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1.
Article in English | WPRIM | ID: wpr-922103

ABSTRACT

OBJECTIVE@#To investigate the mechanisms underlying elemene-induced analgesia in rats with spared nerve injury (SNI).@*METHODS@#Sixty-five rats were equally divided into 5 groups using a random number table: naive group, sham group, SNI group, SNI + elemene (40 mg·kg@*RESULTS@#The SNI rat model exhibited a significant decrease in paw withdrawal threshold and exploratory behaviour in the EPM (P<0.05). Consecutive administration of elemene alleviated SNI-induced mechanical allodynia and anxiety in rats (P<0.05). Immunohistochemical data showed that elemene decreased SNI-induced upregulation of NDRG2 within the SDH (P<0.05). Double immunofluorescent staining data further showed that elemene decreased SNI-induced upregulation of the number of GFAP immunoreactive (-ir), NDRG-ir, and GFAP/NDRG2 double-labelled cells within the SDH (P<0.05). Immunoblotting data showed that elemene decreased SNI-induced upregulation of GFAP and NDRG2 within the SDH (P<0.05).@*CONCLUSION@#Elemene possibly alleviated neuropathic pain by downregulating the expression of NDRG2 in spinal astrocytes in a rat model of SNI.


Subject(s)
Animals , Astrocytes , Disease Models, Animal , Emulsions , Hyperalgesia/drug therapy , Nerve Tissue Proteins , Neuralgia/drug therapy , Rats , Rats, Sprague-Dawley , Sesquiterpenes , Spinal Cord , Spinal Cord Dorsal Horn
2.
Acta Pharmaceutica Sinica ; (12): 1820-1825, 2021.
Article in Chinese | WPRIM | ID: wpr-887023

ABSTRACT

We established a simple and sensitive GC-MS method for the determination of β-elemene in rat plasma and measured the pharmacokinetics of citronella grass extract in rats. Plasma samples were pretreated using liquid-liquid microextraction: 100 μL of plasma sample (containing naphthalene as the internal standard) was extracted with 50 μL of n-hexane. The determination was performed on DB-5ms column (30 m×0.25 mm, 0.25 μm). The initial column temperature was 60 ℃ and raised to 160 ℃ at a rate of 50 ℃·min-1, maintained for 3 min, and finally increased to 260 ℃ for 3 min. Helium was the carrier gas and the flow rate was 0.15 mL·min-1. The injection volume was 2 μL. EI and selected monitored ions pattern were used for ion scanning with m/z 128 (naphthalene) and m/z 93 (β-elemene). Citronella grass extract was administered to rats by intragastric administration and intravenous administration (containing β-elemene 55 mg·kg-1), and plasma was collected and prepared using an automated blood collection system. The linear range of β-elemene in plasma was 1.0-250 ng·mL-1 (r = 0.997), the limit of quantification was 1.0 ng·mL-1, the accuracy was -4.47% - -0.85%, the extraction recovery was between 56.02%-66.89%, and no obvious matrix effect (94.28%-108.63%) was found. The main pharmacokinetic parameters of β-elemene were AUC0-t (23.56 ± 4.40) ng·mL-1, tmax (1.67 ± 0.58) h, Cmax (7.36 ± 0.69) ng·mL-1, MRT0-t (2.76 ± 0.27) h, t1/2z (2.73 ± 1.36) h, Vz (7.39 ± 3.18) L·kg-1, CLz (1.95 ± 0.51) L·h-1·kg-1, and the absolute bioavailability was about 8.78%. The method is simple, accurate, and sensitive, and is suitable for the pharmacokinetic analysis of β-elemene in citronella grass extract in rats. All animal studies were implemented according to protocols, which were reviewed and approved by the Institutional Animal Care and Use Committee at Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences.

