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1.
Article in Chinese | WPRIM | ID: wpr-771514

ABSTRACT

To achieve a comprehensive understanding of heavy metals and harmful elements residues in Niuhuang Qingwei Pills,49 samples from 18 manufactures were collected from 31 provinces in China.Risk assessment and control preparations were applied innovatively in evaluation of exogenous pollution in traditional Chinese Medicine.Determination methods for Pb,Cd,As,Hg and Cu were established by inductively coupled plasma mass spectrometry(ICP-MS).Based on the procedures including hazard identification,hazard characterization,exposure assessment and risk characterization,risk assessment was performed and residual limits for Pb,Cd,As,Hg and Cu in the drug were formulated.The results showed that the hazardous quotients(HQ) of the elements were decreased in the following order:Pb>As>Cu>Hg>Cd,and the total hazardous index(HI) of heavy metals and harmful elements in Niuhuang Qingwei Pills was above 1,implying health risk of the drug.Under the proposed limits,5 elements in the control preparation as well as Cd and Cu in the samples were within the limits range,but the excess rates of Pb,As and Hg in the samples were 12%,12% and 14%,respectively.For the first time,basic steps for risk assessment of Chinese patent medicine were established,which provided model and reference for risk assessment and limit formulation of other drugs.


Subject(s)
China , Drug Contamination , Drugs, Chinese Herbal , Reference Standards , Metals, Heavy , Risk Assessment
2.
Acta Pharmaceutica Sinica ; (12): 2316-2325, 2019.
Article in Chinese | WPRIM | ID: wpr-780346

ABSTRACT

In this study, the lipid membrane-wrapped nanoparticles loaded with metformin polymer (PolyMet) and doxorubicin (DOX) was prepared and then evaluated therapeutic effect on breast cancer. An anionic chain PGA-DOX based on γ-polyglutamic acid (PGA) with DOX was synthesized via amidation reaction and characterized by 1H NMR. The PGA-DOX and PolyMet were loaded via electrostatic attraction to prepare the co-delivery nanoparticles system (PolyMet-DOX-NPs). Then, PolyMet-DOX-NPs were coated with cationic liposome membrane to form the core-membrane structural system (PolyMet-DOX-lipid-nanoparticles, PolyMet-DOX-LNPs). The structure and morphology of PolyMet-DOX-LNPs were observed by transmission electron microscope. The particle size, zeta potential, encapsulation efficiency (EE), drug loading (DL), release behavior in vitro of PolyMet-DOX-LNPs were investigated. The MTT assay was used to examine the cytotoxicity of PolyMet combined with DOX on 4T-1 cells. The 4T1Fluc tumor-bearing mice model was used to evaluate the therapeutic efficacy of PolyMet-DOX-LNPs in vivo. All animal experiments were performed in line with ethical standards and approved by the Animal Experiments Ethical Committee of Zhejiang Chinese Medical University. 1H NMR spectrum showed that PGA-DOX was successfully synthesized with DOX grafting rate of (72.03 ± 1.29) %. The EE and DL of PolyMet-DOX-LNPs was (72.76 ± 1.92) % and (1.16 ± 0.12) %, respectively. PolyMet-DOX-LNPs exhibited a suitable size of (159.3 ± 7.4) nm and positive charge of (+36.3 ± 1.9) mV with good spheroidal morphology and dispersibility. The release profiles in vitro showed that PolyMet-DOX-LNPs exhibited a slowly and maintained release behavior at physiological pH value (pH 7.4) within 48 h. Further studies showed that PolyMet combined with DOX could synergistically enhance the cytotoxicity on 4T-1 cells. Bioluminescence imaging (BLI) result showed that the luminescence signal intensity of 4T-1Fluc cells was reduced after treatment with PolyMet-DOX-LNPs and the tumor volume growth was also inhibited. Additionally, the H&E staining and changes of body weight showed that PolyMet could reduce the toxicity of DOX. To sum up, PolyMet has a good synergistic effect with DOX in the treatment of breast cancer, which provide the foundation for this novel metformin polymer on the anti-tumor application.

