-phenanthroline method was used to determine iron content in rats' plasma and mice's organs following high and low doses of nanoparticles injected through tail vein, and the blood concentration-time curve was drawn, the calculated t1/2 of two groups were greater than 7 h. The results of tissue distribution showed that only a small part of nanoparticles were swallowed by the liver and spleen, while none in the heart, lung and kidney. At the same times, the phagocytosis of nanoparticles did not change with the dose. The results of MRI showed that renal excretion occurred 4 hours after injection, and signal to noise ratio (SNR) of liver and kidney returned to normal levels 24 hours after injection. There were no nanoparticles in the lungs. So a part of nanoparticles escaped from phagocytosis of liver and spleen, and it owned lower toxicity and longer half-life. indicated its use for tumor-targeting imaging. All of these indicated its use for tumor-targeting imaging.

Effect of imatinib at different concentrations on rat C6 glioma cell apoptosis and cell cycle / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effect of imatinib on rat C6 glioma cell apoptosis and cell cycle.</p><p><b>METHODS</b>MTT assay was used to determine the OD value of C6 glioma cells following treatment with imatinib at different concentrations (0.156, 10 and 15 micromo/L) for 24, 48 and 72 h. The cell apoptosis was assayed by Hochest/PI staining and the cell cycle changes were analyzed by flow cytometry.</p><p><b>RESULTS</b>Imatinib treatment resulted in increased number of apoptotic cells in a time- and dose-dependent manner. A 72-h treatment of the cells with imatinib at 10 and 15 micromo/L caused increased cell percentage in G(0)/G(1) phase to (68.53-/+0.83)% and (70.41-/+0.62)%, (P<0.01), decreased the percentage of G(2) phase cells to (14.48-/+0.12)% and (13.84-/+2.86)% (P<0.01), and decreased the percentage of S phase cells to (16.98-/+0.72)% and (15.78-/+2.28)%, respectively (P<0.01).</p><p><b>CONCLUSION</b>Imatinib can induce apoptosis and affect the distribution of the cell cycle of C6 cells in vitro.</p>

Island skin flap supplied by superficial temporal vessel for the whole ear lobe defect / 中华整形外科杂志

<p><b>OBJECTIVE</b>To introduce a new method for reconstruction of the whole ear lobe defect.</p><p><b>METHODS</b>The free island skin flap supplied by superficial temporal vessel which was designed at the area anterior and superior to crus helicis. The flap was transferred through subcutaneous tunnel and self-folded to reconstruct the whole ear lobe defect.</p><p><b>RESULTS</b>Since 1999, 6 cases were treated with no complication. The ear lobe shape and skin colour were very natural.</p><p><b>CONCLUSIONS</b>The island skin flap supplied by superficial temporal vessel is very suitable for the whole ear lobe defect with good cosmetic results.</p>

Effects of bagasse polysaccharide on the immune functions of immunosuppressed mice / 南方医科大学学报

<p><b>OBJECTIVE</b>To observe the effects of bagasse polysaccharide on the immune functions of immunosuppressed mice.</p><p><b>METHODS</b>Immunosuppressed mouse models were established by intraperitoneal injections with cyclophosphamide followed by daily intragastric administration of bagasse polysaccharide. After the treatments, the mice were examined for immune organ weight index, phagocytotic function of the macrophages, delayed type hypersensitivity, serum IgM level following exposure to chicken red blood cells, formation of hemolytic plaques, T cell percentage and lymphocyte transformation.</p><p><b>RESULTS</b>Treatment of the immunosuppressed mice with bagasse polysaccharide at the daily dose of 200 and 400 mg/kg significantly increased the weight of the immune organs, phagocytotic function of the macrophages, delayed type hypersensitivity, serum IgM level against chicken red blood cells, formation of hemolytic plaques, T cell percentage and lymphocyte transformation.</p><p><b>CONCLUSION</b>Bagasse polysaccharide can enhance the immune functions of immunosuppressed mice.</p>

Comparison of transdermal permeation in vitro of lidocaine tincture and microemulsion / 南方医科大学学报

<p><b>OBJECTIVE</b>To compare lidocaine tincture and microemulsion for their transdermal permeation.</p><p><b>METHODS</b>The experimental model for percutaneous administration of lidocaine preparations in vitro was prepared using modified Franz diffusion cell.</p><p><b>RESULTS</b>The accumulated infiltration amount of lidocaine microemulsion in unit area was higher than that in its cream or tincture preparations.</p><p><b>CONCLUSION</b>The transdermal permeation of lidocaine microemulsion in vitro can be more efficient than that of the tincture preparation, and the permeation is linearly dependent on the dose administered within a certain range.</p>