3.
Article in Chinese | WPRIM | ID: wpr-846423

ABSTRACT

Objective: To prepare polydopamine-modified elemene-loaded mesoporous silica nanoparticles (D/MSN-ELE), and conduct research on formulation process optimization, quality evaluation, in vitro release, in vitro antitumor activity, and ability to promote apoptosis. Methods: Elemene-loaded mesoporous silica nanoparticles (MSN-ELE) were prepared by solution adsorption method, D/MSN-ELE and polydopamine-modified mesoporous silica nanoparticles (D/MSN) were prepared by polymerization. The morphology of the nanoparticles was characterized by transmission electron microscopy. The PDA graft ratio was calculated by thermogravimetric analysis. The loading and encapsulation efficiency of D/MSN-ELE were evaluated using HPLC, the dialysis bag method was used to investigate the release characteristics in vitro of D/MSN-ELE. MTT staining was used to analyze the cytotoxicity of different nanoparticles on HELF and A549 cells. Flow cytometry was used to detect the levels of D/MSN-ELE reactive oxygen species and mitochondrial membrane potential. Results: The optimal preparation process was the drug loading ratio of 6:1, the temperature was 50℃, and the time was 8 h. The D/MSN-ELE prepare under the process condition have a were uniform distribution with a particle size of (288.70 ± 3.88) nm. The average drug loading and encapsulation efficiency were (11.58 ± 0.73)% and (59.82 ± 0.57)%, respectively. In vitro drug release was pH-responsive, and cumulative drug release increased with decreasing pH. The half-lethal concentrations of ELE, MSN-ELE and D/MSN-ELE on A549 cells were 91.29, 27.56 and 6.02 μg/mL, respectively. The detection results of reactive oxygen species and mitochondrial membrane potential further indicated that drug-loaded nanoparticles were able to promote tumor target cell apoptosis. Conclusion: D/MSN-ELE under the optimized process has a higher drug loading, pH-responsive drug release and greatly enhanced antitumor activity. This study provides further experiments basis for tumor-targeted delivery of elemene drugs based on mesoporous silica nanoparticles.

4.
Article in Chinese | WPRIM | ID: wpr-846215

ABSTRACT

β-Elemene is the main active ingredient of elemene, a broad-spectrum anti-cancer botanical drug, which is also the main isomer of elemene's four isomers. The synthesis of some key intermediates were generalized and summarized during the derivatization of β-elemene, wherein the preparation methods, reaction conditions, yields, characterization data of these intermediates were listed. The purpose of this paper is to facilitate people in understanding and grasping the most optimal synthesis of these intermediates up to date, to inspire people pursuing further synthesis improvement, and to stimulate generation of new ideas for future derivatization of β-elemene.

5.
Article in Chinese | WPRIM | ID: wpr-823002

ABSTRACT

@#This study aimed to investigate whether β-elemene could improve the dysfunction of vascular endothelial cells induced by low shear force (LSS), and the proliferation and migration of vascular smooth muscle cells induced by oxidized low-density lipoprotein (ox-LDL). Parallel plate flow chambers and ox-LDL were used to establish vascular endothelial cells (ECs) dysfunction model and vascular smooth muscle cell (VSMCs) proliferation and migration model, respectively, and the effects of β-elemene on ECs dysfunction and VSMCs proliferation and migration were examined. The activity of ROS in ECs was measured by DHE and the activity of NO in ECs was tested by DAF-FM DA. The protein phosphorylation of Akt and ERK in ECs were detected by Western blot. The proliferation of VSMCs was measured by MTT. The migration of VSMCs was examined by cell scratch test and Transwell assay. The gene expression of MMP-2 and MMP-9 in VSMCs was measured by RT-qPCR. In ECs, β-elemene could significantly reduce the LSS-induced increase in ROS, significantly increase the LSS-induced decrease in NO, decrease the phosphorylation of ERK, and increase the phosphorylation of Akt. In VSMCs, β-elemene could significantly reduce the proliferation and migration of VSMCs induced by ox-LDL, and reduce the gene expression of MMP-2 and MMP-9. To conclude, β-elemene can improve the LSS-induced ECs dysfunction and ox-LDL-induced VSMCs proliferation and migration.