3.
Acta Pharmaceutica Sinica ; (12): 84-89, 2018.
Article in Chinese | WPRIM | ID: wpr-779848

ABSTRACT

This study was designed to explore the mechanism of Coix seed oil (Coix) impact on the drug resistance, bioluminescence imaging (BLI) and the efflux of D-luciferin potassium salt, the substrate of ABC transporters, in doxorubicin-resistant breast cancer cells. Multidrug resistance (MDR) gene and protein expression were analyzed in the cells by q-PCR and Western blot. First, in order to investigate the effect of the efflux function by ABC protein, a cell line with overexpressed luciferase was established in MCF-7 cell line. BLI was used to monitor the efflux kinetics of D-luciferin potassium salt before and after Coix treament. The results showed that the efflux of D-fluorescein potassium from MCF-7/DOXFluc was lessened when pretreated with Coix, which means that Coix may decrease the efflux of other chemotherapies using ABC transporters. Both of the results of q-PCR and Western blot showed that gene and protein expression of ABC transporters such as ABCG2, ABCC1 and ABCB1 were down-regulated by Coix treatment. The efficacy of Coix reversing MDR was verified with the chemotherapy medication doxorubicin (DOX). MTT assay showed that Coix increased the inhibitory effect of DOX on proliferation of MCF-7/DOX, and the optimal combination of ratio was 25 times that of DOX. The results suggest that Coix may reverse MDR of the substrate of ABC transporters from two aspects, one is to cut down the ABC protein efflux function, and the other is to decrease the quantity of ABC gene and protein expression.

4.
Article in Chinese | WPRIM | ID: wpr-689863

ABSTRACT

Astragalus membranaceus pathogenesis-related protein 10 (AmPR-10) is largely expressed in case of environmental pressure and pathogen invasion. This study aims to explore the biochemical functions of AmPR-10. The dried root of Astragalus membranaceus was mechanically homogenized and extracted by Tris-HCl buffer to obtain its crude extract, which was then purified by anion exchange chromatography and gel filtration chromatography to obtain electrophoretically pure AmPR-10. The nuclease activity of AmPR-10 was tested with different RNAs by detecting the absorption value at 260 nm. The results demonstrated potent nuclease activity toward yeast tRNA, yeast RNA, Poly (A) and Poly (C). The optimum reaction temperature was 50 °C and pH was 7-8. EDTA showed no effect on its activity, while Mg²⁺ exhibited potent activation effect on the activity, and Co²⁺, Ca²⁺ and Zn²⁺ manifested moderately inhibition of the activity. Since AmPR-10 had no sequence homology with other known nucleases, AmPR-10 was probably a novel nuclease. The inhibition kinetic data against papain was analyzed by Lineweaver-Burk plots, and the results showed that the inhibition of papain followed noncompetitive-type kinetics. AmPR-10 played an important role in Astragalus membranaceus defense mechanism against environmental pressure and pathogen invasion, which may be achieved by inhibiting cycteine enzymes activity.

5.
Article in Chinese | WPRIM | ID: wpr-710180

ABSTRACT

AIM To study the effects of Elemene Injection (ELE) on the kinetics of intracellular transport of Gefitinib (GEF) in PC-9/GR cells and to probe the role of ELE in reversing oncological multidrug resistance.METHODS The intracellular pharmacokinetic behavior of D-luciferin potassium salt,a substrate of an ATP-binding cassette (ABC) protein,was investigated in PC-9/GRFluc cells using real-time bioluminescence imaging.The resistance of PC-9/GR cells to GEF was determined by MTT assay.Compusyn software was used to analyze the synergistic effect of GEF and ELE,and HPLC to detect the uptake of GEF in PC-9/GR cells.RESULTS The respective GEF IC50 values of 0.01 μg/mL in PC-9 cells and 1.50 μg/mL in PC-9/GR cells revealed the 150 times drug resistance of PC-9/GR to PC-9 cells.The significantly enhanced intracellular fluorescence intensity of D-fluorescein potassium salt by the intervention of ELE also indicated remarkable GEF uptake increase in PC-9/GR cell line (P < 0.05) due to the synergistic result.CONCLUSION Partly as the mechanism in reversing oncological multidrug resistance,ELE,a booster for the fluorescence intensity of D-luciferin potassium salt,promotes cellular uptake of GEF by inhibiting efflux function of ABC proteins.