Treatment of recurrent condyloma acuminatum with solid lipid nanoparticle gel containing podophyllotoxin: a randomized double-blinded, controlled clinical trial / 南方医科大学学报

<p><b>OBJECTIVE</b>To observe the clinical efficacy and safety of podophyllotoxin delivered via solid lipid nanoparticle gel for topic treatment of recurrent condyloma acuminatum.</p><p><b>METHODS</b>In a randomized double-blinded study, podophyllotoxin solid lipid nanoparticles gel and routine podophyllotoxin gel preparation was applied respectively for treatment of 97 volunteer patients with recurrent condyloma acuminatum. The therapeutic effect, condyloma acuminatum relapse following the treatment and adverse effect were evaluated.</p><p><b>RESULTS</b>The wart clearance rate in the condyloma acuminatum patients in the first treatment course with podophyllotoxin solid lipid nanoparticle gel reached 97.1%, close to that with the routine preparation of 90.6%, but the nanoparticle preparation significantly reduced the recurrence rate and adverse effect (P<0.01).</p><p><b>CONCLUSION</b>Podophyllotoxin delivered via solid lipid nanoparticle gel can effectively clear condyloma acuminatum and reduce its recurrence rate with only mild, tolerable adverse effect.</p>

Preparation of gemcitabine polybutylcyanoacrylate nanoparticles / 南方医科大学学报

<p><b>OBJECTIVE</b>To optimize the preparation process of gemcitabine polybutylcyanoacrylate nanoparticles (GCTB- PBCA-NP).</p><p><b>METHODS</b>According to the particle size, the entrapment efficiency and the loading quantity of GCTB-PBCA-NP, single factor analysis was carried out to optimize the component composition and preparation process based on an orthogonal design.</p><p><b>RESULTS</b>The mean particle size of the NP was (112-/+9) nm with an entrapment efficiency of (54.12-/+2.43)% and drug loading of (11.08-/+0.89)%.</p><p><b>CONCLUSION</b>An optimized nanoparticular drug delivery system is obtained by emulsion polymerization.</p>

Determination of octafluoropropane content in human albumin micropheres loaded with octafluoropropane / 南方医科大学学报

<p><b>OBJECTIVE</b>To develop a method for determinating the octafluoropropane (OFP) content in human albumin micropheres loaded with OFP.</p><p><b>METHODS</b>OFP content in the loaded human albumin micropheres was determined by means of gas chromatography coupled with mass spetrum/selected ion monitoring (GC-MS/SIM).</p><p><b>RESULTS</b>The calibration curve was linear within the concentration range of 40.92-16,368 nmol/L (R(2)=0.9999). The limit of detection was 8.18 nmol/L, and the recovery rate was (100.98-/+1.4)% (204 nmol/L), (102.63-/+2.29)% (2,046 nmol/L) and (97.5-/+2.2)% (8,184 nmol/L), respectively. The intra-day and inter-day RSDs were 0.6%-2.0% and 0.86%-2.3%, respectively.</p><p><b>CONCLUSION</b>The method of GC-MS/SIM is accurate, sensitive, precise and applicable for OFP determination in the microspheres.</p>

Evaluation of cyclodextrin inclusion of the volatile components in compound traditional Chinese medicine / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the factors affecting cyclodextrin (CD) inclusion of the volatile components in compound traditional Chinese medicines and evaluate the stability of the inclusion compound.</p><p><b>METHODS</b>This study took Gengnian compound as an example to examine the factors affecting the inclusion process according to the inclusion compound utilization ratio. Orthogonal design method was employed optimize the parameters in the inclusion process. The moisture absorption rate of the beta-CD inclusion compound was determined in different humidity and Q10 was used to predict its.</p><p><b>RESULTS</b>The inclusion method, inclusion compound dosage, temperature, inclusion time, and the drying method could all obviously influence the inclusion process. The results of orthogonal design study showed that the optimal beta-CD inclusion of Gengnian compound volatile components could be achieved by adding 8-fold volume of beta-CD and stirring for 3 h at room temperature. Stability experiment showed that the humility did not significantly influence the inclusion compound, which can be stable for 1.26 years.</p><p><b>CONCLUSION</b>This study comprehensively examines the factors affecting the inclusion process and the stability of the inclusion compound, and provides experimental basis for application and study of the inclusion technology.</p>