6.
Braz. j. med. biol. res ; 53(6): e8885, 2020. tab, graf
Article in English | ColecionaSUS, LILACS, ColecionaSUS | ID: biblio-1132519

ABSTRACT

In this study, we aimed to analyze the anti-cancer effects of β-elemene combined with paclitaxel for ovarian cancer. RT-qPCR, MTT assay, western blot, flow cytometry, and immunohistochemistry were used to analyze in vitro and in vivo anti-cancer effects of combined treatment of β-elemene and paclitaxel. The in vitro results showed that β-elemene+paclitaxel treatment markedly inhibited ovarian cancer cell growth, migration, and invasion compared to either paclitaxel or β-elemene treatment alone. Results demonstrated that β-elemene+paclitaxel induced apoptosis of SKOV3 cells, down-regulated anti-apoptotic Bcl-2 and Bcl-xl gene expression and up-regulated pro-apoptotic P53 and Apaf1 gene expression in SKOV3 cells. Administration of β-elemene+paclitaxel arrested SKOV3 cell cycle at S phase and down-regulated CDK1, cyclin-B1, and P27 gene expression and apoptotic-related resistant gene expression of MDR1, LRP, and TS in SKOV3 cells. In vivo experiments showed that treatment with β-elemene+paclitaxel significantly inhibited ovarian tumor growth and prolonged the overall survival of SKOV3-bearing mice. In addition, the treatment inhibited phosphorylated STAT3 and NF-κB expression in vitro and in vivo. Furthermore, it inhibited migration and invasion through down-regulation of the STAT-NF-κB signaling pathway in SKOV3 cells. In conclusion, the data suggested that β-elemene+paclitaxel can inhibit ovarian cancer growth via down-regulation of the STAT3-NF-κB signaling pathway, which may be a potential therapeutic strategy for ovarian cancer therapy.


Subject(s)
Animals , Male , Female , Rabbits , Ovarian Neoplasms/drug therapy , Sesquiterpenes/administration & dosage , Cell Movement/drug effects , NF-kappa B/adverse effects , Paclitaxel/administration & dosage , Apoptosis/drug effects , Cell Proliferation/drug effects , Ovarian Neoplasms/metabolism , Ovarian Neoplasms/pathology , Immunohistochemistry , Transfection , Signal Transduction , Blotting, Western , NF-kappa B/metabolism , Cell Line, Tumor , Real-Time Polymerase Chain Reaction , Mice, Inbred BALB C
7.
Biosci. j. (Online) ; 35(4): 1198-1212, july/aug. 2019. tab, graf
Article in English | LILACS | ID: biblio-1048859

ABSTRACT

In this study the potential bioinseticide of the essential oil (OE) extracted from the rhizomes of the species Curcuma zedoaria (Zingiberaceae) was evaluated. The rhizomes were collected during dormancy (winter) and budding (summer). The EO was obtained by hydrodistillation (2h) and identified by GC/MS. In addition, a multivariate exploratory analysis was done to determine the analysis of the major compounds (PCA). The EO yield in dormancy was 0.61± 0.07 (%) and in budding 0.55 ± 0.08 (%). The bioassays on Aedes aegypti larvae and pupae were done by immersion test at different EO concentrations which ranged from 500.00 to 0.003 mg mL-1 (v/v). The results on the larvae and pupae indicated LC99.9 of (0.01 and 1.38 mg mL-1) for EO in dormancy, and (0.08 and 2.63 mg mL-1) for EO during budding, respectively. The action mechanism of EOs in both periods was determined by autobiographic method evaluating the inhibitory potential on the acetylcholinesterase enzyme, indicating greater inhibition of the EO enzyme during dormancy (0.039 mg mL-1) when compared to the EO during budding (0.156 mg mL-1). The projection representation of the EO chemical classes in both evaluated periods indicated that oxygenated sesquiterpenes are the major compound class (46.99% in dormancy) and (43.59% in budding). The projection of major chemical compounds of EOs presented three compounds with greater mass flow distancing: epicurzerenone (18.20% and 12.10%); 1.8 cineole (15.76% and 12.10%) and ß-elemene (4.43 and 0.01%) that are found in greater amounts in the dormancy EO when compared to budding, respectively. These results corroborate with the greater potential on Ae. aegypti larvae and pupae found for the dormancy EO. The results are promising because they show in which vegetative cycle phase C. zedoaria EO presents greater bioinsecticidepotential.


