Shougang Jiang

Northeast Forestry University, Charbin, Heilongjiang Sheng, China

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Publications (8)17.22 Total impact

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    ABSTRACT: Abstract Context: Docetaxel is now a major antitumor drug in clinical use for the treatment of a variety of tumors. The ethanol/Tween 80 solvent required in the formulation to increase the docetaxel solubility is at least partly responsible for the hypersensitivity reaction, decreased uptake by tumor tissue, and increased exposure to other body compartments. Objective: The present study was aimed at developing hydrosoluble DTX-FA-HSANPs targeting tumor cells and to investigate antitumor activities of the nanoparticles. Materials and methods: The DTX-HSANPs were prepared using a desolvation technique and the carboxylic groups of NHS-folate were conjugated with the amino groups of the human serum albumin nanoparticles, and studied their size and zeta potential, drug loading efficiency, surface morphology, release properties in vitro, and antitumor activities. Results: The spherical nanoparticles obtained were negatively charged with a zeta potential of about -30 mV and characterized around 150 nm with a narrow size distribution. Drug loading efficiency was approximately 17.2%. The folate-decorated nanoparticles targeted a human hepatoma cell line effectively. The in vitro drug release of DTX-FA-HSANPs in the first 96 h corresponded with the following equation: Q = 18.87851 - 0.13866t + 0.21276t(2 )- 0.00704t(3) + 0.0000847854t(4 )- 0.00000034991t(5) (R(2 )= 0.98155). Moreover, the in vitro antitumor activities of DTX-FA-HSANPs were close to the activities of the positive control (docetaxel). The in vivo inhibition ratios of DTX-FA-HSANPs and docetaxel were 66.2% and 59.5%, respectively, at a dose of 5 mg/kg. Discussion and conclusion: In light of the observed antitumor activities, it would be of considerable interest to collect sufficient data for the clinical application of docetaxel-loaded nanoparticles.
    Drug Delivery 01/2014; · 2.02 Impact Factor
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    ABSTRACT: Coenzyme Q10 (CoQ10) has been found to be effective in cardiovascular diseases and neurodegenerative diseases. However, the extremely poor solubility of CoQ10 in water is hampering its bioavailability as a therapeutic agent. To overcome solubility problem, we micronized the CoQ10 powder to the nanometer level by the supercritical solution (RESS) process, which does not employ any toxic organic solvent. The obtained CoQ10 nanoparticles were 147.9 +/- 27.3nm in diameter and their physicochemical properties were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), liquid chromatography-mass spectrometry (LC-MS), X-ray diffractometry (XRD) and differential scanning calorimetry (DSC) analyzes. Moreover, the pharmacokinetics of the CoQ10 nanoparticles, in comparison with the unprocessed CoQ10 powder, were investigated in rats. From the results of physicochemical and pharmacokinetic studies, the CoQ10 nanoparticles had high solubility in water and possessed less crystalline structure, which can enhance the bioavailability of CoQ10, and provide a water-soluble solid dosage form of CoQ10.
    Pharmazie 02/2012; 67(2):161-7. · 0.96 Impact Factor
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    ABSTRACT: 7-Xylosyl-10-deacetylpaclitaxel is a natural hydrophilic paclitaxel derivative. It has long been used in Chinese clinics to treat cancer. In order to further explore the underlying intracellular target of 7-xylosyl-10-deacetylpaclitaxel towards the PC-3 cell line, the ultra-structural morphology of mitochondria, the intracellular Ca (2+), the intracellular ATP, the intracellular hydrogen peroxide and pro-apoptotic Bax and Bcl-2 protein expression were measured. Additionally, the changes of mitochondrial morphology and membrane potential ( ΔΨm) were analyzed by atomic force microscopy (AFM) and flow cytometry, respectively. Our results suggest that the intracellular target of 7-xylosyl-10-deacetylpaclitaxel may be the mitochondrial permeability transition pore (mPTP). To further evaluate this hypothesis, we assessed the effect of a specific mPTP inhibitor (cyclosporine A) on the toxic action of 7-xylosyl-10-deacetylpaclitaxel. The 7-xylosyl-10-deacetylpaclitaxel-induced decrease in mitochondrial inner transmembrane potential (ΔΨm) was abolished by the addition of cyclosporine A (CsA) in PC-3 cells, indicating that 7-xylosyl-10-deacetylpaclitaxel may target mPTP. Furthermore, treatment with 7-xylosyl-10-deacetylpaclitaxel increased ROS levels in PC-3 cells. This effect was counteracted by 10 µM cyclosporine A. These data indicate that oxidative damage is involved in mPTP.