6.
Article in Chinese | WPRIM | ID: wpr-852643

ABSTRACT

Objective The relationship between the in vivo absorption kinetics and the in vitro release kinetics of various components (including flavonoids and terpenoids) contained in Ginkgo biloba extract (GBE) sustained-release pellets were evaluated using multi-component integration kinetics which could provide a reference for more accurate assessment of in vitro and in vivo correlation. Methods The release rates in vitro of main ingredients (quercetin, isorhamnetin, bilobalide, ginkgolide A, ginkgolide B and ginkgolide C) were detected by HPLC-MS/MS. The integrated drug concentration was calculated, and the release rates in vitro of integrated components were then depicted according to the results. Plasma was collected at different time points after oral administration of GBE sustained-release pellets, multiple components contained in GBE sustained-release pellets were then determined. A novel approach of self-defined weighting coefficient (Wj) based on the area under the curve from zero to infinity AUC0—∞ had been created to obtain the holistic pharmacokinetic profiles of GBE sustained-release pellets. To evaluation the in vitro-in vivo correlation of GBE sustained-release pellets, the percent of integrated in vivo absorption calculated by the Wagner-Nelson methodwas plotted versus the percent of integrated in vitro drug release at the same time. Results The components contained in sustained- release pellets had a good release, the Wj of each component in GBE sustained-release pellets were as follows: quercetin, 0.248 1; isorhamnetin, 0.009 2; bilobalide, 0.228 2; ginkgolide A, 0.296 4; ginkgolide B, 0.132 4; ginkgolide C, 0.090 3. The in vivo-in vitro correlation equation was Y = 0.930 8 X + 12.84, r = 0.962 9, indicated that the correlation between in vivo absorption kinetics and in vitro release kinetics is good. Conclusion The efficacy of the herbal medicines depends on a variety of components combined effect, using the integrated pharmacokinetic to analyze IVIVC could take the characteristic of each component into account, which is helpful for the study of the correlation between in vivo absorption kinetics and in vitro release kinetics.

7.
Article in Chinese | WPRIM | ID: wpr-250474

ABSTRACT

To establish the quantitative method of stachydrine hydrochloride and leonurine hydrochloride in the preparations of Leonuri Herba. The contents of stachydrine hydrochloride and leonurine hydrochloride in the preparations of Leonuri Herba were determined by HPLC-MS. The chromatographic column was Waters XBridge Amide(4.6 mm×250 mm,5 μm). The mobile phase was acetonitrile-0.1% formic acid in gradient mode,at the flow rate of 1.0 mL• min⁻¹,with the split ratio of 1∶4. MS conditions for the ESI ion source,positive ion mode,selective ion scan(SIM) of stachydrine hydrochloride(m/z 144.0) and leonurine hydrochloride(m/z 312.0) was measured. The linear ranges of stachydrine hydrochloride was 0.562 8-281.4 μg•L-1(r=0.999 8). The linear ranges of leonurine hydrochloride was 0.521 2-260.6 μg•L-1(r=0.999 8). The method is accurate,simple,and reliable,and can be used to determine the contents of stachydrine hydrochloride and leonurine hydrochloride in the preparations of Leonuri Herba.

8.
Article in Chinese | WPRIM | ID: wpr-294033

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the saponin in Shengmai injection.</p><p><b>METHOD</b>On the basic of studing the chemical constituents of red ginseng and Shengmai injection, 20 compositions had been identifided by LC-MS/MS.</p><p><b>RESULT</b>Twenty identifided compositions were the common components of Shengmai injection and red ginseng extracts.</p><p><b>CONCLUSION</b>The analytical method for saponins in Shengmai injection was established which could be used as the basis for further study and quality control.</p>


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Mass Spectrometry , Molecular Structure , Saponins , Chemistry
9.
Article in Chinese | WPRIM | ID: wpr-290785

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the treatment of postoperative chyle leak after surgery for digestive malignancies.</p><p><b>METHODS</b>From December 2008 to February 2012, in the Sun Yat-sen Memorial Hospital of Sun Yat-sen University, clinical data of 19 patients with chyle leak after digestive system cancer surgery were retrospective analyzed.</p><p><b>RESULTS</b>Nineteen cases of chyle leak were all identified between the second and the fourth postoperative day and were all initially managed with conservative treatment including early fasting, parenteral nutrition(PN), 24-hour continuous infusion of somatostatin, and low pressure suction drainage. Eight patients were treated successfully for 6 to 10 days with a significant reduction of the daily drainage volume. Ten patients had enteral nutrition(EN) and their drain tubes were repeatedly washed with 30 ml of compound meglumine diatrizoate injection every day until the drainage volume decreased to 200 ml/day. The time to resolution of chyle leak in these ten patients ranged from 12 to 24 days. One patient had no significant decrease in fluid drainage and developed abdominal distension after one week of conservative treatment. Surgical closure of chyle leak was performed on the 11th postoperative day, abdominal cavity drainage tube was removed on the 4th postoperative day. The patient was discharged home in good condition.</p><p><b>CONCLUSION</b>Most postoperative chyle leak after surgery for digestive malignancies can be successfully managed with conservative treatment. Somatostatin and the drainage are the main therapeutic approaches. When chyle leak is not resolved with conservative treatment, surgical treatment should be considered to prevent serious complications.</p>


Subject(s)
Adult , Aged , Anastomotic Leak , Therapeutics , Chyle , Digestive System Neoplasms , General Surgery , Female , Humans , Male , Middle Aged , Postoperative Complications , Therapeutics , Retrospective Studies
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