Neste trabalho foi avaliado o potencial bioinseticida do óleo essencial (OE) extraído dos rizomas da espécie Curcuma zedoaria (Zingiberaceae), coletados no período de dormência (inverno) e brotação das gemas (verão). O OE foi obtido por hidrodestilação (2h) e identificado por CG/EM foi observado rendimento 0,61 ± 0,07 (%) no óleo da dormência, quando comparado no período de brotação 0,55 ± 0,08 (%). Os bioensaios sobre as larvas e pupas de Aedes aegypti foram realizados pelo teste de imersão em diferentes concentrações dos OEs, que variaram de 500,00 a 0,003 mg mL-1 (v/v). Os resultados sobre as larvas e pupas indicaram uma CL99,9 de (0,01 e 1,38 mg mL-1) para o OE da dormência, e (0,08 e 2,63 mg mL-1) para o OE do período de brotação, respectivamente. Indicando maior atividade do OE da dormência. O mecanismo de ação dos OEs nos dois períodos foi determinado pelo método autobiográfico avaliando o potencial inibitório sobre a enzima acetilcolinesterase. Os resultados indicaram maior inibição da enzima do OE no período de dormência (0,039 mg mL-1), quando comparado ao OE de brotação (0,156 mg mL-1). A análise química destacou três compostos: epicurzerenone (18,20% e 12,10%) e 1,8 cineol (15,76% e 14,05%) e ß- elemeno (4,43 e 0,01%) em maior quantidade no período de dormência quando comparado ao período de brotação, respectivamente. Esta diferença pode explicar a maior ação inseticida do OE de dormência sobre as larvas e pupas do Ae. aegypti. Os resultados são promissores, pois estabelece em qual período do ciclo vegetativo o OE da C. zedoaria apresenta maior potencial bioinseticida.


Subject(s)
Oils, Volatile , Aedes , Curcuma , Insecticides , Biological Assay
8.
Article in Chinese | WPRIM | ID: wpr-851421

ABSTRACT

Objective To verify the synergistic effect of transferrin modified β-elemene and celastrol co-loaded microemulsion (Tf-EC-MEs) on anti-colorectal cancer treatment. Methods The optimal mass ratio of β-elemene and celastrol to growth inhibition of Lovo and HT-29 colorectal cancer cells was optimized by MTT staining method in vitro. Tf-EC-MEs was prepared by “mixing-dripping” method, and the preparation and physicochemical properties of the particles were characterized by high performance liquid chromatography (HPLC), laser particle analyzer, and transmission electron microscope. The MTT staining, HPLC-BCA combined method, and Annexin V-PE/7-Aminoactinomycin D (Annexin V-PE/7-AAD) kit were used to investigate the antitumor activity of Tf-EC-MEs in vitro, and its effect on cell uptake, and apoptosis of tumor cells. The tumor-bearing nude mice model was established by subcutaneous injection of Lovo cells, and the tumor growth, weight, and survival time were observed after intravenous injection of β-elemene + celastrol, β-elemene-celastrol co-loaded microemulsion (EC-MEs), and Tf-EC-MEs. Results The combined administration of β-elemene and celastrol (40:1) had significant synergistic effect on the anti-colorectal cancer of Lovo and HT-29 cells. IC50 of β-elemene + celastrol in Lovo and HT-29 cells were (17.5 ± 2.9) and (36.4 ± 3.6) μg/mL, with the CI as 0.89 and 0.96, respectively. IC50 of Tf-EC-MEs in Lovo and HT-29 cells were (11.7 ± 0.6) and (27.4 ± 1.2) μg/mL, with the CI as 0.61 and 0.72 respectively. The 4 h of Lovo uptake of Tf-EC-MEs was 7.2 μg/mg, which was 3.3 times higher than that of β-elemene + celastrol. Tf-EC-MEs induced apoptosis in 59.2% of Lovo cells, which was significantly higher than that in beta-elemene + celastrol and EC-MEs groups. Tf-EC-MEs showed the overwhelming inhibition of growth of Lovo tumor-bearing tumors. The survival rate of Tf-EC-MEs-treated mice was 37.5% at day 60. In Tf-EC-MEs treated group, HE staining sections of tumor tissues showed substantial cell necrosis and the Ki-67 immunohistochemical sections displayed the significant inhibition of proliferation of tumor cells. Conclusion Compared with the combination group (beta-elemene and celastrol) and EC-MEs groups, Tf-EC-MEs has a promising potential in the synergistic anti-colorectal cancer treatment.