    Planta Medica 02/2011; 77(10):1005-12. · 2.35 Impact Factor
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    ABSTRACT: 7-Xylosyl-10-deacetylpaclitaxel is an active compound used in traditional Chinese medicine to treat cancer. However, pharmacokinetic studies yielded low plasma concentrations of 7-xylosyl-10-deacetylpaclitaxel after its oral administration in preclinical trials. Therefore, we investigated whether the observed low oral bioavailability of this compound is due to poor absorption. We studied the transepithelial flux of 7-xylosyl-10-deacetylpaclitaxel using the human colonic cell line Caco-2 as a model and found out that its flux (at a concentration range of 0.5-20 µM) across the Caco-2 cell layer was linear with time for up to 3 hr. The apparent maximal concentration (K (M)) of the active efflux component was 93.4 µM. Verapamil (50 µM) and tetrandrine (25 µM) significantly decreased the active transport component. These data support the conclusion that rapid passive diffusion of 7-xylosyl-10-deacetylpaclitaxel through the intestinal epithelium is partially counteracted by the action of an outwardly directed efflux pump, presumably P-glycoprotein. The relatively high apparent permeability coefficient ( P(app)) for the apical to basolateral 7-xylosyl-10-deacetylpaclitaxel transport (16.3 ± 6.3 × 10 (-6) cm/s; n = 3) suggests that the drug may still be effectively absorbed in the intestinal tract.
    Planta Medica 04/2010; 76(14):1592-5. · 2.35 Impact Factor
  • Shougang Jiang, Yu Zhang, Yuangang Zu, Zhuo Wang, Yujie Fu
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    ABSTRACT: Water decoctions from the leaves of Taxus cuspidata are used in traditional Chinese medicine to treat cancer, suggesting that water soluble constituents from these leaves may possess anticancer properties. Interestingly, hydrophilic paclitaxel derivatives, as opposed to paclitaxel itself, can be detected by high pressure liquid chromatography in water decoctions from these leaves. The remainder extracts, which are free of paclitaxel and hydrophilic paclitaxel derivatives, from the T. cuspidata leaves were investigated for antitumor activity in vivo and in vitro for the first time in this study. EE80B, 7-xylosyl-10-deacetylpaclitaxel and 7-xylosyl-10-deacetylpaclitaxel C displayed the most antitumor activity in vivo. However, in vitro studies with tumor cell lines showed that EE80B had a significantly smaller antitumor effect than paclitaxel. We hypothesize that water decoctions from T. cuspidata leaves exhibit antitumor effects in vivo, which may be aided by the activation of specific host mechanisms (e.g. stimulation of antitumor immunity) which are not present in vitro.
    The American Journal of Chinese Medicine 01/2010; 38(6):1107-14. · 2.28 Impact Factor
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    ABSTRACT: Paclitaxel, a natural product originally isolated from Taxus brevifolia, belongs to the most successful anticancer drugs. Nevertheless, its poor water solubility represents a considerable disadvantage in clinical use, and novel derivatives with improved pharmacological features are required. We isolated 7-xylosyl-10-deacetylpaclitaxel from Taxus chinensis, which reveals higher water solubility than paclitaxel. This compound induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA laddering, and transmission electron microscopy. Pro-apoptotic Bax and Bad protein expression was up-regulated and anti-apoptotic Bcl-2 and Bcl-XL expression down-regulated, which lead to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. In turn, caspase-9 activated downstream caspases-3 and -6, but not caspase-8. Bid was also activated by caspase-3. Reversely, treatment with a caspase-10-specific inhibitor could not protect PC-3 cells from 7-xylosyl-10-deacetyl-paclitaxel-triggered apoptosis. Moreover, 7-xylosyl-10-deacetylpaclitaxel had no effect on the expression of CD95 and NF-kappaB proteins, indicating that apoptosis was induced through the mitochondrial-dependent pathway in PC-3 cells.