Qualitative fingerprint and quantitative determination of caffeic acid in compound dandelion enema / 南方医科大学学报

<p><b>OBJECTIVE</b>To establish a qualitative and quantitative reversed-phase high-performance liquid chromatography (RP-HPLC) with fingerprinting technique for quality control of compound dandelion enema.</p><p><b>METHODS</b>HPLC was utilized for quality assessment of 10 batches of samples. RP-HPLC analysis was performed on a Hypersil BDS C18 column (4.6 mm x 250 mm, 5 microm) with the mixture of acetonitrile (A) and potassium phosphate solution (B) (pH3.2) as the mobile phase in gradient mode. The concentrations of solvent A were 10%, 80% and 80% at 0, 38 and 40 min, respectively. The column temperature was set at 35 degrees C, the flow rate at 0.7 ml/min and the detection wavelength at 254 nm.</p><p><b>RESULTS</b>HPLC fingerprinting was established from the 10 batches, and the data showed 23 characteristic peaks in the compound dandelion enema for use as index peaks for qualitative identification. Comparison of the retention time and the on-line UV spectra of the samples with the chemical standards identified peaks 3, 4 and 8 as protocatechualdehyde, caffeic acid and ferulic acid, respectively. The contents of caffeic acid in the compound dandelion enema ranged between 63.7 and 136.8 microg/ml.</p><p><b>CONCLUSION</b>High specific chromatographic fingerprinting and quantitative measurement of caffeic acid allows rigorous quality control of compound dandelion enema.</p>

Sampling of exhaled gas after intravenous administration of octafluoropropane-containing human albumin micropheres in dogs / 南方医科大学学报

<p><b>OBJECTIVE</b>To develop a method for quantitative collection of exhaled gas in anesthetized dogs at given time following intravenous administration of octafluoropropane (OFP)-containing human albumin micropheres for assessing the gas kinetics of OFP.</p><p><b>METHODS</b>OFP-containing albumin micropheres were administered intravenously at 0.4, 0.8 and 1.2 ml/kg, respectively, in anesthetized and ventilated dogs. The exhaled air samples were analyzed by gas chromatography-tandem mass spectrometry (GC-MS-MS).</p><p><b>RESULTS</b>The correlation curve between the area under curve (AUC) and administered dose was roughly linear (Y=1162.5X-417.38, r square=0.949 9). The total recovery rate was (119.49-/+27.62)% which was not significantly different from the rate of 100% (P>0.05). GC-MS-MS was accurate, sensitive, precise and applicable for OFP determination.</p><p><b>CONCLUSION</b>The sampling method is useful for characterizing OFP pharmacokinetics in dogs, and also applicable for studying the pharmacokinetics of other gas-containing drugs.</p>

Preparation and characterization of superparamagnetic iron oxide nanoparticles / 南方医科大学学报

<p><b>OBJECTIVE</b>To determine the physical and magnetic properties of superparamagnetic iron oxide (SPIO) nanoparticle prepared in our laboratory and evaluate its possibility for use as contrast agents in magnetic resonance imaging (MRI).</p><p><b>METHODS</b>The SPIO nanoparticle was obtained by means of classical coprecipitation in dextran solution and its size determined by electron microscopy and photon-correlation spectroscopy. The iron content was determined by phenanthroline photometry, and T(2) values as well as relaxivity evaluated with a clinical MR system at 1.5T.</p><p><b>RESULTS</b>Dextran-coated magnetite particles with a hydrodynamic diameter of 85.9 nm were prepared. The iron core size was 15 nm and the formation of Fe(3)O(4) crystal in SPIO nanoparticles was confirmed by X-ray diffraction (XRD) analysis. These particles possessed some characteristics of superparamagnetic and show a smaller spin-spin relaxation, with relaxivity and saturation magnetization of 0.1567 mmol(-1)/ms(-1) and 80 emu/g Fe, respectively.</p><p><b>CONCLUSIONS</b>A stable SPIO nanoparticle with a dextran coating have been developed, and in vitro evaluation of its physical and magnetic properties suggests its potential for use as the contrast agent in MRI.</p>

Preparation and electron microscopic observation of lidocaine microemulsion / 南方医科大学学报