9.
Article in Chinese | WPRIM | ID: wpr-850817

ABSTRACT

A demonstration research on Chinese herbal decoction pieces of Curcumae Rhizoma was performed based on the concept of quality markers (Q-markers), standard establishment, and research modes. The chemical constituents of both steamed processed pieces of Curcumae Rhizoma and vinegar-processed pieces of Curcumae Rhizoma decoction pieces were identified by ultra- performance liquid chromatography/quadrupole-time of flight mass spectrometry (UPLC-Q/TOF-MS). The major effective components were analyzed through pharmacodynamics, drug property, pharmacokinetics studies, and correlation analysis of chemical constituents. The Q-markers were determined by all the results. At last, five compounds including curdione, curcumol, germacrone, furanodiene and β-elemene were selected as Q-markers. The quality control methods of multi-component assaying and fingerprint were also established. Overall, this study provides a demonstration for the study of quality markers of Chinese herbal decoction pieces.

10.
Article in Chinese | WPRIM | ID: wpr-701146

ABSTRACT

AIM:To investigate the effect of β-elemene on reversing hepatocyte growth factor(HGF)-induced resistance to gefitinib in PC-9 cells, and to explore its possible mechanisms.METHODS: The gefitinib-resistant PC-9 cells induced by HGF were treated with β-elemene or/and gefitinib.The cell activity was measured by MTT assay.The effect of β-elemene on the invasion ability in HGF-induced resistance to gefitinib in PC-9 cells was detected by Transwell migration assay.The protein levels of p-Met, c-Met, p-AKT and AKT in PC-9 cells of each group were determined by Western blot.RESULTS:The results of MTT assay showed that the cell activity of PC-9 cells was significantly inhibited by β-elemene(P<0.05).IC50of β-elemene for PC-9 cells was 169.31 mg/L.IC50of gefitinib for PC-9 cells was 0.30 μmol/L.Exogenously adding recombinant HGF induced significantly resistance to gefitinib in PC -9 cells.Moreover, SU11274(an inhibitor of c-Met)significantly decreased the viability of the cells exposed to HGF and gefitinib(P <0.05).Combined treatment with β-elemene and gefitinib in the presence of HGF(50 μg/L)significantly decreased the viability of PC-9 cells as compared with the PC-9 cells treated with gefitinib alone in the presence of HGF(P<0.05),so did the result of the cell migration.The protein levels of p-Met and p-AKT were significantly up-regulated by HGF,while the protein levels of p-Met and p-AKT were markedly down-regulated in the cells treated with β-elemene and gefitinib com-pared with gefitinib alone in the presence of HGF.CONCLUSION: β-elemene reverses HGF-induced resistance to ge-fitinib in lung cancer PC-9 cells,likely due to the inhibition of HGF-induced activation of c-Met and its down streams sig-naling pathways(P<0.01).