    International Journal of Oncology 08/2008; 33(1):103-11. · 2.66 Impact Factor
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    ABSTRACT: The separation and enrichment of 10-deacetylbaccatin III (10-DAB III) and 7-xylosyl-10-deacetyl paclitaxel were studied on seven macroporous resins with special structures. The performance of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III on macroporous resins including AB-8, ADS-17, ADS-21, ADS-31, ADS-8, H1020 and NKA-II was compared according to their adsorption and desorption properties. AB-8 provided a much higher adsorption capacity for 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III than other resins, and its adsorption data fitted well to the Langmuir and Freundlich isotherm. According to the adsorption and desorption capacities and the adsorption isotherms, AB-8 demonstrated a remarkable capability for the preparative separation of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III from the remainder extracts free of paclitaxel. In order to optimize parameters of separation, dynamic adsorption and desorption experiments were carried out on the columns packed with AB-8 resin. The optimal conditions were: the processing volume 15 BV; concentrations of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III in feed solution 0.0657 mg/mL and 0.1494 mg/mL; flow rate 1 mL/min; temperature 35 degrees C. The gradient elution program was as follows: 30% ethanol for 3 BV, then 80% of ethanol for 6 BV, flow rate 1 mL/min. After the AB-8 resin treatment, the contents of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III in the product had increased from 0.053% and 0.2% to 3.34% and 1.69%, which were 62.43-fold and 8.54-fold of those in the untreated extracts, respectively, and the recoveries of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III were 85.85% and 52.78%. The performance achieved good separation and higher recovery of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III from remainder extracts free of paclitaxel by using AB-8 resin. It is a fast and effective method for the separation and enrichment of 7-xylosyl-10-deacetyl paclitaxel and 10-DAB III.
    Journal of Chromatography A 02/2008; 1177(1):77-86. · 4.61 Impact Factor
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    ABSTRACT: Vitexin is a flavonoid drug with poor water solubility commonly used to prevent heart diseases. The poor water solubility of vitexin limits its dissolution, which strongly impairs drug bioavailability. The aim of this work was to improve its bioavailability by reducing particle size in a supercritical antisolvent process (SAS) using supercritical carbon dioxide as an antisolvent agent and dimethyl sulfoxide (DMSO) as a solvent. In order to optimize the parameters of SAS process, the whole experiment was designed and conducted in an orthogonal array design (OAD), OA 16(45). The obtained optimum micronization conditions were as follows: precipitation pressure 25 MPa, precipitation temperature 50 °C, concentration of vitexin solution 2 mg/mL and vitexin solution flow rate at 6.7 mL/min. Under this condition, the mean particle size (MPS) of vitexin was reduced to 126 ± 18.5 nm.In addition, both the processed vitexin particles and the unprocessed one were characterized by Scanning Electron Microscopy (SEM), Dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), Liquid chromatography tandem mass spectrometry (LC-MS/MS), X-ray diffraction (XRD) and Differential scanning calorimeters (DSC). The results showed that SAS micronization process did not induce degradation of vitexin and the processed vitexin particles had lower crystallinity. Finally, the dissolution rates of the processed and unprocessed vitexin were evaluated, the results showed that there was a significant increase of the dissolution rate of the processed vitexin comparing with the unprocessed vitexin. Moreover, vitexin nanosuspension of high concentration can be prepared by dissolving processed vitexin in physiological saline. These results suggest that micronized vitexin may have a great potential in cardiovascular and cerebrovascular diseases therapy.
    Powder Technology. 228:47–55.