<p><b>OBJECTIVE</b>To prepare and determine the proportion of the components of lidocaine microemulsion.</p><p><b>METHODS</b>Pseudoternary phase diagrams of the prepared lidocaine microemulsion with different Km (surfactant/cosurfactant) were generated to determine the optimal Km according to the size of the microemulsion area. The diameter and its distribution range, viscosity, electric conductivity and refractivity of lidocaine microemulsion drop was determined, and the appearance and system type of the microemulsion was observed using electron microscope. RESULTS; Maximum microemulsion area in the pseudoternary phase diagrams was obtained with the Km of 3, and the drop size of the microemulsion averaged 29.8+/-14.4 nm (with up to 98% of the drop size ranging between 15.1-45.5 nm and 2% between 77.9-261.3 nm). At 25 degrees C, the viscosity, electric conductivity and refractivity of the microemulsion was 25 mPa.S, 130 micros/cm and 1.473, respectively, and the lidocaine microemulsion was identified to belong to O/W type. The microemulsion drop appeared in spherical shape of heterogeneous sizes in a multi-disperse system.</p><p><b>CONCLUSION</b>The optimal proportion of the components in lidocaine microemulsion can be obtained by analyzing pseudoternary phase diagrams, and the drop size, distribution, shape and system type can be determined or observed through Maerwen Zetasizer combined with electron microscopic observation.</p>

Determination of perfluoropropane in canine whole blood by purge and trap concentrator-GC-MS / 药学学报

<p><b>AIM</b>To develop a method for direct determination of perfluoropropane in canine whole blood and to study its pharmacokinetics after a suspension of perfluoropropane-containing albumin microcapsules was administered intravenously.</p><p><b>METHODS</b>Perfluoropropane-containing albumin microcapsule suspension was administered intravenously to anesthetized canines at the dosage of 0.6 mL x kg(-1). Whole blood samples were collected and added directly into the purging glass tube in Tekmar 3000 Purge and Trap Concentrator coupled with a GC-MS for the determination of perfluoropropane. The pharmacokinetic parameters of perfluoropropane were calculated by non-compartment model statistics.</p><p><b>RESULTS</b>The linear range was 0.0168-4.03 mg x L(-1). The main pharmacokinetic parameters of perfluoropropane was obtained as follows: mean residence time (MRT) was (63 +/- 5) s, T1/2 was (44 +/- 4) s, Tmax was 30 s, Cmax was (2.20 +/- 0.20) mg x L(-1), AUC0-infinity was (96 +/- 11) mg x s x L(-1).</p><p><b>CONCLUSION</b>The method is sensitive, specific and simple. It can be used to determine fluorocarbon contained in microcapsule ultrasound contrast agents for studying its pharmacokinetics.</p>

Effects of two metabolites of cultured marine fungus, Halorosellinia oceanicum 323, on the contraction of isolated guinea-pig ileum / 药学学报

<p><b>AIM</b>To investigate the effects of 323-A and 323-B, two isomers extracted from the metabolites of cultured marine fungus, Halorosellinia oceanicum 323, on the contraction of isolated guinea pig ileum (GPI).</p><p><b>METHODS</b>The GPI contractions were recorded with a two-channel-physiological recorder with tension transducers. Cumulative dose-response curves of contractions of isolated GPI induced by histamine (Hist), acetylcholine (ACh) and potassium chloride (KCl) were constructed, then the influences of 323-A and 323-B on each curve were observed. Furthermore, possible mechanisms underlying effects of the two compounds were explored by analyzing their influences on the biphasic contractile response to ACh, with comparison of a calcium antagonist, verapamil (Ver).</p><p><b>RESULTS</b>The data indicated that both 323-A and 323-B inhibited the contractile actions of GPI triggered by Hist, ACh and KCl in a concentration-dependent manner, with pD2' values of 5.13, 4.97, 5.36 and 5.51, 5.56, 5.62, respectively. The initial phase component of the ACh-elicited contractions, in the absence of external Ca2+, was significantly reduced by 323-A, 323-B, as well as Ver, whereas the subsequent sustained tonic contractions induced by adding Ca2+ to the bath solution were almost unaffected.</p><p><b>CONCLUSION</b>These results suggest that 323-A and 323-B have calcium antagonistic effects similar to that of Ver in mechanisms, and they might have potential to be developed as calcium antagonists.</p>