11.
Article in Chinese | WPRIM | ID: wpr-693446

ABSTRACT

Objective To observe the effect of elemene injection for the maintenance treatment of malignant pleural effusion.Methods A total of 90 patients with malignant pleural effusion from May 2014 to Apirl 2016 in First Affiliated Hospital of Heilongjiang University of Traditional Chinese Medicine were collected.They were divided into observation group (n =45) and control group (n =45) according to the random number table method.The patients of the two groups were treated with pleural effusion drainage through thoracocentesis,and Mannatide (Lifein) and carboplatin were poured.The observation group sequentially received maintenance treatment of elemene injection.The therapeutic effects of the two groups were compared.Results At the 12th month after treatment,the difference of relapse rate between the two groups was statistically significant(82.2% vs.100.0%,x2 =8.780,P =0.003).The median progression-free survival (95% CI) of the observation group and the control group were 10.00 (9.15-10.85) months and 6.00(4.74-7.26) months respectively,with a significant difference (x2 =40.475,P < 0.001).The improvement rates of life quality of the observation group were 82.22%,57.78%,54.55% respectively at one,six,twelve months after perfusion treatment,and the improvement rates of the control group were 84.44%,23.26%,0 respectively.The data differences between the two groups were statistically significant at six,twelve months (x2 =10.840,P =0.001;x2 =32.390,P < 0.001).The one year survival rates of the observation group and the control group were 97.78% and 95.56%,and the difference was statistically significant (P =1.000).Conclusion The effect of elemene injection for the maintenance treatment of malignant pleural effusion is obvious,which can prolong the progression-free survival time and can significantly improve the quality of life.

12.
Braz. j. med. biol. res ; 51(11): e7356, 2018. tab, graf
Article in English | LILACS | ID: biblio-951728

ABSTRACT

Essential oils (EO) are volatile liquids responsible for the aroma of plants. Pterodon polygalaeflorus seeds have received widespread use in folk medicine for the treatment of inflammatory diseases. For this reason and because Pterodon polygalaeflorus seeds have great EO content, which is frequently pharmacologically active, the present study aimed to evaluate the antinociceptive effect of EO from Pterodon polygalaeflorus (EOPPgfl) and its acute toxic effects. The EEOPPgfl sample, which was extracted by steam distillation of the seeds, had a yield of 2.4% of the seeds weight and had, as major constituents, beta-elemene (48.19%), trans-caryophyllene (19.51%), and epi-bicyclosesquiphellandrene (12.24%). The EOPPgfl sample showed mild acute toxicity and its calculated median lethal dose (LD50) was 3.38 g/kg. EOPPgfl (20-60 mg/kg) showed antinociceptive activity as evidenced by several tests and inhibited writhing induced by acetic acid. The maximum effect was obtained with the 30 mg/kg dose and at 60 min after its administration. EOPPgfl also decreased formalin-induced nociception, as verified by the inhibition of the first and second phase of the formalin test. At 30 mg/kg, EOPPgfl also decreased thermally stimulated nociception. Nociception may be related to inflammatory and antiedematogenic activity and at doses ranging 10-100 mg/kg, EOPPgfl blocked dextran- and carrageenan-induced edema. The results demonstrated that EOPPgfl presented, at doses approximately 100 times smaller than LD50, an antinociceptive effect that probably was due to anti-inflammatory activities.


Subject(s)
Animals , Rabbits , Plant Oils/pharmacology , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Nociception/drug effects , Analgesics/pharmacology , Fabaceae/chemistry , Seeds/chemistry , Time Factors , Pain Measurement , Random Allocation , Reproducibility of Results , Treatment Outcome , Anti-Inflammatory Agents/pharmacology
13.
Article in Chinese | WPRIM | ID: wpr-852158

ABSTRACT

β-elemene is the sesquiterpene active monomer, as a national second-class non-cell toxic antitumor drugs which extracted from Zingiberaceae Curcuma rcenyujin. Moreover, β-elemene is currently used in clinic for treatment of lung cancer, liver cancer as well as breast cancer, and so on. Because of its broad-spectrum, safe, efficient, economical and other outstanding advantages in antitumor activities, leading to a broad application prospect in clinic. With the deep study of component and anticancer mechanisms of β-elemene, in order to promote its bioavailability and anticancer activity, researchers have screened a great deal of significant effective derivatives, and designed its liposome, microemulsion and other new drug delivery systems, which provide scientific theoretical guidance for further development and utilization of β-elemene. In this study, a systematic illustration was made for the current advance of pharmacological effects and mechanisms of β-elemene on treating cancer. In addition, the important derivatives, new drug delivery systems, and adverse reactions of β-elemene also be clarified, aiming to provide ideas for further scientific research and innovation of β-elemene.

14.
Chinese Journal of Lung Cancer ; (12): 458-462, 2018.
Article in Chinese | WPRIM | ID: wpr-772417

ABSTRACT

BACKGROUND@#Malignant pleural effusion (MPE) refers to pleural effusion which arises from primary malignant tumor of pleura or other pleural metastatic tumors. Injection of elemene in chest makes good effect on the treatment of MPE, and is widely used in clinic. Adverse effects also exist, but the severe adverse effects and relevant managements are rarely reported. The aim of this study is to observe the adverse reactions induced by the treatment of malignant pleural effusion through elemene injection and to explore the solutions.@*METHODS@#A retrospective analysis was made on 14 cases of patients receiving intra-pleural injections with elemene, and the incidence of severe adverse reactions of 7 cases were disscussed in detail.@*RESULTS@#Most of the severe adverse reactions caused by elemene were severe chest pain, dyspnea, wheezing, clouding of consciousness and coagulopathy.@*CONCLUSIONS@#Strict screening, full preprocessing and close monitoring are necessary to prevent serious adverse reactions caused by elemene injection in the treatment of malignant pleural effusion.


Subject(s)
Aged , Female , Humans , Injections , Male , Middle Aged , Pleural Effusion, Malignant , Drug Therapy , Retrospective Studies , Sesquiterpenes , Therapeutic Uses , Thorax
15.
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.

16.
Drug Evaluation Research ; (6): 119-124, 2017.
Article in Chinese | WPRIM | ID: wpr-514996

ABSTRACT

Curcumae Rhizoma comes from Curcuma genus,functional breaking blood stasis,detumescence and acesodyne for treatment of Zhengjia accumulation,amenorrhea,traumatic injury and bruising pain.Modem pharmacological studies have shown that the main monomer composition of zedoary turmeric has a good anti-inflammatory and anti-tumor effects.The main monomer composition of zedoary turmeric copies of curcumol,beta etemene,curcumin anti-inflammatory anti-tumor mechanism of review,provide the basis for the further research progress and clinical application of zedoary turmeric.

17.
Article in Chinese | WPRIM | ID: wpr-509214

ABSTRACT

Objective To establish a RP-HPLC method for the determination of encapsulation efficiency (EE) and medicine loading (ML) in β-elemene-loaded Nano Polymeric Micelles; To study its release characteristic in vitro. Methods DSPE-PEG2000 was used as carrier to prepare medicine-loaded micelles. EE and ML were determined by petroleum ether extraction method, and its release characteristic in vitro was studied by dialysis method. Results The average EE and ML ofβ-elemene-loaded Nano Polymeric Micelles were 89.47%and 8.33%, respectively. Its release characteristic was slow. Conclusion The method for EE and ML determination is simple and accurate, and the prepared micelles have the property of sustained release.

18.
Article in Chinese | WPRIM | ID: wpr-658287

ABSTRACT

Objective To systematically evaluate the effectiveness and safety of Elemene combined with radiotherapy for intervention in brain metastasis from pulmonary neoplasms. Methods Articles of clinical randomized controlled trials about Elemene combined with radiotherapy for intervention in brain metastasis from pulmonary neoplasms from the establishment of the databases to October of 2016 from CNKI, CBM, Chongqing Weipu, Wanfang database, Cochrane Library, PubMed and Embase were retrieved by computers. Bias risk assessment tools in Cochrane systematic evaluation handbook 5.1.0 was used to conduct quality evaluation for included articles. RevMan5.3 software was used to carry out Meta-analysis. Results Totally 12 articles and 839 patients were included. Results of Meta-analysis showed that Elemene combined with radiotherapy had more obvious curative effect on narrowing the neoplasm compared with pure radiotherapy [OR=2.73, 95%CI (1.97, 3.77), P<0.000 01], and improve patients' life quality at the same time [OR=3.85, 95%CI (2.23, 6.65), P<0.000 01], and relieve adverse reactions [OR=4.16, 95%CI (2.40, 7.22), P<0.000 01]. Conclusion Elemene combined with radiotherapy for intervention in brain metastasis from pulmonary neoplasms shows confirmed efficacy, and is relatively safe. But whether the program should be widely used in clinic, more large sample, multi-center, and high-quality clinical randomized controlled trials are still needed.

19.
Article in Chinese | WPRIM | ID: wpr-666854

ABSTRACT

Objective To investigate the effects of elemene combined with chemotherapy on S100A4 and MMP-9 protein expression in Lewis lung carcinoma mice and to explore the possible mechanism. Methods Twenty-four mice inoculated with Lewis cells were randomly divided into 4 groups,including lung carcinoma model group,chemotherapy group,elemene group,and combination group,6 mice in each group. On day 11 after inoculation, the mice in chemotherapy group were given intraperitoneal injection of etoposide (3 mg·kg-1·d-1)and cisplatin (3 mg·kg-1·d-1),the mice in elemene group were given intraperitoneal injection of elemene (100 mg·kg-1·d-1), the mice in the combination group were given intraperitoneal injection of elemene (100 mg·kg-1·d-1),etoposide (3 mg·kg-1·d-1),and cisplatin (3 mg·kg-1·d-1). After 7-day continuous treatment,the tumor body mass, spleen index, thoracic gland index, growth-inhibition rate, and metastasis-inhibition rate in various groups were measured,the contents of protein S100A4 and matrix metalloproteinase 9 (MMP-9)in tumor tissues were determined by enzyme-linked immunosorbent assay (ELISA),and the protein expression levels of S100A4 and MMP-9 were detected by immunohistochemical staining. Results In the combination group, the growth-inhibition rate and the inhibitory rate of metastases were increased obviously, the spleen index and thoracic gland index were also increased, the contents of S100A4 and MMP-9 were decreased, and the protein expression rates of S100A4 and MMP-9 were reduced(P < 0.05 or P < 0.01 compared with the chemotherapy group). Conclusion Elemene combined with chemotherapy could inhibit the Lewis lung carcinoma growth and metastasis in mice, and the possible mechanism might be associated with the decrease of S100A4 and MMP-9 protein expression in the tumor tissues.

20.
China Pharmacy ; (12): 4826-4829, 2017.
Article in Chinese | WPRIM | ID: wpr-663599

ABSTRACT

OBJECTIVE:To study the effect of Elemene emulsion combined with ganciclovir on invasive ability and TIMP-1 mRNA expression in C6 brain tumor stem cells. METHODS:Cells with 3 generations were isolated and cultured from rats'C6 ma-lignant glioma cell lines,and immunocytochemistry was adopted to detect the protein expressions of stem cell markers CD133,Nes-tin. 20 rats were randomly divided into blank control group(normal saline),ganciclovir group(intragastrically administrated,216 mg/kg),Elemene emulsion injection group (intravenously injected in tail,36 mg/kg) and combination group (intragastrically ad-ministrated 216 mg/kg of ganciclovir+intravenously injected 36 mg/kg of Elemene emulsion injection in tail),5 in each group, once every day,for 10 d. After 2 h of last administration,the blood of rats in each group was collected,serum was isolated and co-cultured 24 h with C6 BTSCs in in vitro culture medium. Boyden invasion test was used to detect the invasive ability of C6 BTSCs,and real-time quantitative polymerase chain reaction(RT-PCR)method was used to determine the TIMP-1 mRNA expres-sion of C6 BTSCs. RESULTS:Cells with 3 generations had obvious protein expressions in CD133 and Nestin,indicating they were BTSCs. Compared with blank control group,the cell invasion rates of C6 BTSCs in ganciclovir group,Elemene emulsion in-jection group and combination group were obviously decreased,TIMP-1 mRNA expression was obviously enhanced,with statisti-cal significances(P<0.05). Compared with ganciclovir group and Elemene emulsion injection group,the cell invasion rate of C6 BTSCs in combination group was obviously decreased,TIMP-1 mRNA expression was obviously enhanced,with statistical signifi-cances(P<0.05). CONCLUSIONS:Elemene emulsion injection combined with ganciclovir can obviously inhibit the cell invasion of C6 BTSCs,the mechanism may be associated with promoting the TIMP-1 generation,and combination use shows better effect than single use.

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